TW201117722A - Fungicidal mixtures - Google Patents

Abstract

Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, wherein R1, R2, Q1 and Q2 are as defined in the disclosure; and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed is a composition comprising: (a) at least one compound selected from the compounds of Formula 1 described above, N-oxides, and salts thereof; and at least one invertebrate pest control compound or agent.

Description

201117722 六、發明說明： 【發明所屬之技術領域】 本發明關於咪唑衍生物之殺真菌混合物，及其N-氧化物與鹽，以及關於包含此些混合物之組合物及使用 此些混合物當做殺真菌劑之方法。 【先前技術】 防治真菌類植物病原造成之植物疾病對於達成高 作物產率係極為重要的。觀賞作物、蔬菜作物、田間作 物、穀類作物以及果實作物之植物疾病損害可造成顯著 的產量降低及因此導致消費者的花費增加。更由於通常 極具破壞性’植物疾病可能難以防治且可能對於市售之 殺菌劑發展出抗藥性。殺菌劑的組合物通常用來調節疾 病的防治，用以擴大防治的範圍以及減緩抗藥性的發 展。更進一步來說，這樣罕見的殺菌劑組合物展現了 1 加1大於2的效果（即協同作用），提供商業等級地重 要的植物疾病防治程度。根據這些因素，例如經治療的 特定的植物麵妓植㈣病，以及這錄物是在經植 物真菌病源體感染前从後，特“ _組合物的優點 公認會隨之改變。因此，需要提供新的具㈣之組合物 ^供！同的選擇來最大从對特定植物疾病的防治 扁求。這樣的組合物目前已經發現。 【發明内容】 151284.doc 201117722 本發明係關於一種殺真菌劑組合物（即組成），包 3 (a)至少一種選自式1化合物（包含所有立體異構 物）、其N-氧化物及其鹽類的化合物： R1201117722 VI. INSTRUCTIONS OF THE INVENTION: TECHNICAL FIELD OF THE INVENTION The present invention relates to fungicidal mixtures of imidazole derivatives, and N-oxides and salts thereof, and to compositions comprising such mixtures and the use of such mixtures as fungicidal Method of the agent. [Prior Art] Plant diseases caused by the control of fungal plant pathogens are extremely important for achieving high crop yields. Plant disease damage in ornamental crops, vegetable crops, field crops, cereal crops, and fruit crops can result in significant yield reductions and thus increased consumer spending. It is also more difficult to control because of the often extremely destructive 'plant disease' and may develop resistance to commercially available fungicides. Bactericide compositions are commonly used to modulate disease control to expand the range of control and slow the development of resistance. Furthermore, such rare fungicidal compositions exhibit an effect of 1 plus 1 greater than 2 (i.e., synergistic effect), providing a commercial grade of importance for plant disease control. Based on these factors, such as the treatment of specific plant surface (4) diseases, and the fact that the contents are infected before and after infection by plant fungal pathogens, the advantages of the composition are generally changed. Therefore, it is necessary to provide The new composition of (4) is the same choice to maximize the prevention and control of specific plant diseases. Such a composition has been found so far. [Abstract] 151284.doc 201117722 The present invention relates to a fungicide combination (i.e., composition), package 3 (a) at least one compound selected from the group consisting of a compound of formula 1 (comprising all stereoisomers), its N-oxides and salts thereof: R1

Q I Q2 Q係苯基、噻吩基、噻唑基、吡唑基、咪唑基、吡 啶基、嗒畊基、嘧啶基、喹啉基或节基，各視 情況以多達4個獨立選自R3的取代基在碳原 子環員上取代，及選自R4的取代基在氮原子 環員上取代； Q疋笨基、嗟吩基、嗟唾基、β比唑基、咪唑基、吼 啶基、嗒畊、嘧啶、喹啉基或苯曱基，每一 個5可最多單獨地，選擇性地取代4個選自 R奴原子環家族以及R6氮原子環家族之取 代基； R及R係獨立為齒素、氰基、硝基、Ci_C3烧基、 CK：3歸基、ce快基、環丙基、crc3鹵烷 f、C2-C3㈣基、Ci-C3烧氧基、c]-c3鹵炫 氧基Cl-C3烷硫基、Crc3齒烷硫基或crC7 氫氧烷基； 151284.doc 201117722 各R3及R5係獨立為鹵素、氰基、羥基、硝基、CVC7 炫基、C2-C7稀基、C2-C7快基、C2-C7氰烧基、 CrC7函烷基、C2-C7 _烯基、C3-C7環烷基、 C3-C7鹵環烧基、CfCio烧環烧基、C4，Ci〇環 烷烷基、c6-c14環烷環烷基、c3-c7環烷氧基、 匸3_〇7鹵環烧氧基、C1-C7烧氧基、C2-C7氮烧 氧基、CVC7鹵烷氧基、CrQ烷硫基、crc7 齒烧硫基、C]-C7烧亞績酿基、C1-C7烧續酿 基、crc7鹵烷亞磺醯基、crc7鹵烷磺醯基、 α-(：7烷胺基、C2-C7雙烷胺基、c2-c7烷羰基、 CH：7烷氧羰基、胺羰基、c2_c7烷胺羰基、 q-C7雙烷胺羰基、c2_c7烷羰胺基、c3-C10三 烷矽基、-SCN、C(=S)NH2 或-X-U-Z ; 各R4及R6係獨立為氰基、Q-C6烷基、C3-C6烯基、 c3-c6炔基、crC6齒烷基、c3-c6環烷基、crc6 烧氧基、C2-C6烷氧烷基、c2-c6烷獄基、c2_c6 烧氧羰基、C2-C6烷胺烷基或c3-c6雙烷胺烷 基； 各X係獨立為〇、s(=0)n、NR7或一直接鍵結； 各11係獨立為CrCHt烷基、c2-c6伸烯基、c3-c6 伸炔基、CrC6環伸烷基或C3-C6環伸烯基， 其中多達3個碳原子係獨立選自c(=0)，各視 情況以多達5個獨立選自齒素、氰基、硝基、 經基、CVC6烷基、crc6自烷基、crc6烷氧 基及CrC6函烷氧基的取代基所取代； 各 z 係獨立為 NR8aR8b、〇R9 或 s(=〇)nRio ; 151284.doc • 6 _ 201117722 各R7係獨立為H'CVQ烷基、CrC6鹵烷基、C2-C6 烷羰基、c2-c6烷氧羰基、c2-c6(烷硫基）羰基、 c2_c6烷氧基(硫羰基）、c4-c8環烷基羰基、 c4-c8環烷氧羰基、c4-c8(環烷硫基）羰基或 cvcpf烷氧基(硫羰基）； 各1183及R8b係獨立為Η、C「C6烷基、CrC6鹵烷 基、c2-c6烯基、c3-c6炔基c3-c6環烷基、c3-c6 烷基環烷基、c2-c6烷羰基、c2-c6烷氧羰基、 c2-c6(烷硫基）羰基、c2-c6烷氧基(硫羰基）、 C4_C8環烷基|ί炭基、c4-c8環烷氧Μ基、c4-c8(環 烷硫基)羰基或（:4-(:8環烷氧基(硫羰基）； 各R9及R10係獨立為Η、〇(：6烷基、CrC6鹵烷基、 C2-C6 缔基、C3-C6 炔基、C3-C6 環燒基、C3-C6 院基環烧基、C2-C6烧幾基、C2-C6烧氧幾基、 QrC6(烷硫基）羰基、c2-C6烷氧基(硫羰基）、 CrQ環院基幾基、Q-C8環烧氧幾基、C4-C8(環 烧硫基）羰基或C4-C8環烷氧基(硫羰基）； 各η係獨立為〇、1或2 ;及 (b)至少一附加的殺真菌化合物。 本發明亦關於一種組合物，其包含：（a)至少一種 選自前述式1化合物、其N-氧化物及其鹽類；以及至 少一種無脊椎害蟲防治的化合物或是藥劑。 本發明亦關於一種組合物，其包含其中一種前述組 合物，該組合物包含組分（a)以及至少一種選自由介 面活=劑、固體稀釋劑以及紐稀釋劑組成的群組的‘ 151284.doc 201117722 本發明亦關於一種防治由真菌類植物病原造成的 植物疾病的方法，該方法包含於植物或其之一部分，或 是植物種子，施予前述之組合物之一的有效殺真菌劑 量。 前述方法亦可經描述為一種保護植物或植物種 子，以避免其感染由真菌類植物病原體造成的植物疾病 的方法，該方法包含在植物（或部份植物體）或是植物 種子（直接或是藉由植物或植物種子之環境（例如：生 長介質））施予前述組合物之一的有效殺真菌劑量。 更進一步之態樣為，本發明亦關於如前述定義之選 自式1化合物（包括所有立體異構物）、其N-氧化物及 其鹽類 當Q1係苯基、塞吩基、嗟β坐基、°比β坐基、味。坐 基、°比咬基、塔ρ井基、°密唆基、喧琳基或节 基時，各視情況以多達4個獨立選自尺33的 取代基在碳原子環員上取代及選自R4a的取 代基在氮原子環員上取代；其中 各R3a係獨立為鹵素、氰基、羥基、硝基、 CrC7 烷基、C2-C7 烯基、C2-C7 炔基、CrC7 鹵烧基、C2-C7鹵烤基、C3-C7壞烧基、C3-C7 鹵王哀烧基、C4-C10烧极烧基、C4-Ci〇i哀烧烧 基、c6-c14環烷環烷基、c3-c7環烷氧基、 C3-C7鹵環烧氧基、CVC7烧氧基、CVC7鹵 烧氧基、Ci-C6炫硫基、C1-C7 _烧硫基、 C1-C7烧亞續酿基、C】-C7烧續酿基、C1-C7 鹵烧亞續酿基、CpC7鹵烧續酷基、C1-C7 151284.doc 201117722 烧胺基、C2-C7雙烷胺基、C2-C7烷羰基、 c2-c7烧氧羰基、c2_c7烷羰胺基、c3_Ci〇三 烧矽基、-SCN、C(=S)NH2 或-X-U-Z ;以及 各尺43係獨立為氰基、crc6烷基、c3-c6烯 基、c3-c6炔基、c3-c6環烷基、crc6烷氧 基、c2-c6烷氧烷基、C2-C6烷羰基、c2-c6 烧氧羰基、c2-c6烷胺烷基或c3-c6雙烷胺 烧基； 而Q係本基、β塞吩基、β塞嗤基、吼唾基、β米唾 基、°比啶基、嗒嗜基、嘧啶基、喹啉基或苯 基’各以1至4個獨立選自R5的取代基在 碳原子環員上取代及選自R6的取代基在氮 原子環員上取代；其限制條件為至少一個在 碳原子環員上之取代基係c2-c7氰烷基、 CVC7氰烧氧基、胺幾基、eve?院胺幾基或 CrC7雙烷胺羰基，或在氮原子環員上之取 代基係CpC6齒烧基。 本發明亦關於一種殺真菌組合物，包含一種選自前 述進一步態樣之化合物之殺真菌有效劑量以及至少一 種選自由介面活性劑、固體稀釋劑及液體稀釋劑組成的 群組的額外組分。本發明更進一步關於一種用於防治由 真菌類植物病原體所造成的植物疾病的方法，該方法包 含施予植物、其部分組織或植物種子一選自前述進一步 態樣之化合物之殺真菌有效劑量。 【實施方式】 151284.doc 201117722 「八=本^用，術語「包含」、「包括」、「具有」、 3有」、「特徵為」或該術語任何其他的變化，旨在涵 f非f他性的包含，並受到任何明確表示的限制。例 ^包含元素列表的組合物、混合物、製程或方法不必 f限於那些元素，而是可以包括未明確列出的或該組合 物、混合物、製程或方法所固有的其他元素。 主連接詞「由……組成」則排除任何未明確說明的元 素、步驟或成分。如果是在申請專利範圍中，這樣的用 詞將會封财請專利範圍，使其除了錢常會與其相關 ，雜質之外’不包括那些在列舉以外的物質。當連接詞 由…組成」出現在一個請求項的字句中，而不是立 刻緊撵著前言，則該連接詞只限定在前述子句中出現的 元素，整體而言並未在請求項中排除其他元素。 〜連接詞「主要由……組成」用於定義包括除了那些 字面上所揭露以外的材料、步驟、特徵、成份或元素的 組=物或方法，但前提是這些附加的材料、步驟、特徵、 成份或疋素並不會實質影響申請專利範圍所主張發明 ^基本和新穎特性。術語「主要由......組居於「包 含」與「由…組成」之間的中間地帶。 當申請人用開放式術語，像是「包含」，定義發明 或其中一部分時，應容易理解（除非另有說明）該敘述 應解釋為也使用術語「主要由......組成」或「由......組 成」來說明該發明。 此外，除非另有明確地相反陳述，否則「或」係指 包含性的「或」，而不是指排他性的「或」。例如，以下 任何一種情沉均滿紐件A或B : A為真（或存在的） I5I284.doc • 10- 201117722 且B為假（或不存在的）、A為假（或碎在的）且b 為真（或存在的’以及A和B均為真（或存在的）。 且’出現在發明中的—個元素或是化合物之前的不 定冠詞「-個」傾向於非限定關於（即發生） 化合物的例子的數目。因,士「 -¾「一 /田^ 、 囚此一」或 個」應理解為 包括-個或至少-個’且該元素或成份的單數詞形也 括複數，除非該數目顯然是指單數。 如本揭露内容及申料利範圍巾所提到，「植物」 包括植物界的成員’特別是所有生命階段的種子植物 (Spermat〇PSida)，包括幼嫩植物（如發芽種子發育成 為幼苗）及成熟生殖階段（如產生花及種子的植物）。 植物上的部分包括通常在生長介質表面（如土壤）下生 長的向地部为，像是根、塊莖、鱗莖和球莖，以及在生 長介質上生長的部分，像是葉子（包括莖及葉）、花、 果貫和種子。 如本文中所提到，術語「幼苗」，無論是單獨使用 或與其他字組合，意指從一種子胚芽發育的幼嫩植物。 在此所用的術語「烧化劑」關於一個化合物其中一 個3石反的自由基介由一個碳原子鍵結到—個脫離基，該 脫離基例如鹵化物或是磺酸鹽，其可以藉由鍵結一個親 核劑到前述之碳原子來經替換。除非特別強調，術語「烧 化」不限定含碳自由基為烷基；烷化劑中的含碳自由基 包括多種鍵結碳的取代自由基’特別是，例如R1以及 R2。 以上詳述中’術語「烷基」，可單獨或是與化合物 使用。文字例如「烷硫基」或是「鹵烷基」包含直鏈或 151284.doc -11 - 201117722 疋支鏈院基，例如，曱乙基、正丙基、異丙基、或不同 的丁基、戊基、己基或伸庚基異構物。「烯基」包含直_ 鏈或是支鏈烯屬烴例如乙烯基、^丙烯基、2_丙烯基、 以及不同的丁烯基、戊烯基、己烯基及庚烯基異構物。 「烯基」也包括多烯例如1，2_丙烯基以及2,4_己二烯。 「炔基」包括直鏈或支鏈炔屬烴例如乙炔基、卜丙炔 基、2-丙炔基以及不同的丁炔基、戊炔基、己炔基和庚 炔基異構物。「炔基」亦可包括包含多個三鍵的部份， 例如2,5-己二快基。「苯甲腈」表示一個直鏈或支鏈的 雙烧基。「伸烷基」的例子包括ch2、ch2ch2、ch(ch3)、 CH2CH2CH2、CH2CH(CH3)以及不同的伸丁基、伸戊基 與伸己基異構物。「伸烯基」表示一個直鏈或支鏈双烯 基包含酮烯鍵。「伸烯基」的實例包括CH=CH、 CH2CH=CH、CH=C(CH3)。「伸炔基」意指包含一個參 鍵的直鏈或支鏈快二基。「伸炔基」的實例包括 CH2〇C、OCCH2和各種伸丁炔基、伸戊炔基和伸己 炔基異構物。 「烷氧基」包括，舉例來說，曱氧基、乙氧基、正 丙氧基、異丙氧基以及不同的丁氧基、戊氧基、己氧基 與庚氧基異構物。「烷硫基」包括支鏈或直鏈烷硫基部 分’例如曱硫基、乙硫基，以及不同的丙硫基、丁硫基、 戊硫基、己硫基與庚硫基異構物。「烷亞磺醯基」包括 一個烷亞磺醯基群組的二鏡像異構物。「烷亞磺醯基」 之例子包括 ch3s(=o) 、CH3CH2S(=0)、 ch3ch2ch2s(=o)、（ch3)2chs(=o)以及不同的丁烷亞磺 酿基、戊烧亞續酿基、己烧亞續酿基與庚烧亞續酿基異 151284.doc •12· 201117722 構物。「烷磺醯基」之例子包括ch3s(=o)2、 ch3ch2s(=o)2、ch3ch2ch2s(=o)2、（CH3)2CHS(=0)2、 以及不同的丁烷磺醯基、戊烷磺醯基、己烷磺醯基與庚 烷磺醯基異構物。「烷胺基」包括一個以直鏈或支鏈烷 基取代的NH自由基。「烷胺基」之例子包括 CH3CH2NH、CH3CH2CH2NH，以及（CH3)2CHCH2NH。「二 烷胺基」之例子包括（CH3)2N，（CH3CH2CH2)2N以及 CH3CH2(CH3)N。 「氰烷基」表示一個以酮氰基群組取代的烷基。「氰 烷基」之例子包括ncch2、ncch2ch2以及 CH3CH(CN)CH2。「烷氧烷基」表示於烷基位置的烷氧 基取代。「烷氧烷基」之例子包括CH3OCH2、 CH3OCH2CH2、CH3CH2OCH2、CH3CH2CH2CH2OCH2 以 及CH3CH2OCH2CH2。「（烷硫基)羰基」表示一個鍵結到 一個部分c(=o)之直鏈或是支鏈的烷硫基群組。「（烷硫 基）羰基」的實例包括ch3sc(=o)、ch3ch2ch2sc(=o) 和（ch3)2chsc(=o)。「烷氧基（硫羰基）」意指鍵結到 c(=s)部分的直鏈或支鏈烷氧基團。「烷氧基（硫羰基）」 之例子包括 CH3OC(=S)、CH3CH2CH2OC(=S)以及 (CH3)2CHOC(=S)。「烷胺烷基」表示烷基位置的烷胺基 取代。「烷胺烷基」之例子包括CH3NHCH2、 ch3nhch2ch2 、 ch3ch2nhch2 、 CH3CH2CH2CH2NHCH2 以及 CH3CH2NHCH2CH2。「二烷 胺烷基」之例子包括（(ch3)2ch)2nch2 、 (CH3CH2CH2)2NCH2 以及 CH3CH2(CH3)NCH2CH2。術語 「烷羰胺基」表示鍵結在部份C(=0)NH的烷基。「烷羰 151284.doc -13- 201117722 胺基」的實例包括 ch3ch2c(=o)nh 和 ch3ch2ch2c(=o)nh。 「羥烷基」表示一個以酮羥基群組取代的烷基。「羥 烧基」的例子包括HOCH2CH2、CH3CH2(OH)CH以及 HOCH2CH2CH2CH2。 「環烧基」包括，例如環丙基、環丁基、環戊基、 %；•己基以及J衣庚基。術S吾「烧J哀烧基」表示部分環院基 上的烷基取代，且包括，舉例來說，乙環丙基、異丙環 丁基、甲環戊基以及曱環己基。術語「環烷烷基」意指 在烷基部分上經環烷基取代。「環烷烷基」的實例包括 環丙曱基、環戊乙基和其他鍵結到直鏈或支鏈烧基團的 環烷基部分。術語「環烷環烷基」表示其它環烷基環之 環烷基取代，其中每個環烷基環獨立地具有3到7個碳 原子環員。環燒環烧基的例子包括環丙環丙基（例如： 1，Γ-二環丙基-1-基，^’-二環丙基_2_基環己環戊基 (例如：4-環戊環己基）及環己環己基（例如：1，1，_二 環己基-1-基），及不同的順向與反向環烷基環烷基異構 物（例如.（1R，2S)-1，1，-二環丙基-2-基及^ 二環丙基_2_基）。術語「環烷氧基」表示黏附以及鍵結 -氧原子的環燒基，其包括，例如：環戊氧基及環己氧 基。「環烧基絲」表示鍵結至—C(=Q)基團之環烧基， ^含，例如：環丙羰基及環戊羰基。術語「環烷氧羰基」 ^指鍵結到C(=〇)基團的環烧氧基，例如環丙氧魏基和 環戊氧羰基。術語「環伸烷基」意指環烷二基環。「環 伸燒基」的實例包括環伸丙基、環伸T基、環伸戊基和 151284.doc •14· 201117722 環伸己基。術語「環伸烯基」表示含一烯鍵之環稀二基 環。「環伸烯基」的實例包括環丙烯二基和環戊烯基。 「烷羰基」表示一鍵結至c(=o)部份之直鏈或支鏈 烷基。「烷羰基」之實例包含ch3c(=o)、 CH3CH2CH2C(=0)及(CH3)2CHC(=0)。「烷氧羰基」之實 例包含 ch3oc(=o) 、 ch3ch2oc(=o)、 ch3ch2ch2oc(=o)、（ch3)2choc(=o)及不同的丁氧羰 基、戊氧幾基及己氧幾基異構物。 「三烷矽基」包括3個經由矽原子附著以及連結之 支鏈及/或直鏈烷基，例如：三甲矽烷基、三乙矽烷基 及三級-丁二曱矽烷基。 術語「齒素」，無論是單獨使用或在像是「齒烷基」 的複合詞中使用’或者在像是「經函素取代的烷基」的 敘述中使用時，包括氟、氣、溴或碘。此外，當在像是 「鹵烷基」的複合詞中使用時，或者在像是「經函素取 代的烷基」的敘述中使用時，所述烷基可能經相同或不 同的鹵素原子部份或全部取代。實例如「鹵烷基」或「以 鹵素取代的烷基」，包括F3c、C1CH2、CF3CH2及 CFsCCl2。術語「鹵烯基」、「鹵烷氧基」、「鹵烷硫基」、 「鹵烷亞磺醯基」、「齒烷磺醯基」、「烷基環烷基」、「鹵 環烷氧基」等等，與術語「鹵烷基」定義相似。「鹵烯 基」之實例包括C12C=CHCH2及CF3CH2CH=CHCH2。「鹵 烷氧基」的實例包括cf3o、cci3ch2o、f2chch2ch2o 及cf3ch2o。「鹵烷硫基」的實例包括CC13S、cf3s、 CC13CH2S及C1CH2CH2CH2S。「鹵烷亞磺醯基」的實例 包括 CF3S(=〇)、CC13S(=0)、CF3CH2S(=0)及 151284.doc 15 201117722 cf3cf2s(=o)。「鹵烷磺醢基」的實例包括cf3s(=o)2、 CC13S(=0)2、CF3CH2S(=0)2 及 CF3CF2S(=0)2。「烷基環 烷基」的實例包括2-氯環丙烷、2-氟環丁烷、3-溴環戊 烷及4-氯環己烷。「氟烷基」、「氟曱烷基」、「氟烷氧基」 及「氟曱氧基」的定義與「函烷基」以及「鹵烷氧基」 類似，除非特別指明。因此，「氟曱氧基」包括CH2FO、 CHF20 及 CF3〇 〇 取代基中碳原子數目是根據「Ci-Cj」字首，其中i 及j係數字1至14 ^例如，C1-C4烧橫醯基表示曱續醯 基至丁磺醯基；C2烷氧烷基代表CH3OCH2 ; c3烷氧烷 基代表，例如：CH3OCH2CH2或CH3CH2OCH2 ;以及 C4烧氧烧基代表一個烧基的多種異構物，以一個包含總 數4個碳原子的烷氧基取代，實例包括 CH3CH2CH2OCH2 以及 CH3CH2OCH2CH2。 術語「未經取代的」係針對一個基群’例如一個環 或是環系統意為該基群除了其一或是多個式i其餘部 份之附屬外不具有任何取代基。術語「視情況經取代」 意為取代基之數量可能為零。除非另有說明，可選擇地 經取代的基團可經和可容許數目一樣多的可選擇性取 代基取代，藉由以非氫取代基在任何可得的碳原子或氮 原子上取代氫原子。如同在此使用的，術語「視情況地 取代」可與「可取代地或不可取代地」互相替換。 選擇性取代基的數目可經表明的限制所限制。例 如：片語「視情況以多達4個選自R3之取代基在碳原 I環員上取代及選自R4取代基在氮原子環員上取代」 意為可呈現G、卜2、3或4個取代基（如果潛在的連 151284.doc 16 201117722 接點數目允許的話）。當特定於取代基數目的範圍超出 在環上允許的取代基位置數目，在範圍中真實的較高端 經辨識為可用的位置數目。 在本發明的内容中，實例如Q1或Q2包含一個苯 基、α比α定基、塔0井基、鳴β定或嗤淋基環，各環之臨位、 間位及對位係關於該環與式1其餘部份之連接。更進一 步，當Q1或Q2包含一經由CH2連接鍵而附著至式1其 餘部份之苯環（意即苄基），苯環之臨位、間位及對位 係關於該環與ch2連接鍵之間之連結。 在該技術領域中，有多種已知的可製備芳香雜環及 環系統的方法；廣泛的回顧參見Comprehensive Heterocyclic Chemistry 第 8 卷冊，總編輯 a. R.QI Q2 Q is a phenyl, thienyl, thiazolyl, pyrazolyl, imidazolyl, pyridyl, hydrazine, pyrimidinyl, quinolinyl or a benzyl group, each optionally having up to 4 independently selected from R3. a substituent is substituted on a carbon atom ring member, and a substituent selected from R4 is substituted on a nitrogen atom ring member; Q疋 stupyl, porphinyl, oxime, β-pyrazolyl, imidazolyl, acridinyl, Each of 5 can selectively replace at least four substituents selected from the group consisting of the R atomic ring family and the R6 nitrogen atom ring family; each of R and R is independently Octocin, cyano, nitro, Ci_C3 alkyl, CK: 3 decyl, ce fast, cyclopropyl, crc3 halo, f, C2-C3 (tetra), Ci-C3 alkoxy, c]-c3 Oxy Cl-C3 alkylthio, Crc3 dentate thio or crC7 hydroxyalkyl; 151284.doc 201117722 Each R3 and R5 are independently halogen, cyano, hydroxy, nitro, CVC7 leukox, C2-C7 , C2-C7 fast radical, C2-C7 cyanocarbyl, CrC7 alkyl, C2-C7-alkenyl, C3-C7 cycloalkyl, C3-C7 haloalkyl, CfCio alkyl, C4, Ci〇cycloalkane, c6-c14 cycloalkanecycloalkyl C3-c7 cycloalkoxy, 匸3_〇7 halocycloalkyloxy, C1-C7 alkoxy, C2-C7 nitrogen alkoxy, CVC7 haloalkoxy, CrQ alkylthio, crc7 , C]-C7, succulent base, C1-C7 calcined base, crc7 haloalkyl sulfinyl, crc7 halosulfonyl, α-(: 7 alkylamino, C2-C7 bisalkylamine , c2-c7 alkylcarbonyl, CH: 7 alkoxycarbonyl, amine carbonyl, c2_c7 alkylamine carbonyl, q-C7 bisalkylamine carbonyl, c2_c7 alkylcarbonylamino, c3-C10 trialkyl fluorenyl, -SCN, C (= S) NH2 or -XUZ; each R4 and R6 are independently cyano, Q-C6 alkyl, C3-C6 alkenyl, c3-c6 alkynyl, crC6 aldentyl, c3-c6 cycloalkyl, crc6 oxygenated a group, a C2-C6 alkoxyalkyl group, a c2-c6 alkyl group, a c2_c6 alkoxycarbonyl group, a C2-C6 alkylamino group or a c3-c6 bisalkylaminoalkyl group; each X system is independently 〇, s (=0 n, NR7 or a direct bond; each of the 11 series is independently a CrCHt alkyl group, a c2-c6 alkenyl group, a c3-c6 alkynyl group, a CrC6 cycloalkyl group or a C3-C6 cycloalkenyl group, wherein The three carbon atoms are independently selected from c(=0), each optionally up to five independently selected from the group consisting of dentate, cyano, nitro, thiol, CVC6 alkyl, crc6 from alkyl, crc6 alkoxy. And CrC6 Substituted by alkoxy substituents; each z is independently NR8aR8b, 〇R9 or s(=〇)nRio; 151284.doc • 6 _ 201117722 Each R7 is independently H'CVQ alkyl, CrC6 haloalkyl, C2 -C6 alkylcarbonyl, c2-c6 alkoxycarbonyl, c2-c6(alkylthio)carbonyl, c2_c6 alkoxy (thiocarbonyl), c4-c8 cycloalkylcarbonyl, c4-c8 cycloalkoxycarbonyl, c4-c8 (cycloalkylthio)carbonyl or cvcpfalkoxy (thiocarbonyl); each of 1183 and R8b is independently Η, C "C6 alkyl, CrC6 haloalkyl, c2-c6 alkenyl, c3-c6 alkynyl c3- C6 cycloalkyl, c3-c6 alkylcycloalkyl, c2-c6 alkylcarbonyl, c2-c6 alkoxycarbonyl, c2-c6(alkylthio)carbonyl, c2-c6 alkoxy (thiocarbonyl), C4_C8 ring Alkyl | ί carbon, c4-c8 cycloalkoxy, c4-c8 (cycloalkylthio)carbonyl or (: 4-(:8 cycloalkoxy (thiocarbonyl); each R9 and R10 are independently Η, 〇 (: 6 alkyl, CrC6 haloalkyl, C2-C6-branched, C3-C6 alkynyl, C3-C6 cycloalkyl, C3-C6-based cycloalkyl, C2-C6 alkyl, C2 -C6 aerobic acid group, QrC6 (alkylthio)carbonyl group, c2-C6 alkoxy group (thiocarbonyl group), CrQ ring-based group, Q-C8 ring-oxygen group, C4-C8 (cyclic sulfur group) a carbonyl group or a C4-C8 cycloalkoxy group (thiocarbonyl group); each η system is independently hydrazine, 1 or 2; and (b) at least one additional fungicidal compound. The invention also relates to a composition comprising: (a) at least one compound selected from the foregoing formula 1, a N-oxide thereof and salts thereof; and at least one compound or agent for the control of invertebrate pests. The invention also relates to a composition comprising one of the foregoing compositions comprising component (a) and at least one selected from the group consisting of an interface active agent, a solid diluent, and a diluent. Doc 201117722 The invention also relates to a method of controlling a plant disease caused by a fungal plant pathogen, the method comprising administering to the plant or a part thereof, or a plant seed, an effective fungicidal dose of one of the foregoing compositions. The foregoing method can also be described as a method of protecting a plant or plant seed from infection with a plant disease caused by a fungal plant pathogen, the method comprising the plant (or part of the plant) or the plant seed (directly or by borrowing An effective fungicidal dose of one of the foregoing compositions is administered by the environment of the plant or plant seed (e.g., growth medium). In a still further aspect, the invention also relates to a compound selected from Formula 1 (including all stereoisomers), N-oxides thereof and salts thereof as defined above, when Q1 is phenyl, thiophene, 嗟β Sitting base, ° than β base, taste. When sitting on a base, a ratio of a bite base, a tower base, a thiol group, a sulfhydryl group, or a sulfhydryl group, each of the four substituents independently selected from the ulnar 33 is substituted on the carbon atom ring. a substituent selected from R4a is substituted on a nitrogen atom ring; wherein each R3a is independently halogen, cyano, hydroxy, nitro, CrC7 alkyl, C2-C7 alkenyl, C2-C7 alkynyl, CrC7 haloalkyl , C2-C7 halogen baking base, C3-C7 bad burning base, C3-C7 halogen king smoldering base, C4-C10 calcining base, C4-Ci〇i smoldering base, c6-c14 cycloalkane cycloalkyl , c3-c7 cycloalkoxy, C3-C7 halocycloalkyloxy, CVC7 alkoxy, CVC7 halogen alkoxy, Ci-C6 thiol, C1-C7 _ sulphur-based, C1-C7 sinter Stuffed base, C]-C7 calcined base, C1-C7 halogenated subcontinuation base, CpC7 halogenated continuous base, C1-C7 151284.doc 201117722 Amine base, C2-C7 dialkylamine, C2- a C7 alkylcarbonyl group, a c2-c7 alkoxycarbonyl group, a c2_c7 alkylcarbonylamino group, a c3_Ci〇 tris-sulfonyl group, -SCN, C(=S)NH2 or -XUZ; and each of the 43 series is independently a cyano group, a crc6 alkyl group , c3-c6 alkenyl, c3-c6 alkynyl, c3-c6 cycloalkyl, crc6 alkoxy, c2-c6 alkoxyalkyl, C2-C6 alkylcarbonyl, c2-c6 Oxycarbonyl, c2-c6 alkylaminoalkyl or c3-c6 bisalkylamine alkyl; and Q-based, β-septyl, β-sulphate, oxime, β-salt, pyridine a fluorenyl group, a pyrimidinyl group, a quinolyl group or a phenyl group each substituted with 1 to 4 substituents independently selected from R 5 on a carbon atom ring member and a substituent selected from R 6 substituted on a nitrogen atom ring member; The limiting condition is that at least one substituent on the carbon atom ring is a c2-c7 cyanoalkyl group, a CVC7 cyano alkoxy group, an amine group, an eve? aminyl group or a CrC7 bisalkylamine carbonyl group, or a ring of a nitrogen atom. The substituent on the member is a CpC6 tooth-burning group. The invention also relates to a fungicidal composition comprising a fungicidal effective amount of a compound selected from the foregoing further aspects and at least one additional component selected from the group consisting of an surfactant, a solid diluent and a liquid diluent. The invention still further relates to a method for controlling a plant disease caused by a fungal plant pathogen, which comprises administering a plant, a part of its tissue or a plant seed, a fungicidal effective amount selected from the compounds of the foregoing further aspect. [Embodiment] 151284.doc 201117722 "Eight = this use, the terms "including", "including", "having", "having", "characteristic" or any other change of the term, is intended to mean f He is sexually included and subject to any express restrictions. The compositions, mixtures, processes or methods that comprise a list of elements are not necessarily limited to those elements, but may include other elements not specifically listed or inherent to the composition, mixture, process or method. The primary conjunction "consisting of" excludes any element, step or ingredient that is not explicitly stated. If it is in the scope of patent application, such a term will cover the scope of the patent, so that it will not include anything other than the enumeration. When a conjunction is composed of a word that appears in a request item, rather than immediately following the preface, the conjunction is limited to the elements that appear in the preceding clause, and the other is not excluded from the request as a whole. element. The term "consisting essentially of" is used to define a group or method that includes materials, steps, features, components or elements other than those disclosed herein, provided that such additional materials, steps, features, The ingredients or elements do not materially affect the basic and novel characteristics of the claimed invention. The term "mainly consists of ... in the middle zone between "contains" and "consisting of". When an applicant uses an open term, such as "contains", to define an invention or part thereof, it should be easy to understand (unless otherwise stated) that the statement should be interpreted as also using the term "mainly composed of" or The "consisting of" describes the invention. In addition, unless expressly stated to the contrary, "or" means an inclusive "or" rather than an exclusive "or". For example, any of the following is full of the new A or B: A is true (or exists) I5I284.doc • 10- 201117722 and B is false (or non-existent), A is false (or broken) And b is true (or exists 'and both A and B are true (or exist). And the indefinite article "-" before the element or compound that appears in the invention tends to be unqualified (ie Occurs) The number of examples of compounds. Because, "-3⁄4"一/田^, prisoner one or one" should be understood to include - or at least - and the singular form of the element or component also includes the plural Unless the number is obviously singular. As mentioned in the disclosure and the scope of the application, "plants" include members of the plant kingdom - especially all life stages of seed plants (Spermat〇PSida), including young plants. (eg, sprouting seeds develop into seedlings) and mature reproductive stages (such as plants that produce flowers and seeds). The parts of the plant include the ground parts that are usually grown on the surface of the growth medium (such as soil), such as roots, tubers, Bulbs and bulbs, as well as growing The parts that grow qualitatively, such as leaves (including stems and leaves), flowers, fruit and seeds. As mentioned in this article, the term "seedlings", whether used alone or in combination with other words, means from one kind of Young plant with germ development. The term "burning agent" as used herein relates to a compound in which a 3 stone counter radical is bonded to a debonding group via a carbon atom, such as a halide or sulfonic acid. a salt, which can be replaced by bonding a nucleophilic agent to the aforementioned carbon atom. Unless specifically emphasized, the term "burning" does not limit the carbon-containing radical to an alkyl group; the carbon-containing radical in the alkylating agent includes a plurality of The substituted radicals of the bonded carbons are, in particular, R1 and R2. The term 'alkyl group' in the above detailed description may be used alone or in combination with a compound such as "alkylthio" or "haloalkyl". Linear or 151284.doc -11 - 201117722 疋 branched chain base, for example, decyl ethyl, n-propyl, isopropyl, or different butyl, pentyl, hexyl or heptyl isomers. Contains a straight _ chain or a branched olefin Hydrocarbons such as vinyl, propylene, 2-propenyl, and different butenyl, pentenyl, hexenyl, and heptenyl isomers. "Alkenyl" also includes polyenes such as 1,2-propylene. And 2,4-hexadiene. "Alkynyl" includes straight-chain or branched acetylene hydrocarbons such as ethynyl, propynyl, 2-propynyl and different butynyl, pentynyl, hexyne And heptynal isomers. "Alkynyl" may also include a moiety comprising a plurality of triple bonds, such as 2,5-hexanediyl. "Benzonitrile" means a straight or branched double burn. Examples of "alkylene" include ch2, ch2ch2, ch(ch3), CH2CH2CH2, CH2CH(CH3), and different butyl, pentyl and hexyl isomers. "Acekenyl group" means that a straight or branched double alkenyl group contains a ketoene bond. Examples of "alkenyl groups" include CH=CH, CH2CH=CH, and CH=C(CH3). "Alkynyl" means a straight or branched fast diyl group containing a single bond. Examples of the "alkynyl group" include CH2?C, OCCH2, and various butyrynyl, pentynyl and hexynyl isomers. "Alkoxy" includes, by way of example, decyloxy, ethoxy, n-propoxy, isopropoxy and the different butoxy, pentyloxy, hexyloxy and heptyl isomers. "Alkylthio" includes branched or straight-chain alkylthio moieties such as sulfonylthio, ethylthio, and different propylthio, butylthio, pentylthio, hexylthio and heptylthio isomers. . "Alkylsulfinyl" includes a diastereomer of a group of alkylsulfinyl groups. Examples of "alkylsulfinyl" include ch3s(=o), CH3CH2S(=0), ch3ch2ch2s(=o), (ch3)2chs(=o), and different butane sulfinyls, pentacene Stuffed base, hexahydrate and succulent base and Geng Shaoya continuation base 151284.doc •12· 201117722 Structure. Examples of "alkylsulfonyl" include ch3s(=o)2, ch3ch2s(=o)2, ch3ch2ch2s(=o)2, (CH3)2CHS(=0)2, and different butanesulfonyl, pentane Alkylsulfonyl, hexanesulfonyl and heptanesulfonyl isomers. The "alkylamino group" includes an NH radical substituted with a linear or branched alkyl group. Examples of the "alkylamino group" include CH3CH2NH, CH3CH2CH2NH, and (CH3)2CHCH2NH. Examples of the "dialkylamino group" include (CH3)2N, (CH3CH2CH2)2N and CH3CH2(CH3)N. "Cyanoalkyl" means an alkyl group substituted with a ketocyano group. Examples of "cyanoalkyl" include ncch2, ncch2ch2, and CH3CH(CN)CH2. "Alkoxyalkyl" means an alkoxy group at the alkyl position. Examples of the "alkoxyalkyl group" include CH3OCH2, CH3OCH2CH2, CH3CH2OCH2, CH3CH2CH2CH2OCH2, and CH3CH2OCH2CH2. "(Alkylthio)carbonyl" means a straight or branched alkylthio group bonded to a moiety c(=o). Examples of the "(alkylthio)carbonyl group" include ch3sc (=o), ch3ch2ch2sc (=o), and (ch3)2chsc (=o). "Alkoxy (thiocarbonyl)" means a straight or branched alkoxy group bonded to the c(=s) moiety. Examples of the "alkoxy (thiocarbonyl)" include CH3OC(=S), CH3CH2CH2OC(=S), and (CH3)2CHOC(=S). "Alkylaminoalkyl" means an alkylamino group at the alkyl position. Examples of the "alkylamine alkyl group" include CH3NHCH2, ch3nhch2ch2, ch3ch2nhch2, CH3CH2CH2CH2NHCH2, and CH3CH2NHCH2CH2. Examples of the "dialkylaminoalkyl group" include ((ch3)2ch)2nch2, (CH3CH2CH2)2NCH2, and CH3CH2(CH3)NCH2CH2. The term "alkylcarbonylamino" means an alkyl group bonded to a portion of C(=0)NH. Examples of the "alkylcarbonyl 151284.doc -13- 201117722 amine group" include ch3ch2c(=o)nh and ch3ch2ch2c(=o)nh. "Hydroxyalkyl" means an alkyl group substituted with a ketohydroxy group. Examples of the "hydroxyalkyl group" include HOCH2CH2, CH3CH2(OH)CH, and HOCH2CH2CH2CH2. "Cycloalkyl" includes, for example, cyclopropyl, cyclobutyl, cyclopentyl, %; hexyl and J-heptyl. The term "burning" refers to an alkyl group substitution on a partial ring, and includes, for example, ethylcyclopropyl, isopropylcyclobutyl, methylcyclopentyl, and anthracenyl. The term "cycloalkylalkyl" means substituted by a cycloalkyl group on the alkyl moiety. Examples of the "cycloalkylalkyl group" include a cyclopropenyl group, a cyclopentyl group, and other cycloalkyl moieties bonded to a linear or branched alkyl group. The term "cycloalkanecycloalkyl" means a cycloalkyl substitution of another cycloalkyl ring wherein each cycloalkyl ring independently has from 3 to 7 carbon atoms. Examples of the cycloalkyl group include cyclopropylcyclopropyl (for example: 1, fluorenyl-dicyclopropyl-1-yl, ^'-dicyclopropyl-2-ylcyclohexylpentyl (for example, 4- Cyclopentacyclohexyl) and cyclohexylcyclohexyl (for example: 1,1,-dicyclohexyl-1-yl), and different forward and reverse cycloalkylcycloalkyl isomers (eg, (1R, 2S)-1,1,-dicyclopropyl-2-yl and ^dicyclopropyl-2-yl). The term "cycloalkoxy" denotes a ring-bonding group of a bonding and an oxygen atom, which includes For example, cyclopentyloxy and cyclohexyloxy. "Cycloalkylene" means a cycloalkyl group bonded to a -C(=Q) group, and contains, for example, cyclopropylcarbonyl and cyclopentylcarbonyl. "Cycloalkoxycarbonyl" refers to a cycloalkyloxy group bonded to a C(=〇) group, such as cyclopropoxycarbonyl and cyclopentyloxycarbonyl. The term "cycloalkyl" means a cycloalkanediyl ring. Examples of the "cycloalkylene group" include a cyclic propyl group, a cyclic stretching T group, a cyclic pentyl group, and a 151284.doc •14·201117722 ring-extension hexyl group. The term "cycloalkenyl group" means a ring containing an olefinic bond. Examples of the "cycloalkenyl group" include a cyclopropenyl group and a cyclopentenyl group. "Alkylcarbonyl" means a straight or branched alkyl group bonded to the c(=o) moiety. Examples of "alkylcarbonyl" include ch3c(=o), CH3CH2CH2C(=0) and (CH3)2CHC(= 0) Examples of "alkoxycarbonyl" include ch3oc(=o), ch3ch2oc(=o), ch3ch2ch2oc(=o), (ch3)2choc(=o), and different butoxycarbonyl, pentoxy groups and Oxyl isomers. "Trialkylsulfonyl" includes three branched and/or linear alkyl groups attached and linked via a halogen atom, such as trimethylsulfanyl, triacetyl, and tertiary-butane矽alkyl. The term "dentate", whether used alone or in a compound such as "dental alkyl" or used in the description of "alkyl substituted by a conjugate", includes fluorine and gas. , bromine or iodine. In addition, when used in a compound such as "haloalkyl" or in the description of "alkyl substituted by an element", the alkyl group may be the same or different The halogen atom is partially or completely substituted. Examples are "haloalkyl" or "halogen substituted by halogen", including F3c, C1CH2, CF3CH2 and CFsCCl2. Alkenyl", "haloalkoxy", "haloalkylthio", "haloalkylsulfinyl", "dental sulfonyl", "alkylcycloalkyl", "halocycloalkoxy" Etc., similar to the definition of the term "haloalkyl". Examples of "haloalkenyl" include C12C=CHCH2 and CF3CH2CH=CHCH2. Examples of "haloalkoxy" include cf3o, cci3ch2o, f2chch2ch2o and cf3ch2o. Examples of the base include CC13S, cf3s, CC13CH2S, and C1CH2CH2CH2S. Examples of "haloalkylsulfinyl" include CF3S (=〇), CC13S (=0), CF3CH2S (=0), and 151284.doc 15 201117722 cf3cf2s (=o). Examples of "haloalkylsulfonyl" include cf3s(=o)2, CC13S(=0)2, CF3CH2S(=0)2, and CF3CF2S(=0)2. Examples of the "alkylcycloalkyl group" include 2-chlorocyclopropane, 2-fluorocyclobutane, 3-bromocyclopentane and 4-chlorocyclohexane. The definitions of "fluoroalkyl", "fluoroalkyl", "fluoroalkoxy" and "fluoroalkoxy" are similar to "alkyl" and "haloalkoxy" unless otherwise specified. Therefore, the number of carbon atoms in the substituents of "fluorofluorooxy" including CH2FO, CHF20 and CF3 is based on the "Ci-Cj" prefix, where i and j are numbers 1 to 14 ^ For example, C1-C4 burns 醯The group represents a fluorenyl group to a butasulfonyl group; the C2 alkoxyalkyl group represents CH3OCH2; the c3 alkoxyalkyl group represents, for example, CH3OCH2CH2 or CH3CH2OCH2; and the C4 alkoxyalkyl group represents a plurality of isomers of a burning group, An alkoxy group containing a total of 4 carbon atoms is substituted, examples of which include CH3CH2CH2OCH2 and CH3CH2OCH2CH2. The term "unsubstituted" is intended to refer to a group ', e.g., a ring or ring system, meaning that the group does not have any substituents other than one or more of the remainder of the formula i. The term "optionally substituted" means that the number of substituents may be zero. Unless otherwise indicated, an optionally substituted group may be substituted with as many optional substituents as may be tolerated, by substituting a hydrogen atom at any available carbon or nitrogen atom with a non-hydrogen substituent. . As used herein, the term "optionally substituted" may be interchanged with "substitutable or irreplaceable". The number of selective substituents can be limited by the limitations indicated. For example, the phrase "optionally substituted with up to 4 substituents selected from R3 on the carbon ring I ring member and selected from the R4 substituent group on the nitrogen atom ring member" means that G, Bu 2, 3 can be present. Or 4 substituents (if potential 151284.doc 16 201117722 number of contacts allowed). When the range specific to the number of substituents exceeds the number of substituent positions allowed on the ring, the true higher end in the range is recognized as the number of positions available. In the context of the present invention, an example such as Q1 or Q2 comprises a phenyl group, an alpha ratio alpha group, a tower 0 base group, a ringing beta group or a sulfhydryl ring, and the ring, meta and para are associated with each ring. The connection of the ring to the rest of Equation 1. Further, when Q1 or Q2 comprises a benzene ring (ie, benzyl group) attached to the rest of Formula 1 via a CH2 linkage, the pro, meta and para positions of the benzene ring are related to the ring and the ch2 linkage. The link between them. There are a number of known methods in the art for the preparation of aromatic heterocyclic rings and ring systems; for a comprehensive review, see Comprehensive Heterocyclic Chemistry Volume 8, Editor-in-Chief a. R.

Katritzky 及 C. W. Rees, Pergamon Press，Oxford，1984 及 Comprehensive Heterocyclic Chemistry II 第 12 卷冊，總 編輯 A. R. Katritzky，C. W. Rees 及 E. F. V. Scriven， Pergamon Press，Oxford，1996 ° 興尽赞明有關的化合物可以一個或多個立體異構 物的方式存在。各種立體異構物包括鏡像異構物、非鏡 像異構物、阻轉異構物和幾何異構物。熟f該領域之技 藝人士將明瞭’-個立體異構物當相對於其他立體昱構 物經濃化或當從其他立體異構物經分離㈣，可能活性 更高及/或可能展示出有益的效果。此外 域之技藝人士知道如何分離、濃;4邊 张、十.☆辨丄 ，辰化及/或選擇性地製備 所述立體⑽物。本發日⑽化合物相 合，單一立體異構物的方式呈現(例如以= 形式）、、為值得注意的是阻轉異構物，構型異構物， 15l284.doc 201117722 此構型異構物發生在當一個分子的單鍵旋轉經限制在 由於與其他部分的分子的立體交互作用以及在單鍵兩 鈿的取代基不對稱。在本發明中，阻轉異構物發生在式 1的單鍵當旋轉障能夠高時（大約>25 kcal ^οΓ1) 使在室溫下分離異構物變為可能。熟習該領域之技藝人 士將明瞭，一個阻轉異構物當相對於其他阻轉異構物經 濃化或當從其他阻轉異構物經分離出時，可能活性更高 及/或可能展示出有益的效果。此外，該熟習該領域之 技藝人士知道如何分離、濃化及/或選擇性地製備所述 阻轉異構物《阻轉異構物之詳細描述可以在March，Katritzky and CW Rees, Pergamon Press, Oxford, 1984 and Comprehensive Heterocyclic Chemistry II Volume 12, Editor-in-Chief AR Katritzky, CW Rees and EFV Scriven, Pergamon Press, Oxford, 1996 °. The compounds concerned can be one or more The stereoisomers exist in a way. Various stereoisomers include mirror image isomers, non-mirror isomers, atropisomers, and geometric isomers. Those skilled in the art will recognize that a stereoisomer may be more active and/or may exhibit beneficial effects when concentrated relative to other stereogenic structures or when separated from other stereoisomers (4). Effect. Further, those skilled in the art know how to separate and concentrate; 4 sides, 10, ☆, and/or selectively prepare the stereo (10). The compound of the present invention (10) is present in a single stereoisomer (for example, in the form of =), and is notable for the atropisomer, the configuration isomer, 15l284.doc 201117722. The occurrence of a single bond rotation when a molecule is restricted is due to the stereo interaction with the molecules of other moieties as well as the asymmetry of the substituents in the two bonds of the single bond. In the present invention, the atropisomer occurs in the single bond of Formula 1 when the rotation barrier can be high (about > 25 kcal ^οΓ1) making it possible to separate the isomer at room temperature. It will be apparent to those skilled in the art that an atropisomer may be more active and/or may exhibit when concentrated relative to other atropisomers or when isolated from other atropisomers. A beneficial effect. In addition, those skilled in the art will know how to separate, concentrate and/or selectively prepare the atropisomers. A detailed description of the atropisomers can be found in March.

Advanced Organic Chemistry，4th Ed. 1992，101-102 及 Gawronski et al” Chirality 2002, 14, 689-702 中找到。本 發明包括濃化進式1之阻轉異構物的化合物或組合物 相對於其他化合物的阻轉異構物。本發明亦包含式1的 化合物之實質上純的阻轉異構物。 熟習該領域之技藝人士將明瞭，並非所有含氮雜環 皆可形成氮氧化物，因為氮原子需要一個可利用的孤立 電子對以氧化成氧化物；熟習該領域之技藝人士亦將明 瞭三級胺可形成氮氧化物。製備雜環的氮氧化物以及三 級胺的合成方法對於熟習該領域之技藝人士已廣泛知 悉，該方法包括以過氧酸例如過氧乙酸以及間氯過氧苯 乙酸、過氧化氫、烧基氫過氧化物例如過氧化三級丁 基、過侧酸鈉，以及雙環氧乙烧例如二曱基雙環氧乙烧 來氧化雜環以及三級胺。此些製備氮氧化的方法已在文 獻中經廣泛地描述以及回顧’例如.T. L. Gilchrist inAdvanced Organic Chemistry, 4th Ed. 1992, 101-102 and Gawronski et al" Chirality 2002, 14, 689-702. The invention includes compounds or compositions that are concentrated to the atropisomer of Formula 1 relative to others. Atropisomers of the compounds. The present invention also encompasses substantially pure atropisomers of the compounds of Formula 1. It will be apparent to those skilled in the art that not all nitrogen-containing heterocycles can form nitrogen oxides because The nitrogen atom requires an available pair of isolated electrons to oxidize to form oxides; those skilled in the art will also recognize that tertiary amines can form nitrogen oxides. The synthesis of heterocyclic nitrogen oxides and tertiary amines is familiar to It is widely known to those skilled in the art that the process includes peroxyacids such as peroxyacetic acid and m-chloroperoxyphenylacetic acid, hydrogen peroxide, alkyl hydroperoxides such as tributyl peroxide, sodium peracetate. And bis-epoxyethanes such as dimercaptobis epoxide to oxidize heterocycles and tertiary amines. Such methods for preparing nitrogen oxidation have been extensively described in the literature and reviewed 'for example. TL Gilchrist in

Comprehensive Organic Synthesis，vol. 7, pp 748-750, S. 151284.doc 201117722 V. Ley, Ed.，Pergamon Press ; M. Tisler 及 B. Stanovnik in Comprehensive Heterocyclic Chemistry, vol. 3, pp 18-20, A. J. Boulton 及 A. McKillop, Eds.，Pergamon Press;M. R. Grimmett Bl B. R. T. Keene in Advances in Heterocyclic Chemistry, vol. 43, pp 149-161, A. R. Katritzky, Ed., Academic Press ;M. Tisler 及 B. Stanovnik in Advances in Heterocyclic Chemistry, vol. 9, pp 285-291, A. R. Katritzky 及 A. J. Boulton，Eds., Academic Press ; and G. W. H. Cheeseman 及 E. S, G. Werstiuk in Advances in Heterocyclic Chemistry, v〇l. 22, pp 390-392, A. R. Katritzky 及 A. J. Boulton，Eds.，Academic Press。 熟習該領域之技藝人士瞭解到，因為化合物的鹽類 與它們對應的非鹽形式在環境和生理條件下會處於平 衡狀態，所以鹽類會分享非鹽形式的生物效用。因此， 廣泛而多種不同的式1之單獨以及混合之鹽類化合物 對於防治由真菌植物病原所造成的植物疾病是有效 的。（即是農業上適用的）。式丨化合物的鹽類包括含有 機酸或無機酸的酸添加鹽類，酸像是氫溴酸、鹽酸、硝 酸、磷酸、硫酸、乙酸、丁酸、延胡索酸、乳酸、順丁 烯二酸、丙二酸、草酸、丙酸、水楊酸、酒石酸、4_曱 苯石黃酸或戊酸。因此，本發明關於選自式丨、氮氧化物 以及其農業上適用之鹽類的化合物。 選自式1的化合物’幾何的以及其他立體異構物、 氮氧化物以及其鹽類，通tJ^於—侧形式存在，而 式1因此包括式1代表的所有結晶^以及非結晶型化合 物。非晶形包括像是壤和膠的固體實關，也包括像是 151284.doc 201117722 溶液和熔體的液體實施例。結晶型包括必須呈現一單一 結晶型態以及呈現一多形體之混合物的實施例。（即^ 同的結晶型）。術語「多形體」意指一可以結晶成不同 晶形之化合物的特定晶形，這些形式的晶格内分子有不 同的排列及/或構形。雖然多形體可以有同樣的化學組 成，它們也可以在組成上因為共結晶水或其他分子=存 在或不存在而不同，該共結晶水或其他分子可以弱或= 地結合在晶格内。多形體可以在化學、物理和生物特性 有所不同，像是晶體形狀、密度、硬度、顏色、化學穩 定性、熔點、吸濕性、懸浮率、溶解速率和生物利用度: 熟習§亥領域之技藝人士將瞭解到由式1所呈現的化人 物多型性相對於式1呈現的同樣化合物之其他多形體 或是多形體的混合物可展現有益之效果（例如適合於製 備有用的配方以改善生物利用效果）製備或分離由式i 所呈現的特殊化合物多形體可藉由熟席此技術領域人 士所通曉的方法來達成，例如，利用特定的溶劑及溫度 來進行結晶。 如發明概要中所述，本發明中的一個態樣係關於一 個組合物，包含（a)至少一個選自式1之化合物、其 N-氧化物及其鹽類，與（b)至少一種附加的殺真菌化 合物。更特定而言’組份（b )係選自由下列所組成之 群組： (bl)曱基苯并咪唑胺曱酸鹽（MBC)類殺真菌劑； (b2)二羧醯胺類殺真菌劑； (b3)脫曱基作用抑制劑（DMI)類殺真菌劑； (b4)苯胺類殺真菌劑； 151284.doc -20- 201117722 (b5)胺/嗎福林類殺真菌劑； (b6)填脂質生合成抑·類殺真菌劑； (b7)羧醯胺類殺真菌劑； (b8)羥基(2-胺基_)嘧啶類殺真菌劑； (b9)苯胺嘧啶類殺真菌劑； (ΜΟ)Ν-笨基胺甲酸鹽類殺真菌劑； (bU)醌外抑制劑（Q〇I)類殺真菌劑； (b12)苯基°比咯類殺真菌劑； (bl3)喹啉類殺真菌劑； (M4)脂質過氧化抑制劑類殺真菌劑； 〇15)”、'色素生合成抑制劑_還原酶（mbu)類 殺真菌劑； (M6)黑色素生合成抑制劑_脫水酶（mbi_d)殺 真菌劑； (bl7)羥基苯胺類殺真菌劑； (M8)鯊烯-環氧酶抑制劑類殺真菌劑； (M9)多氧菌素（poly〇xin)類殺真菌劑； (b20)苯脲類殺真菌劑； (b21)醌内抑制劑（QiI；)類殺真菌劑； (b22)苯曱醯胺類殺真菌劑； (b23)°比喃糖醛酸抗生素類殺真菌劑； (b24)己。比喃基抗生素類殺真菌劑； :蛋白質合成類殺真 (b25)吡喃葡萄糖苷抗生素： 菌劑； •繭蜜搪酶及肌醇生 (b26)。比喃葡萄糖苷抗生素： 合成殺真菌劑； 151284.doc -21- 201117722 (b27)氰肟乙醯胺類殺真菌劑； (b28)胺曱酸鹽類殺真菌劑； (b29)氧化磷酸化解偶合類殺真菌劑； (b30)有機錫類殺真菌劑； (b31)羧酸殺真菌劑； (b32)芳香雜環類殺真菌劑； (b33)膦酸鹽類殺真菌劑； (b34)鄰胺曱醯苯曱酸類殺真菌劑； (b35)苯並三畊殺真菌劑； (b36)苯-磺醯胺類殺真菌劑； (b37)嗒畊酮類殺真菌劑； (b38)噻吩-羧醯胺類殺真菌劑； (b39)嘧啶醯胺類殺真菌劑； (b40)羧酸醯胺（CAA)類殺真菌劑； (b41)四環素類抗生素殺真菌劑； (b42)硫代胺基曱酸鹽殺真菌劑； (b43)苯曱醯胺類殺真菌劑； (b44)誘發寄主植物防禦類殺真菌劑； (b45)多重作用類殺真菌劑； (b46)其餘非組分（a)及組分（bl)至（b45) 的殺真菌劑；以及 化合物（M)至（b46)的鹽類。 值得注意的是，其中組分（b)包含至少一殺真菌 劑且該殺真菌劑來自選自（bl)到（b46)中的二不同 群組的各一種殺真菌劑的實施例。 151284.doc •22- 201117722 w甲基笨并味唾胺甲酸鹽（MBC)殺真菌劑（b1)」 與板菌劑抗性作用委員會）代碼υ藉由在微 二二〜微管蛋白上來抑制有絲***。抑制 田二、^可中斷細胞分離、細胞以及細胞結構内傳輸。 曱基本开w胺㈣真_包括笨并咪切及多保淨 殺真菌劑。笨并料包括免賴得、貝芬替、t南基苯并 味嗤以及絲心。多保淨包括多保淨以及曱基多保 淨。 〆「二甲醯亞胺殺真菌劑（b2)」（FRAC：代碼2)經 建4來以NADH細胞色素c還原酶干擾抑制真菌中的 脂質過氧化作用。實例包括克氯得、依普同、撲滅寧以 及免克寧。 「脫曱基作用抑制劑（DMI)殺真菌劑（b3 )」（FRAC 代碼3)抑制固醇類產生中具有重要地位的C14_去曱基 酶。固醇，如麥角脂醇，為膜結構及機能所需，因而為 機能細胞壁發展之必要物質。因此，曝露於這些殺真菌 劑中會造成易感真菌的不正常生長並最終導致死亡。 DMI殺真菌劑係可分為數種化學分類：唑（包括***以 及咪唑）、嘧啶、哌畊、以及D比啶。該***類包括阿扎 康唑（azaconazole )、比多農（bitertanol )、溴克座 (bromuconazole )、環克座（cyproconazole )、待克利 (difenoconazole)、達克利（diniconazole)(包括達克 利-M)、依普座（epoxiconazole)、乙環σ坐（etaconazole)、 芬克座（fenbuconazole)、氣啥η全（fluquinconazole)、 護石夕得（flusilazole )、護汰芬（flutriafol )、菲克利 (hexaconazole )、易胺座（imibenconazole )、種菌口坐 151284.doc •23- 201117722 (ipconazole )、滅特座（metconazole )、邁克尼 (myclobutanil )、平克座（penconazole )、普克利 (propiconazole )、丙硫菌口坐（prothioconazole )、奎因 克座（quinconazole)、石夕氟嗤（simeconazole)、得克利 (tebuconazole )、四克利（tetraconazole )、三泰芬 (triadimefon )、三泰隆（triadimenol )、滅菌0坐 (triticonazole)及烯效0坐（uniconazole)。該味〇坐類包 括克霉°坐（clotrimazole )、滅癖洗劑（econazole )、依滅 列（imazalil )、異康唾（isoconazole )、σ米康0坐 (miconazole )、惡 口米0坐（oxpoconazole )、撲克拉 (prochloraz )、彼扶座（pefurazoate )及赛福座 (triflumizole)。該喊〇定類包括芬瑞莫（fenarimol)、尼 瑞莫（nuarimol)及癌菌醇（triarimol)。〇辰p井包括赛福 寧。該°比°定類包括得滅多（buthiobate )及比芬諾 (pyrifenox )。生化研究顯示以上所有殺真菌劑皆為 DMI 殺真菌劑，如 K. H. Kuck et al. in Modern Selective Fungicides-Properties, Applications and Mechanisms of Action, H. Lyr( Ed.)» Gustav Fischer Verlag ： New York » 1995 年，205-258 中所述。 「苯基酰胺殺真菌劑（M)」（FRAC代碼4)是卵 菌黴中RNA聚合酶的特定抑制劑。易感性真菌暴露於 此種殺真菌劑即降低將尿嘧啶結合入rRNA之能力。暴 露於此種殺真菌劑可防止易感真菌之生長以及發展。苯 基醯胺殺真菌劑包括醯丙胺酸類、噁唑烷酮類及丁内酯 類殺真菌劑。該醯丙胺酸類包括本達樂（benalaxyl)、 本達樂-Μ、霜靈（furalaxyl)、滅達樂（metalaxyl)、滅 151284.doc • 24- 201117722 (又為右滅達樂）。噁唑烷酮類包括毆殺斯。丁 内酉旨包括甲呋醯胺。 :胺/嗎福林殺真菌劑（b5)」（FRAc代碼5)抑制 姐固醇類生物合成途徑内的兩個標無位置，Δ8 — Δ7異 ^Ab ^ 逛原_。固醇，如麥角脂醇，為膜結構及 :所而，因而為機能細胞壁發展之必要物質。因此， 死路於此種殺真H劑將使易感真菌產生異常成長，最終 T。胺/嗎福林殺真菌劑（又稱為非DMI固醇生物合 P制物）包括嗎福林、哌啶以及螺縮酮-胺殺真菌劑。 =林包括巴丹、忙環㈣、芬普福、十三嗎啭以及 ㈣酿胺包括笨鏽咬以及粉病靈。螺縮酮胺包 括螺旋胺。 =月曰質生物合成抑制殺真菌劑（b6)」（FRAC代 馬6 )_藉由影響磷脂質生物合成來抑制真菌生長。磷脂 物δ成殺真菌劑包括硫代磷酸酯（ph〇Sph〇r〇thi〇late) 及一塞茂烷（dithiolane)殺真菌劑。硫代磷酸酯包括護 粒松、丙基喜樂松以及白粉松。二錢烧包括亞賜圃。 「羧醯胺殺真菌劑（b7)」（FRAC代碼7)藉由阻 斷克氏循環（TCA eyde)巾稱為琥賴脫氫酶的關鍵 酵素來抑制錯合物11 (琥⑽脫氫酶）真g呼吸作用。 抑制呼吸可預防真菌製造ATP，從而抑制成長以及繁 殖。敌醯胺殺真菌劑包括苯甲酸胺、咬⑽酿胺（furan Carb〇Xamide)、氧硫環羧醯胺（oxathiin carboxamide)、 嗟坐敌醯月女（thiazole carboxamide )、π比0坐叛g盛胺 (pyrazole carboxamide )及吡啶羧醯胺（pyridine carboxamide)。苯甲醯胺包括麥鏽靈、福多寧以及滅普 I51284.doc •25· 201117722Comprehensive Organic Synthesis, vol. 7, pp 748-750, S. 151284.doc 201117722 V. Ley, Ed., Pergamon Press; M. Tisler and B. Stanovnik in Comprehensive Heterocyclic Chemistry, vol. 3, pp 18-20, AJ Boulton and A. McKillop, Eds., Pergamon Press; MR Grimmett Bl BRT Keene in Advances in Heterocyclic Chemistry, vol. 43, pp 149-161, AR Katritzky, Ed., Academic Press; M. Tisler and B. Stanovnik in Advances in Heterocyclic Chemistry, vol. 9, pp 285-291, AR Katritzky and AJ Boulton, Eds., Academic Press; and GWH Cheeseman and E. S, G. Werstiuk in Advances in Heterocyclic Chemistry, v〇l. 22, pp 390-392, AR Katritzky and AJ Boulton, Eds., Academic Press. Those skilled in the art understand that because the salts of the compounds and their corresponding non-salt forms are in equilibrium under environmental and physiological conditions, the salts share the biological utility of the non-salt form. Therefore, a wide variety of different salt compounds of the formula 1 alone and in combination are effective for controlling plant diseases caused by fungal plant pathogens. (ie agriculturally applicable). The salts of the hydrazine compound include acid addition salts containing organic or inorganic acids, such as hydrobromic acid, hydrochloric acid, nitric acid, phosphoric acid, sulfuric acid, acetic acid, butyric acid, fumaric acid, lactic acid, maleic acid, and C. Diacid, oxalic acid, propionic acid, salicylic acid, tartaric acid, 4-pyrenequinic acid or valeric acid. Accordingly, the present invention relates to a compound selected from the group consisting of hydrazine, nitrogen oxides, and agriculturally acceptable salts thereof. The compound selected from the formula 1 is geometric and other stereoisomers, nitrogen oxides and salts thereof, which exist in the form of a side, and the formula 1 thus includes all the crystals represented by the formula 1 as well as the amorphous compound. . Amorphous forms include solids such as soil and gum, as well as liquid examples such as 151284.doc 201117722 solution and melt. Crystalline forms include those which must exhibit a single crystalline form and exhibit a mixture of polymorphs. (ie the same crystalline form). The term "polymorph" means a specific crystal form of a compound which can be crystallized into a different crystal form, and these forms of intramolecular molecules have different arrangements and/or configurations. Although polymorphs may have the same chemical composition, they may differ in composition due to the presence or absence of co-crystallized water or other molecules that may be weakly or = incorporated within the crystal lattice. Polymorphs can differ in chemical, physical, and biological properties, such as crystal shape, density, hardness, color, chemical stability, melting point, hygroscopicity, suspensibility, dissolution rate, and bioavailability: The skilled artisan will appreciate that a mixture of polymorphisms of the same character presented by Formula 1 relative to other polymorphs or polymorphs of the same compound presented by Formula 1 may exhibit beneficial effects (eg, suitable for preparing useful formulations to improve the organism) The preparation or isolation of the particular compound polymorph represented by Formula i can be accomplished by methods well known to those skilled in the art, for example, by the use of specific solvents and temperatures. As described in the Summary of the Invention, one aspect of the invention pertains to a composition comprising (a) at least one compound selected from Formula 1, its N-oxides and salts thereof, and (b) at least one additional Fungicidal compound. More specifically, 'component (b) is selected from the group consisting of: (bl) mercaptobenzimidazolium citrate (MBC) fungicides; (b2) dicarboxyguanamine fungicides (b3) demethylation inhibitor (DMI) fungicide; (b4) aniline fungicide; 151284.doc -20- 201117722 (b5) amine/folin fungicide; (b6 a lipid-synthesis fungicide; (b7) a carboxyguanamine fungicide; (b8) a hydroxy (2-amino-) pyrimidine fungicide; (b9) an aniline pyrimidine fungicide; (ΜΟ)Ν-stupyl carbamate fungicide; (bU) antimony inhibitor (Q〇I) fungicide; (b12) phenylpyrazole fungicide; (bl3) quinoline Fungicides; (M4) lipid peroxidation inhibitor fungicides; 〇15)", pigment biosynthesis inhibitors_reductase (mbu) fungicides; (M6) melanin synthesis inhibitors _ dehydration Enzyme (mbi_d) fungicide; (bl7) hydroxyaniline fungicide; (M8) squalene-epoxidase inhibitor fungicide; (M9) polyoxin fungicide (b20) phenylurea fungicide; (b21) intrasacral inhibition (QiI;) fungicides; (b22) benzoguanamine fungicides; (b23) ° uronic acid antibiotic fungicides; (b24) hexanyl antibiotic fungicides; : protein synthesis class killing (b25) glucopyranoside antibiotics: fungicides; • candied chymase and inositol (b26). glucopyranoside antibiotics: synthetic fungicides; 151284.doc -21- 201117722 ( B27) cyanoguanamine fungicide; (b28) aminide fungicide; (b29) oxidative phosphorylation decoupling fungicide; (b30) organotin fungicide; (b31) carboxy Acid fungicide; (b32) aromatic heterocyclic fungicide; (b33) phosphonate fungicide; (b34) o-amine phthalic acid fungicide; (b35) benzotriazole fungicide (b36) benzene-sulfonamide fungicide; (b37) chlorpyrifos fungicide; (b38) thiophene-carboxamide fungicide; (b39) pyrimidine amide amine fungicide; (b40) a carboxylic acid amide (CAA) fungicide; (b41) a tetracycline antibiotic fungicide; (b42) a thioamin phthalate fungicide; (b43) a benzoguanamine fungicide (b44) lure Host plant defense fungicide; (b45) multiplex fungicide; (b46) other non-component (a) and component (bl) to (b45) fungicide; and compound (M) to ( a salt of b46). It is noted that component (b) comprises at least one fungicide and the fungicide is derived from two different fungicides selected from the group consisting of (bl) to (b46) An embodiment. 151284.doc •22- 201117722 w methyl succinyl sulphate (MBC) fungicide (b1)" and plaque agent resistance committee) code υ by micro 22 ~ tubulin Inhibits mitosis. Inhibition of field II, ^ can interrupt cell separation, cell and cell structure transmission.曱 Basically open w amine (four) true _ including stupid and mites and more than a net fungicide. Stupid materials include free of charge, befenfen, t-nanben benzoate and silk. Multi-guarantee net includes multiple guarantees and 曱 多 多 。. 〆 "Dimethylimine fungicide (b2)" (FRAC: code 2) was constructed to interfere with the inhibition of lipid peroxidation in fungi by NADH cytochrome c reductase. Examples include chlorhexidine, ezine, chlorpyrifos and chlorhexidine. "Demethylation inhibitor (DMI) fungicide (b3)" (FRAC code 3) inhibits the C14_dethiolase, which is important in the production of sterols. Sterols, such as ergosterol, are required for membrane structure and function and are therefore essential for the development of functional cell walls. Thus, exposure to these fungicides can cause abnormal growth of susceptible fungi and ultimately death. DMI fungicides can be classified into several chemical classes: azoles (including triazoles and imidazoles), pyrimidines, piperculosis, and D-pyridines. The triazoles include azaconazole, bitertanol, bromuconazole, cyproconazole, difenoconazole, diniconazole (including Dakli- M), epoxiconazole, etaconazole, fenbuconazole, fluquinconazole, flusilazole, flurifaol, Fickley (hexaconazole), imibenconazole, phlebotomy 151284.doc •23- 201117722 (ipconazole), metconazole, myclobutanil, penconazole, propiconazole , prothioconazole, quinconazole, simeconazole, tebuconazole, tetraconazole, triadimefon, triadimenol , sterilized 0 sitting (triticonazole) and uniconazole (uniconazole). The miso sitting class includes clotrimazole, econazole, imazalil, isoconazole, miconazole, and moxa (oxpoconazole), poker (prochloraz), pefurazoate and triflumizole. The shouting class includes fenarimol, nuarimol, and triarimol. Yu Chen p well includes Sai Fanning. The ° ratios include buthiobate and pyrifenox. Biochemical studies have shown that all of the above fungicides are DMI fungicides, such as KH Kuck et al. in Modern Selective Fungicides-Properties, Applications and Mechanisms of Action, H. Lyr( Ed.)» Gustav Fischer Verlag : New York » 1995 Year, 205-258. "Phenylamide fungicide (M)" (FRAC code 4) is a specific inhibitor of RNA polymerase in the bacterium. Exposure of a susceptible fungus to such a fungicide reduces the ability to incorporate uracil into the rRNA. Exposure to such fungicides prevents the growth and development of susceptible fungi. Benzoguanamine fungicides include guanylalanines, oxazolidinones and butyrolactone fungicides. The alanines include benalaxyl, bunda-ruthenium, furalaxyl, metalaxyl, extinction 151284.doc • 24-201117722 (also dexteridine). Oxazolidinones include chlorpyrifos. Ding is intended to include metofuramide. : Amine/Fallin fungicide (b5)" (FRAc code 5) inhibits two standard no positions in the serotonin biosynthesis pathway, Δ8 - Δ7 iso ^Ab ^ _ original _. Sterols, such as ergosterol, are membrane structures and, therefore, essential for the development of functional cell walls. Therefore, the dead end of this kind of killing H agent will cause abnormal growth of susceptible fungi, and finally T. Amine/fofofin fungicides (also known as non-DMI sterol biopeptides) include orolin, piperidine, and spiroke-amine fungicides. = Lin includes Bataan, Busy Ring (IV), Fenfen, Thirteen, and (iv) Stearic amines including stupid bites and powdered spirits. The snail ketamine includes a helical amine. = lunar biosynthesis inhibits fungicides (b6)" (FRAC represents 6) - inhibits fungal growth by affecting phospholipid biosynthesis. The phospholipid delta fungicides include phosphorothioates (ph〇Sph〇r〇thi〇late) and a dithiolane fungicide. Phosphorothioates include granulated pine, propyl chelsson, and white pine. The two money burns include the Asian gift. Carboxylamine fungicide (b7) (FRAC code 7) inhibits complex 11 (a(10) dehydrogenase by blocking the key enzyme of the TCA eyde towel called abalone dehydrogenase ) true g respiration. Inhibition of breathing prevents fungi from producing ATP, thereby inhibiting growth and reproduction. The entamamine fungicide includes benzoic acid amine, furan Carb〇Xamide, oxathiin carboxamide, thiazole carboxamide, π to 0. Pyrazole carboxamide and pyridine carboxamide. Benzylamine includes wheat rust, butonine and chlorpyrifos I51284.doc •25· 201117722

2003/010149)。㈣_胺包括白克列。 +紅基(2_胺基-)嘴唆殺真菌劑（b8)」（FRAC代喝 8)藉由以腺料去_干擾抑制核酸合成。實例包括 布瑞莫、二曱嘧酚以及依瑞莫。 苯胺基+定殺真菌劑（b9)」（frac代碼9)經 建4於抑制胺基酸甲硫胺酸之生物合成以及阻斷在感 染過程中溶解植物細胞的水解酶分心實例包括赛普 达、@吐I、/ 12 -命麻一 #「Ν-苯基胺甲酸錄真菌劑（⑽） 」（FRAC代碼 =藉由在微管組合時結合到微管蛋白上來抑制有絲 H。抑概管組合可巾斷細胞分離、細胞傳輸及細胞 結構形成。實例包括乙霉咸。2003/010149). (d) _ amines include white gram. + Red base (2-amino-) mouth fungicide (b8)" (FRAC generation drink 8) inhibits nucleic acid synthesis by interfering with gland. Examples include bromo, dipyridamole, and errim. Anilino-based fungicides (b9)" (frac code 9) was established in 4 to inhibit the biosynthesis of amino acid methionine and to block hydrolase dissociation in plant cells during infection, including Cypress Da, @吐I, / 12 -命麻一# "Ν-Phenylamine formic fungicides ((10))" (FRAC code = inhibiting silk H by binding to tubulin when microtubules are combined) The combination of tubes can be used to separate cell separation, cell transport, and cell structure formation. Examples include beta-ammonium.

酿外抑制（qgI)殺真菌劑（b⑴」（FRAC代碼 曰由衫響泛醇氧化酶來抑制真菌巾錯合物ΙΠ粒線 泛醌氡化經阻擋於細胞色素bcl錯合物「醌 置，該錯合物位於真菌内粒線體膜之内。 吊真菌成長以及發展。醌外抑 稀酸、曱氧基胺基曱酸鹽、肟 二氫二η号畊殺真菌劑（整體上 抑制粒線體呼吸可防止正常真菌 制殺真菌劑包括曱氧基丙稀酸、 醚醋酸、肟醚乙醯胺以及二II _ 151284.doc • 26 - 201117722 以曱氧基丙烯酸酯殺真菌劑為大眾所知悉），以及惡唑 烷二酮、咪唑啉酮以及氨基曱酸苄酯殺真菌劑。曱氧基 丙烯酸包括亞托敏、烯肟菌酯（SYP-Z071)以及啶氧 菌醋。該曱氧基胺曱酸鹽類包括百克敏（pyraclostrobin ) 及嗤胺菌S旨（pyrametostrobin )。該經亞胺基醋酸鹽類包 括克收欣（kresoxim-methyl)、唑菌酯（pyraoxystr〇bin ) 及三氟敏（trifloxystrobin)。肟醚乙醯胺包括醚菌胺、 本氧菌胺两喊菌胺以及α-(甲氧亞胺基）_N-甲基 _2-[[[1-[3-(三氟曱基）苯基]乙氧基]亞胺基]甲基]苯醯 胺。二氫二P号畊包括氟嘧菌酯。惡唑烷二酮包括凡 杈同。咪唑啉酮包括咪唑菌酮。苯曱基胺酯包括防 霉丹。 「苯基吡咯殺真菌劑（bl2)」（FRAC代碼12)抑 制與真菌巾渗透信號傳導有_-個MAP蛋白質激 酶半種咯以及咯菌酯為此種殺真菌劑之實例。 「噎魏真菌劑（bl3)」（FRAc«碼⑴經提出 ‘ a早期細胞發出訊號的G蛋白來抑制訊號傳 止直：貞示可干擾真菌之萌芽及/或附著胞形成，防 八=霉病。快諾芬為此種殺真菌劑之實例。 代碼二過氧化作用抑制殺真菌劑（bl4)」（FRAC S用=議可用於抑制脂質過氧化作用韻 利’亦可能影響其他生物程此類樂齊1 ’如依得 物合成。液體過氧化反t直如二吸以及黑色素之生 應杈真函劑包括芳族碳以及 设真菌劑。芳香族碳包括聯苯、氯曱氧苯、 151284.doc -27- 201117722 氯硝胺、五氣石肖基苯、四氣硝基笨以及甲基立枯鱗。 1，2,4-售二β坐包括依得利。 「黑色素生物合成抑制-還原酶（MBI_R)殺真菌劑 (bl5)」（FRAC代碼16.1)抑制黑色素生物合成中萘 降低步驟。黑色素為某些真g傳_魅植物所必須。黑 色素生物合成抑制物-還原酶殺真菌劑包括異苯并呋喃 酮類、°比B各并噎琳類以及嘆坐苯并B塞哇殺真菌劑。異苯 并呋喃酮類包括熱必斯。吡咯并喹啉類包括百快隆^塞 0坐苯并嘆α坐包括三赛σ坐。 「黑色素生物合成抑制-脫水酶（Mbi_d)殺真菌 劑（bl6)」（FRAC代碼16.2)抑制黑色素生物合成中 之細特隆（scytalone)脫水酶。黑色素為某些真菌傳染 宿主植物所必須。黑色素生物合成抑制物脫水酶殺真 菌劑包括環丙烧幾醢胺、緩醢胺以及丙胺殺真菌劑。環 丙烷羧醯胺包括加普胺。羧醯胺包括雙氣氰菌胺。丙胺 包括氰菌胺。 「經基苯胺化物殺真菌劑（M7)」（FRAC代碼Π ) 抑制在固醇類產生中具重要地位的C4-去曱基酶。實例 包括環醯菌胺。 「鯊烯-環氧酶抑制殺真菌劑（bl8)」（FRAC代碼 18)在麥角固醇生物合成途徑中抑制鯊烯_環氧酶。固 醇如麥角固醇為膜結構及機能所需，因而為機能細胞壁 發展之必要物質。因此暴露於此些殺真菌劑導致不正常 的生長以及敏感性真菌的逐漸死亡。鯊烯-環氧酶抑制 物殺真菌劑包括硫胺酯以及烯丙基胺殺真菌劑。硫胺酉旨 包括稗草畏。烯丙基胺包括那夫梯芬以及特比那芬。 J51284.doc -28· 201117722 「多氧黴素殺真菌劑（M9)」（FRAC代碼I9)抑 制幾丁質合成酶。實例包括多氧菌素。 苯脲殺真菌劑（b20)」（FRAC代碼20)經建議 用於影響細齡裂。㈣包括賓克隆。 :酿内抑制（QiI)殺真菌劑（b21)」（FRAC代碼 21)藉由影響轉還原酶來抑制真菌帽合物πι粒線 ，呼及作泛1¾還原酶經阻擔於細胞色素be!錯合物 醌内」（Qi)位置，其位於真菌粒線體膜内。抑制粒 線體呼吸可防止正常真H成長以及發展。醒内抑制物殺 真菌劑包括氰咪唾類以及鄰伽胺三嗤殺真菌劑。氮味 唑包括赛座滅。鄰磺醯胺***殺真菌劑包括吲唑磺菌 胺。 「苯甲醒胺殺真菌劑（b22)」（FRAC代碼22)藉 由結合微管蛋白以及阻斷微管組成來抑制有絲分 裂。抑制微管組合可中斷細胞分離、細胞以及細胞結構 内傳輸。實例包括座賽胺。 「糖酸酸抗生素殺真菌劑（b23)」（FRAC代碼23) 藉由影響蛋白質生物合成來抑制真菌生長。實例包括保 米黴素。 「HexoPyranosyl抗生素殺真菌劑（b24)」（FRAC 代碼24)藉由影響蛋白質生物合成抑制真菌生長。實 例包括嘉賜黴素。 「σ比喃葡萄糖抗生素··蛋白質合成殺真菌劑（b25)」 (FRAC代碼25 )藉由影響蛋白質生物合成抑制真菌生 長。實例包括鏈黴素。 151284.doc •29· 201117722 「°比嘀葡萄糠抗生素：繭蜜糠酶以及肌醇生物合成 殺真菌劑（b26)」（FRAC代碼26)抑制肌醇生物合成 途徑中之繭蜜糖酶。實例包括維利黴素。 「氰基乙酰胺肟蟑真菌劑（b27)」（FRAC代碼27) 包括霜脲氰。 「胺甲酸鹽殺真菌劑（b28)」（FRAC代碼28)經 考慮為真菌生長的多位抑制劑。其可干擾細胞膜中之脂 肪酸合成’之後中斷細胞膜滲透性。普拔克、碘代丙炔 基丁基曱胺酸酯’以及胺丙威是此類殺真菌劑的實例。 「氧化磷酸化非偶合殺真菌劑（b29)」（FRAC代 碼29)藉由非偶合氧化磷酸化抑制真菌呼吸作用。抑 制呼吸預防真菌正常成長以及發展。此類藥劑包括2,6-二氮苯胺如抉吉胺，嘧啶酮腙如富米綜以及二氮苯基丁 稀酸如白粉克、氧乙酸基白粉克以及百蟎克。 「有機錫的殺真菌劑（b30)」（FRAC代碼30)於 氧化磷酸化途徑中抑制腺嘌呤三磷酸鹽（ATP)合成 酶。實例包括三苯醋錫、三苯氣錫以及三苯羥锡。 「羧酸殺真菌劑（b31)」（FRAC代碼31)藉由影 響去氧核糖核酸（DNA)第二型拓撲異構酶（旋轉酶） 來抑制真菌生長。實例包括歐索林酸。Extra-inhibition (qgI) fungicide (b(1)" (FRAC code 曰 by ubiquinone ubiquinol oxidase to inhibit fungal towel complex ΙΠ 线 醌氡 经 经 经 经 经 经 阻挡 阻挡 , , , , , The complex is located in the mitochondrial membrane of the fungus. The growth and development of the fungus. The externally inhibited acid, decyloxy amide, guanidine dihydrogen η fungicide (integrated granules) Cyclooxygen can prevent normal fungal fungicides including methoxy acrylic acid, ether acetic acid, oxime ether acetamide and bis II _ 151284.doc • 26 - 201117722 曱 oxy acrylate fungicides for the public Knows), as well as oxazolidinedione, imidazolinone and benzyl aminoguanate fungicides. The oxime acrylate includes atoreno, enestrobin (SYP-Z071) and oxyfluoride vinegar. The amides include pyracrostrobin and pyramitostrobin. The imidoacetates include kresoxim-methyl, pyraoxystr〇bin and Fluoramine (trifloxystrobin). Ethyl ether acetamide includes ether amide, oxygen Amine acetaminophen and α-(methoxyimino)_N-methyl 2 -[[[1-[3-(trifluoromethyl)phenyl]ethoxy]imino]methyl] Benzoylamine. Dihydrogen P-cultivation includes fluoxastrobin. The oxazolidinedione includes the same. The imidazolidinone includes imidacloprid. The benzoguanamine includes anti-mold. "Phenylpyrrole fungicide Agent (bl2)" (FRAC code 12) inhibits osmotic signaling with fungal towels. There are _ MAP protein kinases, such as cytokines and sclerotins, as examples of such fungicides. "噎魏菌剂(bl3)" FRAc «code (1) has been proposed to 'a early cell signaling G protein to suppress signal transmission: it can interfere with fungal sprouting and / or attachment cell formation, anti-eight = mildew. Vinofin is the fungicide Examples of code two peroxidation inhibition fungicides (bl4)" (FRAC S can be used to inhibit lipid peroxidation rhyme) may also affect other biological processes such as Le Qi 1 'such as the synthesis of the composition. The liquid peroxidation is as good as the second absorption and the melanin is true. The true binder includes aromatic carbon and fungicides. Aromatic carbon includes biphenyl and chloranil. Benzene, 151284.doc -27- 201117722 Chloramine, pentadyl benzene, tetranitro nitro stupid and methyl squamous scales. 1,2,4-selling beta stagnation including eduli. "melanin biosynthesis inhibition -Reductase (MBI_R) fungicide (bl5)" (FRAC code 16.1) inhibits the step of naphthalene reduction in melanin biosynthesis. Melanin is required for certain true g-transplants. Melanin biosynthesis inhibitor-reductase fungicide The agents include isobenzofuranones, ratios of B, and benzophenone B. Isobenzofuranones include Pyrofib. Pyrroloquinoline includes Baikulong ^ plug 0 sit Benz and sigh α sitting including three races σ sitting. "Melanin biosynthesis inhibition-dehydratase (Mbi_d) fungicide (bl6)" (FRAC code 16.2) inhibits scytalone dehydratase in melanin biosynthesis. Melanin is required for certain fungal infections of host plants. Melanin biosynthesis inhibitors Dehydratase fungicides include ciprofloxacin, decylamine, and propylamine fungicides. The cyclopropane carboxamide includes gupamine. Carboxylamamines include dicyanamide. Propylamine includes cyanamide. "Phenylamino azide fungicide (M7)" (FRAC code Π) inhibits C4-dethiolase, which is important in the production of sterols. Examples include cyclosporin. "Squalene-epoxidase-inhibiting fungicide (bl8)" (FRAC code 18) inhibits squalene-epoxidase in the ergosterol biosynthetic pathway. Sterols such as ergosterol are required for membrane structure and function, and are therefore essential for the development of functional cell walls. Exposure to these fungicides therefore leads to abnormal growth and gradual death of sensitive fungi. Squalene-epoxidase inhibitors Fungicides include thiamine and allylamine fungicides. Thiamine is intended to include scutellaria. Allylamines include nalfustatin and terbinafine. J51284.doc -28· 201117722 "Polyoxymycin fungicide (M9)" (FRAC code I9) inhibits chitin synthase. Examples include polyoxin. The phenylurea fungicide (b20) (FRAC code 20) has been suggested to affect the ageing crack. (d) including bin clones. : Intra-suppressed (QiI) fungicide (b21) (FRAC code 21) inhibits the fungal cap π granule by affecting the reductase, and is called to block the cytochrome be! The position of the complex in the sputum (Qi), which is located in the fungal mitochondrial membrane. Inhibition of mitochondrial respiration prevents normal true H growth and progression. Wake-inhibitor fungicides include cyanamides and o-glycol triterpene fungicides. Nitrozole includes races. The o-sulphonamide triazole fungicides include carbazolam. "Benamide amine fungicide (b22)" (FRAC code 22) inhibits mitosis by binding to tubulin and blocking microtubule composition. Inhibition of microtubule combination disrupts cell separation, cell and intracellular transport. Examples include acetochlor. "Souric acid antibiotic fungicide (b23)" (FRAC code 23) inhibits fungal growth by affecting protein biosynthesis. Examples include vanamycin. "HexoPyranosyl antibiotic fungicide (b24)" (FRAC code 24) inhibits fungal growth by affecting protein biosynthesis. Examples include gibberellin. "σ-glucan antibiotic··protein synthesis fungicide (b25)" (FRAC code 25) inhibits fungal growth by affecting protein biosynthesis. Examples include streptomycin. 151284.doc •29· 201117722 “°Peer Grape Antibiotics: Indomethacin and Inositol Biosynthesis Fungicides (b26)” (FRAC code 26) inhibits the indole enzymes in the inositol biosynthesis pathway. Examples include vesicomycin. "Cyanoacetamide bismuth fungicide (b27)" (FRAC code 27) includes cymoxanil. "Aminoformate fungicide (b28)" (FRAC code 28) is considered to be a multi-inhibitor of fungal growth. It can interfere with cell membrane permeability after interfering with fatty acid synthesis in the cell membrane. Propp, iodopropynyl butyl phthalate & and aceprocarb are examples of such fungicides. "Oxidatively phosphorylated non-coupling fungicide (b29)" (FRAC code 29) inhibits fungal respiration by non-coupled oxidative phosphorylation. Inhibition of breathing prevents the normal growth and development of fungi. Such agents include 2,6-diazoaniline such as guanidinamine, pyrimidinone oxime such as fulva, and diazophenyl butyric acid such as leucovorin, oxyacetic acid leucovorin and baike. "Organic tin fungicide (b30)" (FRAC code 30) inhibits adenosine triphosphate (ATP) synthetase in the oxidative phosphorylation pathway. Examples include triphenylacetate, triphenyltin, and triphenyltin. The "carboxylic acid fungicide (b31)" (FRAC code 31) inhibits fungal growth by affecting the DNA type 2 topoisomerase (rotase). Examples include oxolinic acid.

「芳環殺真菌劑（b32)」（FRAC代碼32)經建議 於用來影響DNA/核糖核酸（rna)合成。芳香雜環杀α 真菌劑包括異惡唑以及異噻唑啉酮殺真菌劑。異惡唑= 括殺紋寧，而異噻唑啉酮包括辛噻酮。 L 「膦酸鹽殺真菌劑（b33)」（FRAC代碼33)包括 亞磷酸以及其多種鹽類，包括三乙膦酸鋁。 151284.doc •30- 201117722 「氨曱酰苯甲酸殺真菌劑（b34)」（FRAC代碼34) 包括克枯爛。 「苯並三p井殺真菌劑（b35)」（FRAC代碼35)包 括唑菌嗓。 「笨-嗒畊酮殺真菌劑（b36)」（FRAC代碼36)包 括磺菌胺。 「嗒畊酮殺真菌劑（b37)」（FRAC代碼37)包括 達滅淨。 「噻吩-羧醯胺殺真菌劑（b38)」（FRAC代碼38) 經建議用於影響三磷酸腺甘產生。實例包括矽噻菌胺。 「嘧啶胺化物殺真菌劑（b39)」（FRAC代碼39) 藉由影響磷脂質生物合成以及包含氟嘧菌胺來抑制真 菌的生長。 「羧酸胺化物（CAA)殺真菌劑（b40)」（FRAC 代碼40)經建議用於抑制磷脂質生物合成以及細胞壁 沈積。抑制此等程序可預防目標真菌成長並導致其死 亡。羧酸醯胺殺真菌劑包括肉桂酸醯胺、纈胺醯胺酯以 及苦杏仁酸醯胺殺真菌劑。肉桂酸醯胺包括達滅芬以及 氟嗎啉。該纈胺醯胺胺基甲酸類包括苯噻菌胺 (benthiavalicarb )、 苯°塞菌胺-異丙基 (benthiavalicarb-isopropyl)、丙森鋅（iprovalicarb)及 瓦芬财（valifenalate ) ( valiphenal)。苦杏仁酸胺化物包 括雙炔醯菌胺 、N-[2-[4-[[3-(4-氣苯 基）-2-propyn-l-yl]oxy]-3-甲氧苯基]-乙基]-3-曱基 -2-[(曱磺醯基）胺基]丁醯胺以及N-[2-[4-[[3-(4-氣苯 151284.doc •31 - 201117722 基)-2-propyn_l-yl]〇xy]-3-甲氧苯基]乙基]_3_ 甲基_2_[(乙 基苯基碱)胺基]-丁醯胺。 「四環黴素抗生素殺真菌劑（b41)」（FRAC代碼 41) 藉由影響錯合物1菸鹼醯胺腺嘌呤二核甘酸 (NADH)氧化還原酶抑制真菌生長。實例包括經四環 素。 「硫代氨基曱酸鹽殺真菌劑（b42)」（FRAC代碼 42) 包括磺菌胺。 「苯曱醯胺殺真菌劑（b43)」（pRAc代碼43)藉 由血影樣蛋白質的非定域化作用抑制真菌生長。實例包 括acylpicoiide殺真菌劑如氟吡菌胺以及氟吡菌醯胺。 「伤主植物防禦誘發殺真菌劑（b44)」（FRAC代 碼P)誘發宿主植物防禦機制。誘發宿主植物防禦殺真 菌劑包括笨并噻二唑、苯并異噻唑類以及噻二唑_羧醯 胺殺真菌劑。苯并噻二唑類包括阿拉酸式苯_s_甲基。 笨并異嗟唑類包括撲殺熱。嗔二唑_緩醯胺包括售酿菌 胺以及異噻菌胺。 「多位接觸殺真菌劑（b45)」藉由多位作用以及具 有接觸/預防性活性來抑制真菌生長。此類殺真菌劑包 括：「銅殺真菌劑（b45.1)(FRAC代碼Ml)」、「硫殺真 菌劑（b45.2) (FRAC代碼M2)」、「二硫代胺基甲酸殺 真菌劑（b45.3) (FRAC代碼M3)」、「鄰苯二曱醯亞胺 殺真菌劑（b45.4) (FRAC代碼M4)」、「有機氣劑及其 混合劑殺真菌劑（b45.5) (FRAC代碼M5)」、「磺胺類 殺真菌劑（b45.6) (FRAC代碼M6)」、「胍殺真菌劑 (b45.7) (FRAC代碼M7)」「三氮雜苯殺真菌劑 151284.doc -32- 201117722 (b45.8) (FRAC代碼M8)」以及「醌殺真菌劑（b45.9) (FRAC代碼M9)」。「銅殺真菌劑」是含銅的無機化合 物，典型為二價氧化銅狀態；實例中包括銅氧氣化物、 硫酸銅以及銅氫氧化物，其包括組合物例如波多混合液 (三元硫酸銅）。「硫殺真菌劑」是包含硫原子環或鏈的 無機化學物質；實例包括元素硫。「二硫代胺基甲酸殺 真菌劑」包含一個《 一硫代胺基甲酸分子之_ __部分；實例 包括鋅猛乃浦、代森聯殺菌劑、丙森鋅、二甲胺甲硫經 羰酸鐵、代森猛、福美雙、代森鋅以及吉闌。「鄰苯二 曱醯亞胺殺真菌劑」包括一個鄰苯二曱醯亞胺分子之一 部份；實例包括滅菌丹、卡普坦以及四氯丹。「有機氯 劑及其混合劑殺真菌劑」包括一個以氯及氰基取代的芳 環；實例包括百菌清。「磺胺類殺真菌劑」包括抑菌靈 以及對曱抑菌靈。「胍殺真菌劑」包括多果定、雙胍鹽 以及雙胍辛胺。「三氮雜苯殺真菌劑」包括敵菌靈。「醌 殺真菌劑」包括二噻農。 「除了成份（a)以及成份（bl)到（b45) ; (b46) 的殺真菌劑」殺真菌劑包括了作用機轉尚不明瞭的殺黴 成分。這些包括：（b46.1)「噻唑羧醯胺殺真菌劑（FRAc 代碼U5)」、（b46.2)「苯基-乙醯胺殺真菌劑（Frac代 碼U6)」、（b46.3)「奎唑林酮殺真菌劑（FRac代碼 U7)」、（b46.4)「二苯基酮殺真菌劑（FRAC代碼U8)」 以及（46.5)「triazolopyrimidylamine 殺真菌劑」（別名 「***殺真菌劑」）（FRAC代碼45)。噻唑羧醯胺包括 噻唑菌胺。苯基-乙醯胺包括環氟菌胺以及N_[[(環丙基 甲氧基)胺基][6-(二氟甲氧基)-2,3-二氟苯基]-亞曱基]苯 151284.doc -33- 201117722 醯胺。奎唑林酮包括丙氧喹啉以及2-丁氧基-6-碘-3-丙 基-4H-1-苯并哌喃-4-酮。該二苯基酮類包括滅芬農 (metrafenone )及派芬農（pyriofenone ) 〇 三0坐并。密0定 基胺包括辛唑嘧菌胺（5_乙基-6-辛基[1，2,4]***[l，5-a] 喊唆-7-fe)且據t可藉由結合到泛酿-細胞色素bcl還 原酶上一個未闡明的位置來抑制錯合物III粒線體之呼 吸作用。（b46)此類亦包含貝殺新、新阿蘇仁（鐵曱砷 酸銨）、芬派殺、吡咯尼群、滅蟎猛、泰伏勤、2-[[2-氟 -5-(三It曱基）苯基]thio]-2-[3-(2-曱氧苯基)-2-四氫售β坐 亞基]乙腈（ΟΚ-5203)、3-[5-(4-氣苯基)-2,3-二曱基-3-異噁唑烷基]吼啶(SYP-Z048)、4-氟苯基Ν-[Η[[ΐ-(4-氰 基苯基）乙基]續醯基]甲基]丙基]胺甲酸鹽（XR-539)、 Ν-(4-氣-2-硝基苯)-Ν-乙基-4-曱基苯磺醯胺（TF-991)、 5-氣-6-(2,4,6-三氟苯基)-7-(4-曱基六氫σ比0定-1-基)[1，2,4] ***[l，5-a]嘧啶（BAS600)、氯-3-(三氟曱基） 苯氧基]-2,5-二曱苯基]-N-乙基雙甲脒，及1-[(2-丙烯 硫基）羰基]-2-(1-曱乙基)-4-(2-甲基苯基)-5-胺基-1H-吼 唑-3-酮。 在本發明的實施例中，包含以下戶斤述，提及式1時 包含其N-氧化物及其鹽類，且提及「一種式1化合物」 時，降非在實施例中特別定義，否則包含在發明内容中 強調的取代基定義。 實施例1·該組合物包含在發明内容概要中提到的組 分（a)及組分（b)，其中式1中’ R1及H2係獨 立為齒素、氛基、Ci-C3燒基、C2_C3稀基、C2_C3 炔基、環丙基、C]-C3 _烷基、C2-C3南烯基、 151284.doc -34- 201117722 CVC2烷氧基、crc2函代烷氧基、crc2烷硫基 或Q-C3羥烷基。 實施例2.實施例1的組合物，其中R1及R2係獨立 為鹵素、氰基、乙烯基、乙炔基、甲氧基或是曱 硫基；或視情況以一個選自鹵素、-OH及曱基的 取代基所取代的甲基。 實施例3.實施例2的組合物，其中R1及R2係獨立 為鹵素、氰基或甲氧基；或視情況以一個選自 F、C1或甲基的取代基所取代的甲基。 實施例4.實施例1的組合物，其中R1及R2係獨立 為鹵素、氰基或CrC3烷基。 實施例5.實施例3或4的組合物其中R1及R2係獨 立為Ο、Br、I是CrC2烷基。 實施例6.實施例5的組合物，其中R1及R2係獨立 為Cl、Br或曱基。 實施例7.在發明内容概要或實施例1至6任一實施 例中所描述的組分（a)及（b)的組合物，其中 式1中，Q1係苯基、°塞吩基、°塞。坐基、°比0坐基、 11 米°坐基、σ比咬基、。荅p井基、°密π定、啥淋基或¥基， 各視情況以多達3個獨立選自R3的取代基在碳 原子環員上取代以及選自R4的取代基在氮原子 環員上取代。 實施例8.實施例7的組合物，其中Q1係苯基、噻吩 基、嚷ti坐基、比吐基、α米吐基、σ比咬基、塔u井基、 嘧啶基或苄基，各視情況以多達3個獨立選自 151284.doc -35- 201117722 R的取代基在碳原子環員上取代以及選自“的 取代基在氮原子環員上取代。 實施例9.實施例8的組合物，其中Qi係苯基、吡啶 基或苄基’各視情況以多達3個獨立選自R3的 取代基在碳原子環員上取代。 實施例10.實施例9的組合物，其中qi係苯基或吡 啶基環，視情況以多達3個獨立選自R3的取代 基在碳原子環員上取代。 實施例11.實施例9或1〇的組合物，其中當qi係一 視情況經取代之吡啶環時，該吡啶環附著於式1 之吡啶基環3號位置（即3_吡啶基）。 實施例12.實施例1〇的組合物，其中Qi係一視情況 以多達3個獨立選自R 3的取代基所取代的苯環。 貫施例13.包含在發明内容概要或實施例丨至12中 任一貫施例中所描述包括組分（a)及（b)的組 合物，其中式1中，Q2係苯基、噻吩基、噻唑 基、吡唑基、咪唑基、吡啶基、嗒畊基、嘧啶基、 喹啉基或苄基，各視情況以多達3個獨立選自 R的取代基在碳原子環員上取代及選自R6的取 代基在氮原子環員上取代。 實施例14.實施例13的組合物，其中Q2係苯基、噻 吩基、噻唑基、吡唑基、咪唑基、吡啶基、嗒畊 基、嘧啶基或苄基，各視情況以多達3個獨立選 自R的取代基在碳原子環員上取代以及選自R6 的取代基在氮原子環員上取代。 151284.doc -36 · 201117722 實施例15.實施例14的組合物，其中q2係4 咬基或苄基’各視情況以多達3個獨立、= 的取代基在碳原子環員上取代。 &自H5 實施例I6.實施例I5的組合物，其中Q2係 或吡啶環，各視情況以多達3個獨立選個^基 取代基在碳原子環員上取代。 ' 尺的 實施例17·實施例15或16的組合物，复中火2 一視情況經取代之吡啶環，該吡啶環附二Q係 之吡啶環3號位置（即3-吡啶基）/者於式1 實施例18.實施例16的組合物，其+ 視情況以多達3個獨立選自R5的取;= 實施例19.在發明内容或實施例1至18中任_ — =所描述包含組分(心⑴的组合物貫： 中式1中’當Q以及Q2各獨立包 /、 =而❼作中之-的環經以2或;;2 =代，而q及Q的其他環經。至3個取代基ς 實施::立:Γ/9的級合物，其中當Q1以及Q2 f社包含-個錢或t定環時，Q1以及^ 二之-_經以2或3取代基取代，❿Ql以及 與Q的其他環經！至2個取代基取代。 貝施^21.實施例2〇的級合物，其中當Q】及Q、 立的包含:個笨環或。㈣環時，Ql以及〇2其 之-的環經以2或3取代基取代，❿Ql以及 Q的其他環經1個取代基取代。 151284.doc -37· 201117722 實施例22.包含在發明内容或實施例1至21中任一 實施例中所描述組分（a)及（b)的組合物，其 中式1中，當Q1以及Q2各獨立的包含一個苯環 或吡啶環，Q1以及Q2其中之一環經至少一取代 基在一鄰位上取代，而Q1以及Q2的其他環經至 少一個取代基在間位或對位取代。 實施例23.包含在發明内容或實施例1至22中任一 實施例中所描述組分（a)及（b)的組合物，其 中式1中，每個R3以及R5係獨立的鹵素、氰基、 CVC3烷基、C2-C3烯基、C2-C3炔基、CVC3鹵烷 基、壞丙基、C1-C3烧氧基、C1-C3鹵代烧氧基、 C1-C3烧硫基、C1-C3烧胺基、C2-C4二院胺基、 c2-c4烷羰基、c2-c4烷氧羰基或c2-c4烷羰胺基。 實施例24.實施例23的組合物，其中每個R3以及 R5係獨立的鹵素、氰基、CrC3烷基、C2-C3烯 基、CrC3鹵烷基、CrC3烷氧基、CrC3鹵代烷 氧基、CrC3烷硫基或CrC3烷胺基。 實施例25.實施例24的組合物，其中每個R3以及 R5係獨立的鹵素、氰基、CrC3烷基、CVC3鹵 烷基、CrC3烷氧基或CrC3齒代烷氧基。 實施例26.實施例25的組合物，其中每個R3以及 R5係獨立的F、C卜Br、氰基、CrC2烷基、CrC2 鹵烧基、C1-C2烧氧基或C1-C2鹵代烧氧基。 實施例27.實施例26的組合物，其中每個R3以及 R5係獨立的F、Q、氰基、曱基、CrC2烷氧基 或氟曱氧基。 151284.doc •38· 201117722 實施例28·包含在發明内容或實施例1至27中任一 實施例中所描述組分（a)及（b)的组合物，其 中式1中，每個R4以及R6係獨立的氰基、(：丨-(：3 炫基或環丙基。 實施例29.實施例28的組合物，其中每個R4以及 R6係獨立的Q-Q烷基。 實施例30.實施例29的組合物，其中每個R4以及 R6係獨立的曱基。 實施例31_包含在發明内容概要或實施例1至3〇中 任一實施例中所描述組分（a )及（b )的組合物， 其中式1中，每個X係獨立的〇或NR7。 實施例32.包含在發明内容概要或實施例1至η中 任一實施例中所描述組分（a)及（b)的組合物， 其中式1中，每個R7係Η。 實施例33.包含在發明内容概要或實施例1至32中 任一實施例中所描述組分（a)&(b)的組合物， 其中式1中’每個U係獨立的c2-C4伸烷基。 實施例34·包含在發明内容概要或實施例1至33中 任一實施例中所描述組分（a)及（b)的組合物， 其中式1中，每個Z係獨立的NR8aR8b或0R9。 實施例35.包含在發明内容概要或實施例丨至34中 任一實施例中所描述組分（a )及（b )的組合物， 其中式1中，每個R8a以及尺此係獨立的h、Ci_C6 烷基或Q-Q ii烷基。 實施例36.包含在發明内容概要或實施例丨至35中 任一實施例中所描述組分（a)及（b)的組合物， 151284.doc -39- 其中式1中，每個R9係獨立的H、crc6烷基或 CVC6鹵焼•基。 實施例37.包含在發明内容概要或實施例1至27中 任一實施例中所描述組分（a)及（b)的組合物， 其中式1中’ Q1以及Q2其中之一環係一個笨環 或3-°比°定孩，其在一個間位或對位經一個選自 F、C1、曱基、曱氧基以及氟曱氧基的取代基取 代，以及視情況以一個F在剩餘位置取代；而 Q1以及Q2的其他環係一個苯基環，其同時在鄰 位以F取代以及在一個間位或對位以一個選自 氰基以及CrC2烷氧基的取代基取代。 實施例38.包含在發明内容概要或實施例1至27以 及37中任一實施例中所描述組分（a)及（b) 的組合物，其中組分（a)包括一個選自由以下 組分組成之群組的化合物 4-氯-5-(2,6-二氟-4-曱氧苯基)-1-(3-氟苯基)_2_甲 基-1H-咪唾（化合物181)、 3- [4-氣-1-(4-氣苯基)-2-甲基-1Η-°米唾-5-基]_2,4_ 二氟苯腈（化合物292)、 2-溴基-1-(2,6-二氟-4-曱氧苯基)-5-(3-氟笨基 曱基-1H-咪唑（化合物469)、 4- [2-氣-1-(6_氣-3-吡啶基）-4-甲基-1H-咪唑_5_ 基]-3,5-二氟苯腈（化合物513)、 2-溴基-4-氯-5-(4-乙氧基-2,6-二氟苯基)小(3_氣 苯基)-1Η-咪唑（化合物514)、 201117722 心氯乙氧基-2,6-二氟苯基)-2-曱基-1-(4-甲 苯基MH-咪唑（化合物515)、 4-氣乙氧基-2,6-二氟笨基)-1-(4-氟苯基)-2-曱基-1H-咪唑（化合物516)、 4-氯-5-(4-乙氧基_2,6·二氟苯基)小(3_氟苯基)_2_ 曱基-1H-咪唑（化合物517)、 2-漠基-4-氯-43-(二氟甲氧基）苯基]_5-(4乙氧 基-2,6·二氟苯基)-1Η-咪唑（化合物518)、 2,4-二氯小[3_(二氟甲氧基）苯基]_5_(4_乙氧基 -2,6-二氟苯基)_m_咪唑（化合物519)、 4-[2-氣-l_(6_曱氧基_3_吡啶基)_4_甲基_m_咪唑 -5-基]-3,5-二氟苯腈（化合物52〇)、 4_[2_溴基小(6-曱氧基-3-吡啶基)-4-曱基-1H-咪 唾-5-基]-3,5-二氟苯腈（化合物521)、 4_[2-溴基-4-氣-1-(4-甲笨基)-1Η-咪唑-5-基]-3,5-二氟苯腈（化合物522)、 4-氯-1-[3-(二氟甲氧基）苯基]-5-(4-乙氧基_2,6_ 一氟苯基)-2-甲基-1H-咪嗤（化合物523)、 4-[2-溴基 _4-氯-1-(3-氟苯基)_1H-咪唑-5-基]-3,5- 一鼠苯腈（化合物524)、 4-[4-氣·ΐ-(3,4-二氟苯基）_2•曱基-1H-咪唑-5-基]-3,5-二氟苯腈（化合物525)、 4-[4-氣小(3-氟苯基)-2-曱基-1Η-咪唑-5-基]-3,5-一氟苯腈（化合物526)、 4-[2-溴基-4-氯-1-(4-氟苯基)-1Η-咪唑·5_ 基]-3,5-二氟苯腈（化合物527)、 151284.doc •41 · 201117722 2-氣-i-[4_(二氟曱氧基）苯基]·5_(2,6_二氟_4_曱 氧苯基Μ-曱基-1Η-咪唑（化合物528)、 4·[2-氣-1-(4·氣苯基)_4_ 甲基-ΙΗ-咪唑-5-基]-3,5-二氟笨腈（化合物529)、 4_[2-氣-1-(3-氟苯基)_4_ 甲基-1Η-咪唑-5-基]-3,5-二氟苯腈（化合物530)、 4_[4-氣-1-(2,4-二氟苯基）-2-曱基-1Η-咪唑-5-基]-3,5-二氟苯腈（化合物531)、 M2-氯·1-[3-(二氟曱氧基)苯基]_4-曱基-1H-咪唑 -5-基]-3,5-二氟苯腈（化合物532)、 4-[2,4-二氣二氟曱氧基）苯基；]-1Η-咪唑-5- 基]-3,5-二氟苯腈（化合物533 )、 4_[4-氯-1-(2-氟-4-甲苯基）-2-曱基-1Η-咪唑-5-基]-3,5-二氟苯腈（化合物534)、 4·[4-溴基-1-(2-氟-4-曱苯基)-2-曱基-1H-咪唑-5-基]-3,5-二氟苯腈（化合物535 )，以及 4·[2,4-二溴-1-(3-氟苯基)_1H-咪唑-5-基]-3,5-二 氟本猜（化合物536)。 實施例39.實施例38的組合物，其中組分（a)包括 一個選自由化合物516、化合物517、化合物 520、化合物523、化合物525、化合物526、化 合物529、及化合物536所組成的群組的化合物。 實施例40.包含在發明内容概要或實施例1至39中 任一實施例中所描述組分（a)及（b)的組合物， 其中式1中’當Q2係視情況以苯基取代，以及 Q1係在間位沒有經取代的苯基，其在一個第一 151284.doc • 42- 201117722 鄰位以鹵素或R2〇取 選自鹵素或R20的取並視情況在其他鄰位以 位以-個選自取代，並且視情況在對 面條件中的至少二=真的取代基取代’而後下 (a) 當第一鄰位以鹵夸跑 位皆不以R、代H代，縣其它鄰位或對 (b) 當第一鄰位以R2〇 .b, /上 取代，那麼其它鄰位或對 位皆不以（鹵素或R20)取代， ::γ分別係羥基、烷氧基、鹵代烷氧基、 衣H Ζ ’其中Χ係〇，U係伸烷基， Z^R R或⑽，一係Η或燒基，R、烧 基或環烷基，以及R9係烷基。"Aromatic ring fungicide (b32)" (FRAC code 32) has been suggested to affect DNA/ribonucleic acid (RNA) synthesis. Aromatic heterocyclic alpha fungicides include isoxazole and isothiazolinone fungicides. Isoxazole = chlorpyrifos, and isothiazolinone includes octyl ketone. L "phosphonate fungicide (b33)" (FRAC code 33) includes phosphorous acid and various salts thereof, including aluminum triethylphosphinate. 151284.doc •30- 201117722 "Aminophthalic acid benzoic acid fungicide (b34)" (FRAC code 34) includes gram rot. "Benzene tri-p fungicide (b35)" (FRAC code 35) includes azole. "Stupid - sulphonic fungicide (b36)" (FRAC code 36) includes sulfamethoxazole. "Small ketone fungicide (b37)" (FRAC code 37) includes chlorpyrifos. "Thiophene-carboxamide pro-fungicide (b38)" (FRAC code 38) has been suggested to affect glandular production of adenosine triphosphate. Examples include thiastrobin. "pyrimidinium aminide fungicide (b39)" (FRAC code 39) inhibits the growth of fungi by affecting phospholipid biosynthesis and containing fluzalazine. The "Carboxylic Acid Amine (CAA) Fungicide (b40)" (FRAC code 40) is recommended for inhibiting phospholipid biosynthesis and cell wall deposition. Inhibition of these procedures prevents the growth of the target fungus and causes it to die. The guanamine amide fungicides include decyl cinnamate, amidoxime ester, and amyramine penicillin fungicide. Indole cinnamate includes dadefen and flumorph. The amidoxime amides include benthiavalicarb, benthiavalicarb-isopropyl, iprovalicarb, and valifenalate (valiphenal). Amygdalin Amines include di-propargylamine, N-[2-[4-[[3-(4-phenylphenyl)-2-propyn-l-yl]oxy]-3-methoxyphenyl] -ethyl]-3-mercapto-2-[(oxasulfonyl)amino]butanamine and N-[2-[4-[[3-(4-benzene 151284.doc •31 - 201117722) Base)-2-propyn_l-yl]〇xy]-3-methoxyphenyl]ethyl]_3_methyl_2_[(ethylphenyl)amino]-butanamine. "Tetracycline antibiotic fungicide (b41)" (FRAC code 41) inhibits fungal growth by affecting the complex 1, nicotine indoleamine adenine dinucleotide (NADH) oxidoreductase. Examples include tetracycline. "Thioaminoguanidine Fungicide (b42)" (FRAC code 42) includes sulfamethamine. "Phenylamine fungicide (b43)" (pRAc code 43) inhibits fungal growth by delocalization of blood-like proteins. Examples include acylpicoiide fungicides such as fluopyram and fluopyram. "Injured host plant defense-induced fungicides (b44)" (FRAC code P) induces host plant defense mechanisms. Inducing host plant defense fungicides include stupid thiadiazoles, benzisothiazoles, and thiadiazole-carboxyguanamine fungicides. Benzothiadiazoles include phenyl-s-methyl groups of arsenic acid. Stupid and isoxazoles include culling heat. Oxadiazoles - valine amines include snails and isotianil. "Multiple contact fungicides (b45)" inhibit fungal growth by multiple actions and with contact/prophylactic activity. Such fungicides include: "copper fungicide (b45.1) (FRAC code Ml)", "sulfur fungicide (b45.2) (FRAC code M2)", "dithiocarbamic acid fungicide" Agent (b45.3) (FRAC code M3)", "phthalimide fungicide (b45.4) (FRAC code M4)", "organic gas agent and its mixture fungicide (b45. 5) (FRAC code M5)", "sulfonamide fungicide (b45.6) (FRAC code M6)", "fungal fungicide (b45.7) (FRAC code M7)" "triazabenzene fungicide Agent 151284.doc -32- 201117722 (b45.8) (FRAC code M8)" and "killing fungicide (b45.9) (FRAC code M9)". "Copper fungicide" is a copper-containing inorganic compound, typically in the form of a divalent copper oxide; examples include copper oxides, copper sulfate, and copper hydroxide, including compositions such as a mixture of waves (copper sulfate) . A "sulfur fungicide" is an inorganic chemical containing a ring or chain of sulfur atoms; examples include elemental sulfur. The "dithiocarbamic acid formic fungicide" comprises a _ _ _ moiety of a monothiocarbamic acid molecule; examples include zinc mannapril, dexamethasone bactericide, propyl zinc, dimethyl methoxide Iron carboxylate, Daisen Meng, Fumei double, Daisen zinc and Ji Yu. The "o-phthalimide fungicide" includes a portion of a phthalimide molecule; examples include sterilized Dan, Captan, and Tetrachlor. "Organic chlorine agents and their mixture fungicides" include an aromatic ring substituted with chlorine and a cyano group; examples include chlorothalonil. "Sulfonate fungicides" include bacteriostatic and bacteriostatic. "Fungicides" include docetaxel, biguanide salts and bis-octylamine. "Triazabenzene fungicides" include carbendazim. "醌Fungicides" include dithianon. "In addition to ingredient (a) and ingredients (bl) to (b45); (b46) fungicides" fungicides include fungicidal ingredients that are unclear. These include: (b46.1) "thiazole carboxamide fungicide (FRAc code U5)", (b46.2) "phenyl-acetamide fungicide (Frac code U6)", (b46.3) "Quizozolone fungicide (FRac code U7)", (b46.4) "diphenyl ketone fungicide (FRAC code U8)" and (46.5) "triazolopyrimidylamine fungicide" (alias "Triazole killing" Fungal agent") (FRAC code 45). Thiazole carboxamide includes ethaboxam. Phenyl-acetamide includes cycloflufenamide and N_[[(cyclopropylmethoxy)amino][6-(difluoromethoxy)-2,3-difluorophenyl]-arylene Benzene 151284.doc -33- 201117722 decylamine. Quizolinone includes propoxyquinoline and 2-butoxy-6-iodo-3-propyl-4H-1-benzopipene-4-one. The diphenyl ketones include metrafenone and pyrofenone 〇30. Intimate amine includes octazolam (5-ethyl-6-octyl[1,2,4]triazole [l,5-a] shouting -7-fe) and can be combined by t Respiratory effects of the complex III mitochondria are inhibited by an unexplained position on the ubiquitin-cytochrome bcl reductase. (b46) This class also includes beijing new, new azuren (iron strontium arsenate), fenfen, pyrrolnitrin, chlorpyrifos, tafuqin, 2-[[2-fluoro-5-(three It is a phenyl]thio]-2-[3-(2-indolylphenyl)-2-tetrahydro sulphide β succinyl] acetonitrile (ΟΚ-5203), 3-[5-(4-gas Phenyl)-2,3-dimercapto-3-isoxazolealkyl]acridine (SYP-Z048), 4-fluorophenylindole-[Η[[ΐ-(4-cyanophenyl)) Methyl]propyl]amine formate (XR-539), Ν-(4-gas-2-nitrophenyl)-indole-ethyl-4-mercaptobenzenesulfonamide TF-991), 5-gas-6-(2,4,6-trifluorophenyl)-7-(4-mercaptohexahydro-sigma ratio 0--1-yl)[1,2,4] Azole [l,5-a]pyrimidine (BAS600), chloro-3-(trifluoromethyl)phenoxy]-2,5-diphenylene]-N-ethylbisformamidine, and 1-[ (2-Propylthio)carbonyl]-2-(1-indolyl)-4-(2-methylphenyl)-5-amino-1H-indazol-3-one. In the examples of the present invention, the following formulas are included, and when the formula 1 is referred to, the N-oxide and its salts are included, and when referring to "a compound of the formula 1," the definition is not specifically defined in the examples. Otherwise, the definition of substituents highlighted in the Summary of the Invention is included. Example 1· The composition comprises component (a) and component (b) mentioned in the summary of the invention, wherein 'R1 and H2 in the formula 1 are independently dentate, an aryl group, a Ci-C3 alkyl group. , C2_C3 dilute, C2_C3 alkynyl, cyclopropyl, C]-C3 _alkyl, C2-C3 nalkenyl, 151284.doc -34- 201117722 CVC2 alkoxy, crc2 alkoxy, crc2 alkane Base or Q-C3 hydroxyalkyl. Embodiment 2. The composition of Embodiment 1, wherein R1 and R2 are independently halogen, cyano, vinyl, ethynyl, methoxy or sulfonylthio; or optionally selected from halogen, -OH, and A methyl group substituted with a substituent of a fluorenyl group. Embodiment 3. The composition of Embodiment 2 wherein R1 and R2 are independently halogen, cyano or methoxy; or, optionally, a methyl group substituted with a substituent selected from F, C1 or methyl. Embodiment 4. The composition of Embodiment 1, wherein R1 and R2 are independently halogen, cyano or CrC3 alkyl. Embodiment 5. The composition of Embodiment 3 or 4 wherein R1 and R2 are independently Ο, Br, and I is a CrC2 alkyl group. Embodiment 6. The composition of Embodiment 5 wherein R1 and R2 are independently Cl, Br or fluorenyl. Embodiment 7. A composition of components (a) and (b) as described in the Summary of the Summary of the Invention or any of Embodiments 1 to 6, wherein in Formula 1, Q1 is a phenyl group, a thiophene group, ° Plug. Sitting base, ° than 0 sitting base, 11 meters ° sitting base, σ than bite base.荅p well base, 密 π 啥, 啥 基 or ¥ base, each optionally substituted with up to 3 substituents independently selected from R 3 on a carbon atom ring member and a substituent selected from R 4 in a nitrogen atom ring Replaced by members. Embodiment 8. The composition of Embodiment 7, wherein Q1 is phenyl, thienyl, 嚷ti, pyrenyl, α-methane, σ-bityl, sulfonyl, pyrimidinyl or benzyl, Each of the substituents substituted on the carbon atom ring member and up to 3 substituents selected from 151284.doc -35 - 201117722 R are optionally substituted on the nitrogen atom ring member. Example 9. Example A composition of 8, wherein the phenyl group, the pyridyl group or the benzyl group is optionally substituted on the carbon atom ring with up to three substituents independently selected from R3. Embodiment 10. Composition of Example 9. Wherein qi is a phenyl or pyridyl ring, optionally substituted on the carbon atom ring with up to 3 substituents independently selected from R3. Embodiment 11. The composition of Example 9 or 1〇, wherein When the pyridine ring is substituted as the case may be, the pyridine ring is attached to the position of the pyridyl ring No. 3 of the formula 1 (i.e., the 3-pyridyl group). Embodiment 12. The composition of the embodiment 1 wherein the Qi system is one view. The case is a benzene ring substituted with up to 3 substituents independently selected from R 3. Embodiment 13. Inclusion in Summary of the Summary of the Invention or Examples 丨 to 12 Compositions comprising components (a) and (b) as described in the usual examples, wherein in formula 1, Q2 is phenyl, thienyl, thiazolyl, pyrazolyl, imidazolyl, pyridyl, hydrazine, A pyrimidinyl group, a quinolyl group or a benzyl group, each optionally substituted with up to 3 substituents independently selected from R on a carbon atom ring member and a substituent selected from R6 substituted on a nitrogen atom ring member. The composition of embodiment 13, wherein Q2 is phenyl, thienyl, thiazolyl, pyrazolyl, imidazolyl, pyridyl, hydrazine, pyrimidinyl or benzyl, each optionally up to 3 independently selected The substituent from R is substituted on the carbon atom ring and the substituent selected from R6 is substituted on the nitrogen ring ring. 151284.doc -36 · 201117722 Example 15. The composition of Example 14, wherein the q2 system 4 bites The base or benzyl group is optionally substituted on the carbon atom ring with up to 3 independent, = substituents. & from H5. The composition of Example I5, wherein the Q2 system or the pyridine ring, each Whereas, up to 3 independently selected substituents are substituted on the carbon atom ring member as appropriate. Example 17 of the ruler. Example 15 or 16 Compound, complex medium fire 2, as the case may be substituted pyridine ring, the pyridine ring is attached to the Q-position of the pyridine ring No. 3 position (ie 3-pyridyl group) / in the formula of Example 18. Example 16. And, as the case may be, up to 3 independently selected from R5; = Example 19. In the Summary of the Invention or Examples 1 to 18, the composition comprising the component (heart (1) is: In Equation 1, the loops of 'when Q and Q2 are each independently/, = and are in the middle are 2 or 2; 2 = generation, and the other loops of q and Q. To 3 substituents 实施 Implementation: Li: a ruthenium/9 complex, in which when Q1 and Q2 f contain - money or t-ring, Q1 and ^--- are substituted with 2 or 3 substituents, ❿Ql and other rings with Q through! Replace with 2 substituents.施施^21. The hydrazine of Example 2, wherein when Q] and Q, the inclusion comprises: a stupid ring or. (d) In the ring, the ring of Ql and 〇2 is substituted with a 2 or 3 substituent, and the other rings of ❿Q1 and Q are substituted with 1 substituent. 151284.doc -37·201117722 Embodiment 22. A composition comprising the components (a) and (b) described in the Summary of the Invention or any of Embodiments 1 to 21, wherein in Formula 1, when Q1 and Q2 each independently comprises a benzene ring or a pyridine ring, one of Q1 and Q2 is substituted at least in the ortho position, and the other rings of Q1 and Q2 are substituted at the meta or para position via at least one substituent. Embodiment 23. The composition comprising the components (a) and (b) described in the invention or in any one of embodiments 1 to 22, wherein each of R3 and R5 is independently halogen, Cyano, CVC3 alkyl, C2-C3 alkenyl, C2-C3 alkynyl, CVC3 haloalkyl, propyl, C1-C3 alkoxy, C1-C3 halooxy, C1-C3 sulphur And a C1-C3 aromatine group, a C2-C4 amphoteric amine group, a c2-c4 alkylcarbonyl group, a c2-c4 alkoxycarbonyl group or a c2-c4 alkylcarbonylamino group. Embodiment 24. The composition of Embodiment 23, wherein each R3 and R5 are independently halogen, cyano, CrC3 alkyl, C2-C3 alkenyl, CrC3 haloalkyl, CrC3 alkoxy, CrC3 haloalkoxy, CrC3 alkylthio or CrC3 alkylamine. Embodiment 25. The composition of embodiment 24 wherein each R3 and R5 is independently halogen, cyano, CrC3 alkyl, CVC3 haloalkyl, CrC3 alkoxy or CrC3 dentate alkoxy. Embodiment 26. The composition of embodiment 25, wherein each R3 and R5 are independently F, C, Br, cyano, CrC2 alkyl, CrC2 haloalkyl, C1-C2 alkoxy or C1-C2 halo Alkoxy groups. Embodiment 27. The composition of Embodiment 26 wherein each of R3 and R5 is independently F, Q, cyano, decyl, CrC2 alkoxy or fluorodecyloxy. 151284.doc • 38· 201117722 Embodiment 28. A composition comprising the components (a) and (b) described in the Summary of the Invention or any of Embodiments 1 to 27, wherein each R4 in Formula 1 And R6 is independently a cyano group, (: 丨-(:3 leucoyl or cyclopropyl. Example 29. The composition of Example 28, wherein each R4 and R6 are independently aq. alkyl. Example 30. The composition of embodiment 29, wherein each R4 and R6 are independently fluorenyl. Embodiment 31_ comprises components (a) and (described in the Summary of the Summary of the Invention or in any of Examples 1 to 3) The composition of b), wherein each X is independently ruthenium or NR7 in Formula 1. Example 32. Including component (a) described in the Summary of the Summary of the Invention or in any of Examples 1 to η and The composition of (b), wherein each R7 is in the formula 1. Embodiment 33. Including the components (a) & (b) described in the summary of the summary of the invention or in any of the embodiments 1 to 32 A composition, wherein each U is an independent c2-C4 alkylene group in Formula 1. Example 34 is included in the Summary of the Summary of the Invention or in any of Examples 1 to 33. A composition of the components (a) and (b), wherein each Z is independently NR8aR8b or 0R9 in the formula 1. Embodiment 35 is included in any one of the summary of the invention or the embodiment 丨 to 34. Depicting compositions of components (a) and (b), wherein each R8a and in the formula 1 are independently h, Ci_C6 alkyl or QQ ii alkyl. Embodiment 36. Included in the Summary or Implementation of the Summary of the Invention The composition of the components (a) and (b) described in any of the examples of 35, 151284.doc -39- wherein, in the formula 1, each R9 is independently H, crc6 alkyl or CVC6 halogen Embodiment 37. A composition comprising the components (a) and (b) described in the Summary of the Summary of the Invention or in any of Embodiments 1 to 27, wherein 'Q1 and Q2 are in Formula 1 A ring is a stupid ring or a 3-° ratio, which is substituted in a meta or para position by a substituent selected from the group consisting of F, C1, decyl, decyloxy and fluoromethoxy, and optionally One F is substituted at the remaining position; and the other rings of Q1 and Q2 are a phenyl ring which is substituted at the same time with an F and at a meta or para position with a selected one Substituents substituted with a substituent of a CrC2 alkoxy group. Embodiment 38. A composition comprising the components (a) and (b) described in the Summary of the Summary of the Invention or in any one of Embodiments 1 to 27 and 37, wherein Component (a) comprises a compound selected from the group consisting of 4-chloro-5-(2,6-difluoro-4-indolyloxyphenyl)-1-(3-fluorophenyl)_2. _Methyl-1H-imidyl (Compound 181), 3-[4-Ga-1-(4-Phenylphenyl)-2-methyl-1Η-°Methyl-5-yl]_2,4_Difluoro Benzonitrile (Compound 292), 2-Bromo-1-(2,6-difluoro-4-indolyloxyphenyl)-5-(3-fluorophenylidinyl-1H-imidazole (Compound 469), 4 - [2-Ga-1-(6-a-3-pyridyl)-4-methyl-1H-imidazole-5-yl]-3,5-difluorobenzonitrile (Compound 513), 2-bromo- 4-Chloro-5-(4-ethoxy-2,6-difluorophenyl) small (3-p-phenyl)-1 Η-imidazole (compound 514), 201117722 Heart Chloroethoxy-2,6- Difluorophenyl)-2-mercapto-1-(4-methylphenyl MH-imidazole (compound 515), 4-oxoethoxy-2,6-difluorophenyl)-1-(4-fluorobenzene 2-mercapto-1H-imidazole (compound 516), 4-chloro-5-(4-ethoxy-2,6.difluorophenyl) small (3-fluorophenyl)_2_ fluorenyl- 1H-imidazole (compound 517), 2- Molyl-4-chloro-43-(difluoromethoxy)phenyl]_5-(4ethoxy-2,6.difluorophenyl)-1Η-imidazole (compound 518), 2,4-di Chloro[3_(difluoromethoxy)phenyl]_5_(4_ethoxy-2,6-difluorophenyl)_m_imidazole (compound 519), 4-[2-gas-l_(6_曱oxy_3_pyridyl)_4_methyl_m_imidazole-5-yl]-3,5-difluorobenzonitrile (compound 52〇), 4_[2_bromo group small (6-decyloxy) -3-pyridyl)-4-mercapto-1H-imidyl-5-yl]-3,5-difluorobenzonitrile (Compound 521), 4-[2-bromo-4-pyrene-1-(4) -methylidene)-1Η-imidazole-5-yl]-3,5-difluorobenzonitrile (Compound 522), 4-chloro-1-[3-(difluoromethoxy)phenyl]-5- (4-Ethoxy-2,6-fluorophenyl)-2-methyl-1H-amidole (Compound 523), 4-[2-Bromo-4-chloro-1-(3-fluorophenyl) )_1H-imidazole-5-yl]-3,5-mono-benzonitrile (compound 524), 4-[4- gas·ΐ-(3,4-difluorophenyl)_2•indolyl-1H-imidazole -5-yl]-3,5-difluorobenzonitrile (compound 525), 4-[4-carbo(3-fluorophenyl)-2-indolyl-1Η-imidazol-5-yl]-3, 5-monofluorobenzonitrile (Compound 526), 4-[2-Bromo-4-chloro-1-(4-fluorophenyl)-1Η-imidazole-5-yl]-3,5-difluorobenzonitrile ( Compound 527), 151284.doc •41 · 2 01117722 2-Gas-i-[4_(difluorodecyloxy)phenyl]·5_(2,6-difluoro-4-yloxyphenylindole-indenyl-1Η-imidazole (Compound 528), 4· [2-Ga-1-(4·Phenylphenyl)_4_methyl-indole-imidazol-5-yl]-3,5-difluoroacostonitrile (Compound 529), 4_[2-Ga-1-(3) -fluorophenyl)_4_methyl-1Η-imidazol-5-yl]-3,5-difluorobenzonitrile (Compound 530), 4-[4-Ga-1-(2,4-difluorophenyl)- 2-mercapto-1Η-imidazol-5-yl]-3,5-difluorobenzonitrile (Compound 531), M2-Chloro-1-[3-(difluorodecyloxy)phenyl]_4-indenyl -1H-imidazol-5-yl]-3,5-difluorobenzonitrile (Compound 532), 4-[2,4-dioxadifluorodecyloxy)phenyl;]-1Η-imidazole-5-yl ]-3,5-difluorobenzonitrile (Compound 533), 4-[4-Chloro-1-(2-fluoro-4-methyl)-2-indolyl-1Η-imidazol-5-yl]-3, 5-difluorobenzonitrile (Compound 534), 4·[4-Bromo-1-(2-fluoro-4-indolyl)-2-indolyl-1H-imidazol-5-yl]-3,5 -difluorobenzonitrile (Compound 535), and 4·[2,4-dibromo-1-(3-fluorophenyl)_1H-imidazol-5-yl]-3,5-difluorobenz (composition 536 ). The composition of embodiment 38, wherein component (a) comprises a group selected from the group consisting of compound 516, compound 517, compound 520, compound 523, compound 525, compound 526, compound 529, and compound 536. compound of. Embodiment 40. A composition comprising components (a) and (b) as described in the Summary of the Summary of the Invention or in any of Embodiments 1 to 39, wherein in Formula 1 'when Q2 is optionally substituted with a phenyl group And Q1 is a phenyl group which is not substituted at the meta position, which is in the first 151284.doc • 42-201117722 ortho position with halogen or R2, which is selected from halogen or R20 and is taken in other ortho positions. Substituting - one for substitution, and optionally replacing at least two of the opposite conditions in the opposite condition, and then substituting (a) when the first ortho position is in the form of a halogen, not R, generation H, county other Ortho or pair (b) When the first ortho position is substituted by R2〇.b, /, then the other orthic or para position is not substituted by (halogen or R20), and ::γ is a hydroxyl group, an alkoxy group, A haloalkoxy group, a fluorene group, a fluorene group, a U alkyl group, Z^RR or (10), a hydrazine or a decyl group, an R group, a alkyl group or a cycloalkyl group, and an R9 alkyl group.

施例41.實施例40的組合物，其中於式1中，當 Q2係視情缝取代的苯基，以及Ql係在間位沒 有經取代的苯基，其在一個第一鄰位以_素或 R取代’並視情況在其他鄰位以選自鹵素或r2〇 取代，則Q1苯基在對位以除了鹵素或r2〇的取 代基取代。 實施例42.實施例41的組合物，其中於式1中，當 Q2係視情況經取代的苯基，以及Q1係在間位沒 有經取代的苯基’其在一個第一鄰位以鹵素或 R20取代’並視情況在其他鄰位以選自鹵素或R20 的取代基取代’則Q1苯基在對位以氰基取代。 實施例43.實施例41的組合物’其中於式1中’當 Q2係視情況經取代的苯基’以及Q1係一個在第 一鄰位以鹵素或r2()取代的苯基，並視情況在其 -43- 151284.doc 201117722 他鄰位以選自齒素或R20的取代基取代，則Q] 苯基在對位以函素或R20之外的取代基取代。 實施例44.實施例43的組合物，其中於式1中，當 Q2係視情況經取代的苯基，以及Q1係一個在第 一鄰位以齒素或R2Q取代的苯基，並視情況在其 他鄰位以選自鹵素或R2。的取代基取代，則Ql 苯基在對位以氰基取代。 實施例45.實施例40的組合物，其中於式1中，當 Q1係在間位沒有經取代的苯基，其在一個第一 鄰位以鹵素或R20取代，視情況在其他鄰位以選 自鹵素或R2G的取代基取代，以及視情況在對位 以選自鹵素或R20的取代基取代，則至少下列條 件之一為真： (a) 當第一鄰位以齒素取代，則其它鄰位及對位 皆不以R2G取代，以及 (b) 當第一鄰位以R2Q取代，則其它鄰位及對位 皆不以（鹵素或R2Q)取代。 實施例46.實施例45的組合物，其中於式1中，當 Q1係在間位未經取代的苯基，其在第一鄰位以 鹵素或R取代’以及視情況在其他鄰位以選自 鹵素或R2G的取代基取代，則Q1苯基在對位以 鹵素或R2G以外的取代基取代。 實施例47·實施例46的組合物，其中於式1中，當 Q1係在間位未經取代的苯基，其在第一鄰位以 鹵素或R2G取代，以及視情況在其他鄰位以選自 151284.doc • 44· 201117722 鹵素或R2G的取代基取代，則Q1苯基在對位以 氰基取代。 實施例48.實施例45的組合物，其中於式1中，當 Q1係在一個第一鄰位以鹵素或R20取代的笨 基，以及視情況在其他鄰位以選自鹵素或R20的 .取代基取代，則Q1苯基在對位以鹵素或R20以 外的取代基取代。 實施例49.實施例48的組合物，其中於式1中，當 Q1係在一個第一鄰位以鹵素或R20取代的笨 基，以及視情況在其他鄰位以選自鹵素或R20的 取代基取代，則Q1苯基在對位以氰基取代。 實施例50.包含在發明内容概要或實施例1至49中 任一實施例中所描述組分（a)及（b)的組合物， 其中式1中’其中當Q2係視情況經取代的苯基 以及Q1係視情況經取代的苯基，則前述Q1苯基 在對位以氰基取代（以及視情況在其他位置經取 代，如發明内容及實施例中所明確指出的）。 實施例51.實施例50的組合物，其中於式1中，當 Q1係視情況經取代的苯基，則前述Q1苯基在對 位以氰基取代（以及視情況在其他位置經取代， 如發明内容及實施例中所明確指出的）。 實施例52.包含在發明内容概要或實施例1至51中 任一實施例中所描述組分（a)及（b)的組合物， 其中式1中，Q1係在對位以氰基取代的苯基（以 及視情況在其他位置經取代，如發明内容及實施 例中所明確指出的）。 I51284.doc •45· 201117722 貫施例53.包含在發明内容概要或實施例〗至52中 任一實施例中所描述組分（a)及（b)的組合物， 當組成一個化合物的組分（a)選自由下列組分 組成的群組 4-氣-1-(4-氣苯基)-5_(2,6-二氟苯基)-2-甲基 °米σ坐（化合物1)、 2,4-二氣-1-(2-氣-4-氟苯基)-5-(4-氣苯基)_ιη-咪 β坐（化合物5 )、 2_漠-4-氣-5·(2,6-一氟本基)-1-苯基·1Η-β米嗤（化 合物6 )、 2-溴-4-氣-1 -(4-氣苯基)-5-(2,4,6-三氟苯基)_ 咪嗤（化合物7 )、 4-氣-1-(4-氣苯基)-5-(2,6-二氟-4-曱氧苯基)_2•曱 基-111-味唾（化合物22)、 4-氣-1-(4-氯苯基)-5-(2,6-二氟-3-甲氧苯基)·2_甲 基-1Η-Ρ米嗤（化合物77)、 4-氯-5-(2,6-二氟-4-甲氧苯基)-2-甲基-1-(4-曱笨 基)-1Η-^β坐（化合物1〇5)、 4-[4-氣-1-(4-氯苯基)-2-曱基-1Η-咪唾-5-基]_3,5_ 二氟苯腈（化合物134)、 4-氯-5-(2,6-二氟-4-甲氧苯基)-1-(3-氟苯基)_2_曱 基-1H-咪唑（化合物181)、 4-氣-1-(4-氣-3-氟苯基)-5-(2,6-二氟-3-曱氧笨 基)-2-甲基-1H-咪唑（化合物263)、 2-氣-5-[2,4-二氣-5-(2,6-二氟-4-曱氧笨基)-1沁咪 唑_1-基]吡啶（化合物273)、 151284.doc •46- 201117722 氣-1-(4-氣笨基)_2_ 曱基_ΐΗ-σ米吐基] 二氟笨腈（化合物292)、 4-氯-5-(2,6-二氟-4-甲氧苯基）-1-(3,4-二氣笨 基)-2-甲基-1H-咪唑（化合物345 )、 4- 氣-1-(3-氯苯基)-5-(2,6-二氟-4-甲氧苯基)-2甲 基·1Η-咪唑（化合物346)以及 5- [2,4-二氯-5-(2,6-二氟-4-甲氧苯基)-1ίί-咪嗤-1-基]-2-曱基吡啶（化合物387)， 則成份（b )包含至少兩種殺真菌劑組成。 本發明實施例，其中包括上述實施例1-53以及任 何其他於此所述之實施方案，可以以任何方式進行組 合，並且實施例之變化的敘述，不僅涉及到化合物的组 成，包含式1之化合物與至少有一其他殺真菌劑，同時 亦涉及式1之化合物與至少一種無脊椎度動物之害蟲 之防治化合物或藥劑，也涉及式1之化合物及其組合 物’也涉及起始化合物以及有益於製備式1之化合物的 過渡化合物。此外，本發明的實施例，其中包括上述實 施例1-53以及任何其他於此所述之實施方案’與任何 其組合，涉及到本發明的方法。 實施例1-53的結合藉由以下所闡述： 實施例A1.組合物包括在發明内容中描述的組分（a) 以及（b)，其中在式1中， Q1是苯基、售吩基、°塞。坐基、D比11坐基、味σ坐 基、°比咬基、塔ρ井基、喷咬或苯甲基’各 視情況以多達3個選自R3的取代基在碳 151284.doc 47· 201117722 原子環員上取代以及選自R4的取代基在 II原子環員上取代； Q2是苯基"塞吩基、料基、対基、味嗤 基、吡啶基、嗒畊基、嘧啶或笨甲基，各 視其況以多達3個選自r5的取代基在碳 原子環員上取代以及選自R6之取代基在 氮原子環員上取代；以及 R以及R S獨立的i素、氰基、乙婦基、乙 炔基、曱氧基或甲硫基；或甲基，其視情 況以一個選自函素、-OH以及曱基的取代 基取代。 實施例A2.實施例A1的組合物，其中式丨中， Q1是苯基、t定基或苯甲基，各視情況以多 達3個獨立選自R3的取代基在碳原子環 員上取代； Q2是苯基、吡啶基或苯曱基，各視情況以多 達3個獨立選自R5之取代基在碳原子環 員上取代；以及 每個R3以及R5是獨立的鹵素、氰基、Ci-C3 烧基、C2-C3烯基、C2-C3块基、Cj-C^鹵 院基、環丙基、CrC3院氧基、Ci-C^鹵代 烧氧基、CVC3燒硫基、CrC3貌胺基， C2-C4二烷胺基，（：2_(：4烷羰基，c2-C4烧 氧羰基或c2-c4烷羰胺基。 實施例A3.實施例A2的組合物，其中式1中， 151284.doc -48 - 201117722 Q1是苯基或3-°比咬環，視情況以多達3個獨 立選自R3的取代基在碳原子環員上取 代；以及 Q2是一個苯基或3-吡啶環，視情況以多達3 個獨立選自R5的取代基在碳原子環員上 取代 實施例A4.實施例A3的組合物，其中式1 _， R1以及R2是獨立的鹵素、氰基或甲氧基；或 視情況以一個選自F、C1或甲基的取代基 取代的甲基；以及 母個R以及R是獨立的鹵素、氰基、Ci_c3 烧基' C2-C3烯基、CrC3鹵烧基、q_C3 烷氧基、eve：3鹵代烷氧基、Ci_C3烷硫基 或CrC3烷胺基。 實施例A5.實施例A4的組合物，其中式1中，Embodiment 41. The composition of Embodiment 40, wherein in Formula 1, when Q2 is a phenyl group substituted, and Q1 is a phenyl group which is not substituted at the meta position, which is in a first ortho position The substitution of the prime or R' and optionally in the other ortho position is selected from halogen or r2, wherein the Q1 phenyl is substituted in the para position with a substituent other than halogen or r2. Embodiment 42. The composition of Embodiment 41, wherein in Formula 1, when Q2 is optionally substituted phenyl, and Q1 is in the meta position without substituted phenyl 'which is halogen in a first ortho position Or R20 is substituted for 'and optionally substituted with a substituent selected from halogen or R20 in the other ortho position', and the Q1 phenyl group is substituted with a cyano group at the para position. Embodiment 43. The composition of Example 41 wherein 'in the formula 1', when Q2 is optionally substituted phenyl' and Q1 is a phenyl group substituted with halogen or r2() in the first ortho position, and The situation is in its -43-151284.doc 201117722. The ortho position is substituted with a substituent selected from dentate or R20, and the Q] phenyl group is substituted at the para position with a substituent other than a peptidin or R20. Embodiment 44. The composition of Embodiment 43, wherein in Formula 1, when Q2 is optionally substituted phenyl, and Q1 is a phenyl substituted with dentate or R2Q in the first ortho position, and optionally In other ortho positions, it is selected from halogen or R2. Substituted by a substituent, the Ql phenyl group is substituted with a cyano group in the para position. The composition of embodiment 40, wherein in Formula 1, when Q1 is a phenyl group which is not substituted at the meta position, it is substituted with a halogen or R20 in a first ortho position, optionally in the other ortho positions. Substituting a substituent selected from halogen or R2G, and optionally substituting a substituent selected from halogen or R20, at least one of the following conditions is true: (a) when the first ortho position is substituted with dentate, Other ortho and para are not replaced by R2G, and (b) when the first ortho position is replaced by R2Q, the other ortho and para are not substituted by (halogen or R2Q). Embodiment 46. The composition of Embodiment 45, wherein in Formula 1, when Q1 is in the meta-substituted phenyl group, which is substituted with a halogen or R in the first ortho position, and optionally in other ortho positions Substituting a substituent selected from halogen or R2G, the Q1 phenyl group is substituted at the para position with a substituent other than halogen or R2G. Embodiment 47. The composition of Embodiment 46, wherein in Formula 1, when Q1 is in the meta-substituted phenyl group, which is substituted with halogen or R2G in the first ortho position, and optionally in other ortho positions From 151284.doc • 44· 201117722 Substituted by a halogen or a substituent of R2G, the Q1 phenyl group is substituted with a cyano group in the para position. The composition of Embodiment 45, wherein in Formula 1, Q1 is a stupid group substituted with a halogen or R20 in a first ortho position, and optionally in another ortho position selected from halogen or R20. Substituting a substituent, the Q1 phenyl group is substituted at the para position with a substituent other than halogen or R20. Embodiment 49. The composition of Embodiment 48, wherein in Formula 1, Q1 is a stupid group substituted with a halogen or R20 in a first ortho position, and optionally substituted with a halogen or R20 in the other ortho position. Substituting, the Q1 phenyl group is substituted with a cyano group in the para position. Embodiment 50. A composition comprising components (a) and (b) as described in the Summary of the Summary of the Invention or in any one of Embodiments 1 to 49, wherein in Formula 1 wherein Q2 is optionally substituted Wherein phenyl and Q1 are optionally substituted phenyl, the aforementioned Q1 phenyl is substituted in the para position with a cyano group (and optionally at other positions, as explicitly indicated in the Summary of the Invention and the Examples). Embodiment 51. The composition of Embodiment 50, wherein in Formula 1, when Q1 is optionally substituted phenyl, the aforementioned Q1 phenyl is substituted at the para position with a cyano group (and optionally at other positions, As explicitly stated in the Summary of the Invention and the Examples). Embodiment 52. A composition comprising components (a) and (b) as described in the Summary of the Summary of the Invention or in any one of Embodiments 1 to 51, wherein in Formula 1, Q1 is substituted at the para position with a cyano group The phenyl group (and optionally substituted at other positions, as explicitly indicated in the Summary of the Invention and the Examples). I51284.doc • 45· 201117722 Example 53. A composition comprising the components (a) and (b) described in the Summary of the Summary of the Invention or in any of the Examples to 52, when a group constituting a compound Fraction (a) is selected from the group consisting of the following components: 4-nitro-1-(4-phenylphenyl)-5-(2,6-difluorophenyl)-2-methyl ), 2,4-diqi-1-(2-vapor-4-fluorophenyl)-5-(4-phenylphenyl)_ιη-mi-β-supplement (compound 5), 2_diet-4-gas- 5·(2,6-fluoro-based)-1-phenyl·1Η-β rice bran (Compound 6), 2-bromo-4-a-1-(4-phenylphenyl)-5-(2 ,4,6-trifluorophenyl)_imide (compound 7), 4-gas-1-(4-phenylphenyl)-5-(2,6-difluoro-4-indolylphenyl)_2 • mercapto-111-flavored saliva (compound 22), 4-ox-1-(4-chlorophenyl)-5-(2,6-difluoro-3-methoxyphenyl)·2-methyl- 1Η-Ρ米嗤 (Compound 77), 4-chloro-5-(2,6-difluoro-4-methoxyphenyl)-2-methyl-1-(4-indolyl)-1Η-^坐Seat (Compound 1〇5), 4-[4-Ga-1-(4-chlorophenyl)-2-indolyl-1Η-imida-5-yl]_3,5-difluorobenzonitrile (Compound 134 , 4-chloro-5-(2,6-difluoro-4-methoxyphenyl)-1-(3-fluorophenyl)_2-mercapto-1H-imidazole (Compound 1) 81), 4-gas-1-(4-a-3-fluorophenyl)-5-(2,6-difluoro-3-indolyl)-2-methyl-1H-imidazole (compound 263 , 2-gas-5-[2,4-dioxa-5-(2,6-difluoro-4-indolyl)-1-indolizyl-1-yl]pyridine (compound 273), 151284. Doc •46- 201117722 Gas-1-(4-gas base)_2_ 曱基_ΐΗ-σ米普基] Difluoro acyl nitrile (compound 292), 4-chloro-5-(2,6-difluoro- 4-methoxyphenyl)-1-(3,4-dioxaphenyl)-2-methyl-1H-imidazole (compound 345), 4- gas-1-(3-chlorophenyl)-5- (2,6-Difluoro-4-methoxyphenyl)-2methyl·1Η-imidazole (Compound 346) and 5-[2,4-Dichloro-5-(2,6-difluoro-4- Methoxyphenyl)-1ίί-imidol-1-yl]-2-mercaptopyridine (compound 387), component (b) comprises at least two fungicide compositions. Embodiments of the present invention, including the above-described Embodiments 1-53 and any other embodiments described herein, may be combined in any manner, and the description of the variations of the embodiments involves not only the composition of the compound, but also the formula 1 a compound and a compound or agent having at least one other fungicide, and also relating to a compound of formula 1 and at least one pest of an invertebrate animal, and also to a compound of formula 1 and a composition thereof' also relates to a starting compound and is beneficial for A transition compound of the compound of formula 1 is prepared. Furthermore, embodiments of the invention, including the above-described embodiments 1-53 and any other embodiments described herein and in any combination thereof, relate to the method of the invention. The combination of Examples 1-53 is illustrated by the following: Example A1. The composition comprises components (a) and (b) described in the Summary of the Invention, wherein in Formula 1, Q1 is phenyl, phenyl , ° plug. Sitting base, D ratio 11 sitting base, taste σ sitting base, ° ratio biting base, tower ρ well base, jet biting or benzyl group, as many as three substituents selected from R3 in carbon 151284.doc 47· 201117722 The substituent on the atomic ring member and the substituent selected from R4 are substituted on the II atom ring member; Q2 is a phenyl group; a thiophene group, a sulfhydryl group, a thiol group, a pyridyl group, a pyridyl group, a hydrazine group, a pyrimidine or a methyl group, each of which is substituted on the carbon atom ring with up to 3 substituents selected from r5 and a substituent selected from R6 on the nitrogen ring ring; and R and RS are independent Or a cyano group, a cyano group, an ethynyl group, a decyloxy group or a methylthio group; or a methyl group, which is optionally substituted with a substituent selected from a hydroxyl group, -OH and a fluorenyl group. Embodiment A2. The composition of Embodiment A1 wherein, in the formula, Q1 is phenyl, t-bond or benzyl, each optionally substituted with up to 3 substituents independently selected from R3 on a carbon atom ring. Q2 is phenyl, pyridyl or phenylhydrazine, each optionally substituted with up to 3 substituents independently selected from R5 on a carbon atom ring; and each R3 and R5 is independently halogen, cyano, Ci-C3 alkyl, C2-C3 alkenyl, C2-C3 block, Cj-C^ halogen-based, cyclopropyl, CrC3, oxy, Ci-C^haloalkoxy, CVC3 sulphur-based, CrC3 amido group, C2-C4 dialkylamino group, (: 2_(: 4 alkylcarbonyl, c2-C4 alkoxycarbonyl or c2-c4 alkylcarbonylamino. Example A3. The composition of Example A2, wherein 1, 151284.doc -48 - 201117722 Q1 is a phenyl or 3-° ratio bite ring, optionally substituted with up to 3 substituents independently selected from R3 on a carbon atom ring; and Q2 is a phenyl group Or a 3-pyridine ring, optionally substituted with up to 3 substituents independently selected from R5, on the carbon atom ring member. The composition of Example A4. Example A3 wherein R1 and R2 are independently halogen , cyano or methoxy Or, optionally, a methyl group substituted with a substituent selected from F, C1 or methyl; and the parent R and R are independent halogen, cyano, Ci_c3 alkyl 'C2-C3 alkenyl, CrC3 haloalkyl, a alkoxy group, an eve: 3 haloalkoxy group, a Ci_C3 alkylthio group or a CrC3 alkylamino group. Embodiment A5. The composition of Embodiment A4, wherein, in Formula 1,

Ri以及R2是獨立的C卜Br、I或烷基； 每個R3以及R5是獨立的F、Cl、Br、氰基、 crc2烧基、Cl_C2南炫基、Ci_C2、烷氧 基或Q-C2鹵代烷氧基；以及Ri and R2 are independent C, Br, I or alkyl; each R3 and R5 are independently F, Cl, Br, cyano, crc2, Cl_C2 Nan, Ci_C2, alkoxy or Q-C2 Haloalkoxy; and

Qi以及Q2任一者之環經2或3個取代基取代 以及Q以及Q2其它的環以1或2個取代 基取代。 實施例A6.實施例A5的組合物，其中式丨中， R1以及R2是獨立的C卜Br或甲基； Q1及Q2任一者之環是一個笨基或13•吡啶環， 其在一個間位或對位以一個選自F、C1、 I51284.doc -49- 甲基、甲氡基以及氟曱氡基的取代基取 代，以及視情況在剩下的饭置以一個F 做取代；以及 Q1及Q2任一者之環疋一個笨基環，其在兩個 鄰位以F取代以及在一個間位或對位以 選自氰基以及CrC2烧氧基所取代。 實施例A7·實施例A6的組合物，其中成份（a)包 含一個選自以下成分的群組的化合物：化合物 181、化合物292、化合物469、化合物513、化 合物514、化合物515、化合物5丨6、化合物517、 化合物518、化合物519、化合物520、化合物 521、化合物522、化合物523、化合物524、化 合物525、化合物526、化合物527、化合物528、 化合物529、化合物53〇、化合物531、化合物 532、化合物533、化合物534、化合物535，以 及化合物536)。 實施例B1.發明内容中掘述的組合物（包括但不限 制於實施例1到53以及A1到A7中任何一個的 組合物），其中組分（b)包括至少一個選自（bl) 甲基苯并咪唑胺甲酸鹽殺真菌劑的化合物，例如 笨菌靈、多菌靈以及甲基硫菌靈。 實施例B2.發明内容中描述的組合物（包括但不限 制於實施例1到53以及A1到A7中任何一個的 紱合物，其中組分（b)包括至少一個選自（b2) 二甲醯亞胺殺真菌劑的化合物，例如腐黴利、異 菌脲以及乙烯菌核利。 201117722 實施例B3.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b3)脫曱基作用抑制殺真菌劑的化合物，例如 依普座、氟σ查吐、三泰隆、石夕氟β坐、種菌唾、賽 福寧、環克座、待克利、護矽得、護汰芬、滅特 座、邁克尼、撲克拉、普克利、丙硫菌吐、得克 利以及四克利。 實施例Β4.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及Α1到Α7中任何一 個的組合物），其中組分（b )包括至少一個選自 (b4)苯基酰胺殺真菌劑的化合物，例如滅達 樂、滅達樂-M、本達樂、本達樂-M、霜靈、曱 呋醯胺以及毆殺斯。 實施例B5.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b5)胺/嗎福林殺真菌劑的化合物，例如殺螟 丹、嗎菌靈、丁苯嗎啉、克啉菌、三嗎啉醯胺、 苯鏽啶、粉病靈以及葚孢菌素。 實施例B6.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物）’其中組分（b)包括至少一個選自 (b6)填脂質生物合成抑制殺真菌劑的化合物， 例如護粒松以及亞賜圃。 151284.doc -51 · 201117722 實施例B7.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b7)羧醯胺殺真菌劑的化合物，例如百殺芬、 白克列、萎鏽靈、異派來桑、氧化萎鏽靈、派福 芬以及吡噻菌胺。 實施例B8.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b8)羥基(2-胺基-)嘧啶殺真菌劑的化合物，例 如乙菌定。 實施例B9.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b9)苯胺基嘧啶殺真菌劑的化合物，例如赛普 洛。 實施例B10.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (blO) N-苯基胺曱酸鹽殺真菌劑的化合物，例 如乙徽威。 實施例B11.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b 11 )酿外抑制殺真菌劑的化合物，例如亞托 敏、百克敏、β坐胺菌酯、克收欣、三氟敏、51 定氧 151284.doc -52- 201117722 菌酯、唑菌酯、防霉丹、凡殺同、咪唑菌酮、迪 斯可0坐賓 （discostrobin )、因可。坐賓 (enestrobin )、醚菌胺、苯氧菌胺、將醚菌胺以 及氟喊菌酯。 實施例B12.發明内容中描述的組合物（包括但不限 制於實施例1到53以及A1到A7中任何一個的 組合物），其中組分（b)包括至少一個選自（bl2) 苯基°比11各殺真菌劑化合物，例如半種p各以及洛菌 酉旨。 實施例B13.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (bl3)喹啉殺真菌劑的化合物，例如快諾芬。 實施例B14.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (bl4)脂質過氧化抑制殺真菌劑的化合物，例 如氣曱氧苯。 實施例B15.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (bl5)黑色素生物合成抑制-還原酶殺真菌劑的 化合物，例如百快隆以及三賽σ坐。 實施例Β16.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及Α1到Α7中任何一 個的組合物），其中組分（b)包括至少一個選自 151284.doc -53- 201117722 (bl6)黑色素生物合成抑制-脫水酶殺真菌劑的 化合物，例如加普胺。 實施例B17.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b )包括至少一個選自 (b 17 )經基苯胺化物殺真菌劑的化合物，例如 環醯菌胺。 實施例B18.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b )包括至少一個選自 (b 18 )鯊烯-環氧酶抑制殺真菌劑的化合物，例 如稗草畏。 實施例B19.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (bl9)多氧黴素殺真菌劑的化合物，例如多氧 黴素。 實施例B20.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b )包括至少一個選自 (b20)苯脲殺真菌劑的化合物，例如賓克隆。 實施例B21.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b21)醌内抑制殺真菌劑的化合物，例如氰霜 0坐以及°弓丨0坐續菌胺。 151284.doc • 54- 201117722 實施例B22.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b22)苯甲醯胺殺真菌劑的化合物，例如座賽 胺。 實施例B23.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b23 )糖越酸抗生素殺真菌劑的化合物，例如 保米黴素。 實施例B24.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b24 )己°比喃抗生素殺真菌劑的化合物，例如 嘉賜黴素。 實施例B25.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b25)吼喃葡萄糖抗生素的化合物：蛋白質合 成殺真菌劑，例如鏈徽素。 實施例B26.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b26 ) °比喃葡萄糖抗生素的化合物：繭蜜糖酶 以及肌醇生物合成殺真菌劑，例如維利黴素。 151284.doc -55- 201117722 實施例B27.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b27)氰基乙醯胺肟殺真菌劑的化合物，例如 霜脲氰。 實施例B28.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b28)胺曱酸鹽殺真菌劑的化合物，例如普拔 克、胺丙威以及碘代丙炔基丁基曱胺酸酯。 實施例B29.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b29)氧化磷酸化非偶合殺真菌劑的化合物， 例如扶吉胺、百蟎克、富米綜、氧乙酸基白粉克 以及敵蟎普。 實施例B30.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b30)有基錫殺真菌劑的化合物，例如三苯醋 錫。 實施例B31.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b )包括至少一個選自 (b31 )叛酸殺真菌劑的化合物，例如歐索林酸。 151284.doc -56- 201117722 實施例B32.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b32)芳環殺真菌劑的化合物，例如殺紋寧。 實施例B33.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b33 )膦酸鹽殺真菌劑的化合物，例如亞填酸 以及其多種鹽類，包括三乙膦酸鋁。 實施例B34.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b34)氨甲酰苯甲酸殺真菌劑的化合物，例如 克枯爛。 實施例B35.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b3 5 )苯并三喷殺真菌劑的化合物，例如吐菌 °秦。 實施例B36.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b3 6 )苯磺酸胺殺真菌劑的化合物，例如石黃菌 胺。 實施例B37.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 151284.doc -57- 201117722 個的組合物），其中組分（b)包括至少一個選自 (b37 )噠°秦酮殺真菌劑的化合物，例如達滅淨。 實施例B38.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b38) β塞吩-羧醯胺殺真菌劑的化合物，例如石夕 噻菌胺。 實施例Β39.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及Α1到Α7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b39 )嘴α定胺化物殺真菌劑的化合物，例如氣 嘴菌胺。 實施例Β40.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及Α1到Α7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b40)羧酸胺化物殺真菌劑的化合物，例如達 滅芬、苯噻菌胺、苯噻菌胺-異丙基、丙森鋅、 及瓦芬耐、雙炔醯菌胺以及氟嗎啉。 實施例B41.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b )包括至少一個選自 (b41)四環黴素抗生素殺真菌劑的化合物，例 如經四環素。 實施例B42.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 151284.doc -58- 201117722 (b42)硫代氨基甲酸鹽殺真菌劑的化合物，例 如確菌胺。 實施例B43.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b )包括至少一個選自 (b43)苯甲醯胺殺真菌劑的化合物，例如氟吡 菌胺以及氟吡菌醯胺。 實施例B44.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b44)宿主植物防禦誘發殺真菌劑的化合物， 例如阿拉酸式苯-S-曱基。 實施例B45.發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包括至少一個選自 (b45 )多位接觸殺真菌劑的化合物，例如銅氧 氯化物、硫酸銅、銅氫氧化物、波爾多組合物（三 元銅硫化物）、元素硫、鋅錳乃浦、代森聯殺菌 劑、丙森辞、二曱胺曱硫羥羰酸鐵、代森錳、福 美雙、代森鋅、吉闌、滅菌丹、卡普坦、四氯丹 以及百菌清。 實施例B46.發明内容概要中描述的組合物（包含但 不限制於實施例1到53以及A1到A7中任何一 個的組合物），其中組分（b)包含至少一個選自 (M6 )殺真菌劑的化合物，除了組分（a )以及 組分（b 1 )到（b45 )的殺真菌劑，例如°塞口坐菌 I51284.doc -59· 胺、環氟菌胺、丙氧喹啉、滅芬農、派芬農、阿 滅特定（ametoctradine)、貝殺新、甲胂鐵銨、 芬派殺、吡咯尼群、滅蟎猛、泰伏勤、5_氣 -6-(2,4,6-三氟苯基）-7-(4-曱基六氫吡啶_ι· 基）[1，2,4]***[l，5-a]嘧啶（BAS600)、2-丁氧基 -6-埃基-3-丙基-4H-1-笨并哌喃冰酮、3-[5-(4-氯 本基）-2,3- —曱基-3-異。惡〇坐烧基]0比咬 (SYP-Z048)、4-氟笨基 Ν-[1·[[[ΐ_(4-氰基苯基）乙 基]續醢基]曱基]丙基]胺曱酸鹽（Xr_539 )、 N_[[(環丙基甲氧基）胺基][6_(二氟曱氧基)_2,3_ 二氟苯基]亞曱基]笨乙醯胺、N，-[4-[4-氣-3-(三氟 甲基）苯氧基]_2,5_二甲苯基]乙基-N-雙甲 脒、2-[[2-氟-5-(三氟甲基)笨基]硫基]_2_[3-(2-曱 氧苯基)-2-四氫噻唑亞基]乙腈(οκ-5203)、N-(4-氣-2-硝基苯)-N-乙基-4-甲基苯續醢胺（TF-991) 及1-[(2-丙稀硫基)幾基]_2_(1_曱基乙基)_4_(2_甲 基苯基)-5-胺基酸-1H-苯甲腈-3-酮。 實施例B47·發明内容概要中描述的組合物（包括但 不限制於實施例1到53以及A1到A7中任何一 個的組合物）其中組分（b)包括至少一個選自 由以下成分組成的殺真菌化合物：亞托敏、克收 欣、三氟敏、百克敏、唑菌酯、唑胺菌酯、啶氧 菌酯、醚菌胺、笨氧菌胺/芬諾米特賓 (fenominostrobin )(、多菌靈、百菌清、快諾 芬、滅芬農、派芬農、環氟菌胺、苯鏽咬、丁笨 嗎啉、溴克座、環克座、待克利、依普座、芬克 201117722 座、護矽得、菲克利、種菌唑、滅特座、邁克尼' 平克座、普克利、丙硫菌唑、丙硫菌唑、得克利、 滅菌唑、凡殺同、撲克拉、吡噻菌胺以及白克列 (nicobifen) 〇 實施例B48.實施例B47的組合物，其令組分（b) 包括至少一種選自由以下成分組成之群組的殺 真菌化合物：亞托敏、克收欣、三氟敏、百克敏、 咬氧菌酯、趟菌胺、苯氧菌胺/芬諾米特賓 (fenominostrobin)、多菌靈、百菌清、快諾芬、 滅芬農、環氟菌胺、苯鏽啶、丁苯嗎琳、填克座、 環克座、待克利、依普座、芬克座、護♦得、菲 克利、種菌唑、滅特座、邁克尼、平克座、普克 利、波克而拮（proquinazid )、丙硫菌唾、得克 利、滅菌唑、凡殺同、撲克拉、吼喧菌胺以及 克列。 實施例B49.實施例B47的組合物，其中組分（b) 包括至少一種選自由以下成分組成之群組的殺 真菌化合物·亞托敏、克收欣、三氣敏、百克敏、 百克敏、唑胺菌酯、咬氧菌酯、趟菌胺、苯氧菌 胺/芬諾米特賓（fenominostrobin)、快諾芬、咸 芬農、派芬農、環氟菌胺、苯鑛咬、丁笨嗎琳、 環克座、待克利、依普座、護矽得、滅特座、邁 克尼、普克利、丙氧喧琳、丙硫菌°坐、得克利、 滅菌唑、凡殺同以及吡噻菌胺。 實施例B50.實施例B49的組合物，其中組分（b) 包括至少一種選自由以下成分組成之群組的殺 I51284.doc •61· 201117722 真菌化合物：亞托敏、克收欣、三氟敏、百克敏、 啶氧菌酯、醚菌胺、苯氧菌胺/芬諾米特賓 (fenominostrobin )、快諾芬、滅芬農、環氟菌 胺、苯鏽啶、丁苯嗎啉、環克座、待克利、依普 座、護矽得、滅特座、邁克尼、普克利、丙氧喹 啉、丙硫菌唑、得克利、滅菌唑、凡殺同以及吡 噻菌胺。 值得注意的是在此所描述的任何一個實施例中的 組合物，包括實施例1到53、Ai到A7,以及B1到B50, 其中關於式1包括其鹽類但不包含其氧化物；因此 片語「一個式1的化合物」可經片語「一個式1的化合 物或其鹽類」所取代。關注的組合物中，成份（a)包 括式1的化合物或其鹽類。 本發明中實施例中亦值得注意的殺真菌劑成分包 括一殺菌有效劑量的組合物，其來自於實施例1到53、 A1到A7’以及B1到B50以及至少一種附加的組合物’ 其選自於由表面活性劑、固體稀釋劑以及液體稀釋劑所 組成的群組。 本發明貫施例進一步包括防治由真菌類植物病原 造成的植物疾病的方法，其包括應用實施例1到53、 A1到A7，以及B1到B5〇之任一有效殺真菌劑量的組 合物在植物或其部份組織、或植物種子或其幼苗，（例 如：如在此描述的配方組成）^本發明實施例亦包括保 «蒦植物或植物種子感染由真菌類植物病原造成的疾病 的方法，其包含應用實施例1到53、Α1到Α7，以及 151284.doc • 62- 201117722 B1到B50之任一有效殺真菌劑量的組合物在植物或植 物種子。 部分本發明的實施例關於防治植物疾病或保護植 物於主要摧殘植物葉子的疾病，以及/或應用本發明的 成分於植物葉子（即植物本體而非種子）。較佳之使用 方法包含上述之較佳的組合物；以及那些具有獨特防治 效果的疾病，包括真菌類植物病原所造成的植物疾病。 組合本發明中所使用的殺真菌劑可調控疾病的防治以 及延緩抗藥性的發展。 實施例進一步包含： 實施例C1. 一個保護植物免於選自以下疾病的方 法：粉狀黴菌、葉銹病以及殼針孢屬疾病，其 包含應用於植物一包括發明内容或實施例1 到53中任一個中所描述的組分（a)以及（b) 的殺真菌有效劑量的組合物。 實施例C2.實施例C1的方法，其中該疾病是一個 粉狀黴菌疾病以及該組合物組分（b)包括至 少一個殺真菌劑化合物，其選自於亞托敏、邁 克尼以及葚孢菌素。 實施例C3.實施例C2的方法，其中該疾病是一個 小麥粉狀黴菌疾病。 實施例C4.實施例C2或C3的方法，其中組成份 (b)包含亞托敏。 實施例C5.實施例C1的方法，其中該疾病是一個 葉銹病疾病以及該組合物組成份（b)包括至 151284.doc •63· 201117722 少一個殺真菌劑化合物，其選自於亞托敏以及 四克利。 實施例C6.實施例C5的方法，其中該疾病是小麥 葉子葉錢病。 實施例C7.實施例C1的方法，其中該疾病是一個 殼針抱屬疾病以及該組合物組分（b)包括至 少一個殺真菌劑化合物，其選自於亞托敏、啶 氧菌酯、快諾芬、四克利、丁苯嗎啉以及葚孢 菌素。 實施例C8.實施例C7的方法，其中該疾病是小麥 葉子斑癌病。 實施例C9.實施例C7或C8的方法，其中組分（b) 包括至少一個殺真菌劑化合物，其選自於亞托 敏、四克利、芬普福（fenpropiomorph )以及 葚孢菌素。 實施例C10.實施例C1的方法，其中該疾病是一 個殼針孢屬疾病以及該組合物組分（b)包括 至少一個殺真菌劑化合物，其選自於（b5)胺 /嗎福林殺真菌劑。 實施例C11.實施例C10的方法’其中該疾病是小 麥葉子斑痣病。 實施例C12.實施例C10或C11的方法，其中組分 (b)包括至少一個殺真菌劑化合物，其選自 於芬普福（fenpropiomorph)以及葚抱菌素。 實施例C13·實施例C1到C12中任一者之方法’ 其中組分（a)以及（b)以協同性的有效劑ΐ -64· 151284.doc 201117722 來應用（以及互相之間以協同性的比例來使 用）。 值％注意的是相對應於實施例C1至C13中，關於 了種用於防治真g植物病源體所造成之植物疾病的方 法，该方法包含將殺真菌有效劑量的本發明之殺真菌組 合物施予該植物或其之一部分。 如以下流程1 - 9所描述的—個或多個方法或其變化 型可用於製備式1化合物。下列式卜16化合物中，除 ^另有說明，否則Q1、Q2、R1或R2如上述發明内容所 定義。式la及lb係式1之亞群，且除非另有說明，否 則所有式la及lb取代基如上述式丨定義。 式1化合物可如流程丨說明，藉由式2化合物之鹵 ，作用或烷化作用製備而得。通常可利用該項領域中所 習知之各種函化劑而達成鹵化作用，例如：齒元素（例 如：CL、Be、I!)、磺醯氣、氣化碘或適當溶劑中之 N-鹵琥轴醯亞胺（例如：NBS、ncs、NIS)，該適當溶 劑係如：N，N-二甲基曱醯胺、四氣化碳、乙腈、二氣曱 烷或醋酸。藉由式2化合物與金屬化劑，及接續之式 W-Lg烷化劑（其中’ Lg係一脫離基，例如：a、Br、 I ’或磺酸鹽，例如：對曱苯磺酸、甲磺酸或三氟曱磺 酸）之間的反應而達成烷化作用。適當的金屬化劑包 含，例如：正丁基鋰（n-BuLi)、二異丙胺鋰（LDA) 或氫化鈉（NaH)。此處所提及之術語「烷化作用」及 「烷化劑」不限於R1烷基，且包含附加的烷基如烷硫 基、i烷基、烯基、鹵烯基、炔基等等。反應條件請參 見 Almansa et al.，Journal of Medicinal Chemistry 2003, 151284.doc •65- 201117722 46(16)，3463-3475 及 Katritzky et al.，Heterocycles 1997, 44, 67-70。同時，於實例5、實例4的步驟B以及實例 6的步驟C中說明流程1之方法。 流程1 …· R1The ring of either Qi and Q2 is substituted with 2 or 3 substituents and the other rings of Q and Q2 are substituted with 1 or 2 substituents. Embodiment A6. The composition of Embodiment A5 wherein, in the formula, R1 and R2 are independent CBr or methyl; the ring of any of Q1 and Q2 is a stupid or 13•pyridine ring, which is in a The meta or para position is substituted with a substituent selected from the group consisting of F, C1, I51284.doc -49-methyl, decyl, and fluoroindolyl, and optionally substituted with one F in the remaining rice; And a ring of any one of Q1 and Q2, which is substituted with F in two ortho positions and substituted with a cyano group and a CrC2 alkoxy group in one meta or para position. Embodiment A7. The composition of Embodiment A6 wherein component (a) comprises a compound selected from the group consisting of Compound 181, Compound 292, Compound 469, Compound 513, Compound 514, Compound 515, Compound 5丨6 Compound 517, Compound 518, Compound 519, Compound 520, Compound 521, Compound 522, Compound 523, Compound 524, Compound 525, Compound 526, Compound 527, Compound 528, Compound 529, Compound 53, Compound 531, Compound 532, Compound 533, Compound 534, Compound 535, and Compound 536). Embodiment B1. The composition of the invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (bl) Compounds of benzimidazole amine formate fungicides, such as carbendazim, carbendazim, and thiophanate-methyl. Embodiment B2. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7, wherein component (b) comprises at least one selected from the group consisting of (b2) dimethyl Compounds of sulphonimide fungicides, such as procymidone, iprodione, and vinyl nucleus. 201117722 Example B3. Compositions described in the Summary of the Summary (including but not limited to Examples 1 to 53 and A1 to A composition according to any one of A7, wherein component (b) comprises at least one compound selected from the group consisting of (b3) deamination-preventing fungicides, for example, Epto, Fluorine Sigma, Tetralium, Shixi Fluoride β sitting, breeding sputum, Safun, ring, Klee, Guardian, defensive, defensive, McKinney, Poker, Puckley, Propionate, Dekli and Sikhli. Example 4. A composition as described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and Α1 to Α7), wherein component (b) comprises at least one selected from the group consisting of (b4) phenyl Amide fungicide compounds, such as indanol, indanol-M Bendal, Bendol-M, creamer, furosemide and acesulfame. Example B5. Compositions described in the Summary of the Summary (including but not limited to Examples 1 to 53 and A1 to A7 Any one of the compositions), wherein component (b) comprises at least one compound selected from the group consisting of (b5) amine/morphine fungicides, such as chlordane, carbendazim, butylmorpholine, chromobacter, Trimorpholinamide, fenpropidin, powder disease, and fusarium. Example B6. Compositions described in the Summary of the Summary (including but not limited to Examples 1 to 53 and any of A1 to A7 The composition (b) wherein the component (b) comprises at least one compound selected from the group consisting of (b6) lipid-storing biosynthesis inhibiting fungicides, such as Pleurotus ostreatus and A. sinensis. 151284.doc -51 · 201117722 Example B7. Invention The composition described in the Summary of Contents (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b7) carboxamide fungicides Compounds such as chlorfenapyr, leucoside, rustling, sinensis, oxidation Rust, penfen, and penthiopyr. Example B8. Compositions described in the Summary of the Summary (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein the components (b) comprising at least one compound selected from the group consisting of (b8) hydroxy(2-amino-)pyrimidine fungicides, for example, succinate. Example B9. Compositions described in the Summary of the Summary (including but not limited to implementation) The composition of any one of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one compound selected from the group consisting of (b9) anilinopyrimidine fungicides, such as spirox. Example B10. Summary of the Invention The composition described in the Summary (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (blO) N-phenylamine citric acid A compound of a salt fungicide, such as B. Embodiment B11. Compositions described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from (b 11 ) A compound that inhibits fungicides, such as atropine, baikemin, beta-sodium citrate, kexinxin, trifluoro-sensitive, 51-oxygen 151284.doc -52-201117722 bactericidal ester, azole, anti-mildew Dan, where the same, imidacloprid, disco 0 sitting (discostrobin), because. Essence (enestrobin), ether oxystrobin, phenoxystrobin, behenamide and flufenicol. Embodiment B12. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (bl2) phenyl ° ratio of 11 fungicide compounds, for example, half of each p and bacterium. Embodiment B13. Compositions described in the Summary of the Summary (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (bl3) quinolin A compound of a bacterin fungicide, such as a fast nofen. Embodiment B 14. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (bl4) lipids A compound that peroxidizes a fungicide suppressant, such as a gas oxybenzene. Embodiment B 15. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (bl5) melanin Compounds that biosynthesize inhibitor-reductase fungicides, such as Baikulong and Sansai Sigma sit. EXAMPLES 16. Compositions described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and Α1 to Α7), wherein component (b) comprises at least one selected from the group consisting of 151284.doc - 53-201117722 (bl6) A compound of melanin biosynthesis inhibition-dehydratase fungicide, such as gupamine. Embodiment B 17. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Embodiments 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from (b 17 ) A compound of a anilide fungicide, such as cyclosporin. Embodiment B 18. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from (b 18 ) Squalene-epoxidase compounds that inhibit fungicides, such as sedge. Embodiment B19. Compositions described in the Summary of the Summary (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (bl9) A compound of oxymycin fungicide, such as polyoxymycin. Embodiment B20. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b20) benzene A compound of a urea fungicide, such as a clone. Embodiment B21. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b21) A compound that inhibits a fungicide, such as a cyanogen 0 sitting and a sputum. 151284.doc • 54- 201117722 Example B22. Summary of the composition described in the Summary (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) includes at least A compound selected from the group consisting of (b22) benzamide fungicides, such as ticlopamide. Embodiment B23. Compositions described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b23) sugars A compound that is more acidic than an antibiotic fungicide, such as benzimycin. Embodiment B24. Compositions described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b24) A compound that is more than an antibiotic fungicide, such as carnitamicin. Embodiment B 25. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Embodiments 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b25) Compounds of glucosamine antibiotics: protein synthesis fungicides, such as stellate. Embodiment B 26. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b26) ° Compounds that are more than glucosamine antibiotics: indolease and inositol biosynthesis fungicides, such as viralimycin. 151284.doc -55-201117722 Embodiment B27. Composition of the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) includes at least A compound selected from the group consisting of (b27) cyanoacetamide fungicides, such as cymoxanil. Embodiment B 28. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one amine selected from the group consisting of (b28) Compounds of phthalate fungicides, such as plunk, amphetamine, and iodopropynyl butyl phthalate. Embodiment B 29. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b29) oxidation Compounds that phosphoreize non-coupling fungicides, such as chlorpromazine, genomics, fulva, oxyacetate, and carbendazim. Embodiment B30. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from (b30) A compound of a base tin fungicide, such as triphenylacetate. Embodiment B31. Compositions described in the Summary of the Summary (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from (b31) rebellion A compound of an acid fungicide, such as oxolinic acid. 151284.doc -56-201117722 Embodiment B32. Summary of the composition described in the Summary (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) includes at least A compound selected from the group consisting of (b32) aromatic ring fungicides, such as chlorpyrifos. Embodiment B33. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b33) phosphine Compounds of acid salt fungicides, such as sub-acids and various salts thereof, include aluminum triethylphosphinate. Embodiment B34. Compositions described in the Summary of the Summary (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b34) ammonia A compound of a formylbenzoic acid fungicide, such as gram rot. Embodiment B35. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b3 5 ) A compound of a benzotriazole fungicide, such as a fungus. Embodiment B36. Compositions described in the Summary of the Summary (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b3 6 ) A compound of a benzilsulfonamide fungicide, such as sulphate. Embodiment B37. Compositions described in the Summary of the Invention (including but not limited to the compositions of Examples 1 to 53 and any of 151284.doc-57-201117722), wherein component (b) comprises At least one compound selected from the group consisting of (b37) guanidinium fungicides, for example, chlorhexidine. Embodiment B38. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b38) β A compound of a pheno-carboxamide fungicide, such as lithosparin. EXAMPLES 39. Compositions described in the Summary of the Summary (including but not limited to the compositions of any of Examples 1 to 53 and Α1 to Α7), wherein component (b) comprises at least one selected from the group consisting of (b39) mouths A compound of an a fixed aminide fungicide, such as a chlorfenapyr. Embodiments 40. Compositions described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and Α1 to Α7), wherein component (b) comprises at least one selected from the group consisting of (b40) carboxylic acid Compounds of acid aminating fungicides, such as dadifene, benzilifen, benzilid-isopropyl, zinc propionate, and valfenic acid, dipropionin, and flumorph. Embodiment B41. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b41) A compound of a cyclomycin antibiotic fungicide, such as tetracycline. Embodiment B42. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of 151284.doc - 58-201117722 (b42) A compound of a thiocarbamate fungicide, such as amphotericin. Embodiment B43. Compositions described in the Summary of the Summary (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b43) benzene Compounds of methotrexate fungicides, such as fluopyram and fluopyram. Embodiment B44. Compositions described in the Summary of the Summary (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one host selected from the group consisting of (b44) A plant defense compound that induces a fungicide, such as phenyl-S-fluorenyl arsenate. Embodiment B45. Compositions described in the Summary of the Summary (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from the group consisting of (b45) Compounds in contact with fungicides, such as copper oxychloride, copper sulphate, copper hydroxide, Bordeaux composition (ternary copper sulfide), elemental sulphur, zinc manganese sulphur, daisenlian fungicide, propyl sin , Diamine, iron thioglycolate, mancozeb, thiram, daisen zinc, jirong, sterilized Dan, captan, tetrachlordane and chlorothalonil. Embodiment B46. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7), wherein component (b) comprises at least one selected from (M6) a compound of a fungicide, in addition to component (a) and a fungicide of components (b 1 ) to (b45 ), for example, S. serrata I51284.doc -59·amine, cycloflufenamide, propoxyquinol , fenfennon, pheninone, amitoctradine, bezoxin, formazan, fentan, pyrrolidine, chlorpyrifos, tafuqin, 5_gas-6-(2, 4,6-trifluorophenyl)-7-(4-mercaptohexahydropyridine_ι·yl)[1,2,4]triazole [l,5-a]pyrimidine (BAS600), 2-butoxy -6-E-propyl-3-propyl-4H-1-indolopyranone, 3-[5-(4-chlorobenzyl)-2,3-indolyl-3-iso. 〇 〇 ] 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 】 Amine citrate (Xr_539), N_[[(cyclopropylmethoxy)amino][6-(difluorodecyloxy)_2,3-difluorophenyl]indolyl] oxaethylamine, N, -[4-[4-Ga-3-(trifluoromethyl)phenoxy]_2,5-dimethylphenyl]ethyl-N-bisformamidine, 2-[[2-fluoro-5-(three Fluoromethyl) phenyl]thio]_2_[3-(2-indolylphenyl)-2-tetrahydrothiazolylene] acetonitrile (οκ-5203), N-(4-gas-2-nitrobenzene )-N-ethyl-4-methylbenzene decylamine (TF-991) and 1-[(2-propionylthio)methyl]_2_(1_mercaptoethyl)_4_(2_methyl Phenyl)-5-amino acid-1H-benzonitrile-3-one. Embodiment B47. The composition described in the Summary of the Invention (including but not limited to the compositions of any of Examples 1 to 53 and A1 to A7) wherein component (b) comprises at least one member selected from the group consisting of Fungal compounds: atoreno, kexinxin, trifluoro-sensitive, baikemin, oxacillin, pyraclostrobin, picoxystrobin, noxifamine, phenoxybenzamine/fennominostrobin (fenominostrobin) , carbendazim, chlorothalonil, vinofenol, fenfenin, phenfenolone, cycloflufenamide, benzene rust biting, butyl streptozoline, bromide, ring gram, holly, yip, fen克201117722 Block, Guardian, Fickley, Oxazole, Gator, McKinney's Dingke, Puckley, Prothioconazole, Prothioconazole, Dekli, Sterilization, Fanzhi, Poker The composition of the compound of Example B47, wherein the component (b) comprises at least one fungicidal compound selected from the group consisting of: Atmomin, and nicobifen. , Kexinxin, trifluoromethane, baikemin, oxycardpenic acid, carbendazim, phenoxystrobin/fenofibrate (fenominostrobin), carbendazim, chlorothalonil, vinofenol, fentanyl, cycloflufenamide, fenpropidin, butyl benzophene, keke, ring gem, holly, yip, fink Block, protect ♦, Fickley, inobutazole, chlorpyrifos, micney, pingke, pugli, poke, proquinazid, thiophene saliva, dexamethasone, sterilized azole, mortal, poker The composition of the embodiment B47, wherein the component (b) comprises at least one fungicidal compound selected from the group consisting of: Atomin, Kexinxin , three gas sensitizer, baikemin, baikemin, pyraclostrobin, oxysporin, carbendazim, phenoxybenzamine/fennomitrol (fenominostrobin), vebufen, salty fennon, senthenin, Cyclofluridamide, benzene ore biting, Ding stupid Lin, Ring Glock, Waiting Klee, Epp seat, Guardian, Deterrence, McKinney, Puckley, propoxylate, propionate The composition of the embodiment B49, wherein the component (b) comprises at least one A species selected from the group consisting of the following ingredients: I51284.doc • 61· 201117722 Fungal compounds: Atomin, Kexinxin, Trifluoro-sensitive, Baikemin, Picoxystrobin, Ethionamide, phenoxystrobin/ Fenominostrobin, fenprofen, fentanyl, cycloflufenamide, fenpropidin, butyl morpholine, cyclazone, holly, yipu, 矽 矽, 灭 特, Mike Nik, pk, propoxyquine, prothioconazole, dexamethasone, sterilized azole, chlorpyrifos and pirfenamide. It is noted that the compositions in any of the embodiments described herein, including the practice Examples 1 to 53, Ai to A7, and B1 to B50, wherein the formula 1 includes a salt thereof but does not include an oxide thereof; therefore, the phrase "a compound of the formula 1" may be in the phrase "a compound of the formula 1 or Replaced by its salts. In the composition of interest, component (a) includes a compound of formula 1 or a salt thereof. A fungicide component which is also notable in the examples of the present invention comprises a bactericidal effective amount of a composition derived from Examples 1 to 53, A1 to A7' and B1 to B50 and at least one additional composition' From the group consisting of surfactants, solid diluents, and liquid diluents. Embodiments of the present invention further comprise a method of controlling a plant disease caused by a fungal plant pathogen comprising applying the composition of any of the effective fungicidal doses of Examples 1 to 53, A1 to A7, and B1 to B5 in plants or Part of the tissue, or plant seed or seedling thereof, (for example, a formulation as described herein). The embodiment of the invention also includes a method of protecting a plant or plant seed from a disease caused by a fungal plant pathogen, comprising Application Examples 1 to 53, Α1 to Α7, and 151284.doc • 62-201117722 Any of the effective fungicidal dosage compositions of B1 to B50 in a plant or plant seed. Some embodiments of the invention are directed to controlling plant diseases or protecting plants from diseases which primarily destroy plant leaves, and/or applying the ingredients of the invention to plant leaves (i.e., plant bodies rather than seeds). Preferred methods of use include the preferred compositions described above; and those diseases which have unique control effects, including plant diseases caused by fungal plant pathogens. The combination of the fungicide used in the present invention can regulate the prevention and treatment of diseases and delay the development of drug resistance. The examples further comprise: Example C1. A method of protecting a plant from a disease selected from the group consisting of a powdery mold, a leaf rust, and a candida disease, comprising the application to the plant, including the inventive content or Examples 1 to 53 A fungic effective amount of a composition of components (a) and (b) as described in any one of the compositions. The method of embodiment C1, wherein the disease is a powdery mold disease and the component (b) comprises at least one fungicide compound selected from the group consisting of atropin, McAfee, and Fusarium. Prime. The method of embodiment C2 wherein the disease is a wheat flour mildew disease. Embodiment C4. The method of Embodiment C2 or C3 wherein component (b) comprises atramine. The method of embodiment C1, wherein the disease is a leaf rust disease and the composition component (b) comprises to 151284.doc • 63· 201117722 one less fungicide compound selected from the group consisting of And four miles. The method of embodiment C5, wherein the disease is wheat leaf leaf disease. The method of embodiment C1, wherein the disease is a scleroderma disease and the component (b) comprises at least one fungicide compound selected from the group consisting of atropine, picoxystrobin, Fast nofen, tetraclimate, butyl morpholine and fusarium. The method of embodiment C7, wherein the disease is wheat leaf spot cancer. The method of embodiment C7 or C8, wherein component (b) comprises at least one fungicide compound selected from the group consisting of azotropin, tetraclimate, fenpropiomorph, and fusarium. The method of embodiment C1, wherein the disease is a genus of the genus Aspergillus and the component of the composition (b) comprises at least one fungicide compound selected from the group consisting of (b5) amine/folin Fungal agent. Embodiment C11. The method of Embodiment C10 wherein the disease is wheat leaf spot disease. The method of embodiment C10 or C11, wherein component (b) comprises at least one fungicide compound selected from the group consisting of fenpropiomorph and oxytocin. The method of any one of the embodiments C1 to C12 wherein the components (a) and (b) are applied with a synergistic effective agent ΐ-64·151284.doc 201117722 (and synergy with each other) The proportion to use). The value % is noted in relation to the embodiments C1 to C13, relating to a method for controlling a plant disease caused by a true g plant pathogen, the method comprising a fungicidal effective dose of the fungicidal composition of the invention The plant or a part thereof is administered. One or more of the methods described in Schemes 1-9 below, or variations thereof, can be used to prepare the compound of Formula 1. In the following compounds of the formula 16, unless otherwise stated, Q1, Q2, R1 or R2 are as defined in the above summary. Formula la and lb are subgroups of formula 1, and unless otherwise stated, all formulas la and lb substituents are as defined above. The compound of formula 1 can be prepared by the halogen, action or alkylation of the compound of formula 2 as illustrated by the scheme. Halogenation can usually be achieved by various functionalizing agents known in the art, such as: tooth elements (eg CL, Be, I!), sulfonium, gasified iodine or N-halogen in a suitable solvent Axil imine (for example: NBS, ncs, NIS), such a suitable solvent is N, N-dimethylguanamine, tetra-carbonized carbon, acetonitrile, dioxane or acetic acid. By the compound of formula 2 and a metallizing agent, and the subsequent formula W-Lg alkylating agent (wherein 'Lg is a leaving group, for example: a, Br, I' or a sulfonate, for example: p-toluenesulfonic acid, The reaction between methanesulfonic acid or trifluoromethanesulfonic acid) achieves alkylation. Suitable metallizing agents include, for example, n-butyllithium (n-BuLi), lithium diisopropylamide (LDA) or sodium hydride (NaH). The terms "alkylation" and "alkylating agent" as used herein are not limited to R1 alkyl and include additional alkyl groups such as alkylthio, i-alkyl, alkenyl, haloalkenyl, alkynyl, and the like. . For reaction conditions, see Almansa et al., Journal of Medicinal Chemistry 2003, 151284.doc • 65-201117722 46(16), 3463-3475 and Katritzky et al., Heterocycles 1997, 44, 67-70. Meanwhile, the method of the flow 1 is explained in the example B, the step B of the example 4, and the step C of the example 6. Process 1 ...· R1

豳化琍 或 1.金屬化劑 2·親電子劑（例如，P-Lg) 式1化合物可以接受各種親核性及金屬化反應以 添加取代基或修飾現有的取代基，並由此提供其他式1 官能化合物。例如，式1化合物，其中Ri與/或R2係鹵 素’可進行親核性置換以提供式1化合物，其中R1與/ 或R係透過一 〇或S原子鏈結至η米嗅環之基團（例如： 與烧氧化物或硫醇化物置換）。通常這些反應係在有適 當基底（例如··氫化鈉、異丁基氧化鉀、碳酸鉀或三乙 胺）的溶劑中進行；該溶劑如：酒精、乙腈或Ν，Ν-二 曱基曱醯胺；反應溫度介於室溫至溶劑之回流溫度之 間。在該領域中已習知用於進行齒素之親核性置換的一 般程序，且可輕易變換以製備本發明之化合物。咪唑相 關步驟請參見 Grimmett et al.，Australian Journal of豳 琍 or 1. metallizing agent 2 · electrophile (for example, P-Lg) The compound of formula 1 can accept various nucleophilic and metallation reactions to add substituents or modify existing substituents, and thereby provide other Formula 1 Functional compound. For example, a compound of formula 1, wherein Ri and/or R2 is a halogen, can be subjected to a nucleophilic displacement to provide a compound of formula 1, wherein R1 and/or R are transmitted through a chain of a hydrazine or S atom to a group of the η meter olfactory ring. (Example: Replacement with burnt oxide or thiolate). Usually these reactions are carried out in a solvent with a suitable substrate such as sodium hydride, potassium isobutylate, potassium carbonate or triethylamine; such solvents as: alcohol, acetonitrile or hydrazine, Ν-dimercaptopurine Amine; the reaction temperature is between room temperature and the reflux temperature of the solvent. The general procedure for performing nucleophilic displacement of dentate is well known in the art and can be readily adapted to prepare compounds of the invention. For imidazole related steps, see Grimmett et al., Australian Journal of

Chemistry 1987, 40(8)，1399-1413。 同時，式1化合物’其中R1與/或R2係溴基或碘基， 其在有纪或鎳觸媒存在時可與式Ri_Met或R2_Met (其 151284.doc -66 - 201117722 中 Met 係 Sn、Zn、B(OH)2、Mg、Li、Cu 或其他適當 的相對離子）化合物交叉耦合以產生式la之化合物， 其中R1與/或R2係氰基、烧基、稀基 '鹵稀基、炔基等 等。較佳觸媒包含但不限於Pd(PPh3)4、PdCl2(；PPh3；)2、 PdClz(二苯基膦二茂鐵）、NiCWPPh3)2以及肆（三-2-咬味 膦基）鈀。各反應之條件將取決於所用之觸媒及式 R1-Met或R2-Met化合物中的相對離子。對於牽涉式 R]-Met或R2-Met化合物的反應而言，基質（例如：驗 金屬碳酸鹽、三級胺或鹼金屬氟化物）之存在是必要 的’式 R^Met 或 R2-Met 中 Met 係 B(OH)2。實例 9、u、 12、13、14及19說明各種用於製備某些式1化合物的 交又耦合反應。 如流程2所示，式1化合物可另外藉由式3化合物 的鹵化作用製備而得，較佳係於咪唑環之4-位，以提供 式4化合物，其中R1係函素；該式4化合物可接著以 第二當量之相同或不同的鹵化劑處理’以提供式1化合 物，其中R1及R2係鹵素。流程2用於製備式4化合物 的方法的實例，參見實例1及22之步驟C。同時，流 程2用於製備式1化合物的方法的實例，其中該化合物 之R1係氯基及R2係溴基，請參見實例22之步驟D。 另外，可利用2當量的鹵化劑處理式3化合物，以直接 得到一式1化合物，其中R1及R2皆係相同的鹵素。用 於製備式1化合物的方法的實例，請參見實例2及實例 3的步驟C，其中該式1化合物的R1及R2皆係相同的 鹵素。 151284.doc -67- 201117722 另外，如流程2所示，可藉由在0°C到室溫之溫度 下，於溶劑中利用試劑將式4化合物金屬化而製得式1 化合物；其中，該式1化合物之R2係鹵素、烷基、烧 硫基、_烷基、烯基、鹵烯基、炔基等等，該溶劑係如： 四氫呋喃、二氧陸圜或甲苯，該試劑係例如：η-丁基裡 (n-BuLi)、二異丙胺鋰（LDA)或氫化鈉（NaH)。該 陰離子接著與一親電子劑接觸以引導一 R2基團加至式 4之上，由此而形成式1之化合物。 流程2Chemistry 1987, 40(8), 1399-1413. Meanwhile, the compound of the formula 1 wherein R1 and/or R2 is a bromo group or an iodo group, which may exist in the presence of a cation or a nickel catalyst with the formula Ri_Met or R2_Met (its 151284.doc -66 - 201117722 Met system Sn, Zn , B(OH)2, Mg, Li, Cu or other suitable relative ionic) compounds are cross-coupled to produce a compound of formula la, wherein R1 and/or R2 are cyano, alkyl, dilute, <halogen, alkyne Base and so on. Preferred catalysts include, but are not limited to, Pd(PPh3)4, PdCl2(;PPh3;)2, PdClz(diphenylphosphinoferrocene), NiCWPPh3)2, and ruthenium (tris-2-tertenephosphino)palladium. The conditions of each reaction will depend on the catalyst used and the relative ions in the formula R1-Met or R2-Met. For the reaction involving a compound of the formula R]-Met or R2-Met, the presence of a substrate (for example, a metal carbonate, a tertiary amine or an alkali metal fluoride) is necessary in the formula 'R^Met or R2-Met Met is B(OH)2. Examples 9, u, 12, 13, 14 and 19 illustrate various cross-coupling reactions for the preparation of certain compounds of formula 1. As shown in Scheme 2, the compound of Formula 1 can be additionally prepared by halogenation of a compound of Formula 3, preferably at the 4-position of the imidazole ring, to provide a compound of Formula 4 wherein R1 is a cyclin; It can then be treated with a second equivalent of the same or different halogenating agent to provide a compound of formula 1, wherein R1 and R2 are halogen. An example of a process for the preparation of a compound of formula 4, see step C of Examples 1 and 22. Also, Scheme 2 is an example of a method for preparing a compound of Formula 1, wherein R1 is a chloro group and R2 is a bromo group of the compound, see Step D of Example 22. Alternatively, the compound of formula 3 can be treated with 2 equivalents of a halogenating agent to provide a compound of formula 1 wherein R1 and R2 are the same halogen. For an example of a method for preparing a compound of formula 1, see step 2 of Example 2 and Example 3, wherein R1 and R2 of the compound of Formula 1 are the same halogen. 151284.doc -67- 201117722 In addition, as shown in Scheme 2, a compound of formula 1 can be obtained by metallizing a compound of formula 4 in a solvent at a temperature of from 0 ° C to room temperature; wherein The R2 compound of the formula 1 is a halogen, an alkyl group, a thiol group, an alkyl group, an alkenyl group, a haloalkenyl group, an alkynyl group or the like. The solvent is, for example, tetrahydrofuran, dioxane or toluene, and the reagent is, for example: Η-butyl (n-BuLi), lithium diisopropylamide (LDA) or sodium hydride (NaH). The anion is then contacted with an electrophile to direct an R2 group to the formula 4, thereby forming a compound of formula 1. Process 2

N Q1 鹵化剞 Q2N Q1 bismuth halide Q2

或 1. 金屬化劑 2. 親電子劑（例如，鹵化辂劑或R2-Lg) 鹵化劑、Or 1. metallizing agent 2. electrophilic agent (for example, antimony halide or R2-Lg) halogenating agent,

.NI2Q 1.NI2Q 1

其中R1是鹵素 如流程3之概述可合成式2化合物。在第一步驟 中，式5化合物係具有式（^X1之鹵化物的N_聚芳基 物，其中X1係I、Cn、Br或F。化學文獻所公開的數個 條件可用於引導一經取代芳基或一雜芳基團加至式5 151284.doc * 68 - 201117722 之上’包含銅-催化條件，其牽涉到在適當的溶劑中使 用適當的銅源（例如：碘化銅⑴或三氟化銅（1))以及碳 酸金屬基底（例如：鉀或碳酸鉋），該適當溶劑係例如： 各、一氧陸圜或乙腈（參見 Buchwald et al.，Tetrahedron Letters 1999, 40, 2657-2660 and Jiang et al., Journal ofWherein R1 is a halogen, as outlined in Scheme 3, a compound of formula 2 can be synthesized. In a first step, the compound of formula 5 is an N-polyaryl compound of the formula (^X1, wherein X1 is I, Cn, Br or F. Several conditions disclosed in the chemical literature can be used to guide a substitution An aryl or a heteroaryl group is added to the formula 5 151284.doc * 68 - 201117722 to contain copper-catalyzed conditions involving the use of a suitable copper source in a suitable solvent (eg copper iodide (1) or Copper fluoride (1)) and a metal carbonate substrate (for example: potassium or carbonic acid planing), such as: each, monooxon or acetonitrile (see Buchwald et al., Tetrahedron Letters 1999, 40, 2657-2660) And Jiang et al., Journal of

Organic Chemistry 2007, 72, 8943-8946)。實例 6 之步驟 A亦說明了流程3中用於製備式6化合物的方法。 在接下來的步驟中，式6化合物可藉由與式βχ1 之鹵化物作用而直接轉化為式2化合物，該反應係於含 有醋酸鈀(II)、三芳基膦配位基以及氟化鉋的溶劑中進 行’該溶劑係如：回流溫度下之二氧陸園、四氫呋喃或 乙腈。代表性之參考文獻請參見Beilina et al.，Journal ofOrganic Chemistry 2007, 72, 8943-8946). Step A of Example 6 also illustrates the process used in Scheme 3 for the preparation of the compound of Formula 6. In the next step, the compound of formula 6 can be directly converted to the compound of formula 2 by the action of a halide of the formula βχ1, which is based on a palladium (II) acetate, a triarylphosphine ligand, and a fluorinated planer. The solvent is carried out in a solvent such as dioxane, tetrahydrofuran or acetonitrile at reflux temperature. For a representative reference, see Beilina et al. ,Journal of

Organic Chemistry 2005, 70, 3997-4005。同時，實例 6 之步驟B說明利用流程3之方法製備式2化合物。此 外，利用正丁基鋰（n-BuLi)或二異丙胺鋰（LDA)鋰 化式6化合物，接著以三烷有機錫氯或亞硼酸（或酯） 處理該陰離子而形成式7化合物。利用熟知之過渡金屬 -催化交叉耦合反應條件以式βΧ1鹵化物處理式7化合 物，而形成式2化合物。通常該反應係於鈀觸媒存在時 進行。各種含鈀化合物及複合物在流程3之方法中係作 為觸媒，包含PdCl2(PPh3)2(二氯雙（三苯膦）鈀（II))、 Pd(PPh3)4(肆(三苯膦)鈀(〇))及Pd2(dba)3。相關參考文獻 請參閱，例如，Ragan et al” Organic Process Research &amp; Development 2003，7(5), 675-683 ;及 Gaare et al.，Acta Chemica Scandinavica 1993, 47, 57-62。 151284.doc -69- 201117722Organic Chemistry 2005, 70, 3997-4005. Meanwhile, Step B of Example 6 illustrates the preparation of the compound of Formula 2 by the method of Scheme 3. Further, the compound of the formula 7 is formed by lithiation of the compound of the formula 6 with n-butyllithium (n-BuLi) or lithium diisopropylamide (LDA) followed by treatment of the anion with trioxane organotin chloride or boronic acid (or ester). The compound of formula 2 is formed by treating the compound of formula 7 with a formula βΧ1 halide using well-known transition metal-catalyzed cross-coupling reaction conditions. Usually the reaction is carried out in the presence of a palladium catalyst. Various palladium-containing compounds and complexes are used as catalysts in the process of Scheme 3, including PdCl2(PPh3)2 (dichlorobis(triphenylphosphine)palladium(II)), Pd(PPh3)4 (肆 (triphenylphosphine) Palladium (〇)) and Pd2 (dba) 3. For related references, see, for example, Ragan et al" Organic Process Research &amp; Development 2003, 7(5), 675-683; and Gaare et al., Acta Chemica Scandinavica 1993, 47, 57-62. 151284.doc - 69- 201117722

5 流程3 Η q2xj --_5 Process 3 Η q2xj --_

其中L是(统基)3Sn或Β(0Η)2 式2化合物亦可以流程4所示之方法製備。在此方 法中，首先在溶劑中利用金屬化劑金屬化式8化合物， a亥金屬化反應係於大約〇°C到室溫之溫度中進行；其 中，該金屬化劑係如：正丁基鋰（n-BuLi)、二異丙胺 鐘（LDA)或氫化鈉（NaH) ’該溶劑係如：四氫吱喃、 二氧陸園或甲苯。該陰離子接著與一親電子劑接觸以引 導一 R2基團加至式8之上，因此而形成式2化合物。 為了進行齒化作用，該親電子劑可以係一齒素衍生物， 例如：N-氯琥珀醯亞胺（NCS )、N-溴琥珀醯亞胺 (NBS)、N-碘琥珀醯亞胺（NIs)、六氯乙烷或1，2-二 溴四氯乙烷。為了進行烷化作用，該親電子劑可以是式 R2-Lg烧化劑（其中Lg係一脫離基’例如：C卜Br、I 或是磺酸鹽，例如：對甲苯磺酸、曱磺酸或三氟甲磺酸） 151284.doc • 70· 201117722 其中R2係烧基、烧硫基、_烧基、稀基、鹵稀基、快 基等等。此處所提及之術語「烷化作用」及「烷化劑」 不限於為烷基之R2。相關參考文獻請參見Wherein L is a compound of the formula 3Sn or Β(0Η)2. The compound of the formula 2 can also be prepared by the method shown in Scheme 4. In this method, first, a metallizing agent is used to metallize a compound of the formula 8 in a solvent, and the a-metallization reaction is carried out at a temperature of about 〇 ° C to room temperature; wherein the metallizing agent is, for example, n-butyl Lithium (n-BuLi), diisopropylamine (LDA) or sodium hydride (NaH) 'This solvent is, for example, tetrahydrofuran, dioxane or toluene. The anion is then contacted with an electrophile to direct an R2 group to the formula 8, thereby forming a compound of formula 2. For toothing, the electrophile may be a dentate derivative such as N-chlorosuccinimide (NCS), N-bromosuccinimide (NBS), N-iodosuccinimide ( NIs), hexachloroethane or 1,2-dibromotetrachloroethane. For alkylation, the electrophile may be a R2-Lg burn-in agent (wherein Lg is a de-based group such as: C, Br, I or a sulfonate such as p-toluenesulfonic acid, sulfonic acid or Trifluoromethanesulfonic acid) 151284.doc • 70· 201117722 wherein R 2 is a calcining group, a sulfur-burning group, a azo group, a dilute group, a halogen group, a fast group, and the like. The terms "alkylation" and "alkylating agent" as referred to herein are not limited to R2 which is an alkyl group. See related references

Almansa et al.,Almansa et al.,

Journal of Medicinal Chemistry 2003，46，3463-3475 同 時，實例4之步驟A說明流程4利用LDA及蛾甲烷之 方法。 流程4Journal of Medicinal Chemistry 2003, 46, 3463-3475 At the same time, Step A of Example 4 illustrates the method of Process 4 using LDA and moth methane. Process 4

式8化合物為已知且可藉由此處所揭示的數個方 法之一製備。例如，利用一類似於流程3所揭露之方 法，由式5化合物，其中R2係H，開始形成式8化合 物。另外，可利用式12或13化合物藉由類似於下方流 程6所述之方法製備式8化合物，其中，該式12戍13 化合物中R1係Η ’（意即當R1係H，式12係對曱苯磺 甲基異氰化物（p-toluenesulfonylmethyl isocyanide)及 式13係苯并***-1-基甲基異氰化物）。利用對甲苯磺曱 基異氣化物合成式8化合物請參見實例1及3之步驟b。 流程5說明的另一方法中，可藉由式9之N_氯胺 化物與式10之烯胺化物的反應製備式2化合物。在此 方法中，藉由一在原位產生之4-嗎啉基_4,5·二氫咪唑之 151284.doc •71 · 201117722 中介性而進行環化作用脫去該嗎啉基團以形成式2化 合物。通吊該反應係於有基底之溶劑中進行；該基底係 如，吡啶、4-(二曱胺）吡啶或三烷基胺，該溶劑係如： 二氣曱烷、二氯曱烷、四氣化碳或曱苯，反應溫度係介 於大約0°C至該溶劑之回流溫度之間。代表性之參考文 獻凊參見 Pocar et al·，Tetrahedron Letters 1976，21, 1839-1842。熟習該領域之技藝人士將會認可式2之咪 嗤環亦可由許多化學文獻中描述的其他方法製備而 得。例如，Wiglenda et al.描述之一般方法，J0urnal 0fCompounds of formula 8 are known and can be prepared by one of several methods disclosed herein. For example, using a method similar to that disclosed in Scheme 3, a compound of formula 5 wherein R2 is H, begins to form a compound of formula 8. Alternatively, a compound of formula 8 can be prepared by a method analogous to that described in Scheme 6 below using a compound of formula 12 or 13 wherein R1 is in the formula 12戍13 (meaning that when R1 is H, formula 12 is paired P-toluenesulfonylmethyl isocyanide and formula 13 benzotriazol-1-ylmethyl isocyanide). For the synthesis of the compound of formula 8 using p-toluenesulfonyl radicals, see step b of Examples 1 and 3. In another method illustrated in Scheme 5, a compound of formula 2 can be prepared by reaction of an N-chloroamine of formula 9 with an enamine of formula 10. In this method, cyclization is carried out by cyclization of a 4-morpholinyl-4,5-dihydroimidazole which is generated in situ to form a morpholino group to form Compound of formula 2. The reaction is carried out in a solvent having a substrate such as pyridine, 4-(diamine)pyridine or a trialkylamine, such as: dioxane, dichlorodecane, tetra Gasification of carbon or toluene, the reaction temperature is between about 0 ° C and the reflux temperature of the solvent. For a representative reference, see Pocar et al., Tetrahedron Letters 1976, 21, 1839-1842. Those skilled in the art will recognize that the ring of formula 2 can also be prepared by other methods described in many chemical literature. For example, the general method described by Wiglenda et al., J0urnal 0f

Medicinal Chemistry 2007, 50(7)，1475-1484 可用於製備 式2化合物；該方法亦可輕易地修改以製備式2化合 物，其中各Q1及/或Q2係一視情況經取代之苄基團。Medicinal Chemistry 2007, 50(7), 1475-1484 can be used to prepare a compound of formula 2; the process can also be readily modified to produce a compound of formula 2 wherein each Q1 and/or Q2 is a optionally substituted benzyl group.

流程5Process 5

式9化合物可由脒及N-氣琥珀醯亞胺根據pocaret al.，Tetrahedron Letters 1976, 21，1839-1842 提供之步驟 輕易合成製得。式10之烯胺化物可由已知方法製備； 例如，參見 van der Gen et al.，Tetrahedron Letters 1979, 26, 2433-24。 15J284.doc ·72· 201117722 如淹海 _ 12之經取你所不，式4化合物可經由式11亞胺與式 并三唾苯4曱基異氰化物或式13之經取代苯 有適卷^甲基異氰化物間的反應而製得，該反應係於 碳酸鉀、第：τ_、订，其中_當基質係如· .β ' 虱氧化鈉、氫化鈉、三級丁胺或 ’ .一丫▲雙每[5.4.0]十一-7, (DBU)，該溶劑溶劑係 如·甲醇、—氧陸圜、四氫呋喃、二甲基乙醯胺、n，n_ 一曱基曱醯胺或1，2-二曱氧乙烷，反應溫度範圍在大約 0到150 C之間。反應條件請參見Almansa et al., Journal of Medicinal Chemistry 2003, 46(16), 3463-3475 andThe compound of formula 9 can be readily synthesized from hydrazine and N-gas amber quinone imide according to the procedure provided by pocaret al., Tetrahedron Letters 1976, 21, 1839-1842. The enamide of formula 10 can be prepared by known methods; for example, see van der Gen et al., Tetrahedron Letters 1979, 26, 2433-24. 15J284.doc ·72· 201117722 If you are immersed in the sea _ 12, the compound of formula 4 can be obtained by the imine of formula 11 and the substituted tris-phenylene isocyanide or the substituted benzene of formula 13 Prepared by a reaction between methyl isocyanide, the reaction is based on potassium carbonate, the first: τ_, order, wherein _ when the matrix is such as .β' sodium hydride, sodium hydride, tertiary butylamine or '. One 丫 ▲ every [5.4.0] eleven-7, (DBU), the solvent solvent is such as methanol, oxonium, tetrahydrofuran, dimethylacetamide, n, n- mercaptoamine Or 1,2-dimethoxyethane, the reaction temperature ranges from about 0 to 150 C. For reaction conditions, see Almansa et al., Journal of Medicinal Chemistry 2003, 46(16), 3463-3475 and

Katritzky et al.，Heterocycles 1997, 44, 67-70。同時，於 實例7、22及24之步驟B中說明流程6之方法。 151284.doc -73· 201117722 流程6Katritzky et al., Heterocycles 1997, 44, 67-70. At the same time, the method of Scheme 6 is illustrated in steps B of Examples 7, 22 and 24. 151284.doc -73· 201117722 Process 6

Q2 11 可藉由脫水條件下，式Q2NH2胺與式QtHO醛之 間的接觸製備式11亞胺，該脫水條件係如：利用 Dean-Stark裝置在甲苯或茬中加熱以除去反映中所形成 的水。在某些案例中，可在反應混合物中加入酸觸媒， 例如：對甲苯磺酸’以促進水的消除。代表性的步驟請 參見 Almansa et al.，Journal of Medicinal Chemistry 2003, 46(16)，3463-3475。同時，實例 1、3、7、22 及 24 的步 驟A說明式11化合物的製備。 式12化合物能在相轉移條件下利用化學文獻中報 導之方法由未經取代對曱苯磺曱基異氰化物製備得 到；例如參見 Leusen et al·，Tetrahedron Letters 1975, 40, 3487-3488 。 經取代式13苯并***-1-基甲基異氰化物能藉由基 質存在時，苯并***-1-基-曱基異氰化物與式r2X1化合 151284.doc • 74· 201117722 物（其中x1係鹵素）的接觸製備得到，該基質係如： 碳酸鉀、氫化鈉或第三丁醇鉀。典型的反應條件參見 Katritzky et al.，Heterocycles 1997, 44, 67-70。熟習該領 域之技藝人士將會認可用於製備式13化合物的其他方 法，例如：由 Katritzky et al.，Journal of the Chemical Society, Perkin Transactions 1, 1990, (7)，1847-1851 描述 的方法。 某些式4化合物，其中R1係鹵素，可如流程7所 示製備。在此方法中，根據Pawar et al·，Tetrahedron Letters 2006，47，5451-5453所教示的一般方法將式Η 氰胺和式15曱烷胺鑌鹽類混合以形成式4化合物。該 反應係在適當溶劑，例如：二氯甲烷或曱苯，中進行， 反應溫度範圍在大約0°C至該溶劑的回流溫度之間。實 例8及10的步驟B說明流程7之方法。 利用類似於先前流程2描述的方法’可在式4咪唑 環的2_位達成鹵化作用，以形成式2化合物，其中R1 係鹵素。實例8、1 〇及24的步驟C、實例18的步驟B 及實例22的步驟D說明此鹵化方法。 流程7'㊉二Q2 11 The imine of formula 11 can be prepared by contact between a compound of formula Q2NH2 and a QtHO aldehyde under dehydrating conditions, such as heating in toluene or hydrazine using a Dean-Stark apparatus to remove the formation of the reflection. water. In some cases, an acid catalyst, such as p-toluenesulfonic acid, may be added to the reaction mixture to promote the elimination of water. For a representative procedure, see Almansa et al., Journal of Medicinal Chemistry 2003, 46(16), 3463-3475. Meanwhile, the step A of Examples 1, 3, 7, 22 and 24 illustrates the preparation of the compound of the formula 11. The compound of formula 12 can be prepared from the unsubstituted p-phenylsulfonyl isocyanide under phase transfer conditions by methods described in the chemical literature; see, for example, Leusen et al., Tetrahedron Letters 1975, 40, 3487-3488. The substituted 13-benzotriazol-1-ylmethylisocyanide can be combined with the formula r2X1 by the presence of a matrix. 151284.doc • 74· 201117722 The contact of (wherein x1 is a halogen) is prepared, such as potassium carbonate, sodium hydride or potassium butoxide. Typical reaction conditions are described in Katritzky et al., Heterocycles 1997, 44, 67-70. Other methods for preparing compounds of Formula 13 will be recognized by those skilled in the art, for example, the method described by Katritzky et al., Journal of the Chemical Society, Perkin Transactions 1, 1990, (7), 1847-1851. Certain compounds of formula 4 wherein R1 is a halogen can be prepared as shown in Scheme 7. In this method, the guanidinium cyanamide and the decylamine hydrazine salt of the formula 15 are mixed according to the general method taught by Pawar et al., Tetrahedron Letters 2006, 47, 5451-5453 to form a compound of the formula 4. The reaction is carried out in a suitable solvent such as dichloromethane or toluene, and the reaction temperature ranges from about 0 ° C to the reflux temperature of the solvent. Step B of Examples 8 and 10 illustrates the method of Flow 7. Halogenation can be achieved at the 2-position of the imidazole ring of formula 4 using a method similar to that described in the previous Scheme 2 to form a compound of formula 2 wherein R1 is a halogen. Steps C of Examples 8, 1 and 24, Step B of Example 18, and Step D of Example 22 illustrate the halogenation process. Flow 7' XII

Λ 15Λ 15

Rl R1Rl R1

I Q2 4 其中R1是鹵素 其中R1及X1是鹵素 151284.doc -75- 201117722 可藉由斯特雷克氨基酸反應（Strecker reaction)方 法，從式Q2NH2胺、式（^CHO醛以及氰化物源得到式 14氰胺。多種溶劑及氰化物源可供使用。路易斯酸， 例如：氣化銦(III)的存在是有利的。典型的條件參見， 例如：Ranu et al.，Tetrahedron 2002, 58, 2529-2532。此 反應已是許多回顧文獻的討論主題。此反應的條件及其 變化，參見下列參考文獻與其中引用的參考文獻：D. Τ. Mowry，Chemical Reviews 1948, 42, 236, Η。Groeger， Chemical Reviews 2003, 103, 2795-2827，及 M. North in Comprehensive Organic Functional GroupI Q2 4 wherein R1 is halogen wherein R1 and X1 are halogen 151284.doc -75- 201117722 can be obtained from the formula Q2NH2 amine, formula (^CHO aldehyde and cyanide source) by the Strecker reaction method. Cyanamide of formula 14. A variety of solvents and cyanide sources are available. Lewis acids, such as the presence of indium(III) oxide, are advantageous. For typical conditions see, for example: Ranu et al., Tetrahedron 2002, 58, 2529 -2532. This reaction has been the subject of many review literature. The conditions of this reaction and its variations are described in the following references and references cited therein: D. ow. Mowry, Chemical Reviews 1948, 42, 236, Η. Groeger , Chemical Reviews 2003, 103, 2795-2827, and M. North in Comprehensive Organic Functional Group

Transformations, A. R. Katritsky，O. Meth-Cohn 及 C. W.Transformations, A. R. Katritsky, O. Meth-Cohn and C. W.

Rees Editors., Volume 3, 615-617; Pergamon, Oxford, 1995。同時，實例8及10的步驟a說明式14化合物之 製備。對於反應性較小的式q2NH2胺來說’例如：含有 鄰位拉電子基的芳基胺，三曱基矽氰與觸媒，例如：胍 鹽酸鹽’的結合使用是有利的。參考文獻請參見，例如： Heydari et al., Journal 〇f Molecular Catalysis A: Chemical 2007, 271(1-2)，142-144。 式15甲烷胺鏽鹽類可於市面上購得，例如：（氯亞 甲基)二甲基氯化銨（意即R1及X1係C1)可由商業來 源得到。可由化學文獻提供的方法合成式15化合物。 式la化合物（意即式1，其中R2係ch2〇H)可如 流程8所示製備。在此方法的第一步驟中，式4化合物 轉換為相對應的式16之2-咪唑曱醛衍生物。此反應牽 涉利用鋰基質，例如：二異丙胺鋰（LDA)，將咪唑環 151284.doc •76- 201117722 的2-位鋰化以得到一負離子，接著以Ν,Ν-二曱基曱醯 胺（DMF)處理該負離子以提供2-咪唑甲醛衍生物。實 例15的步驟Α說明此步驟。流程8之方法的下一個步 驟，該式16之2-咪唑曱醛以氫硼化鈉在曱醇中還原以 形成相對應的式la化合物。反應條件請參見Quan et al.， Journal of Medicinal Chemistry 2005, 48(6), 1729-1744。實例15的步驟B說明此步驟。 流程8Rees Editors., Volume 3, 615-617; Pergamon, Oxford, 1995. At the same time, step a of Examples 8 and 10 illustrates the preparation of the compound of formula 14. For the less reactive formula of the q2NH2 amine, for example, an arylamine having an ortho-electron group, a combination of a trimethylsulfonium cyanide and a catalyst such as hydrazine hydrochloride is advantageous. References can be found, for example: Heydari et al., Journal Mf Molecular Catalysis A: Chemical 2007, 271(1-2), 142-144. The methaneamine rust salts of the formula 15 are commercially available, for example, (chloromethylene)dimethylammonium chloride (i.e., R1 and X1 systems C1) are commercially available. The compound of formula 15 can be synthesized by the methods provided in the chemical literature. The compound of formula la (i.e., formula 1, wherein R2 is ch2〇H) can be prepared as shown in Scheme 8. In the first step of the process, the compound of formula 4 is converted to the corresponding 2-imidazolium aldehyde derivative of formula 16. This reaction involves the use of a lithium substrate, such as lithium diisopropylamide (LDA), to lithinate the 2-position of the imidazole ring 151284.doc •76-201117722 to give an anion followed by hydrazine, hydrazine-didecyl decylamine. The negative ion is treated (DMF) to provide a 2-imidazole formaldehyde derivative. The procedure of Example 15 illustrates this step. In the next step of the process of Scheme 8, the 2-imidazolium furfural of formula 16 is reduced with sodium borohydride in decyl alcohol to form the corresponding compound of formula la. For reaction conditions, see Quan et al., Journal of Medicinal Chemistry 2005, 48(6), 1729-1744. Step B of Example 15 illustrates this step. Process 8

流程9之方法，以三氟化二乙氨基硫（DAST)處 理式17之2-羥曱基化合物然後得到式11}之2_氟甲基衍 生物（意即式1其中R2係-CH2F)。反應條件請參見c.j. Wang, Organic Reactions 2005, Vol. 34 (Wiley, New York, 1951) Chapter 2, pp. 319-321。此步驟於實例 16 _ 說 明。其他式lb之2-鹵曱基類似物可利用該化學文獻中 描述的方法製得。例如：式lb之2-溴曱基類似物可利 用 Beukers et al.，Journal of Medicinal Chemistry 2004, 47(15)，3707-3709所描述的方法’在如冰醋酸之溶劑中 以氫溴酸處理式la之2-羥曱基化合物而製得。 151284.doc •77· 201117722 流程9Process 9 of treating a 2-hydroxyindenyl compound of formula 17 with diethylaminosulfur trifluoride (DAST) and then obtaining a 2-fluoromethyl derivative of formula 11} (i.e., formula 1 wherein R2 is -CH2F) . For reaction conditions, see c.j. Wang, Organic Reactions 2005, Vol. 34 (Wiley, New York, 1951) Chapter 2, pp. 319-321. This step is illustrated in Example 16_. Other 2-haloindolyl analogs of formula lb can be prepared by the methods described in the chemical literature. For example, a 2-bromoindolyl analog of formula lb can be treated with hydrobromic acid in a solvent such as glacial acetic acid using the method described by Beukers et al., Journal of Medicinal Chemistry 2004, 47(15), 3707-3709. It is prepared by the 2-hydroxyindenyl compound of the formula la. 151284.doc •77· 201117722 Process 9

la lb 流程5至7只是幾個本發明之咪唑環製備方法的代 表。熟習該領域之技藝人士將會認可式丨咪唑環可藉由 化學文獻中描述的其他數個方法製備。合成咪唑的主要 參考文獻請參見 Grimmett in Imidazole andLa lb Schemes 5 through 7 are just a few of the preparations of the imidazole rings of the present invention. Those skilled in the art will recognize that the imidazole ring can be prepared by several other methods described in the chemical literature. The main reference for the synthesis of imidazoles can be found in Grimmett in Imidazole and

Benzimidazole Synthesis，Academic Press, California;以 及 Grimmett，Science of Synthesis 2002, 12, 325-528。 上述之式1化合物及其中間物可接受不同親電 的、親核的、自由基、有機金屬、氧化以及還原反應以 增加或修飾取代基’以形成更進一步的式1化合物。 K1、R2、R3、R4、R5或R6為鹵素的化合物（較佳為溴 化物或磁化物），係特別有用的中間物，用於過渡金屬_ 催化交叉偶合反應以製備式1化合物。這些反應類型在 文獻中充分說明；請參見，例如：Tsuji in Transition Metal Reagents and Catalysts: Innovations in Organic Synthesis， John Wiley and Sons, Chichester, 2002 · Tsuji in Palladium in Organic Synthesis, Springer，2005 :以及 Miyaura and Buchwald in Cross-Coupling Reactions ： A Practical Guide，Springer, 2002 ;及其中引用的參考文 獻。 151284.doc •78- 201117722 為習該領域之技藝人士將會認可對於一些式1化 合物6而言，附著於環及Q1及Q2環系統的R3、R4、R5 及1 R取代基’形成中央咪唑環後也許更易於與該環或 Q及Q環系統合為一體。特定而言，當R3、r4、R5 或R6係函素或其他適當的脫離基，該脫離基可利用 多種該領域中已知的親電性、親核性及有機金屬反應取 代’以導入其他官能基，例如：R3、R4、R5及R6。實 例18說明式1化合物的製備，其中Ql苯環上的R3取 代基係氰基(-CN) ’該製備起始於一種化合物，其中Qi 笨環上的r3取代基係溴基。實例25說明式1化合物的 製備，其中Q2笨環上的R5係硫氰酸鹽(_SCN)，該製備 起始於相對應的式1化合物，其中Q2苯環上的R5取代 基係峨基。 作為形成中央咪唑環後官能基化Ql或Q2的進一步 實例，式1化合物，其中R3或R5取代基係經由一氧原 子（例如：視情況經取代的烷氧基）、硫原子（例如： 視情況經取代的烧硫基）或氮原子（例如：烧胺基及雙 烷胺基）連接，可藉由烷化相對應的化合物製備，其中 R3或R5取代基分別係〇H、SH或NH2。一般烧化方法 係熟知於有機化學合成領域中。本實例26說明式！化 合物的製備，其中R3係OCHfN，該製備起始於相對 應的式1化合物，其中R3係OH。式1化合物，其中 R或R取代基視情況以烧亞績酿基或續酸基取代，可 藉由利用該領域熟知之一般氧化方法氧化相對應的式i 化合物製備，其中R3或R5取代基視情況以烷硫基取代。 151284.doc •79· 201117722 此外’式1化合物，其中環或Q1或Q2環系統以 R3或R5取代基取代’其為_X_U_Z (如發明内容定義）， 可由相對應的式1化合物製備，其中R3或R5係鹵素或 其他適當脫離基，例如：藉由PCT專利公開wo 2007/149448中描述的一般方法（參見其中的流程15)。 此參考文獻同時描述其他形成R3或R5取代基作為 -X-U-Z的一般方法（參見其中的流程16_19)。本實例 20至21說明式1化合物的製備，其中R3係_χ_υ_ζ (意 即-CKCHANHCH3) ’該製備相對應的式i化合物，其 中R3係曱氧基。 應認可’上述用於製備式1化合物的一些試劑及反 應條件’可能無法與某些存在於中間物中的官能度相 容。在這些實例中’併入保護/去保護次序或官能基相 互轉換至該合成中，將有助於獲得所欲產物。該保護基 的使用及選擇對於熟習化學合成之人士將是顯而易見 的（可參見如 Greene，T. W.; Wuts, P. G. M. Protective Groups in Organic Synthesis, 2nd ed.; Wiley: New York, 1991)。熟習該領域之技藝人士將能認可，在一些情況 下’在採用如在任何個別流程中所敘述的特定試劑之 後’可能需要進行額外未詳細說明的常規合成步驟以完 成式1化合物的合成。熟習該領域之技藝人士將能認 可，可能需要將上述流程中繪示的步驟以一種不同於所 示特定次序所暗示的順序進行組合，以製備出式1化合 物。 即使沒有進一步的闡述，相信使用上述說明的熟習 該領域之技藝人士仍能夠最大程度地利用本發明。因 151284.doc *80. 201117722 此i以下實例僅為說明之用’而絕非用於限制本發明之 揭露内容。下列實例的步驟朗_整體合成轉變之 驟的-個製程，且用於每個步驟的起始騎可能不 需要藉由-特定製備路程來製備，該狀製備路程的势 程係在其他實例或步驟中有敘述者。τ面實例中，hplc 分析係以uv舰在—她ech Altima C18分析管柱上 得到。溶劑系統為溶劑A :含有0.05%三a乙酸的水( =百分濃度），及溶劑B:含有〇.〇5%三氟乙酸的乙猜(體 積百分濃度）（梯度起騎〇分料有慨溶劑A及 溶劑B並且在2G分鐘後將溶劑B提升至9G%，流° 百分率為按重量計，除了層析溶劑混合= ί =二除:非特別指出’則層析溶劑混合物係體 =及體積百分比。下面實例中所指的質譜⑽）值， 係最面同位«度母離子（Μ+1)的分子量（m/z)，兮 :離子係藉由增加矿（分子量為1)至具有最高同㈣ 豆度的分子而形成’藉由質譜儀利用電喷灑離子化 (ESI)或大氣壓力化學離化法（Αρα)觀察。分子離 η含—或多個較低豐度的高原子量同位素（例如： Cl、8IBr)的存在未經報導。士]^]^1]^光譜係以從四甲 基矽烷至低磁場ppm示之，並以甲基矽烷作為基準；％ 意為單峰，Singlet，「d」意為雙重峰，rt」意為三重峰；&quot; dd」思為雙組雙重峰，「m」意為多重峰，而「心$ 意為寬峰。 實例Benzimidazole Synthesis, Academic Press, California; and Grimmett, Science of Synthesis 2002, 12, 325-528. The above compounds of formula 1 and intermediates thereof can accept different electrophilic, nucleophilic, free radical, organometallic, oxidative, and reduction reactions to add or modify substituents' to form further compounds of formula 1. A compound (e.g., a bromide or a magnetide) wherein K1, R2, R3, R4, R5 or R6 is a halogen is a particularly useful intermediate for the transition metal-catalyzed cross-coupling reaction to prepare a compound of formula 1. These types of reactions are fully described in the literature; see, for example: Tsuji in Transition Metal Reagents and Catalysts: Innovations in Organic Synthesis, John Wiley and Sons, Chichester, 2002 · Tsuji in Palladium in Organic Synthesis, Springer, 2005: and Miyaura and Buchwald in Cross-Coupling Reactions: A Practical Guide, Springer, 2002; and references cited therein. 151284.doc •78- 201117722 It will be recognized by those skilled in the art that for some of the compounds of formula 1, the R3, R4, R5 and 1 R substituents attached to the ring and the Q1 and Q2 ring systems form a central imidazole. It may be easier to integrate with the ring or the Q and Q ring systems after the ring. In particular, when R3, r4, R5 or R6 auxin or other suitable cleavage group, the cleavage group can be replaced by a variety of electrophilic, nucleophilic and organometallic reactions known in the art to introduce other Functional groups, for example: R3, R4, R5 and R6. Example 18 illustrates the preparation of a compound of formula 1 wherein R3 on the Q1 phenyl ring is substituted with a cyano group (-CN). The preparation begins with a compound wherein the r3 substituent on the Qi ring is a bromo group. Example 25 illustrates the preparation of a compound of formula 1 wherein R5 is a thiocyanate (_SCN) on the Q2 ring, and the preparation begins with the corresponding compound of formula 1, wherein the R5 substituent on the Q2 phenyl ring is a fluorenyl group. Further examples of the functionalization of Q1 or Q2 after formation of a central imidazole ring, wherein the R3 or R5 substituent is via an oxygen atom (eg, an optionally substituted alkoxy group), a sulfur atom (eg: The substituted sulfur-substituted or nitrogen atom (for example, an amine group and a dialkylamine group) may be prepared by alkylating a corresponding compound, wherein the R3 or R5 substituents are respectively H, SH or NH2. . The general firing method is well known in the field of organic chemical synthesis. This example 26 illustrates the formula! The preparation of the compound wherein R3 is OCHfN, the preparation begins with the corresponding compound of formula 1, wherein R3 is OH. A compound of formula 1, wherein the R or R substituent is optionally substituted with a calcined or a reductive acid group, which can be prepared by oxidizing a corresponding compound of formula i using a general oxidation method well known in the art, wherein the R3 or R5 substituent Substituting an alkylthio group as appropriate. Further, a compound of formula 1 wherein a ring or a Q1 or Q2 ring system is substituted with a R3 or R5 substituent, which is _X_U_Z (as defined in the Summary of the Invention), may be prepared from a corresponding compound of formula 1, wherein R3 or R5 is a halogen or other suitable cleavage group, for example, the general method described in PCT Patent Publication No. 2007/149448 (see Scheme 15 therein). This reference also describes other general methods for forming R3 or R5 substituents as -X-U-Z (see Scheme 16_19 therein). The present Examples 20 to 21 illustrate the preparation of the compound of the formula 1, wherein R3 is _χ_υ_ζ (i.e., -CKCHANHCH3)'. The corresponding compound of the formula i is prepared, wherein R3 is a decyloxy group. It should be recognized that some of the reagents and reaction conditions described above for the preparation of the compound of Formula 1 may not be compatible with certain functionalities present in the intermediate. In these examples, incorporation of a protection/deprotection sequence or functional group interconversion into the synthesis will aid in obtaining the desired product. The use and selection of such protecting groups will be apparent to those skilled in the art of chemical synthesis (see, e.g., Greene, T. W.; Wuts, P. G. M. Protective Groups in Organic Synthesis, 2nd ed.; Wiley: New York, 1991). Those skilled in the art will recognize that, in some instances, after the use of specific reagents as described in any of the individual schemes, it may be desirable to carry out conventional synthetic procedures, which are not described in detail, to complete the synthesis of the compound of Formula 1. Those skilled in the art will recognize that the steps depicted in the above schemes may be combined in a sequence different from that indicated in the particular order shown to produce Formula 1 compounds. Even without further elaboration, it is believed that those skilled in the art using the above description will be able to make the most of the invention. 151284.doc *80. 201117722 The following examples are for illustrative purposes only and are not intended to limit the disclosure of the present invention. The steps of the following examples are a one-step process of the overall synthesis transformation, and the initial ride for each step may not need to be prepared by a specific preparation route, the potential of the preparation route is in other examples or There are narrators in the steps. In the τ-face example, the hplc analysis was obtained on a uv Altima C18 analytical column with a uv ship. The solvent system is solvent A: water containing 0.05% triacetic acid (=percent concentration), and solvent B: B guess containing 〇.〇5% trifluoroacetic acid (volume percent concentration) Solvent A and Solvent B are generous and raise solvent B to 9G% after 2G minutes, the percentage of flow is by weight, except for chromatographic solvent mixing = ί = divisible: not specifically indicated 'the chromatographic solvent mixture system = and volume percentage. The mass spectrum (10) value referred to in the following examples is the molecular weight (m/z) of the most in-situ «degree parent ion (Μ+1), 兮: ion is increased by mineral (molecular weight is 1) Formation to the molecule having the highest (four) degree of soybeans was observed by mass spectrometry using electrospray ionization (ESI) or atmospheric pressure chemical ionization (Αρα). The presence of molecules from η- or a number of lower-abundance, high-atom isotopes (eg, Cl, 8IBr) has not been reported.士]^]^1]^ spectroscopy is shown from tetramethyl decane to low magnetic field ppm, with methyl decane as the benchmark; % means single peak, Singlet, "d" means double peak, rt" It is a triplet; &quot; dd is a double-group double peak, "m" means a multiple peak, and "heart $ means a broad peak."

製備4_氣-1-(4_氯笨基)士(2,4,6_三氟苯基)1H -咪啥 151284.doc 201117722 步驟A :製備(E)-4-氣具【(2,4,6-三氟苯基)亞甲基】苯 於一種在甲苯（1 〇〇 mL )中的2,4,6-三氟苯甲醛（3.0 g，18.7 mmol)混合物中加入4-氣苯胺（2.39 g，18.7 mmol)。利用Dean-Stark分離器將該反應混合物在回流 溫度加熱，以共沸去除水。16小時後，將該反應混合 物冷卻至室溫，並在減壓下濃縮。將結果得到的殘餘物 藉由矽凝膠層析術純化，利用醋酸乙酯-己烷（1:9)作 為溶析液以得到呈淺黃色固體的標題化合物（4.20 g)。 NMR (CDC13) δ 8.55 (s，1H)，7.37-7.34 (in, 2H)， 7.17-7.13 (m，2Η)，6.83-6.77 (m, 2Η)。 ESIMSm/z 270 (M+l)。 步驟B: 製備1-(4-氣苯基)-5-(2,4,6-三氟苯基)-1Η- 於一種在曱醇及1，2-二曱氧乙烷（2:1，152 mL) 中的(E)-4-氯-N-[(2,4,6-三氟苯基)亞曱基]苯（意即步驟 A的產物）（4.20 g，15.6 mmol)混合物中加入對曱苯 磺甲基異氰酸酯（4.57 g，23.4 mmol)及碳酸鉀（4.30 g， 31.2 mmol)。在85°C加熱該反應混合物4小時、冷卻， 接著在減壓下濃縮。將結果得到的殘餘物以醋酸乙酯 (200 mL)稀釋、以水（75 mL)和飽和氯化納水溶液 (75 mL)洗滌、經由硫酸鈉乾燥、過濾以及在減壓下 濃縮。將結果得到的物質藉由矽凝膠層析術純化，利用 醋酸乙酯-己烷（1:4)作為溶析液以得到呈淺黃色固體、 151284.doc •82· 201117722 在170-1721溶化的標題化合物（1.30 g ’經HPLC分析 純度為98.9%)。 ]R NMR (DMSO-d6) δ 7.29 (s, 1H), 7.11-7.07 (m, 2H), 6.68-6.63 (m, 2H) 〇 MS m/z 309 (M+l)。 步驟C:製備4-氯-1-(4-氣苯基）_5_(2,4,6-三氟苯 基)-1H-咪唑 於一種在三氣曱烧（2 mL)中的1-(4-氣苯 基)-5-(2,4,6-三氟苯基)-1Η-咪唑（意即步驟B的產物） (0.100 g，0.32 mmol)混合物中加入N-氣號拍醯亞胺 (0.046 g，0.34 mmol)。將該反應混合物在回流溫度加 熱16小時，然後冷卻至室溫。將該反應混合物以三氣 曱院（100 mL )稀釋、以水（55 mL)和飽和氣化納水 溶液（55 mL)稀釋、經由硫酸鈉乾燥、過濾並在減壓 下濃縮。將結果得到的物質藉由矽凝膠層析術純化，利 用醋酸乙酯-己烧（1:4 )作為溶析液以得到呈黃白色固 體、在102-104°C時溶化的標題化合物（0.075 g，經HPLC 分析純度為98.9%)。 】H NMR (CDC13) δ 7.68s，1H)，7.37-7.33 (m，2H)， 7.11-7.07 (m，2H)，6.74-6.65 (m, 2H)。 ESI MS m/z 343 (M+l)。 實例2 製備2,4-二氯_1-(4-氯苯基)-5-(2,4,6-三氟苯基)_111-咪唑（化 15l284.doc •83- 201117722 合物4) 於一種在氯仿（10 mL)中的1-(4-氣苯基)-5-(2,4,6-三氟苯基)-1Η-咪唑（意即實例1之步驟B的產物） (0.280 g，0.90 mmol)混合物中加入N-氣琥珀醯亞胺 (0.420 g，3.14mmol)。將該反應混合物在回流溫度加 熱16小時’然後冷卻至室溫。將該反應混合物以三氣 甲烷（100 mL)稀釋、以水（55 mL)和飽和氣化鈉水 溶液（55 mL)稀釋、經由硫酸鈉乾燥、過濾並在減壓 下濃縮。將結果得到的物質藉由矽凝膠層析術純化，利 用醋酸乙酯-己烧（1:4 )作為溶析液以得到呈淺黃色固 體、在112-119°C時溶化的標題化合物（〇 23 g，經HpLC 分析純度為96.7%)。 JH NMR (CDC13) δ 7.40-7.35 (m&gt; 2H), 7.14-7.10 (m, 2H), 6.70-6.61 (m，2H)。 ESI MS m/z 377 (M+l)。 實例3 製備2,4-二氣-1-(4-氣苯基)-5-(2,6-二氟苯基)_ih-咪唑（化合 物2) 步驟A :製備(E)-4-氣·Ν-[(2,6-二氟苯基)亞甲基】苯 於一種在曱苯（100 mL)中的2,6-二氟苯甲醛（4.0 g，18.7 mmol)混合物中加入4-氣苯胺（3.60 g，28.0 mmol)。利用Dean-Stark分離器在回流溫度加熱該反應 混合物，以共沸去除水。16小時後，將該反應混合物 冷卻至室溫’並在減壓下濃縮。將結果得到的殘餘物藉 151284.doc • 84· 201117722 由矽凝膠層析術純化，利用醋酸乙酯-己烷（0.5:9.5)作 為溶析液以得到呈淺黃色固體的標題化合物（6.20 g)。 lU NMR (CDCI3) ： δ 8.64 (s, 1H), 7.44-7.33 (m, 3H), 7.19-7.14 (m，2H)，7.04-6.96 (m，2H)。 步驟B: 製備1-(4-氣苯基)-5-(2,6·二氟苯基)_1H-咪 嗤 於一種在曱醇及1,2-二曱氧乙烷（7:3，160 mL) 中的(E)_4-氣-N-[(2,6-二氟苯基)亞甲基]笨（意即步驟A 的產物）（4.0 g，16.0 mmol)混合物中加入對曱苯績曱 基異氰化物（4.67 g，24.0 mmol)以及碳酸鉀（4.65 g， 24.0mmol)。在85°C加熱該反應混合物4小時，然後冷 卻，然後在減壓下濃縮。將結果得到的殘餘物以醋酸乙 酯（200 mL)稀釋、以水（75 mL)和飽和氣化鈉水溶 液（75 mL)洗滌、經由硫酸鈉乾燥、過濾以及在減壓 下濃縮。將結果得到的物質藉由矽凝膠層析術純化，利 用醋酸乙酯-己烷（3:7)作為溶析液以得到呈淺黃色固 體、在170-172 C時溶化的標題化合物（丨4〇 g，經HpLC 分析純度為98.9%)。 !H NMR (CDCI3) δ 7.79d, J = 〇&gt;9 Hz? 7.34.7 29 (m, 4H)，7.12-7.08 (m，2H)，6.91-6.83 (m，2H)。 ESIMS m/z291 (M+l)。 步驟C:製備2,4_二氣-1-(4-氣苯基)-5-(2,6-二氟苯 基)-1Η-咪唑 151284.doc -85- 201117722 於一種在三氯曱烷（24 mL)中的1-(4-氯苯 基)-5-(2,6-二氟苯基)-1Η-咪唑（意即步驟B的產物） (0.60 g，2.1 mmol)混合物中加入N-氯破拍酿亞胺 (0.69 g，5.2 mmol) β將該反應混合物在回流溫度加熱 16小時，然後冷卻至室溫。將該反應混合物以三氯甲 烷（40 mL)稀釋、以水（30 mL)和飽和氣化鈉水溶 液（30 mL)稀釋、經由硫酸鈉乾燥、過濾並在減壓下 濃縮。將結果得到的物質藉由矽凝膠層析術純化，利用 醋酸乙酯-己烷（1:4)作為溶析液以得到呈黃白色固體、 在123-125 C時溶化的標題化合物（〇 5〇 g，經HPLC分 析純度為97.9%)。 77 ]H NMR (CDC13) δ 7.40-7.30 (m, 3H), 7.16-7.10 (m, 2H)5 6.90-6.84 (m，2H)。 ’ ’ ESI MS m/z 360 (M+l) 〇 實例4 製備4-氣-1-(4-氣苯基)-5-(2,6-二氟苯基)_2_甲基_1H•咪唑 (化合物1) 步驟A:製備H4-氣苯基)-5-(2,6-二氟苯基)_2_甲基 -1H-咪唑 攪拌的同時於一種在四氫呋喃（34mL)中的^(4— 氣苯基)-5-(2,6-二氟苯基)-ih-咪唑（意即實例3步 B^)(l,0g，3.44 入二異丙胺鐘溶液（1.0 V[於四氫呋喃中，2 60 mL, 5 1〇 mmol)。反應混合物在-50X：攪拌L5小時，然後加入碘 151284.doc -86- 201117722 甲烧（1.47 g，1〇 3 mm〇1)四氫呋喃（16紅）溶液。 將該反應混合物慢慢地回溫至室溫，攪拌4小時，然後 在減壓下濃縮。將結果得到的殘餘物以醋酸乙酯（5〇 扯）稀釋、以水（2〇mL)和飽和氣化鈉水溶液（20mL) 洗，、經由硫醆鈉乾燥、過濾以及在減壓下濃縮。將結 果得到的殘餘物藉由矽凝膠層析術純化，利用醋酸乙酯 -己烷（1:4)作為溶析液以得到呈淺黃色固體的標題化 合物（0.74 g)。 !H NMR (CDCI3) δ 7.35-7.30 (m, 2H), 7.24-7.17 (m, 1H), 7.14 (s, 1H), 7.12-7.06 (m, 2H), 6.85-6.78 (m, 2H), 2.33 (s，3H) 〇 ESI MS m/z 305 (M+l)。 步驟B :製備氣-l-(4-氣苯基)-5-(2,6-二氟苯基)-2-甲基-1H-咪唑 攪拌的同時於一種在三氣甲烷（22 mL)中的1-(4-氣苯基)-5-(2,6-二氟苯基)-2-曱基-1H-咪唾（意即步驟 A的產物）（0.740 g，2.40 mmol)混合物中加入N-氣琥 拍醯亞胺（0.34 g ’ 2.55 mmol)。將該反應混合物在回 流溫度加熱16小時，然後冷卻至室溫。將該反應混合 物以三氯曱烷（50 mL)稀釋、以水（30 mL)和飽和 氣化鈉水溶液（30 mL)洗滌、經由硫酸鈉乾燥、過濾 並在減壓下濃縮。將結果得到的物質藉由矽凝膠層析術 純化，利用醋酸乙酯-己烷（1:9)作為溶析液以得到呈 151284.doc -87. 201117722 黃白色固體、在143-145°C溶化的標題化合物（0.35 g， 經HPLC分析純度為98.0%)。 !H NMR (CDC13) δ 7.35-7.29 (m, 3H), 7.10-7.06 (m, 2H), 6.90-6.83 (m, 2H)，2.33 (s，3H)。 ESI MS m/z 339 (M+l)。 實例5 製備4-溴-1-(4-氣苯基)-5-(2,6-二氟苯基)-2曱基-1H-咪唑 (化合物509) 於一種在三氯曱烷（5 mL)中的1-(4-氣苯 基)-5-(2,6-二氟苯基)-2-甲基-1H-咪唑（藉由實例4步驟 A之方法製備）（0.300 g，0.97 mmol)溶液中加入N-漠號珀醯亞胺（0.211 g，1 · 18 mmol)。將該反應混合物 在回流溫度加熱16小時，然後冷卻至室溫。將該反應 混合物以三氯曱烧（20 mL )稀釋、以水（5 mL )和飽 和氯化納水溶液（5 mL )洗滌、經由硫酸納乾燥、過遽 並在減壓下濃縮。將結果得到的殘餘物藉由矽凝膠層析 術純化，利用醋酸乙酯·己烷作為溶析液以得到呈淺黃 色固體、在183-185°C溶化的標題化合物（269 mg)。 ]H NMR (CDCI3) δ 7.35-7.31 (m, 3H), 7.09-7.06 (d, J = 8.7 Hz，2H)，6.88-6.82 (t，J = 7.8 Hz, 2H)，2.31 (s, 3H)。 ESI MS m/z 383 (M+l)。 實例6 製備4-氣-1-(4-氣苯基)-5-(4-氟苯基)-2-甲基-1H-咪唑（化合 151284.doc • 88 - 201117722 物3) 步驟A: 製備1-(4-氣苯基)-2-曱基-1H-咪唑 於一種在N，N-二甲基甲酿胺（lOmL)中的1-氣-4-碘化苯（1.50 g，6.30 mmol)混合物中加入碳酸鉋（3 5〇 g’ 10.9 mmol)、二氣曱烧石頁酸亞銅（〇.1〇 g，〇.5〇 mmol)、 2-曱咪唑（0.46g，5.66mmol)及（1R，2R)-1,2-二氨基環 己烷（0.12 g，1.00 mmol)。將該反應混合物在12〇〇c加 熱16小時’然後冷卻至室溫。將該反應混合物以醋酸 乙酯（80mL)稀釋、以水（2 30mL)和飽和氣化鈉 水溶液（40 mL)洗滌，經由硫酸鈉乾燥、過濾並在減 壓下濃縮。將結果得到的殘餘物藉由矽凝膠層析術純 化，利用醋酸乙酯-己烷（0.5:9.5)作為溶析液以得到呈 褐色固體的標題化合物（〇.60g)。 NMR (CDC13): δ 7.48-7.44 (m，2H)，7.26-7.22 (m，2H)， 7.05 (d，J = 16.8 Hz，2H)，2.35 (s，3H)。 ESI MS m/z 193 (M+l)。 步驟B :製備l-(4_氣苯基)·5·(4·氟苯基)-2-甲基-1H- 於一種在N，N-二甲基曱醯胺（1〇 mL)中的卜(4-氯苯基)-2-甲基-1H-咪唑（意即步驟a之產物）（0.700 g ’ 0.520 mmol)混合物中加入1-氟_4_碘化苯（1.61 g， 7.30 mmol)、三(2-曱基苯基)膦（o.iio g，0.360 mmol)、 氟化铯（1.10 g，7.30 mmol)以及乙酸鈀(η) ( 0.041 g， 0.18 mmol)。將該反應混合物在氬之下攪拌、在回流溫 151284.doc -89 - 201117722 度加熱16小時，然後冷卻至言、w 題化合物（0.20g，經 醋酸乙醋（40 mL)稀釋、以二。將該反應混合物以 納水溶液（20 mL)洗條，經由2〇 mL)和飽和氣化 減壓下濃縮。將結果得ίι丨的鈉乾燥、過濾、並在 化，利用曱醇-二氣曱燒（1.9)、补错由石夕凝膠層析術純 白色固體、在m-mt：溶化2為溶析_得到呈黃 HPLC分析純度為95.3%)。 ^ ]H NMR (CDC13) δ 7.42-7.39 rm .tTX 7.05-6.99 (m，2H)，6.95-6.87 (m 7.11_7·06 (m，3H)’ ESI MS m/z287 (M+l) 〇 ，^ 2-3l (s, 3 H) ° 步驟C : 製備4-氣贫 -1H-咪唑 氟苯基)-2-甲基 其=4一種甲燒（2.5址）中的H4-氯苯 = =340 = 16丨日^ 將錢應混合物在回流溫度加熱 16小時，然後冷卻至室溫1該反應混合物以三氯甲 烧2〇mL)稀釋、以水（1〇mL)和飽和氣化納水溶 液10 mL)稀釋、經由硫酸納乾燥、過遽並在減壓下 濃縮。將結果得_殘餘物知頻縣析術純化，利 用醋I乙Sa。-己垸（1:4)作為溶析液以得到呈黃色固體、 在124 126C洛化的標題化合物（〇 〇65 g，經^pLc分 析純度為95.2%)。 151284.doc •90- 201117722 iH NMR (CDC13) δ 7.40-7.36 (m，2H)，7.14-7.07 (m，2H)， 7.06-7.03 (m，2H)，6.99-6.92 (m, 2H)，2.29 (s，3H)。 ESI MS m/z 322 (M+l) 〇 實例7 製備2-氣-5-(2,6-二氟-4-甲氧苯基)_1(3,5二甲氧苯基)4甲 基-1H-咪唑（化合物473) 步驟A:製備心[(2,6-二氟·4·甲氧苯基)亞甲基】_3,5_ 二甲氧苯胺 -種在甲笨（4〇mL)中的 3,5_dimethoxybenzamine (2.00 g，13.1 mmol)及 2,6·二氟_4_曱氧苯曱（2 3〇 g， 13.1 mmol)混合物，將其用心以触分離器在回流 溫度隔夜加熱以共沸除去水。將該反應混合物冷卻至— 溫並在減壓下濃縮以形成呈固體狀之標題化合物（切至 g)。 ’ 屯 NMR (CDCW δ 8.56 (s，1H)，6 53 (m，2H)，6 3H)，3.85(s，3H)，3.81 (S，6H)。 步驟B ··製備5-(2,6-二氣_4甲氧苯基)小(3,5_ 苯基)·4·甲基咪唑 -種在四氫咬喃（20 mL)中的N_[(2,6_二氣 氧苯基)亞甲基]-3,5-二甲氧基苯胺（意即步驟a之產 (1.80 g，6.0 mmol)、1-[⑴異氰基乙基)石黃醯基]_4甲基 苯（1.90 g，9.0 mmol)及第三丁醇鉀的混合物，將$ 在回流溫度隔夜加熱。將該反應混合物冷卻然後在 151284.doc •91 · 201117722 下濃縮。將結果得到的物質藉由矽凝膠上的中壓液相層 析純化（溶析液為己烷中的醋酸乙酯，其梯度為〇到 100%)以形成呈固體狀的標題化合物（0.20 g)。 ]H NMR (CDC13) δ 7.73 (s, 1Η), 6.45 (m, 2H), 6.38 (s, 1H), 6.27 (s, 2H), 3.78 (s, 3H), 3.70 (m, 6H), 2.18 (s, 3H。 步驟C: 製備2-氣-5-(2,6-二氟-4-甲氧苯基)-l_(3,5- 二曱氧苯基)-4-甲基-1H-咪唑 於一種在四氫呋喃（5 mL)中的5-(2,6-二氟-4-曱 氧苯基)-1-(3,5-二曱氧苯基)-4-曱基-1H-咪唑（意即步驟 B 之產物）（0.280 g，0.78 mmol)及六氯乙烧（l.l〇g， 4.7 mmol)的混合物中，在-78°C下加入二異丙胺鋰（1.0 Μ於四氫σ夫σ南中，0.390 mL，0.78 mmol)。1小時後， 在該反應混合物中加入更多的二異丙胺經（1.0 IV[於四 氫咬°南中，0.150 mL，0.30 mmol)，再持續擾拌1小時， 然後再加入更多的二異丙胺鋰（1.0 Μ於四氫呋喃中， 0.150 mL ’ 0.30 mmol)至該反應混合物中。將該反應 混合物緩緩地降至室溫，攪拌2.5小時，然後在減壓下 濃縮。將結果得到的物質藉由矽凝膠上的中壓液相層析 純化（溶析液為己烷申的醋酸乙酯，其梯度為〇到1 〇 〇 〇/0 ) 以形成呈固體狀的標題化合物（0.011 g)。 ln NMR (CDCI3) δ 6.42 (m, 3Η), 6.31 (m, 2H), 3.77 (s, 3H)，3.72 (s，6H), 2.13 (s, 3H)。 151284.doc -92· 201117722 實例8 製備2-溴-4-氣-5-(2,6-二氟-4_甲氧苯基)小Ο氟苯基)_1仏咪 唑（化合物170) 步驟A :製備2,6-α-[(3·氟苯基)胺)]_4·甲氧苯乙腈 一種在四氫呋喃（40 mL·)中的3-氟苯胺（1J5 g， 10.4 mmol )、2,6-二氟-4-甲氧苯甲醛（2.00 g，η.6 mmol)、氰化鉀（2.70 g ,41.6 mmol)及氯化銦（2.30g ’ 10.4 mmol)混合物於室溫隔夜攪拌。以水（大約100 mL) 稀釋該反應混合物並用醋酸乙酯萃取。在減壓下濃縮合 併之醋酸乙酯萃取物以提供呈油狀的標題混合物，該混 合物直接用於進行步驟B。 步驟B:製備4-氣-5-(2,6-二氟-4-甲氧苯基)-1-(3-氟 苯基)-1Η-味唾 於一種在二氯曱烷（2〇mL·)中的2,6-α-[(3-氟苯基) 胺基)]-4-曱氧苯乙腈（意即步驟Α之產物）（1〇 4mm〇l) 混合物中加入N-(氯亞甲基)_N_二甲基氣化胺（丨6〇 g， 飽和碳酸鈉水溶液騎。該水雜混合物以二氣甲燒萃 取。經由硫_乾燥合併之有機層、輯並在減壓下濃 果得到的物f藉由销膠上的中液相層析純 化（, &gt;谷析液為己烧中的酷酸乙醋，其梯度為0到i 0 0 %) 12.5 mmol)。6亥反應混合物加熱至回流3小時然後以Preparation of 4-gas-1-(4-chlorophenyl)s(2,4,6-trifluorophenyl)1H-imida 151284.doc 201117722 Step A: Preparation of (E)-4-airware [(2 ,4,6-trifluorophenyl)methylene]benzene was added to a mixture of 2,4,6-trifluorobenzaldehyde (3.0 g, 18.7 mmol) in toluene (1 mL). Aniline (2.39 g, 18.7 mmol). The reaction mixture was heated at reflux temperature using a Dean-Stark separator to azeotropically remove water. After 16 hours, the reaction mixture was cooled to room temperature and concentrated under reduced pressure. The residue was purified by EtOAc EtOAc (EtOAc) NMR (CDC13) δ 8.55 (s, 1H), 7.37-7.34 (in, 2H), 7.17-7.13 (m, 2 Η), 6.83-6.77 (m, 2 Η). ESIMSm/z 270 (M+l). Step B: Preparation of 1-(4-phenylphenyl)-5-(2,4,6-trifluorophenyl)-1Η- in a sterol and 1,2-dimethoxyethane (2:1) (E)-4-Chloro-N-[(2,4,6-trifluorophenyl)indenyl]benzene (meaning the product of Step A) (4.20 g, 15.6 mmol) in 152 mL) P-Toluenesulfonylmethyl isocyanate (4.57 g, 23.4 mmol) and potassium carbonate (4.30 g, 31.2 mmol) were added. The reaction mixture was heated at 85 ° C for 4 hours, cooled, and then concentrated under reduced pressure. The resulting residue was diluted with EtOAc (EtOAc)EtOAc. The obtained material was purified by hydrazine gel chromatography using ethyl acetate-hexane (1:4) as a solvent to give a pale-yellow solid, 151284.doc •82·201117722 dissolved at 170-1721. The title compound (1.30 g ', 98.9% purity by HPLC). ] R NMR (DMSO-d6) δ 7.29 (s, 1H), 7.11-7.07 (m, 2H), 6.68-6.63 (m, 2H) 〇 MS m/z 309 (M+l). Step C: Preparation of 4-chloro-1-(4-phenylphenyl)-5-(2,4,6-trifluorophenyl)-1H-imidazole in 1-(3-mL) 4-gas phenyl)-5-(2,4,6-trifluorophenyl)-1 fluorene-imidazole (meaning the product of step B) (0.100 g, 0.32 mmol) was added to the mixture by adding N-gas. Amine (0.046 g, 0.34 mmol). The reaction mixture was heated at reflux for 16 hours and then cooled to room temperature. The reaction mixture was diluted with EtOAc (EtOAc) (EtOAc)EtOAc. The obtained material was purified by hydrazine gel chromatography using ethyl acetate-hexane (1:4) as the eluent to give the title compound as a yellow-white solid, which was dissolved at 102-104 ° C ( 0.075 g, purity by HPLC analysis of 98.9%). H NMR (CDC13) δ 7.68s, 1H), 7.37-7.33 (m, 2H), 7.11-7.07 (m, 2H), 6.74-6.65 (m, 2H). ESI MS m/z 343 (M+l). Example 2 Preparation of 2,4-dichloro-1 -(4-chlorophenyl)-5-(2,4,6-trifluorophenyl)-111-imidazole (15l284.doc •83-201117722 Compound 4) In a chloroform (10 mL) of 1-(4-phenylphenyl)-5-(2,4,6-trifluorophenyl)-1 oxime-imidazole (meaning the product of Step B of Example 1) N-gas amber imine (0.420 g, 3.14 mmol) was added to the mixture at 0.280 g, 0.90 mmol. The reaction mixture was heated at reflux temperature for 16 hours' then cooled to room temperature. The reaction mixture was diluted with EtOAc (EtOAc) (EtOAc)EtOAc. The obtained material was purified by hydrazine gel chromatography using ethyl acetate-hexane (1:4) as a solvent to give the title compound as a pale yellow solid which melted at 112-119 °C ( 〇23 g, purity by HpLC analysis was 96.7%). JH NMR (CDC13) δ 7.40-7.35 (m&gt; 2H), 7.14-7.10 (m, 2H), 6.70-6.61 (m, 2H). ESI MS m/z 377 (M+l). Example 3 Preparation of 2,4-diqi-1-(4-phenylphenyl)-5-(2,6-difluorophenyl)_ih-imidazole (Compound 2) Step A: Preparation of (E)-4-Gas Ν-[(2,6-Difluorophenyl)methylene]benzene was added to a mixture of 2,6-difluorobenzaldehyde (4.0 g, 18.7 mmol) in toluene (100 mL) Gas aniline (3.60 g, 28.0 mmol). The reaction mixture was heated at reflux temperature using a Dean-Stark separator to azeotropically remove water. After 16 hours, the reaction mixture was cooled to rt and concentrated under reduced pressure. The resulting residue was purified by EtOAc EtOAc EtOAc EtOAc (EtOAc) g). lU NMR (CDCI3): δ 8.64 (s, 1H), 7.44-7.33 (m, 3H), 7.19-7.14 (m, 2H), 7.04-6.96 (m, 2H). Step B: Preparation of 1-(4-phenylphenyl)-5-(2,6.difluorophenyl)_1H-imiline in a sterol and 1,2-dimethoxyethane (7:3, (E)_4-Ga-N-[(2,6-difluorophenyl)methylene] stupid (meaning the product of Step A) (4.0 g, 16.0 mmol) in a mixture of 160 mL) Benzoyl isocyanide (4.67 g, 24.0 mmol) and potassium carbonate (4.65 g, 24.0 mmol). The reaction mixture was heated at 85 ° C for 4 hours, then cooled and then concentrated under reduced pressure. The resulting residue was diluted with EtOAc (EtOAc)EtOAc. The obtained material was purified by hydrazine gel chromatography using ethyl acetate-hexane (3:7) as a solvent to give the title compound as a pale yellow solid, which melted at 170-172 C. 4〇g, the purity was 98.9% by HpLC analysis. !H NMR (CDCI3) δ 7.79d, J = 〇&gt;9 Hz? 7.34.7 29 (m, 4H), 7.12-7.08 (m, 2H), 6.91-6.83 (m, 2H). ESIMS m/z 291 (M+l). Step C: Preparation of 2,4-di-2-(4-phenylphenyl)-5-(2,6-difluorophenyl)-1 oxime-imidazole 151284.doc -85-201117722 in a trichlorin 1-(4-Chlorophenyl)-5-(2,6-difluorophenyl)-1Η-imidazole (meaning the product of Step B) (0.60 g, 2.1 mmol) in a mixture of hexanes (24 mL) N-Chlorobromide (0.69 g, 5.2 mmol) was added. The reaction mixture was heated at reflux for 16 h then cooled to rt. The reaction mixture was diluted with methylene chloride (40 mL), EtOAc (EtOAc) The obtained material was purified by hydrazine gel chromatography using ethyl acetate-hexane (1:4) as a solvent to give the title compound as a yellow-white solid, which melted at 123-125 C. 5 〇 g, purity by HPLC analysis of 97.9%). 77 ]H NMR (CDC13) δ 7.40-7.30 (m, 3H), 7.16-7.10 (m, 2H)5 6.90-6.84 (m, 2H). ' ' ESI MS m/z 360 (M+l) 〇 Example 4 Preparation of 4-gas-1-(4-phenylphenyl)-5-(2,6-difluorophenyl)_2-methyl_1H• Imidazole (Compound 1) Step A: Preparation of H4-Voxyphenyl)-5-(2,6-difluorophenyl)_2-methyl-1H-imidazole while stirring in a tetrahydrofuran (34 mL) 4-Hydroxyphenyl)-5-(2,6-difluorophenyl)-ih-imidazole (meaning Example 3 Step B^) (1,0 g, 3.44 into diisopropylamine clock solution (1.0 V [in tetrahydrofuran Medium, 2 60 mL, 5 1 〇mmol). The reaction mixture was at -50X: stirring for 5 hours, then adding iodine 151284.doc -86- 201117722 A-burn (1.47 g, 1〇3 mm〇1) tetrahydrofuran (16 red) The reaction mixture was slowly warmed to room temperature, stirred for 4 hours, then concentrated under reduced pressure. The obtained residue was diluted with ethyl acetate (5 EtOAc) and water (2 〇mL) It was washed with a saturated aqueous solution of sodium sulphate (20 mL), dried over EtOAc EtOAc (EtOAc) The title compound (0.74 g) was obtained as a pale yellow solid. !H NMR (CDCI3) δ 7.35-7.30 (m, 2H), 7.24-7.17 (m, 1H), 7.14 (s, 1H), 7.12-7.06 (m, 2H), 6.85-6.78 (m, 2H), 2.33 (s,3H) 〇ESI MS m/z 305 (M+l). Step B: Preparation of gas-l-(4-phenylphenyl)-5-(2,6-difluorophenyl)-2- Methyl-1H-imidazole was stirred while 1-(4-phenylphenyl)-5-(2,6-difluorophenyl)-2-mercapto-1H in tri-methane (22 mL) - N-salt (meaning the product of Step A) (0.740 g, 2.40 mmol) was added N-sodium succinimide (0.34 g '2.55 mmol). The reaction mixture was heated at reflux for 16 h then cooled The reaction mixture was diluted with EtOAc (EtOAc) (EtOAc)EtOAc. The obtained material was purified by hydrazine gel chromatography using ethyl acetate-hexane (1:9) as a solvent to afford 151284.doc -87. 201117722 yellow white solid at 143-145 The title compound was dissolved in C (0.35 g, purity 98.0% by HPLC). !H NMR (CDC13) δ 7.35-7.29 (m, 3H), 7.10-7.06 (m, 2H), 6.90-6.83 (m, 2H), 2.33 (s, 3H). ESI MS m/z 339 (M+l). Example 5 Preparation of 4-bromo-1-(4-phenylphenyl)-5-(2,6-difluorophenyl)-2-indenyl-1H-imidazole (Compound 509) in a trichloromethane (5 1-(4-Phenylphenyl)-5-(2,6-difluorophenyl)-2-methyl-1H-imidazole (prepared by the method of Example 4, Step A) (0.300 g, N-indicarbamide (0.211 g, 1 · 18 mmol) was added to the solution at 0.97 mmol). The reaction mixture was heated at reflux temperature for 16 hours and then cooled to room temperature. The reaction mixture was diluted with trichloromethane (20 mL), washed with water (5 mL) and sat. NaHCI (5 mL), dried over sodium sulfate, dried and evaporated. The residue obtained was purified by EtOAc EtOAc (EtOAc) elute ]H NMR (CDCI3) δ 7.35-7.31 (m, 3H), 7.09-7.06 (d, J = 8.7 Hz, 2H), 6.88-6.82 (t, J = 7.8 Hz, 2H), 2.31 (s, 3H) . ESI MS m/z 383 (M+l). Example 6 Preparation of 4-gas-1-(4-phenylphenyl)-5-(4-fluorophenyl)-2-methyl-1H-imidazole (Compound 151284.doc • 88 - 201117722) 3 Step A: Preparation of 1-(4-phenylphenyl)-2-mercapto-1H-imidazole in 1-N-4-phenyliodonated benzene (1.50 g, in N,N-dimethylacetamide (10 mL) 6.30 mmol) was added with carbonic acid planing (3 5 〇g' 10.9 mmol), bismuth sulphate (〇.1〇g, 〇.5〇mmol), 2-imidazole (0.46g, 5.66). Methyl) and (1R, 2R)-1,2-diaminocyclohexane (0.12 g, 1.00 mmol). The reaction mixture was heated at 12 ° C for 16 hours' and then cooled to room temperature. The reaction mixture was diluted with EtOAc (EtOAc) (EtOAc)EtOAc. The residue obtained was purified by EtOAc EtOAc (EtOAc:EtOAc) NMR (CDC13): δ 7.48-7.44 (m, 2H), 7.26-7.22 (m, 2H), 7.05 (d, J = 16.8 Hz, 2H), 2.35 (s, 3H). ESI MS m/z 193 (M+l). Step B: Preparation of 1-(4-hydroxyphenyl)·5·(4·fluorophenyl)-2-methyl-1H- in one of N,N-dimethyldecylamine (1 mL) Add 1-fluoro-4-isopropenylbenzene (1.61 g, 7.30) to a mixture of (4-chlorophenyl)-2-methyl-1H-imidazole (that is, the product of step a) (0.700 g '0.520 mmol). Methyl), tris(2-mercaptophenyl)phosphine (o.iio g, 0.360 mmol), cesium fluoride (1.10 g, 7.30 mmol) and palladium acetate (η) (0.041 g, 0.18 mmol). The reaction mixture was stirred under argon and heated at reflux temperature 151284.doc -89 - 201117722 for 16 hours, then cooled to the title compound (0.20 g, diluted with ethyl acetate (40 mL). The reaction mixture was washed with aq. EtOAc (20 mL) and evaporated. The sodium which is the result of ίι丨 is dried, filtered, and neutralized, using decyl alcohol-two gas smoldering (1.9), calibrating by pure daylight gel chromatography, and melting in m-mt: melting 2 Analysis _ obtained yellow HPLC analysis purity of 95.3%). ^ ]H NMR (CDC13) δ 7.42-7.39 rm .tTX 7.05-6.99 (m,2H), 6.95-6.87 (m 7.11_7·06 (m,3H)' ESI MS m/z287 (M+l) 〇, ^ 2-3l (s, 3 H) ° Step C: Preparation of 4-gas lean-1H-imidazolium fluorophenyl)-2-methyl which = 4 H4-chlorobenzene in a methylaceous (2.5 site) == 340 = 16 丨 ^ The mixture of the money should be heated at reflux temperature for 16 hours, then cooled to room temperature 1 The reaction mixture was diluted with 2 〇 mL of trichloromethane, water (1 〇 mL) and saturated aqueous solution of sodium 10 mL) was diluted, dried over sodium sulfate, dried and concentrated under reduced pressure. The result was obtained by _ residue known as the frequency analysis, using vinegar I B. - hexane (1:4) as a solvent to give the title compound (yield: 65 g, purity: 95.2%). 151284.doc •90- 201117722 iH NMR (CDC13) δ 7.40-7.36 (m,2H), 7.14-7.07 (m,2H), 7.06-7.03 (m,2H),6.99-6.92 (m, 2H), 2.29 (s, 3H). ESI MS m/z 322 (M+l) 〇 Example 7 Preparation of 2- gas-5-(2,6-difluoro-4-methoxyphenyl)-1(3,5-dimethoxyphenyl)4 methyl -1H-imidazole (Compound 473) Step A: Preparation of heart [(2,6-difluoro.4.methoxyphenyl)methylene]_3,5-dimethoxyaniline-species in a stupid (4〇mL) a mixture of 3,5_dimethoxybenzamine (2.00 g, 13.1 mmol) and 2,6·difluoro_4_deoxybenzoquinone (23 g, 13.1 mmol), which was carefully heated overnight at reflux temperature with a contact separator Azeotropic removal of water. The reaction mixture was cooled to EtOAc (EtOAc m.)屯 NMR (CDCW δ 8.56 (s, 1H), 6 53 (m, 2H), 6 3H), 3.85 (s, 3H), 3.81 (S, 6H). Step B · Preparation of 5-(2,6-dioxa-4-methoxyphenyl) small (3,5-phenyl)·4·methylimidazole-N-[in tetrahydrocyanate (20 mL) (2,6-dioxyphenyl)methylene]-3,5-dimethoxyaniline (meaning production of step a (1.80 g, 6.0 mmol), 1-[(1)isocyanoethyl) A mixture of diabase, _4 methylbenzene (1.90 g, 9.0 mmol) and potassium butoxide, was heated at reflux temperature overnight. The reaction mixture was cooled and concentrated under 151284.doc •91 · 201117722. The obtained material was purified by medium pressure liquid chromatography on a hydrazine gel (the lysate was ethyl acetate in hexane to a gradient of 100%) to give the title compound as a solid (0.20) g). ]H NMR (CDC13) δ 7.73 (s, 1Η), 6.45 (m, 2H), 6.38 (s, 1H), 6.27 (s, 2H), 3.78 (s, 3H), 3.70 (m, 6H), 2.18 (s, 3H. Step C: Preparation of 2-ox-5-(2,6-difluoro-4-methoxyphenyl)-l-(3,5-dioxaphenyl)-4-methyl-1H -Imidazole in a 5-(2,6-difluoro-4-indolylphenyl)-1-(3,5-dioxaoxyphenyl)-4-mercapto-1H in tetrahydrofuran (5 mL) - a mixture of imidazole (meaning the product of Step B) (0.280 g, 0.78 mmol) and hexachloroethane (ll 〇g, 4.7 mmol), at a temperature of -78 ° C, lithium diisopropylamine (1.0 Μ in IV) Hydrogen sigma sigma, 0.390 mL, 0.78 mmol). After 1 hour, more diisopropylamine was added to the reaction mixture (1.0 IV [in tetrahydrohexane, 0.150 mL, 0.30 mmol). Stirring was continued for an additional hour, then more lithium diisopropylamide (1.0 Torr in tetrahydrofuran, 0.150 mL '0.30 mmol) was added to the reaction mixture. The reaction mixture was slowly cooled to room temperature and stirred. After a few hours, it was concentrated under reduced pressure. The obtained material was purified by medium-pressure liquid chromatography on a hydrazine gel. The gradient is 〇 to 1 〇〇〇/0) to give the title compound (0.011 g) as a solid. ln NMR (CDCI3) δ 6.42 (m, 3 Η), 6.31 (m, 2H), 3.77 (s, 3H ), 3.72 (s, 6H), 2.13 (s, 3H). 151284.doc -92· 201117722 Example 8 Preparation of 2-bromo-4-gas-5-(2,6-difluoro-4-methoxyphenyl) ) hydrazine fluorophenyl) 1 hydrazine imidazole (compound 170) Step A: Preparation of 2,6-α-[(3.fluorophenyl)amine)]_4·methoxybenzoacetonitrile in tetrahydrofuran (40 mL·) 3-fluoroaniline (1J5 g, 10.4 mmol), 2,6-difluoro-4-methoxybenzaldehyde (2.00 g, η.6 mmol), potassium cyanide (2.70 g, 41.6 mmol) and indium chloride (2.30 g ' 10.4 mmol) The mixture was stirred at room temperature overnight. The reaction mixture was diluted with water (ca. 100 mL) and extracted with ethyl acetate. The combined ethyl acetate extracts were concentrated under reduced pressure to give the title mixture as an oil. Step B: Preparation of 4-gas-5-(2,6-difluoro-4-methoxyphenyl)-1-(3-fluorophenyl)-1 oxime-flavored in a dichloromethane (2〇 2,6-α-[(3-fluorophenyl)amino)]-4-oxo-oxyphenylacetonitrile (meaning the product of the step )) in mL·) (1〇4mm〇l) (Chloromethylidene)_N_dimethylamined amine (丨6〇g, saturated sodium carbonate solution ride. The mixed mixture is extracted with two gas. The organic layer is combined by sulfur-drying, and the mixture is reduced. The substance f obtained by pressing the concentrated fruit is purified by medium-liquid chromatography on the pin rubber (, &gt; the trough is a sulphuric acid in hexane, the gradient is 0 to i 0 0 %) 12.5 mmol) . 6 hai reaction mixture was heated to reflux for 3 hours and then

2H),6.41 (d, 2H),3.77 (s, 3H) 〇 (m, 1H), 6.96 (m, 151284.doc -93. 201117722 步驟C :製備2-漠-4-氯-5_(2,6_二範_4_甲氧笨 基)-1-(3_氟苯基)-1Η-味唾 一種在N，N-二曱基曱醯胺（15mL)中經攪拌之 4-氯-5-(2,6-二氟-4-曱氧苯基)-1-(3·氟笨基)_iH-咪唾（音 即步驟B之產物）（LOO g，3.0 _〇1)及N-漠玻^ 亞胺（0.641 g’ 3.6 mmol)混合物在咐加熱25天。 以飽和碳酸鈉水溶液稀釋該反應混合物，並以二氯甲燒 萃取稀釋所得之水溶液混合物。經由硫酸鎂乾燥合併2 有機層、韻、並在減壓下濃縮。將結果得到的物質藉由 石夕凝膠上的中壓液相層析純化（溶析液為己烧中的醋酸 W旨’其梯度為0到以形成呈固體狀的標題化 合物（0.67 g)。 H NMR (CDC13) δ 7.37 (m，1H)，7.13 (m，iH)，7.13 (m， 1H)，6.96 (m，2H)，6.41 (d，2H)，3.77 (s，3H)。 實例9 製備4-氣-5-(2,6-二氟-4-甲氧苯基)_1_(3_氟苯基)2_甲基_111_ 咪唑（化合物181) 一種在二氧陸圜（5 mL)及水（2滴）中的2-溴基 -4-氯-5-(2,6-二氟-4-曱氧苯基)·ι_(3·氟苯基)_ih-咪唑 (思即貫例8步驟C之產物）（0.200 g，0.490 mmol)、 三甲基環氧硼烷（0.062 g，0.490 mmol)、碳酸鉋（0.479 g，1.47 mmol)、二氣雙(三苯膦)鈀（0.035 g，0.05 mmol) 混合物在回流溫度隔夜加熱。在該反應混合物中加入更 151284.doc -94· 201117722 多三甲基環氧硼烷（0.062 g，0.490 mmol)及二氣雙（三 苯膦）鈀（ 0.035 g，0.05 mmol)，並將該混合物再次於 混流溫度隔夜加熱。在減壓下濃縮該反應混合物，並以 矽凝膠上的中壓液相層析純化結果所得之物質（溶析液 為己烷中的醋酸乙酯，其梯度為0到100%)以形成呈 固體狀之標題化合物（0.090 g)。 lH NMR (CDC13) δ 7.35 (m, 1Η), 7.09 (m, 1H), 6.94 (d, 1H), 6.89 (m, 1H), 6.39 (m, 2H), 3.76 (s, 3H), 2.31 (s, 3H)。 實例10 製備2,4-二溴-5-(2,6-二氟-3-甲氧苯基)-1-(4-氟苯基)-1Η-咪 唑（化合物350) 步驟A : 製備2,6-α-[(4-氟苯基)胺基]-3-甲氧苯乙腈 一種在四氫呋喃（50mL)中的4-氟苯胺（1.17g， 10.6 mmol)、2,6·二氟-3-曱氧苯曱醛（2.00 g，11·6 mmol)、I化鉀（2.80 g，42.4 mmol)及氯化銦（2.30 g， 10.4 mmol)混合物，在室溫隔夜攪拌。以水（大約100 mL)稀釋該反應混合物並用醋酸乙酯萃取。在低壓下 濃縮合併之醋酸乙酯層以提供呈油狀的標題混合物，該 混合物直接用於進行步驟B。 步驟B: 製備4-溴-5-(2,6-二氟-3-甲氧苯基)-1-(4-氟 苯基)-1Η-咪唑 151284.doc -95- 201117722 於一種在1，2-二氣乙烷（20mL)中的2,6-α-[(4-氟 本基)胺基]·3-曱氧苯乙腈（意即步驟Α之產物）（10.6 mmol)混合物中加入N-(溴甲烯基)-N-二甲基溴化胺 (2.80 g，12.7 mmol)。將該反應混合物在8(rc加熱一 分鐘，然後加入飽和碳酸鈉水溶液，並以二氣曱烧萃取 該水/谷液混合物。經由硫酸鎮乾燥合併之有機層、過滤 並在減壓下濃縮。將結果得到的物質藉由矽凝膠上的中 壓液相層析純化（溶析液為己烧中的醋酸乙I其梯度 ，〇到刚％)以形成呈固體狀的標題化 。 9m , 1 (m, 1H), 7.15 (m, 2H), 7.05 (m, )’ .（m, 1H), 6.82 (m，1H)，3 85 (s，3H)。 步驟C:製備2，夂_ $ ^ 一廣-5-(2,6-二氟_3_曱氧苯 基)·Η4'氟笨基)_1H_味唑 之4二在5=—^•基甲醯胺（15mL)中的、經攪拌 W 氧苯基叫4-氟苯基)1㈣ 唑（意即步驟B之產物1 )(0.500 g ’ 1.3 mmol)及 N-淳 琥珀醯亞胺（0.285 g，！ α ,、 為丄 A.60 mm〇l)混合物，在60〇C加 r〇9sn 1ΛΛ ι、物中加入更多Ν-溴琥珀醢亞胺 ^ g m〇 ，然後再次將該混合物於60°C隔 1 40、S爯又力:入更多的N_溴琥珀醯亞胺(0.250 g， 1·4〇 mmol)與再一次於6Ω。 丄 &amp; 溶液稀釋該反應混合物，=熱°以飽和碳酸納水 合物。經由硫酸鎮乾燥合併=:燒萃:該水溶液混 濃縮。將結果得到的物機層、顧並在減壓下 買猎由石夕凝膠上的中壓液相層析 151284.doc -96- 201117722 純化（溶析液為己烷中的醋酸乙酯，其梯度為0到100%) 以形成呈固體狀的標題化合物（0.36 g)。 !H NMR (CDC13) δ 7.19 (m, 2H), 7.07 (m, 2H), 6.95 (m, 1H), 6.79 (m, 1H), 3.83 (s，3H)。 實例11 製備5-(2,6-二氟-3-甲氧苯基)-1-(4-氟苯基)-2,4-二曱基-1H- 咪唑（化合物383) 一種在二氧陸圜（5 mL )及水（2滴）中的2,4-二 溴-5-(2,6-二氟-3-曱氧苯基)-1-(4-氟苯基)-1Η-咪唑（意 即實例10之產物）（0.314 g，0.68 mmol)、三曱基環氧 删烧（0.085 g’ 0.490 mmol )、碳酸铯（0.665 g，2.04 mmol) 以及二氣雙（三苯膦）鈀（0.049 g，0.07 mmol)的混合物， 在回流溫度加熱3天。在該反應混合物中加入更多三曱 基環氧硼烷（ 0.085 g，0.68 mmol)以及二氣雙(三苯膦) 鈀（0.049 g，0.70 mmol)，並將該混合物於回流溫度隔 夜加熱。在減壓下濃縮該反應混合物，並以矽凝膠上的 中壓液相層析純化結果所得之物質（溶析液為己院中的 醋酸乙酯，其梯度為0到100%)以形成呈固體狀之標 題化合物（0.097 g)。 ]H NMR (CDC13) δ 7.11 (m, 2H), 7.02 (m, 2H), 6.84 (m, 1H), 6.73 (m, 1H), 3.81 (s, 3H), 2.29 (s, 3H), 2.16 (s, 3H)。 實例12 151284.doc -97- 201117722 製備4-氣二氟甲氧基)苯基卜5_(2,6_二氟_3_甲氧苯 基)-2-乙烯基-1Η-味唑（化合物4〇6) 一種在二氧陸圜（5mL)及水（2滴）中的2_溴_4_ 氣-1-[3-(二氟曱氧基）苯基]_5_(2,6_二氟_3_曱氧苯 基)-1Η-咪唑（藉由相似於實例8步驟c 2Λ6-^^.^^(0.1〇3§;〇；3ΐ〇^^ 酸絶（0.420 g、1.29 mmol)以及二氣雙(三笨鱗)把（〇 〇28 g，0.040 mmol)的混合物，在回流溫度加熱25天。在 減壓下濃縮該反應混合物，並以矽凝膠上的中壓液相層 析純化結果所得之物質（溶析液為己烷中的醋酸乙酯， 其梯度為0到100%)以形成呈固體狀之標題化合物（3〇 mg)。 H NMR (CDC13) δ 7.37 (m，1H)，7.16 (m，1H), 7.05 (d， 1H), 6.93 (m, 2H), 6.78 (m, 1H), 6.35 (m, 3H), 5.43 (m, 1H)，3.82 (s, 3H)。 ’ ’ 實例13 製備4-氣-1-(4-氣苯基)-5-(2,3,6-三氟苯基)_1H•咪唑_2碳化 睛（化合物38) 一種在N，N-一曱基甲酿胺（3 mL )中的2-漠基_4_ 氟氯本基)-5-(2,3,6-二氟笨基)_ih_味嗤（藉由相似 於實例8步驟C的流程製備）、氰化鋅（〇 〇33 g，〇 28〇 mmol)、二氣雙(二苯膦基)二茂鐵]鈀⑴)二氣甲烷 複合物（1:1)( 0.016 g，0.02 mmol)以及四曱基乙二胺 (0.01 g，0.095 mmol)的混合物，將其在 Bi〇tage 151284.doc •98- 2011177222H), 6.41 (d, 2H), 3.77 (s, 3H) 〇(m, 1H), 6.96 (m, 151284.doc -93. 201117722 Step C: Preparation 2-Di-4-chloro-5_(2, 6_二范_4_methoxyphenyl)-1-(3-fluorophenyl)-1Η-flavored a 4-chloro-- stirred in N,N-dimercaptodecylamine (15mL) 5-(2,6-Difluoro-4-indolylphenyl)-1-(3·fluorophenyl)_iH-mipropene (the product of step B) (LOO g, 3.0 _〇1) and N - the mixture of the imine (0.641 g' 3.6 mmol) was heated in hydrazine for 25 days. The reaction mixture was diluted with a saturated aqueous solution of sodium carbonate and the obtained aqueous mixture was diluted with methylene chloride. The layer, the rhyme, and the concentration are concentrated under reduced pressure. The obtained material is purified by medium pressure liquid chromatography on a Lixi gel (the solution is the acetic acid in the hexane), the gradient is 0 to The title compound (0.67 g) was obtained as a solid. H NMR (CDC13) δ 7.37 (m, 1H), 7.13 (m, iH), 7.13 (m, 1H), 6.96 (m, 2H), 6.41 (d, 2H), 3.77 (s, 3H). Example 9 Preparation of 4-ox-5-(2,6-difluoro-4-methoxyphenyl)_1-(3-fluorophenyl)2-methyl-111-imidazole Compound 181) 2-bromo-4-chloro-5-(2,6-difluoro-4-indolylphenyl)·ι_(3·fluorophenyl) in dioxane (5 mL) and water (2 drops) ) _ih-imidazole (the product of Example 8 Step C) (0.200 g, 0.490 mmol), trimethylepoxyborane (0.062 g, 0.490 mmol), carbonic acid planer (0.479 g, 1.47 mmol), two gas The bis(triphenylphosphine)palladium (0.035 g, 0.05 mmol) mixture was heated overnight at reflux temperature. More 151284.doc -94·201117722 polytrimethylepoxyborane (0.062 g, 0.490 mmol) was added to the reaction mixture. And dioxane bis(triphenylphosphine)palladium (0.035 g, 0.05 mmol), and the mixture was heated again overnight at a mixed flow temperature. The reaction mixture was concentrated under reduced pressure and a medium pressure liquid layer on a ruthenium gel. The title compound (0.090 g) was obtained as a solid. m.p. NMR (CDC13) δ 7.35 (m, m. 1Η), 7.09 (m, 1H), 6.94 (d, 1H), 6.89 (m, 1H), 6.39 (m, 2H), 3.76 (s, 3H), 2.31 (s, 3H). Example 10 Preparation of 2,4-dibromo-5-(2,6-difluoro-3-methoxyphenyl)-1-(4-fluorophenyl)-1 oxime-imidazole (Compound 350) Step A: Preparation 2 ,6-α-[(4-fluorophenyl)amino]-3-methoxybenzeneacetonitrile, 4-fluoroaniline (1.17 g, 10.6 mmol), 2,6·difluoro- in tetrahydrofuran (50 mL) A mixture of 3-nonoxybenzaldehyde (2.00 g, 11.6 mmol), potassium (2.80 g, 42.4 mmol) and indium chloride (2.30 g, 10.4 mmol) was stirred overnight at room temperature. The reaction mixture was diluted with water (ca. 100 mL) and extracted with ethyl acetate. The combined ethyl acetate layer was concentrated under reduced pressure to give the title mixture as an oil, which was used directly for step B. Step B: Preparation of 4-bromo-5-(2,6-difluoro-3-methoxyphenyl)-1-(4-fluorophenyl)-1Η-imidazole 151284.doc -95- 201117722 2,6-α-[(4-fluorobenzyl)amino]3-oxo-oxyphenylacetonitrile (the product of the step oxime) (10.6 mmol) in 2-diethane (20 mL) N-(Bromomethyl)-N-dimethylammonium bromide (2.80 g, 12.7 mmol) was added. The reaction mixture was heated at rt (1 min) then a saturated aqueous solution of sodium carbonate was added and the mixture was evaporated and evaporated. The resulting material was purified by medium pressure liquid chromatography on a hydrazine gel (the lysate was a gradient of acetic acid in hexanes, and then spurred to 5%) to form a solid title. 1 (m, 1H), 7.15 (m, 2H), 7.05 (m, )' . (m, 1H), 6.82 (m, 1H), 3 85 (s, 3H). Step C: Preparation 2, 夂_ $ ^ 一广-5-(2,6-Difluoro_3_indolylphenyl)·Η4'fluorophenyl)_1H_isazole 4 2 in 5=—^• carbamide (15 mL) , stirred W oxyphenyl is called 4-fluorophenyl) 1 (tetra) azole (meaning product of step B) (0.500 g '1.3 mmol) and N-nonyl succinimide (0.285 g, ! α , ,丄A.60 mm〇l) mixture, add more Ν-bromosuccinimide ^ gm〇 at 60 ° C plus r 〇 9sn 1 ΛΛ ι, and then again separate the mixture at 60 ° C 1 40, S爯 and force: add more N-bromosuccinimide (0.250 g, 1.4 〇mmol) and once again at 6 ΩThe reaction mixture was diluted with 丄 &amp; solution = = hot to sat Na carbonate. Drying by sulfuric acid drying = = calcination: the aqueous solution was concentrated and concentrated. The obtained machine layer and Gu under the reduced pressure were purified by medium-pressure liquid chromatography 151284.doc-96-201117722 on the Lixi gel (the solution was ethyl acetate in hexane, The gradient was 0 to 100%) to give the title compound (0.36 g) as a solid. !H NMR (CDC13) δ 7.19 (m, 2H), 7.07 (m, 2H), 6.95 (m, 1H), 6.79 (m, 1H), 3.83 (s, 3H). Example 11 Preparation of 5-(2,6-difluoro-3-methoxyphenyl)-1-(4-fluorophenyl)-2,4-dimercapto-1H-imidazole (Compound 383) 2,4-dibromo-5-(2,6-difluoro-3-indolylphenyl)-1-(4-fluorophenyl)-1Η in Lu (5 mL) and water (2 drops) -imidazole (meaning the product of Example 10) (0.314 g, 0.68 mmol), tridecyl epoxy de-burning (0.085 g' 0.490 mmol), cesium carbonate (0.665 g, 2.04 mmol) and dioxane (triphenylphosphine) A mixture of palladium (0.049 g, 0.07 mmol) was heated at reflux for 3 days. More trimethylsulfone oxide borane (0.085 g, 0.68 mmol) and dioxobis(triphenylphosphine)palladium (0.049 g, 0.70 mmol) were added to the reaction mixture, and the mixture was heated at reflux overnight. The reaction mixture was concentrated under reduced pressure, and the obtained material was purified by medium-pressure liquid chromatography on a hydrazine gel (the eluent was ethyl acetate in the house, and the gradient was 0 to 100%). The title compound (0.097 g) was obtained as a solid. H NMR (CDC13) δ 7.11 (m, 2H), 7.02 (m, 2H), 6.84 (m, 1H), 6.73 (m, 1H), 3.81 (s, 3H), 2.29 (s, 3H), 2.16 (s, 3H). Example 12 151284.doc -97- 201117722 Preparation of 4-gas difluoromethoxy)phenyl b-5-(2,6-difluoro-3-methoxyphenyl)-2-vinyl-1 oxime- azole (compound) 4〇6) A 2-bromo-4_qi-1-[3-(difluorodecyloxy)phenyl]_5_(2,6_2) in dioxane (5mL) and water (2 drops) Fluorine_3_indolylphenyl)-1Η-imidazole (by similar step 8 of Example 8 c 2Λ6-^^.^^(0.1〇3§;〇;3ΐ〇^^ acid (0.420 g, 1.29 mmol) And a mixture of two gas double (three squama) ((28 g, 0.040 mmol), heated at reflux temperature for 25 days. The reaction mixture was concentrated under reduced pressure, and the medium pressure liquid layer on the ruthenium gel The title compound (3 〇 mg) was obtained as a solid (H NMR (CDC13) δ 7.37 (m). , 1H), 7.16 (m, 1H), 7.05 (d, 1H), 6.93 (m, 2H), 6.78 (m, 1H), 6.35 (m, 3H), 5.43 (m, 1H), 3.82 (s, 3H). ' ' Example 13 Preparation of 4-gas-1-(4-phenylphenyl)-5-(2,3,6-trifluorophenyl)_1H•imidazole-2 carbonized eye (Compound 38) One in N , 2-di-N-mercaptoamine (3 mL) Base_4_ fluorochlorobenzyl)-5-(2,3,6-difluorophenyl)_ih_ miso (prepared by a procedure similar to that of Example 8 Step C), zinc cyanide (〇〇33 g, 〇28〇mmol), dioxobis(diphenylphosphino)ferrocene]palladium(1)) digas methane complex (1:1) (0.016 g, 0.02 mmol) and tetradecylethylenediamine (0.01 g, 0.095 mmol) of the mixture, which is in Bi〇tage 151284.doc •98- 201117722

Initiator™微波裝置中以60°C加熱200秒。在減壓下濃縮 該反應混合物’並以矽凝膠上的中壓液相層析純化結果 所得之物質（溶析液為己烷中的醋酸乙酯，其梯度為〇 到100% )以形成呈固體狀(0.030 g)、在i47-149°C溶化 之標題化合物，即為本發明之化合物。 !H NMR (CDC13) δ 7.45 (m, 2H), 7.28 (m, 1H), 7.21 (m, 2H), 6.89 (m，1H)。 實例14 製備4-氣-5-(2,6-二氟苯基)-2-乙炔基氟苯基)_ih-咪唾 (化合物29) 步驟A :製備4·氣-5-(2,6·二氟苯基）小(3-氟苯 基)-2_[2_(三甲矽基）乙炔基】-1Η-咪唑 一種在三乙胺（15 mL)中的2-溴基-4-氯-5-(2,6· 一氟苯基)-1-(3-氟苯基)-1Η·咪嗤（藉由相似於實例8步 驟C的流程製備）（0.823 g，2.10 mmol)、二氣雙(三笨 膦）把（0.147 g，0.21 mmol)以及碘化銅⑴（〇 〇81 g， 0.74 mmol)的混合物，在氮氣流經位於該反應混合物 之表面下方的注射針的同時，將該反應混合物攪拌5分 鐘。在該反應混合物中加入三甲基乙炔矽烷（0.216g， 2.2 mmol)，並持續攪拌2小時，然後在回流溫度隔夜 加熱δ玄混合物。在§玄反應混合物中加入更多的二氯雙 (二苯膦）把（0.147 g’〇,21 mmol)以及三曱基石夕乙块 (0.216 g，2.2 mmol) ’並在回流溫度加熱該混合物4 小時。以飽和碳酸鈉水溶液稀釋該反應混合物並以醋酸 151284.doc -99- 201117722 乙酯進行萃取，以飽和乙二胺四乙酸水溶液清洗經合併 之有機層、經由硫酸鎂乾燥、過濾並在減壓下濃縮。將 結果得到的物質藉由矽凝膠上的中壓液相層析純化（溶 析液為己烷中的醋酸乙酯，其梯度為0到100%)以形 成呈固體狀的標題化合物（〇.244 g)。 !H NMR (CDC13) δ 7.34 (m, 2H), 7.05 (m, 3H), 6.89 (m, 2H)，0.13 (s，9H)。 步驟B: 製備4-氣-5-(2,6-二氟苯基)-2-乙炔基-1-(3- 氟苯基)-1Η-咪唑 一種在氫氧化納之溶液以及甲醇（1%，w/w，2 mL) 中的4-氣-5-(2,6-二氟苯基)-1-(3-氟苯基)-2-[2-(三曱矽 基）乙炔基]-1H-咪唑（意即步驟A之產物）（0.231 mg， 0.570 mmol)混合物，將其在室溫攪拌3小時。以醋酸 乙酉旨以及飽和氣化敍水溶液稀釋該反應混合物，分層， 並以醋酸乙酯將水性層萃取出來。經由硫酸鎂乾燥經合 併之有機層、過濾並在減壓下濃縮以形成固體狀之標題 化合物（0.135 g)。 ]H NMR (CDC13) δ 7.35 (m, 2H), 7.11 (m, 1H), 7.00 (m, 2H), 6.89 (m，2H)，3.17 (s，1H)。 實例15 製備4-氣-5-(2,6-二氟-4-甲氧苯基)-1-(4-氟苯基)-1Η-咪唑-2- 甲醇（化合物199) 151284.doc •100· 201117722 步驟A: 製備4-氯-5-(2,6-二氟-4-甲氧苯基)-1-(4-氟 苯基)-1Η-咪唑-2-甲醛 於一種在二乙基鍵0〇mL)中的4-氣-5-(2,6-二氟 -4-甲氧苯基)-1 -(4-氟苯基)-1H-咪唑（藉由相似於實例8 步驟A與B的流程製備）（I.35 g ’ 4.0 mmol)經攪拌 混合物中，在0°C下加入二異丙胺鋰（2 M於四氫°夫°南 中，2.2 mL，4.4 mmol)。在〇 C中將該反應混合物稅拌 1小時，然後加入N，N-二甲基曱醯胺（0.47 mL ’ 6.0 mmol)。於0。(：再攪拌1小時後’將該反應混合物回溫 至室溫。1小時後，以檸檬酸水溶液稀釋該反應混合物 (20%，30 mL)並以二乙基醚（100 mL)進行萃取。 經由硫酸鎂乾燥有機層、過濾並在減壓下濃縮。將結果 得到的物質藉由矽凝膠上的快速管柱層析術純化（溶析 液為正氣化丁烧中的醋酸乙酯，其梯度為〇到2〇0/〇 )以 得到淺黃色的固體狀標題化合物（0.397 g )。 NMR (CDC13) δ 9.71 (s，1H)，7.19-7.17 (m，2H)，7.06 (t, J - 7.5 Hz, 2H), 6.44 (m, 1H), 6.42 (s, 1H), 3.78 (s, 3H)。 ’ ESI MS m/z 367 (M+l) ° 步驟B:製備4-氣-5-(2,6-二氟·4·甲氧苯基^•(扣氟 苯基)-1Η-味嗤-2-甲醇 於一種在曱醇（10 mL)中的4-氣-5-(2,6-二氟-4_ 甲氧苯基)-1-(4-氟苯基)-1Η-咪唑_2-甲醛（意即步驟a 之產物）混合物中加入氫硼化鈉（U0 g，2 64 mm〇1)。 151284.doc • 101 . 201117722 1小時後，在該反應混合物加入水（25 mL)，以二乙基 醚（50 mL )萃取水性混合物、經由硫酸鎮乾燥、過遽， 並在減壓下濃縮。將結果得到的物質藉由矽凝膠上的中 壓液相層析純化（溶析液為己烷中的醋酸乙酯，其梯度 為0到30%)以形成呈固體狀的標題化合物（0.156 g)。 !Η NMR (CDC13) δ 7.26-7.25 (m, 2H), 7.07 (t, J = 7.5 Hz, 2H), 6.42 (s, 1H), 6.39 (s, 1H), 4.54 (d, J = 3 Hz, 2H), 4.13 (t，J = 6 Hz，1H)，3.77 (s，3H)。 實例16 製備4·氣-5-(2,6-二氟-4-甲氧苯基)-2-(氟甲基)-1-(4-氟苯 基)-1Η-咪唑（化合物221) 於一種在二氯甲烷（2 mL)中的4-氣-5-(2,6-二氟 -4-曱氧苯基)-1-(4-氟苯基)-1Η-咪唑-2-曱醇（意即實例 15之產物）混合物中加入三氟化二乙氨基疏（60 pL， 0.45 mmol)。2小時後，以水稀釋該反應混合物、以二 氣曱烷（100 mL)萃取、經由硫酸鎂乾燥、過濾並在減 壓下濃縮。將結果得到的物質藉由矽凝膠上的中壓液相 層析純化（溶析液為己烷中的醋酸乙酯，其梯度為0到 20%)以形成呈白色固體狀的標題化合物（0.031 g)。 ]H NMR (CDC13) δ 7.25-7.23 (m, 2Η), 7.08 (t, J = 6 Hz, 2H), 6.43 (s, 1H), 6.41 (s, 1H), 5.25 (s, 1H), 5.13 (s, 1H), 3.78 (s，3H)。 實例17 151284.doc •102- 201117722 製備4-漠基-2-(演曱基)-1-(4-氯苯基)-5-(2,6-二氣苯基)_ih_ 咪唑（化合物326) 一種在四氣化碳（8 mL)中的4-溴基_ι_(4-氯苯 基)-5-(2,6-二氟苯基)_2-曱基-111-咪唑（意即實例5之產 物）（1.00 g，2.6 mmol)、N-溴號珀醯亞胺（0 510 g， 2.87 mmol)以及 2,2’-偶氮雙(2-異丁睛）（0.021 g，13〇 mmol)，將其在回流溫度隔夜加熱。在減壓下濃縮該反 應混合物’並以矽凝膠上的中壓液相層析純化結果所得 之物質（溶析液為己烷中的醋酸乙酯，其梯度為〇到 100%)以形成呈固體狀之標題化合物（0.94〇g)。 !H NMR (CDC13) δ 7.35 (m, 3H), 7.24 (m, 2H), 6.87 (m, 2H)，4.36 (s, 2H)。 實例18 製備3-[2-漠-4-氣-1-(4-氯苯基)-1Η-味唾-5-基】-2,4-二敦苯甲 腈（化合物283) 步驟A: 製備3-[4-氣-1-(4-氯苯基）_1H_咪唑_5_ 基卜2,4-二氟苯曱腈 一種在二曱基乙醯胺（3 mL)中的5-(3-溴基-2,6-二氣苯基)-4-氣-1-(4-氣苯基)-1Η-咪唾（藉由相似於實例 8步驟A與B的流程製備）（0.440 g，0.490 mmol )、氰 化鋅（0.058 g’ 0.490 mmol)、二氣[1，1，_雙(二苯膦基) 二茂鐵]鈀(II):二氯甲烷複合物（1:1 ) (0.044 g，0.0545 mmol)以及 N，N，N’，N’，四曱基乙二胺（ 0.022 g，0.22 mmol)的混合物，將其利用BiotageInitiatorTI&quot;^波裝置 151284.doc -103- 201117722 在200加熱5分鐘。在減壓下濃縮該反應混合物，並以 砂凝膠上的中壓液相層析純化結果所得之物質（溶析液 為己统中的醋酸乙酯，其梯度為〇到1 〇〇% )以形成呈 固體狀之標題化合物（0.217 g)。 !H NMR (CDC13) δ 7.72 (s, 1H), 7.69 (m, 1H), 7.38 (m, 2H), 7.07 (m, 3H) ° ’ 步驟B:製備3-[2-溴-4-氣-1-(4-氣苯基)-m-咪唾_5 基]-2,4-二氣苯甲腈 一種在二甲基曱醯胺（4mL)中的3·[4-氣-1&lt;4_氣 苯基)-1Η-咪唾-5-基]-2,4-二氟苯甲腈（意即步驟β之產 物）（0.217 g’ 0.62 mmol)以及Ν-溴琥珀醯亞胺（〇165 g，0.930 mmol)的混合物，將其在60¾隔夜加熱。在 該反應混合物中分批添加更多的N-溴琥珀酿亞胺 (0.386 g，2.17 mmol)，並在60〇C再次隔夜加熱。將該 反應混合物以醋酸乙酯稀釋、以飽和氣化鈉水溶液= 滌、經由硫酸鈉乾燥、過濾並在減壓下濃縮。將結果得 到的物質藉由矽凝膠上的中壓液相層析純化（溶析液^ 己烷中的醋酸乙酯，其梯度為〇到100%)以形成呈固 體狀的標題化合物（0.196 g)。 («1， 巾 NMR (CDC13) δ 7.67 (m，1H)，7.40 (m，2H)，7.13 2H)，7.03 (m，1H)。 實例19 製備3-【4_氯-l-(4·氣苯基)-2-甲基-1H-咪唑-5-基]-2,4-二翁&amp; 一&quot;規*采 151284.doc -104- 201117722 甲腈（化合物292) 一種在二氧陸園（4 mL)及水（2滴）中的3-[2-溴基-4-氯-1-(4-氯苯基)-1Η-β米唾-5-基]-2,4-二氟苯甲腈 (意即實例18之產物）（0.150 g，0.350 mmol)、三曱 基環氧棚院（0.088 g、0.700 mmol)、碳酸铯（0.342 g， 1.05 mmol)以及二氯雙（三苯膦）鈀（ 0.025 g，0.035 mmol)的混合物，將其再回流溫度加熱3小時。在減 壓下濃縮該反應混合物，並以石夕凝膠上的中壓液相層析 純化結果所得之物質（溶析液為己烧中的醋酸乙酯，其 梯度為0到100%)以形成呈固體狀之標題化合物（0.088 g) 0 ]H NMR (CDC13) δ 7.65 (m, 1Η), 7.39 (m, 2H), 7.09 (m, 2H)，7.01 (m, 1H)，2.32 (s，3H)。 實例20 製備4-【4-氣-2-甲基-1-(4-甲基苯基)-1Η-咪唑_5-基】-3,5_二氟 苯酚（化合物437) 一種在二氯曱烷（10 mL)中的4-氣-5-(2,6-二氟-4-甲氧苯基)-2-甲基-1-(4-甲基苯基)-1Η-咪唑（藉由相似於 實例9的流程製備）（0.500 g，1.43 mmol)經擾拌混合 物，在-78°C下加入三溴化硼（1 Μ在二氯甲烷中，4.3 mL，4.3 mmol)。將該反應混合物回溫至室溫，並隔夜 攪拌。於室溫下在該反應混合物中加入更多三溴化硼（1 Μ在二氣曱烷中，1.4 mL，1.40 mmol) ’並持續授拌4 小時。在該反應混合物中加入氫氯酸（1 N，8.0 mL)， I5I284.doc .105- 201117722 然後加入飽和碳酸鈉水溶液以將該水性混合物， 性pH值。以醋酸乙酯萃取該水性混合物，並經由二1 鎂乾燥該萃取物、過濾及在減壓下濃縮。將結果得 物質藉由矽凝膠上的中壓液相層析純化（溶析液為！的 中的醋酸乙酯’其梯度為0到1〇〇%)以形成呈^己燒 的標題化合物（0.41 g)。 !H NMR (CDC13) δ 10.68 (S, lH), 7.24 (d, 2H), 7 〇9 2H)，6.43 (m，2H)，2.31 (s，3H)，2.18 (s，3H)。（ ’ 實例21 製備3-[4·[4-氯-2-曱基-1-(4-甲基苯基)_1H-咪唑-5基】·3,5· 二氟苯氧基】-Ν-甲基-1-丙醯胺鹽酸鹽（化合物5〇3) 步驟Α:製備苯曱基Ν-[3-【4_[4-氣-2-甲基·ΐ_(4-甲基 苯基）-1Η-咪唑-5-基】-3,5-二氟苯氧基]丙 基】-Ν-氨基甲酸甲酯 一種在Ν，Ν-二曱基曱醯胺（3 mL)中的4-[4-氯-2-曱基-1-(4-甲基笨基)_1H_咪唑_5_基]_3,5_二氟苯酚（意即 實例20之產物）（〇.2〇〇g ’ 0598mm〇1)以及4入分子 篩（1.55 g)的混合物，將其在室溫攪拌3小時，然後 加入一種在N，N-二曱基曱醯胺（！ 中的苯甲基N_(3_ 氣丙基)-N-氨基甲酸曱酯（利用如pCT公開號w〇 2007/149448中所描述的方法製備）（ 0.434 g，1.80 mmo1)以及碘化四丁銨（0.044 g，0.120 mmol)的溶液。 15分鐘後’在該反應混合物中加入碳酸鉋（0.584 g， 1·80 mmolh 15分鐘後，在75乞加熱該反應混合物2 151284.doc •106- 201117722 小時。過濾該反應混合物，並在減壓下濃縮該濾液。將 結果得到的物質藉由矽凝膠上的中壓液相層析純化（溶 析液為己烷中的醋酸乙酯，其梯度為〇到1〇〇%)以形 成呈固體狀的標題化合物（21〇mg)。 ESIMS m/z 541 (M+1) 〇 步驟B:製備3_[4-丨4-氣-2-甲基_ι_(4-甲基苯基)-1Η- 味也-5-基]-3,5-二氟苯氧基】_N_甲基丙醯 胺鹽酸鹽 一種苯曱基N-[3-[4-[4-氣_2_曱基-1-(4-甲基苯 基)-1Η-咪唑-5-基]_3,5-二氟笨氧基]丙基]_N_氨基曱酸 曱醋（意即步驟A之產物）（〇 197 g，〇 365 mm〇i)、氫 氣酸（2M在一乙基醚中’ 1 mL)以及曱醇（30mL) 的混合物’以氮氣沖洗30分鐘，然後加入纪破（1〇0/〇， 0.058 g，0.055 mmol)並繼續維持氮氣沖洗15分鐘。 I5分鐘後’停止氮氣沖洗並將充滿氫氣的氣球與反應 燒瓶連接，在室溫攪拌該反應混合物3小時。以氮氣沖 洗該反應混合物，並藉由通過銲接玻璃漏斗上的砂床及 Celite® (矽藻助濾劑）以濾除鈀碳觸媒。在減壓下濃縮 δ亥濾、液以形成主固體狀之標題化合物（〇. 1g )。 ]H NMR (DMSO-d6) δ 8.90 (br s, 2H), 7.25 (d, 2H), 7.11 (d, 2H), 6.76 (d, 2H), 4.08 (t, 2H), 2.98 (m, 2H), 2.54 (m, 3H), 2.31 (s, 3H), 2.19 (s, 3H), 2.04 (d, 2H) 〇 實例22 -107- 151284.doc 201117722 製備5-[2-溴-4-氣-5-(2,6-二氟-4-甲氧苯基)_1H-咪唑-1-基]-2-(三氟曱基)吡啶（化合物481) 步驟A : 製備N-[(2,6_二氟-4-甲氧苯基）亞甲 基】-6-(三氟甲基)-3_〇比咬胺 一種在曱苯（100 mL)中的6-(三氟甲基)·3-吡咬胺 (5.00 g，30.8 mmol)以及 2,6-二氟-4-甲氧苯曱酸（5.30 g ’ 30.8 mmol)的混合物，將其加熱至回流2.5天。將 該反應混合物冷卻至室溫並在減壓下濃縮以形成呈固 體狀之標題化合物（9.9 g)。 iH NMR (CDC13) δ 8.56 (s，1H)，8.52 (d，1H)，7.71 (d， 1H)，7.60 (m，1H)，6.57 (m，2H)，3.88 (s，3H)。 步驟B:製備5-[5-(2,6-二氟-4-甲氧苯基)·1Η咪唑 -1-基】-2-(三氟甲基)《»比咬 一種在二曱氧乙烷（20 mL)及曱醇（20 mL)中 的Ν·[(2,6·二氟甲氧苯基)亞甲基]·6_(三氟曱比 啶胺（意即步驟Α之產物）、1-[(1-異氰基乙基）續醯 基]-4-曱基苯（4.6 g，24 mmol)以及碳酸卸（4.4 g，32 mmol)的混合物，將其在75°C隔夜加熱。在減壓下濃 縮該反應混合物，並以矽凝膠上的中壓液相層析純化結 果所得之物質（溶析液為己烷中的醋酸乙酯，其梯度為 0到100%)以形成呈固體狀之標題化合物（4 63 g)。 ]H NMR (CDC13) δ 8.59 (m, 1Η), 7.86 (s, 1H), 7.71 (m, 2H), 7.33 (m, 1H), 6.46 (m, 2H), 3.80 (s, 3H) 〇 151284.doc -108- 201117722 步驟C:製備5-[4-氯-5_(2,6-二氟_4_甲氧苯基)_111_ 咪唑-1-基]-2-(三氟甲基)吼唆 —種在四氣化碳（8 mL)中的5_[5_(2,6_二氟-‘曱 氧笨基)-1Η-咪唑-l_基]·2-(三氟曱基)吡啶（意即步驟B 之產物）（1.50 g，4.20 mmol))、Ν-氣琥珀醯亞胺（〇56 g ’（2 mm〇l)以及 2,2，·偶 i雙(2·異丁睛）（〇 〇38 g，〇 23 的混合物，將其在65°C加熱3.5天。以飽和碳 酉文鈉水溶液稀釋該反應混合物，並以二氣甲烷萃取。經 $硫酸鎂乾燥合併之有機層、過濾並在減壓下濃縮。將 結果得到的物質藉由矽凝膠上的中壓液相層析純化（溶 析液為己烷中的醋酸乙酯，其梯度為〇到1〇〇%)以形 成呈固體狀的標題化合物（〇.65〇g)。 Ή NMR (CDC13) δ 8.59 (m, 1Η), 7.73 (m, 3H), 6.49 (m, 2H), 3.82 (s，3H)。 ’ 步驟D ·製備5-[2-漠-4-氣-5-(2,6-二氟-4-曱氧苯 基)-1Η-咪唑-1-基】-2-(三氟甲基)吼啶 一種在Ν，Ν· 一曱基曱醯胺（10 niL )中的5-[4-氯 -5-(2,6-一氟-4-甲氧苯基)-1Η-β米唾_ι_基]_2_(三氟曱基) 口比咬（意即步驟C之產物）（0.650 g，/及 N-溴琉珀酿亞胺（0.356 g，2.0 mmol)的混合物，將其 在65°C隔夜加熱。在該反應混合物中加入更多的N—溴 琥珀醯亞胺（0.195 g，1.1 mm〇l)，並將該混合物在&amp; °C加熱2.5天。以飽和碳酸鈉溶液稀釋該反應混合物， 並以二氣甲烷萃取。經由硫酸鎂乾燥合併之有機層、過 151284.doc -109· 201117722 濾並在減壓下濃縮。將結果得到的物質藉由矽凝膠上的 中壓液相層析純化（溶析液為己烧中的醋酸乙醋，其梯 度為0到100%)以形成呈固體狀的標題化合物（0.108 g)。 lU NMR (CDC13) δ 8.58 (s, 1H), 7.78 (m, 2H), 6.43 (m, 2H), 3.79 (s，3H)。 實例23 製備5-[4-氣-5-(2,6-二氟-4-曱氧苯基)-2-甲基-1H-咪唑-1-基】-2-(三氟甲基)吡啶（化合物487) 一種在二氧陸圜（3 mL)及水（1滴）中的5-[2-溴基-4-氯-5-(2,6-二氟-4-甲氧苯基）-1Η-咪唑-1· 基]-2-(三氟曱基)吡啶（意即實例22之產物）（0.093 g， 0.20 mmol )、三曱基環氧棚烧（0.025 g，0.20 mmol)、 碳酸鉋（0.195 g，0.60 mmol)以及二氣雙（三苯膦）鈀 (0.014 g，0.20 mmol)的混合物，將其隔夜加熱至回 流。然後在減壓下濃縮該反應混合物，並以矽凝膠上的 中壓液相層析純化結果所得之物質（溶析液為己烷中的 醋酸乙酯，其梯度為0到100%)以形成呈固體狀之標 題化合物（0.021 g)。 ]H NMR (CDCI3) δ 8.55 (s, 1H), 7.75 (m, 1H), 7.69 (m, 1H)，6.42 (m，2H)，3.78 (s，3H), 2.35 (s，3H)。 實例24 製備2-氣-5-[2-氣-1-(2,6-二氟-4-甲氧苯基)-4-曱基-1H-咪唑 151284.doc -110- 201117722 -5-基I吡啶（化合物475) 步驟A: 製備N-[(6-氣-3·«比啶基）亞甲基卜2,6-二氣 -4-甲氧基苯胺 將6-氣-3-°比咬曱酸（1.0 g，6.3 mmol)加入一種在 曱苯（20〇11〇中的2,6_二氟-4-曱氧基苯胺（〇.98〇 &amp; 5 6.9 mmol)混合物中。利用Dean-Stark分離器將該反鹿 混合物加熱至回流，以共沸去除水。16小時後，將# 反應混合物冷卻至室溫，並在減壓下濃縮。結果所得之 物質在真空烘箱中於55°C乾燥隔夜，以形成呈淺17加啡 色固體狀之標題化合物（1.66g)。 ]H NMR (CDCI3) δ 8.74 (s, 1Η), 8.73 (d, J = 2.44 Hz, 1H) 8.32 (dd, J = 2.20 Hz, J = 8.29 Hz, 1H), 7.44 (d, J = 8 29 Hz，1H)，6.59-6.52 (m，2H)，3.82 (s，3H)。 19F NMR (CDC13) δ -121.48 至-121.40 (m，2F)。 步驟B: 製備2-氣-5-[l-(2,6-二氟-4-甲氧苯基)_4-甲 基-1H-咪唑-5-基】吡啶 將對曱苯磺曱基異氰化物0.35 g，6.5 mmol)及 第三丁醇鉀（0.86 g ’ 7.7 mmol)加入一種在四氫咬〇南 (15 mL)中的N-[(6-氣-3』比啶基)亞曱基]-2,6-二氟_4_ 甲氧基苯胺（意即步驟A之產物）（1.66 g，5.9 mmol) 的混合物中。將該反應混合物在85°C加熱4小時、冷 卻並濃縮。以醋酸乙S旨稀釋結果所得之物質並以飽和氯 化鈉水溶液洗滌。經由硫酸鎂乾燥有機層、過遽並濃 縮。以矽凝膠上的中壓液相層析純化結果所得之物質 151284.doc 201117722 (/合析液為己烷中的醋酸乙酯），然後以正氣化丁烷_己 烷研磨以得到呈棕褐色固體狀(〇5〇 g)的標題化合物， 其熔點為117-118¾。 NMR (CDC13) δ 8.16d5 J = 2.44 Hz, 1H), 7.55 (s, 1H), 7.44 (dd，J = 2.68 及 8.29 Hz，1H)，7.28 (dd，J = 0.49 及 8.29 Hz, 1H), 6.54-6.48 (m, 2H), 3.81 (s, 3H), 2.33 (s, 3H)。 F NMR (CDC13) δ -118.21 至]18 15 (m，2F)。 步称c·製備2-氣-5-[2-氣·ι_(2,6-二氟-4-甲氧苯 基)·4_甲基-1Η-咪唾_5_基】”比咬 於種在Ν，Ν-二曱基曱醯胺（2 〇 mL)中的2_氣 -5-[l-(2,6-二氟-4-曱氧苯基)甲基_1H_咪唑_5_基]吡啶 (意即步驟B之產物）（〇.15()g，G 45inm〇1)混合物中 加入N-氣琥珀醢亞胺（〇.〇66 g，〇 49 mm〇1)，並在6〇 C加熱該反應混合物。3〇分鐘後，將該反應混合物冷 部至室溫’以醋酸乙醋（4〇 mL)稀釋，並以水及飽和 氯化鈉水溶液絲。經由硫_乾财機層、過遽並在 減壓下濃縮。以⑪轉上的巾m液相層析純化結果所得 :物：（/合析液為已烷中的醋酸乙酯），以形成呈灰白 hNMiuax^jf化之標題化合物⑷心）。 8.29 Hz, J = 2.44 = 2 20 HZ&gt; ^ 7 43 ^ ^ (^Ι = 9.02Ηζ,2Η)，3?，7,26(Μ = 8·54ΗΖ?1Η)ϊ6·53 )，3·82 (s，3H)，2.28 (s，3H)。 151284.doc •112· 201117722 實例25The InitiatorTM microwave device was heated at 60 ° C for 200 seconds. The reaction mixture was concentrated under reduced pressure and the resulting material was purified by medium pressure liquid chromatography on a hydrazine gel (the lysate was ethyl acetate in hexane with a gradient of 〇 to 100%) to form The title compound which is solid (0.030 g), which is dissolved at i47-149 ° C, is a compound of the invention. !H NMR (CDC13) δ 7.45 (m, 2H), 7.28 (m, 1H), 7.21 (m, 2H), 6.89 (m, 1H). Example 14 Preparation of 4-gas-5-(2,6-difluorophenyl)-2-ethynylfluorophenyl)_ih-mipropan (Compound 29) Step A: Preparation of 4·Ga-5-(2,6 Difluorophenyl) small (3-fluorophenyl)-2_[2_(trimethylmethyl)ethynyl]-1 fluorene-imidazole 2-bromo-4-chloro- in triethylamine (15 mL) 5-(2,6·monofluorophenyl)-1-(3-fluorophenyl)-1 oxime oxime (prepared by a procedure similar to that of Example 8 Step C) (0.823 g, 2.10 mmol), two gas a mixture of (0.147 g, 0.21 mmol) and copper iodide (1) (〇〇81 g, 0.74 mmol), while flowing nitrogen through an injection needle located below the surface of the reaction mixture The reaction mixture was stirred for 5 minutes. Trimethyl acetylene decane (0.216 g, 2.2 mmol) was added to the reaction mixture, and stirring was continued for 2 hours, then the δ mixture was heated overnight at reflux temperature. Add more dichlorobis(diphenylphosphine) (0.147 g'〇, 21 mmol) and triterpene base (0.216 g, 2.2 mmol) to the § Xuan reaction mixture and heat the mixture at reflux temperature. 4 hours. The reaction mixture was diluted with a saturated aqueous solution of sodium carbonate and extracted with ethyl acetate 151284.doc -99 - 201117722 ethyl acetate. The combined organic layers were washed with a saturated aqueous solution of ethyldiaminetetraacetic acid, dried over magnesium sulfate, filtered and evaporated. concentrate. The resulting material is purified by medium pressure liquid chromatography on a hydrazine gel (the lysate is ethyl acetate in hexane, gradient from 0 to 100%) to give the title compound as a solid. .244 g). !H NMR (CDC13) δ 7.34 (m, 2H), 7.05 (m, 3H), 6.89 (m, 2H), 0.13 (s, 9H). Step B: Preparation of 4-gas-5-(2,6-difluorophenyl)-2-ethynyl-1-(3-fluorophenyl)-1Η-imidazole as a solution in sodium hydroxide and methanol (1 4-Ga-5-(2,6-difluorophenyl)-1-(3-fluorophenyl)-2-[2-(tridecyl)acetylene in %, w/w, 2 mL) A mixture of -1H-imidazole (i.e., product of Step A) (0.231 mg, 0.570 mmol) was stirred at room temperature for 3 hours. The reaction mixture was diluted with ethyl acetate and a saturated aqueous solution of sodium sulfate, and the aqueous layer was extracted with ethyl acetate. The combined organic layer was dried with EtOAcjjjjjjjjjj H NMR (CDC13) δ 7.35 (m, 2H), 7.11 (m, 1H), 7.00 (m, 2H), 6.89 (m, 2H), 3.17 (s, 1H). Example 15 Preparation of 4-Ga-5-(2,6-difluoro-4-methoxyphenyl)-1-(4-fluorophenyl)-1 oxime-imidazole-2-methanol (Compound 199) 151284.doc • 100· 201117722 Step A: Preparation of 4-chloro-5-(2,6-difluoro-4-methoxyphenyl)-1-(4-fluorophenyl)-1Η-imidazole-2-carbaldehyde in one of two 4-Ga-5-(2,6-difluoro-4-methoxyphenyl)-1 -(4-fluorophenyl)-1H-imidazole in the ethyl group 0〇mL) (by similar example 8 Procedure for the preparation of Steps A and B) (I.35 g '4.0 mmol) In a stirred mixture, add lithium diisopropylamide (2 M in tetrahydrofuran, 2.2 mL, 4.4 mmol) at 0 °C. ). The reaction mixture was mixed for 1 hour in 〇 C, then N,N-dimethyl decylamine (0.47 mL '6.0 mmol) was added. At 0. (After stirring for an additional 1 hour, the reaction mixture was warmed to room temperature. After 1 hour, the reaction mixture was diluted with aqueous citric acid (20%, 30 mL) and extracted with diethyl ether (100 mL). The organic layer was dried over magnesium sulfate, filtered and concentrated under reduced pressure. The obtained material was purified by flash column chromatography on a gel. The title compound (0.397 g) was obtained as a pale yellow solid. NMR (CDC13) δ 9.71 (s, 1H), 7.19-7.17 (m, 2H), 7.06 (t, J - 7.5 Hz, 2H), 6.44 (m, 1H), 6.42 (s, 1H), 3.78 (s, 3H). 'ESI MS m/z 367 (M+l) ° Step B: Prepare 4-Ga-5 -(2,6-difluoro.4. methoxyphenyl^•(decafluorophenyl)-1Η-miso-2-methanol in a 4-gas-5- (in sterol (10 mL)) Adding sodium borohydride (U0 g, a mixture of 2,6-difluoro-4_methoxyphenyl)-1-(4-fluorophenyl)-1 quinone-imidazole-2-formaldehyde (meaning the product of step a) 2 64 mm 〇 1) 151284.doc • 101 . 201117722 After 1 hour, water (25 mL) was added to the reaction mixture to give diethyl ether (50 m) L) extracting the aqueous mixture, drying it by sulphuric acid, hydrating, and concentrating under reduced pressure. The obtained material is purified by medium pressure liquid chromatography on a gel (the solution is acetic acid in hexane). Ethyl ester, gradient (0 to 30%) to give the title compound (0.156 g) as a solid. NMR (CDC13) δ 7.26-7.25 (m, 2H), 7.07 (t, J = 7.5 Hz, 2H ), 6.42 (s, 1H), 6.39 (s, 1H), 4.54 (d, J = 3 Hz, 2H), 4.13 (t, J = 6 Hz, 1H), 3.77 (s, 3H). Example 16 Preparation 4·Ga-5-(2,6-difluoro-4-methoxyphenyl)-2-(fluoromethyl)-1-(4-fluorophenyl)-1Η-imidazole (compound 221) 4-Ga-5-(2,6-difluoro-4-indolyloxyphenyl)-1-(4-fluorophenyl)-1indole-imidazole-2-indole in dichloromethane (2 mL) To the mixture of the product of Example 15 was added diethylaminophosphonium trifluoride (60 pL, 0.45 mmol). After 2 hours, the reaction mixture was diluted with water and extracted with dioxane (100 mL). Drying, filtering and concentrating under reduced pressure. The obtained material was purified by medium pressure liquid chromatography on a gel (the solution was ethyl acetate in hexane, The title compound (0.031 g) was obtained as a white solid. ]H NMR (CDC13) δ 7.25-7.23 (m, 2Η), 7.08 (t, J = 6 Hz, 2H), 6.43 (s, 1H), 6.41 (s, 1H), 5.25 (s, 1H), 5.13 (s, 1H), 3.78 (s, 3H). Example 17 151284.doc •102- 201117722 Preparation of 4-Molyl-2-(derivative)-1-(4-chlorophenyl)-5-(2,6-diphenyl)ih_imidazole (Compound 326 a 4-bromo-(I-chlorophenyl)-5-(2,6-difluorophenyl)_2-indenyl-111-imidazole in four gasified carbon (8 mL) (ie The product of Example 5) (1.00 g, 2.6 mmol), N-bromopyrmine (0 510 g, 2.87 mmol) and 2,2'-azobis(2-isobutyl) (0.021 g, 13 〇mmol), which was heated overnight at reflux temperature. The reaction mixture was concentrated under reduced pressure and the resulting material was purified by medium pressure liquid chromatography on a hydrazine gel (the lysate was ethyl acetate in hexane with a gradient of 〇 to 100%) to form The title compound (0.94 〇g) was obtained as a solid. !H NMR (CDC13) δ 7.35 (m, 3H), 7.24 (m, 2H), 6.87 (m, 2H), 4.36 (s, 2H). Example 18 Preparation of 3-[2-di-4-ox-1-(4-chlorophenyl)-1Η-flavor-5-yl]-2,4-di-benzonitrile (Compound 283) Step A: Preparation of 3-[4-Ga-1-(4-chlorophenyl)_1H-imidazole_5_ kib 2,4-difluorobenzonitrile A 5-(in 2-decyl acetamide (3 mL) 3-bromo-2,6-diphenyl)-4- ox-1-(4-phenylphenyl)-1 oxime-methanol (prepared by a procedure similar to that of Example 8, Steps A and B) (0.440) g, 0.490 mmol ), zinc cyanide (0.058 g' 0.490 mmol), diox [1,1,_bis(diphenylphosphino)ferrocene]palladium(II):dichloromethane complex (1:1 (0.044 g, 0.0545 mmol) and a mixture of N,N,N',N', tetradecylethylenediamine (0.022 g, 0.22 mmol), using Biotage Initiator TI&quot;wave device 151284.doc -103- 201117722 Heat at 200 for 5 minutes. The reaction mixture was concentrated under reduced pressure, and the obtained material was purified by medium-pressure liquid chromatography on a sand gel (the eluent was ethyl acetate in hexane, and the gradient was 〇 to 1 〇〇%) The title compound (0.217 g) was obtained as a solid. !H NMR (CDC13) δ 7.72 (s, 1H), 7.69 (m, 1H), 7.38 (m, 2H), 7.07 (m, 3H) ° 'Step B: Preparation of 3-[2-bromo-4- gas 1-(4-Phenylphenyl)-m-imidyl-5-yl]-2,4-dibenzobenzonitrile 3-[4-Ga-1&lt;&lt;&gt;&gt;; 4_gas phenyl)-1Η-imidapy-5-yl]-2,4-difluorobenzonitrile (meaning the product of step β) (0.217 g '0.62 mmol) and guanidine-bromoammonium imine A mixture of (〇 165 g, 0.930 mmol) was heated at 603⁄4 overnight. More N-bromosuccinimide (0.386 g, 2.17 mmol) was added portionwise to the reaction mixture and heated again overnight at 60 °C. The reaction mixture was diluted with EtOAc (EtOAc)EtOAc. The obtained material was purified by medium pressure liquid chromatography on a hydrazine gel (ethyl acetate in hexanes, hexanes to 100%) to give the title compound as a solid (0.196 g). («1, towel NMR (CDC13) δ 7.67 (m, 1H), 7.40 (m, 2H), 7.13 2H), 7.03 (m, 1H). Example 19 Preparation of 3-[4-chloro-l-(4. p-phenyl)-2-methyl-1H-imidazol-5-yl]-2,4-dion &amp; a &quot; Regulations 151284. Doc -104- 201117722 carbonitrile (compound 292) 3-[2-bromo-4-chloro-1-(4-chlorophenyl) in dioxane (4 mL) and water (2 drops) -1Η-β-salt-5-yl]-2,4-difluorobenzonitrile (meaning the product of Example 18) (0.150 g, 0.350 mmol), tridecyl epoxy shed (0.088 g, 0.700 mmol) A mixture of cesium carbonate (0.342 g, 1.05 mmol) and dichlorobis(triphenylphosphine)palladium (0.025 g, 0.035 mmol) was heated at reflux for a further 3 hours. The reaction mixture was concentrated under reduced pressure, and the obtained material was purified by medium pressure liquid chromatography on a silica gel (the eluent was ethyl acetate in hexane, the gradient was 0 to 100%). The title compound (0.088 g) was obtained as a solid. </ RTI> NMR (CDC13) δ 7.65 (m, 1 Η), 7.39 (m, 2H), 7.09 (m, 2H), 7.01 (m, 1H), 2.32 (s , 3H). Example 20 Preparation of 4-[4-Ga-2-methyl-1-(4-methylphenyl)-1Η-imidazole-5-yl]-3,5-difluorophenol (Compound 437) A dichloride 4-Ga-5-(2,6-difluoro-4-methoxyphenyl)-2-methyl-1-(4-methylphenyl)-1Η-imidazole in decane (10 mL) The mixture was prepared by a procedure similar to that of Example 9 (0.500 g, 1.43 mmol), and boron tribromide (1 Μ in dichloromethane, 4.3 mL, 4.3 mmol) was added at -78 °C. The reaction mixture was warmed to room temperature and stirred overnight. More boron tribromide (1 Torr in dioxane, 1.4 mL, 1.40 mmol) was added to the reaction mixture at room temperature and stirring was continued for 4 hours. Hydrochloric acid (1 N, 8.0 mL), I5I 284.doc .105 - 201117722 was added to the reaction mixture and then a saturated aqueous solution of sodium carbonate was added to afford the aqueous mixture. The aqueous mixture was extracted with ethyl acetate and the extract was dried over EtOAc, filtered and concentrated under reduced pressure. The resulting material was purified by medium pressure liquid chromatography on a gel (the ethyl acetate in the eluent was 0 to 1%) to form the title compound. (0.41 g). !H NMR (CDC13) δ 10.68 (S, lH), 7.24 (d, 2H), 7 〇9 2H), 6.43 (m, 2H), 2.31 (s, 3H), 2.18 (s, 3H). ( 'Example 21 Preparation 3-[4·[4-Chloro-2-indolyl-1-(4-methylphenyl)_1H-imidazol-5yl]·3,5·difluorophenoxy]-Ν -Methyl-1-propanamide hydrochloride (Compound 5〇3) Step Α: Preparation of phenylhydrazinium-[3-[4_[4-Ga-2-methyl·ΐ_(4-methylphenyl) )-1Η-imidazole-5-yl]-3,5-difluorophenoxy]propyl]-anthracene-carbamic acid methyl ester 4 in Ν, Ν-dimercaptodecylamine (3 mL) -[4-Chloro-2-mercapto-1-(4-methylphenyl)_1H-imidazole_5-yl]_3,5-difluorophenol (meaning the product of Example 20) (〇.2〇〇) a mixture of g '0598mm〇1) and 4 into a molecular sieve (1.55 g), which was stirred at room temperature for 3 hours, and then added with a benzyl N-(3_ in N,N-didecylguanamine (! Gas propyl)-N-carbamic acid oxime ester (prepared by the method described in pCT Publication No. 2007/149448) (0.434 g, 1.80 mmo1) and tetrabutylammonium iodide (0.044 g, 0.120 mmol) Solution. After 15 minutes, add the carbonic acid planer to the reaction mixture (0.584 g, 1·80 mmolh for 15 minutes, then heat the reaction mixture at 75 乞2 151284.doc •106-201117722 hours. Filter the reaction The filtrate is concentrated under reduced pressure. The obtained material is purified by medium pressure liquid chromatography on a hydrazine gel (the solvent is ethyl acetate in hexane, and the gradient is 〇1) 〇〇%) to form the title compound (21 〇mg) as a solid. ESIMS m/z 541 (M+1) 〇Step B: Preparation of 3_[4-丨4-Ga-2-methyl_ι_(4 -Methylphenyl)-1Η-味-5-yl]-3,5-difluorophenoxy]_N_methylpropionamine hydrochloride benzoquinone N-[3-[4-[ 4-gas_2_mercapto-1-(4-methylphenyl)-1Η-imidazol-5-yl]_3,5-difluoro phenyloxy]propyl]_N_amino decanoic acid vinegar That is, the product of step A) (〇197 g, 〇365 mm〇i), a mixture of hydrogen acid (2M in 1 ethyl ether in ether) and decyl alcohol (30 mL) was flushed with nitrogen for 30 minutes, then added to the Break (1〇0/〇, 0.058 g, 0.055 mmol) and continue to maintain nitrogen purge for 15 minutes. After 1 min, 'stop nitrogen flushing and connect the hydrogen-filled balloon to the reaction flask and stir the reaction mixture for 3 hours at room temperature. The reaction mixture was flushed with nitrogen and passed through a sand bed on a glass funnel and Celite® (矽The diatom filter aid was used to filter off the palladium on carbon catalyst. The title compound (〇. 1 g) was obtained as a crude solid. H NMR (DMSO-d6) δ 8.90 (br s, 2H), 7.25 (d, 2H), 7.11 (d, 2H), 6.76 (d, 2H), 4.08 (t, 2H), 2.98 (m, 2H) ), 2.54 (m, 3H), 2.31 (s, 3H), 2.19 (s, 3H), 2.04 (d, 2H) 〇 Example 22 -107- 151284.doc 201117722 Preparation 5-[2-Bromo-4-gas -5-(2,6-Difluoro-4-methoxyphenyl)_1H-imidazol-1-yl]-2-(trifluoromethyl)pyridine (Compound 481) Step A: Preparation of N-[(2, 6-(Difluoro-4-methoxyphenyl)methylene]-6-(trifluoromethyl)-3_indole amine 6-(trifluoromethyl) in toluene (100 mL) A mixture of 3-pyridylamine (5.00 g, 30.8 mmol) and 2,6-difluoro-4-methoxybenzoic acid (5.30 g '30.8 mmol) was heated to reflux for 2.5 days. The reaction mixture was cooled to room temperature and concentrated under reduced pressure to afford title compound (9.9 g). iH NMR (CDC13) δ 8.56 (s, 1H), 8.52 (d, 1H), 7.71 (d, 1H), 7.60 (m, 1H), 6.57 (m, 2H), 3.88 (s, 3H). Step B: Preparation of 5-[5-(2,6-difluoro-4-methoxyphenyl)·1Ηimidazol-1-yl]-2-(trifluoromethyl)"» than a bite in dioxane Ν·[(2,6·Difluoromethoxyphenyl)methylene]·6_(trifluoropyridiniumamine) in ethane (20 mL) and decyl alcohol (20 mL) a mixture of 1-[(1-isocyanoethyl) hydrazino]-4-mercaptobenzene (4.6 g, 24 mmol) and carbonic acid (4.4 g, 32 mmol) at 75 ° C The mixture was heated overnight. The reaction mixture was concentrated under reduced pressure and the obtained material was purified by medium-pressure liquid chromatography on hydrazine gel (the solvent was ethyl acetate in hexane, gradient from 0 to 100%) To form the title compound (4 63 g) as a solid.]H NMR (CDC13) δ 8.59 (m, 1 Η), 7.86 (s, 1H), 7.71 (m, 2H), 7.33 (m, 1H), 6.46 (m, 2H), 3.80 (s, 3H) 〇 151284.doc -108- 201117722 Step C: Preparation of 5-[4-chloro-5-(2,6-difluoro_4-methoxyphenyl)_111_imidazole -1-yl]-2-(trifluoromethyl)anthracene 5-[5_(2,6-difluoro-'nonyloxyphenyl)-1Η-imidazole in four gasified carbon (8 mL) -l_yl] 2-(trifluoromethyl)pyridine (meaning the product of step B) (1.50 g, 4. 20 mmol)), a mixture of Ν-gas amber yttrium (〇56 g '(2 mm〇l) and 2,2,· even i bis (2·isobutan) (〇〇38 g, 〇23, This was heated for 3.5 days at 65 ° C. The reaction mixture was diluted with aq. EtOAc EtOAc (EtOAc m. The material was purified by medium pressure liquid chromatography on a hydrazine gel (the lysate was ethyl acetate in hexane with a gradient of 〇 to 1%) to give the title compound as a solid. 65〇g) Ή NMR (CDC13) δ 8.59 (m, 1Η), 7.73 (m, 3H), 6.49 (m, 2H), 3.82 (s, 3H). 'Step D ·Preparation 5-[2- 4- gas-5-(2,6-difluoro-4-indolylphenyl)-1Η-imidazol-1-yl]-2-(trifluoromethyl)acridine is a kind in Ν,Ν·曱5-[4-chloro-5-(2,6-fluoro-4-methoxyphenyl)-1Η-β-miso_ι_yl]_2_(trifluoroanthracene) in guanamine (10 niL) A mixture of 0.650 g, and N-bromopterin (0.356 g, 2.0 mmol) was heated at 65 ° C overnight. More N-bromosuccinimide (0.195 g, 1.1 mm 〇l) was added to the reaction mixture, and the mixture was heated at &lt;0&gt;C for 2.5 days. The reaction mixture was diluted with a saturated sodium carbonate solution and extracted with di-methane. The combined organic layers were dried over MgSO4, filtered and evaporated. The resulting material was purified by medium pressure liquid chromatography on a hydrazine gel (the lysate was ethyl acetate in hexane, gradient from 0 to 100%) to give the title compound as a solid (0.108) g). lU NMR (CDC13) δ 8.58 (s, 1H), 7.78 (m, 2H), 6.43 (m, 2H), 3.79 (s, 3H). Example 23 Preparation of 5-[4-Ga-5-(2,6-difluoro-4-indolyloxyphenyl)-2-methyl-1H-imidazol-1-yl]-2-(trifluoromethyl) Pyridine (compound 487) 5-[2-bromo-4-chloro-5-(2,6-difluoro-4-methoxybenzene) in dioxane (3 mL) and water (1 drop) Base)-1Η-imidazole-1·yl]-2-(trifluoromethyl)pyridine (meaning the product of Example 22) (0.093 g, 0.20 mmol), tridecyl epoxide (0.025 g, 0.20 mmol) A mixture of carbonic acid planing (0.195 g, 0.60 mmol) and dioxobis(triphenylphosphine)palladium (0.014 g, 0.20 mmol) was heated to reflux overnight. The reaction mixture was then concentrated under reduced pressure, and the obtained material was purified by medium pressure liquid chromatography on a hydrazine gel (the solvent was ethyl acetate in hexane, gradient from 0 to 100%). The title compound (0.021 g) was obtained as a solid. H NMR (CDCI3) δ 8.55 (s, 1H), 7.75 (m, 1H), 7.69 (m, 1H), 6.42 (m, 2H), 3.78 (s, 3H), 2.35 (s, 3H). Example 24 Preparation of 2-Ga-5-[2-Ga-1-(2,6-difluoro-4-methoxyphenyl)-4-mercapto-1H-imidazole 151284.doc -110- 201117722 -5- Base Ipyridine (Compound 475) Step A: Preparation of N-[(6-Gas-3·«pyridyl)methylene b 2,6-dioxa-4-methoxyaniline 6-Ga-3- ° Add a mixture of 2,6-difluoro-4-nonyloxyaniline (〇.98〇&amp; 5 6.9 mmol) in toluene (20〇11〇) in a mixture of phthalic acid (1.0 g, 6.3 mmol). The anti-deer mixture was heated to reflux using a Dean-Stark separator to azeotropically remove water. After 16 hours, the # reaction mixture was cooled to room temperature and concentrated under reduced pressure. Dry overnight at 55 ° C to give the title compound (1. 6 g) as a pale brown solid (yield: </ RTI> </ RTI> </ RTI> </ RTI> NMR (CDCI3) δ 8.74 (s, 1 Η), 8.73 (d, J = 2.44 Hz, 1H) 8.32 (dd, J = 2.20 Hz, J = 8.29 Hz, 1H), 7.44 (d, J = 8 29 Hz, 1H), 6.59-6.52 (m, 2H), 3.82 (s, 3H). 19F NMR (CDC13 δ -121.48 to -121.40 (m, 2F). Step B: Preparation of 2-gas-5-[l-(2,6-difluoro-4-methoxyphenyl)-4-methyl-1H-imidazole- 5-phenyl]pyridine Cyanide 0.35 g, 6.5 mmol) and potassium butoxide (0.86 g '7.7 mmol) were added to a N-[(6-gas-3"pyridyl) subunit in tetrahydrogenate (15 mL). A mixture of fluorenyl-2,6-difluoro_4_methoxyaniline (meaning the product of Step A) (1.66 g, 5.9 mmol). The reaction mixture was heated at 85 &lt;0&gt;C for 4 h, cooled and concentrated. The resulting material was diluted with ethyl acetate and washed with a saturated aqueous solution of sodium chloride. The organic layer was dried over magnesium sulfate, dried and concentrated. The obtained material was purified by medium pressure liquid chromatography on a hydrazine gel 151284.doc 201117722 (/the eluate was ethyl acetate in hexane), and then ground with normalized butane hexane to obtain brown The title compound is obtained as a brown solid (m.p. NMR (CDC13) δ 8.16d5 J = 2.44 Hz, 1H), 7.55 (s, 1H), 7.44 (dd, J = 2.68 and 8.29 Hz, 1H), 7.28 (dd, J = 0.49 and 8.29 Hz, 1H), 6.54-6.48 (m, 2H), 3.81 (s, 3H), 2.33 (s, 3H). F NMR (CDC13) δ -118.21 to] 18 15 (m, 2F). Step by step c·Preparation of 2-gas-5-[2-gas·ι_(2,6-difluoro-4-methoxyphenyl)·4_methyl-1Η-microsodium _5_yl] 2-nitro-5-[l-(2,6-difluoro-4-indolyloxyphenyl)methyl-1H-imidazole in hydrazine, hydrazine-dihydrazinamide (2 〇mL) _5_基基pyridine (meaning the product of step B) (〇.15()g, G 45inm〇1) was added N-gas amber quinone imine (〇.〇66 g, 〇49 mm〇1) And the reaction mixture was heated at 6 ° C. After 3 minutes, the reaction mixture was cooled to room temperature to be diluted with ethyl acetate (4 mL) and taken with water and saturated aqueous sodium chloride. _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ Grayish hNMiuax^jf title compound (4) heart) 8.29 Hz, J = 2.44 = 2 20 HZ&gt; ^ 7 43 ^ ^ (^Ι = 9.02Ηζ, 2Η), 3?, 7, 26 (Μ = 8·54ΗΖ ?1Η)ϊ6·53),3·82 (s,3H), 2.28 (s,3H). 151284.doc •112· 201117722 Example 25

製備4-[4-氯-5-(2,6-二氟-4-甲氧苯基)-2-甲基-1H-咪唑-1-基I 苯硫氰酸鹽（化合物510) 一種在N，N-二曱基曱醯胺（5 mL)中的4-氯-1-(4-峨苯基)-5-(2,6-二氟-4-甲氧苯基)-2-曱基-1H-咪唑（藉由 類似於實例9之步驟製備）（〇·2 g，0.43 mmol)、硫氰 化銅(I) (0.08 g，0.65 mmol)以及硫氰酸卸（0.06 g， 〇·65 mmol)的混合物，將其隔夜加熱至14〇°c。將該反 應混合物冷卻至室溫，然後進一步以水及醋酸乙酯分配 成為有機層和水層’並以醋酸乙酯萃取水層。藉由硫酸 鎂乾燥合併之有機層、過濾並在減壓下濃縮。將結果得 到的物質藉由矽凝膠上的中壓液相層析純化（溶析液為 己烧中的醋酸乙酯’其梯度為2〇:8〇、60:40至80:20) 以形成呈固體狀的標題化合物（〇 〇7 g)。 H NMR (CDC13) δ 7.53 (d, 2Η), 7.22 (d, 2H), 6.40 (d, 2H)，3.78 (s，3H), 2.31 (s，3H)。 實例26 製備2·【4-[4-氣小(3-氣苯基)-2-甲基_1H-咪心5_基】_3,5_二 氟苯氧基]乙腈（化合物512) 種在N，N-一曱基甲醯胺（4 mL)中的4-[4-氣 -H3-氟苯基)-2-甲基-1H-咪唑-5_基]_3 5_二氟苯酚（從 4备5-(2,6-二氟-4-甲氧苯基)小(3_氟苯基)_2_甲基·1H_ 咪唾（意即實例9之產物）藉由類似於實例2〇的步驟 製備；〇.30g，8.9 mmol)、漠乙猜（〇13g，Umm〇i) 151284.doc •113. 201117722 以及碳酸鉀的混合物，將其在40¾攪拌2小時。然後 在減壓下濃縮該反應混合物，並以矽凝膠上的中壓液相 層析進行純化（溶析液為己烷中的醋酸乙酯，其梯度為 0到100%)，以形成呈固體狀之標題化合物（〇28g)， 即本發明之化合物。 H NMR (CDC13) δ 7.37 (m，1H)，7.11 (m，1H)，6.91 (m， 2H)，6.52 (m，2H)，4.76 (s，2H)，2.31 (s，3H)。 藉由本文中所述製程以及該領域中習知方法，可製 備出下面表1到表62D的化合物。下述為表中所使用的 簡稱，其如下MVie表示甲基，Et表示乙基，Ph表示笨 基’ MeO表示曱氧基，MeS是曱硫基，CN表示氰基， Bn表示苯曱基以及n〇2表示硝基。 表1 R1Preparation of 4-[4-chloro-5-(2,6-difluoro-4-methoxyphenyl)-2-methyl-1H-imidazol-1-yl Iphenylthiocyanate (Compound 510) 4-Chloro-1-(4-indolyl)-5-(2,6-difluoro-4-methoxyphenyl)-2- in N,N-dimercaptoamine (5 mL) Mercapto-1H-imidazole (prepared by a procedure similar to that of Example 9) (〇·2 g, 0.43 mmol), copper (I) thiocyanate (0.08 g, 0.65 mmol), and thiocyanate (0.06 g, Mix a mixture of 〇·65 mmol) and heat it to 14 °C overnight. The reaction mixture was cooled to room temperature, and then further partitioned into an organic layer and a water layer with water and ethyl acetate, and the aqueous layer was extracted with ethyl acetate. The combined organic layers were dried over magnesium sulfate, filtered and evaporated. The resulting material was purified by medium pressure liquid chromatography on a gel (the solution was ethyl acetate in hexane) with a gradient of 2〇:8〇, 60:40 to 80:20) The title compound (〇〇7 g) was obtained as a solid. H NMR (CDC13) δ 7.53 (d, 2 Η), 7.22 (d, 2H), 6.40 (d, 2H), 3.78 (s, 3H), 2.31 (s, 3H). Example 26 Preparation 2·[4-[4-Gas(3-Phenylphenyl)-2-methyl_1H-mole 5_yl]_3,5-difluorophenoxy]acetonitrile (Compound 512) 4-[4-Gas-H3-fluorophenyl)-2-methyl-1H-imidazol-5-yl]_3 5-difluorophenol in N,N-monodecylcarbamide (4 mL) (from 4, 5-(6,6-difluoro-4-methoxyphenyl) small (3_fluorophenyl)_2-methyl·1H_, which is the product of Example 9, by analogy with an example 2〇Step Preparation; 〇.30g, 8.9 mmol), Molybdenum (〇13g, Umm〇i) 151284.doc •113. 201117722 and a mixture of potassium carbonate, which was stirred at 403⁄4 for 2 hours. The reaction mixture is then concentrated under reduced pressure and purified by medium pressure liquid chromatography on a hydrazine gel (the eluent is ethyl acetate in hexane, gradient from 0 to 100%) to form The title compound (〇28g) as a solid, is a compound of the invention. H NMR (CDC13) δ 7.37 (m, 1H), 7.11 (m, 1H), 6.91 (m, 2H), 6.52 (m, 2H), 4.76 (s, 2H), 2.31 (s, 3H). The compounds of Tables 1 to 62D below can be prepared by the processes described herein and by conventional methods in the art. The following are the abbreviations used in the table, wherein MVie represents a methyl group, Et represents an ethyl group, Ph represents a stylyl group; MeO represents a decyloxy group, MeS is a thiol group, CN represents a cyano group, and Bn represents a phenyl fluorenyl group and N 〇 2 represents a nitro group. Table 1 R1

Q2是4-Cl-Ph ’ R丨是C1以及R2是MeQ2 is 4-Cl-Ph ’ R丨 is C1 and R2 is Me

(R3) m (R3) m (R3) m (R3) m (R3) m 2,6·二· 2,4-二-Cl 4-CN，2,6-二 -F 2-CF3, 4-F v / m 2-Cl, 4-N〇2 2,4,6-三-F 2-C1，4,6-二 -F 2,6-二-F， 4-Me 2-CF2HO, 4-F 2-N〇2, 4-F 2,3,6-三·ρ 2-C1, 6-F 2-Cl, 5-CF3 2-CN, 6-F 2,5-二-Cl， 2,4,5-三-f 2-Br, 6-F 2-C1，4-Me 2,5-二-Cl 4-F 2,3-二-Cl， 4-F 151284.doc •114· 201117722 q2 ’R4;)cl，Ph，R丨是 Cl 以及 R2 是 m 2,3,4-三-p(R3) m (R3) m (R3) m (R3) m (R3) m 2,6·2·2,4-di-Cl 4-CN,2,6-di-F 2-CF3, 4- F v / m 2-Cl, 4-N〇2 2,4,6-tri-F 2-C1,4,6-di-F 2,6-di-F, 4-Me 2-CF2HO, 4- F 2-N〇2, 4-F 2,3,6-tris ρ 2-C1, 6-F 2-Cl, 5-CF3 2-CN, 6-F 2,5-di-Cl, 2, 4,5-tri-f 2-Br, 6-F 2-C1,4-Me 2,5-di-Cl 4-F 2,3-di-Cl, 4-F 151284.doc •114· 201117722 q2 'R4;) cl, Ph, R丨 is Cl and R2 is m 2,3,4-tri-p

2-C1, 4-F2-C1, 4-F

2-Br, 4-F 2,4-二-p 2.6- 二-ci 2.6- 二-p，2-Br, 4-F 2,4-di-p 2.6-di-ci 2.6-di-p,

4-EtO4-EtO

2-C1，3,6-二 -F (R3) 2-F, 6-CF3 2-F, 6-CHF2〇2-C1,3,6-di-F (R3) 2-F, 6-CF3 2-F, 6-CHF2〇

2-1，4-F2-1,4-F

4-C1，2,6-二 -F 2,6-二-F， 4-MeO 2-C1, 6-F, 4- MeO 2-C1, 6-F,4-C1,2,6-di-F 2,6-di-F, 4-MeO 2-C1, 6-F, 4-MeO 2-C1, 6-F,

5- MeO5- MeO

MeMe

(R3) 2-C1, 4-MeO 2-Br, 4-MeO 2.6- 二-F, 3-C1(R3) 2-C1, 4-MeO 2-Br, 4-MeO 2.6- Di-F, 3-C1

2.6- 二-F， 3-CN2.6- two-F, 3-CN

2.6- 二-F， 3-MeO 2.6- 二-F，2.6- two-F, 3-MeO 2.6-di-F,

4-CF2HO4-CF2HO

2.6- 二-F， 3-CFzHO (R3) 2-CF3, 4-MeO 2-F, 6-Me 2.6- 二-F， 3- Me 2-CF32.6- Di-F, 3-CFzHO (R3) 2-CF3, 4-MeO 2-F, 6-Me 2.6- Di-F, 3-Me 2-CF3

2- CF3O 2.6- 二-F， 4- NO2 2.6- 二-F，2- CF3O 2.6- di-F, 4- NO2 2.6- di-F,

3- EtO (R3)3- EtO (R3)

2-C1，5-CN 2,4-二-F, 5-CN 2- C1, 6-F, 3-MeO 2.6- 二-F, 3- NCCH2O 2.6- 二-F, 4- NCCH2O 本發明揭露的内容亦包括表1A到715A，其每一表 格建立方式與上述表1相同，除了表1開頭的列（即「Q2 是4-Cl-Ph、R1是ci以及R2是Me」）以下述各別的列 開頭所取代。例如，在表1A列開頭是「Q2是4-Cl-Ph， Rl是Br以及r2是Me」，以及（R3) m係在上述表1中 經定義°因此’表1A中的第一表值具體地揭露4-溴基 -H4-氯苯基)-5-(2,6-二氟苯基)-iH-咪唾。表2A到715A 以相似的方式建立。 表 列標題 1A Q疋4-Cl-Ph ’ R丨是Br以及R2是Me。 2A Q2 是 4-Cl-Ph ’ R丨是 Cl 以及 R2 是 CFH2。 3A Q 是 4-Cl-Ph，Ri 是 j 以及 R2 是 Me。 4A Q2是4-Cl-Ph ’ R丨是Me以及R2是Me。 5A Q2是4-Cl-Ph ’ R丨是Me以及R2是C1。 6A Q2是4-Cl-Ph ’ R丨是Me以及R2是Br。 7A Q2是4-Cl-Ph，R丨是Me以及R2是J。 8A Q2 是 4-Cl-Ph，R1 是 Me 以及 R2 是 MeO。 I51284.doc -115- 201117722 表 列標題 9A Q2 是 4-Cl-Ph，R1 是 MeO 以及 R2 是 Me。 10A Q2 是 4-Cl-Ph，R1 是 Br 以及 R2 是 Br。 11A Q2 是 4-Cl-Ph，R1 是 Br 以及 R2 是 Cl。 12A Q2 是 4-Cl-Ph，R1 是 Cl 以及 R2 是 Br。 13A Q2 是 4-Cl-Ph，R1 是 Cl 以及 R2 是 Cl。 14A Q2 是 4-Cl-Ph，R1 是 Me 以及 R2 是 MeS。 15A Q2 是 4-Cl-Ph，R1 是 MeS 以及 R2 是 Me。 16A Q2 是 4-Cl-Ph，R1 是 Et 以及 R2 是 Br。 17A Q2 是 4-Cl-Ph，R1 是 Et 以及 R2 是 CM。 18A Q2 是 4-Cl-Ph，R1 是 Et 以及 R2 是 Me。 19A Q2 是 4-Cl-Ph，R1 是 Me 以及 R2 是 Et。 20A Q2 是 4-Cl-Ph，R1 是 Cl 以及 R2 是 Et。 21A Q2 是 4-Cl-Ph，R1 是 Me 以及 R2 是 CN。 22A Q2 是 3-Cl-Ph，R1 是 Cl 以及 R2 是 Me。 23A Q2 是 3-Cl-Ph，R1 是 Cl 以及 R2 是 CFH2。 24A Q2 是 3-Cl-Ph，R1 是 Br 以及 R2 是 Me。 25A Q2 是 3-Cl-Ph，R1 是 I 以及 R2 是 Me。 26A Q2 是 3-Cl-Ph，R1 是 Me 以及 R2 是 Me。 27A Q2 是 3-Cl-Ph，R1 是 Me 以及 R2 是 Cl。 28A Q2 是 3-Cl-Ph，R1 是 Me 以及 R2 是 Br。 29A Q2 是 3-Cl-Ph，R1 是 Me 以及 R2 是 I。 30A Q2 是 3-Cl-Ph，R1 是 Br 以及 R2 是 Br。 31A Q2 是 3-Cl-Ph，R1 是 Br 以及 R2 是 a。 .32A Q2 是 3-Cl-Ph，R1 是 Cl 以及 R2 是 Br。 33A Q2 是 3-Cl-Ph，R1 是 Cl 以及 R2 是 Cl。 34A Q2 是 4-F-Ph，R1 是 Cl 以及 R2 是 Me。 35A Q2 是 4-F-Ph，R1 是 Cl 以及 R2 是 CFH2。 36A Q2 是 4-F-Ph，R1 是 Br 以及 R2 是 Me。 37A Q2 是 4-F-Ph，R1 是 I 以及 R2 是 Me。 38A Q2 是 4-F-Ph，R1 是 Me 以及 R2 是 Me。 39A Q2是4-F-Ph，R1是Me以及R2是C卜 40A Q2 是 4-F-Ph，R1 是 Me 以及 R2 是 Br。 41A Q2 是 4-F-Ph，R1 是 Me 以及 R2 是 I。 42A Q2 是 4-F-Ph，R1 是 Br 以及 R2 是 Br。 43A Q2 是 4-F-Ph，R1 是 Br 以及 R2 是 Cl。 151284.doc -116- 201117722 表 列標題 44A Q2 是 4-F-Ph，R1 是 Cl 以及 R2 是 Br。 45A Q2 是 4-F-Ph，R1 是 Cl 以及 R2 是 Cl。 46A Q2 是 3-F-Ph，R1 是 Cl 以及 R2 是 Me。 47A Q2 是 3-F-Ph，R1 是 Cl 以及 R2 是 CFH2。 48A Q2 是 3-F-Ph，R1 是 Br 以及 R2 是 Me。 49A Q2 是 3-F-Ph，R1 是 I 以及 R2 是 Me。 50A Q2 是 3-F-Ph，R1 是 Me 以及 R2 是 Me。 51A Q2 是 3-F-Ph，R1 是 Me 以及 R2 是 Cb 52A Q2 是 3-F-Ph，R1 是 Me 以及 R2 是 Br。 53A Q2 是 3-F-Ph，R1 是 Me 以及 R2 是 I。 54A Q2 是 3-F-Ph，R1 是 Br 以及 R2 是 Br。 55A Q2 是 3-F-Ph，R1 是 Br 以及 R2 是 Cl。 56A Q2 是 3-F-Ph，R1 是 Cl 以及 R2 是 Br。 57A Q2 是 3-F-Ph，R1 是 Cl 以及 R2 是 Cl。 58A Q2 是 3-CF2HO-Ph，Ri 是 Cl 以及 R2 是 Me。 59A Q2 是 3-CF2HO-Ph，R1 是 Cl 以及 R2 是 CFH2 · 60A Q2 是 3-CF2HO-Ph，R1 是 Br 以及 R2 是 Me。 61A Q2 是 3-CF2HO-Ph，R1 是 I 以及 R2 是 Me。 62A Q2 是 3-CF2HO-Ph，R1 是 Me 以及 R2 是 Me。 63A Q2 是 3-CF2HO-Ph，R1 是 Me 以及 R2 是 Cl。 64A Q2 是 3-CF2HO-Ph，R1 是 Me 以及 R2 是 Br。 65A Q2 是 3-CF2HO-Ph，R1 是 Me 以及 R2 是 I。 66A Q2 是 3-CF2HO-Ph，R1 是 Br 以及 R2 是 Br。 67A Q2 是 3-CF2HO-Ph，R1 是 Br 以及 R2 是 Cl。 68A Q2 是 3-CF2HO-Ph，R1 是 Cl 以及 R2 是 Br。 69A Q2 是 3-CF2HO-Ph，R1 是 Cl 以及 R2 是 Cl。 70A Q2 是 4-Me-Ph，R1 是 Cl 以及 R2 是 Me。 71A Q2 是 4-Me-Ph，R1 是 Cl 以及 R2 是 CFH2。 72A Q2 是 4-Me-Ph，R1 是 Br 以及 R2 是 Me。 73A Q2 是 4-Me-Ph，R1 是 I 以及 R2 是 Me。 74A Q2 是 4-Me-Ph，R1 是 Me 以及 R2 是 Me。 75A Q2 是 4-Me-Ph，R1 是 Me 以及 R2 是 a。 76A Q2 是 4-Me-Ph，R1 是 Me 以及 R2 是 Br。 77A Q2 是 4-Me-Ph，R1 是 Me 以及 R2 是 I。 78A Q2 是 4-Me-Ph，R1 是 Br 以及 R2 是 Br。 151284.doc · 117· 201117722 表 列標題 79A Q2 是 4-Me-Ph，R1 是 Br 以及 R2 是 Cl。 80A Q2 是 4-Me-Ph，R1 是 Cl 以及 R2 是 Br。 81A Q2 是 4-Me-Ph，R1 是 Cl 以及 R2 是 α。 82A Q2 是 3-Me-Ph，R1 是 Cl 以及 R2 是 Me。 83A Q2 是 3-Me-Ph，R1 是 Cl 以及 R2 是 CFH2。 84A Q2是3-Me-Ph，R丨是Br以及R2是Me。 85A Q2 是 3-Me-Ph，R1 是 I 以及 R2 是 Me。 86A Q2 是 3-Me-Ph，R1 是 Me 以及 R2 是 Me。 87A Q2 是 3-Me-Ph，R1 是 Me 以及 R2 是 a。 88A Q2 是 3-Me-Ph，R1 是 Me 以及 R2 是 Br。 89A Q2 是 3-Me-Ph，R1 是 Me 以及 R2 是 I。 90A Q2 是 3-Me-Ph，R1 是 Br 以及 R2 是 Br。 91A Q2 是 3-Me-Ph，R1 是 Br 以及 R2 是 Cl。 92A Q2 是 3-Me-Ph，R1 是 Cl 以及 R2 是 Br。 93A Q2 是 3-Me-Ph，R1 是 Cl 以及 R2 是 a。 94A Q2 是 4-Et-Ph，R1 是 Cl 以及 R2 是 Me。 95A Q2 是 4-Et-Ph，R1 是 Cl 以及 R2 是 CFH2。 96A Q2 是 4-Et-Ph，R1 是 Br 以及 R2 是 Me。 97A Q2 是 4-Et-Ph，R1 是 I 以及 R2 是 Me。 98A Q2 是 4-Et-Ph，R1 是 Me 以及 R2 是 Me。 99A Q2 是 4-Et-Ph，R1 是 Me 以及 R2 是 Cl。 100 A Q2 是 4-Et-Ph，R1 是 Me 以及 R2 是 Br。 101A Q2 是 4-Et-Ph，R1 是 Me 以及 R2 是 I。 102 A Q2 是 4-Et-Ph，R1 是 Br 以及 R2 是 Br。 103A Q2 是 4-Et-Ph，R1 是 Br 以及 R2 是 Q。 104A Q2 是 4-Et-Ph，R1 是 Cl 以及 R2 是 Br。 105A Q2 是 4-Et-Ph，R1 是 Cl 以及 R2 是 Cl。 106A Q2 是 4-C1、3-F-Ph，R1 是 Cl 以及 R2 是 Me。 107A Q2 是 4-CU、3-F-Ph，R1 是 Cl 以及 R2 是 CFH2。 108A Q2 是 4-C1、3-F-Ph，R1 是 Br 以及 R2 是 Me。 109A Q2 是 4-C1、3-F-Ph，R1 是 I 以及 R2 是 Me。 110A Q2 是 4-C1、3-F-Ph，R1 是 Me 以及 R2 是 Me。 111A Q2 是 4-C1、3-F-Ph，R1 是 Me 以及 R2 是 Cn。 112A Q2 是 4-C1、3-F-Ph，R1 是 Me 以及 R2 是 Br。 113A Q2 是 4-C1、3-F-Ph，R丨是 Me 以及 R2 是 I。 151284.doc -118- 201117722 表 列標題 114A Q2是 4-C1 、3-F-Ph ，R1是Br以及R2是Br。 115A Q2是 4-C1 、3-F-Ph ，R1是Br以及R2是Cl。 116A Q2是 4-C1 、3-F-Ph ，R1是Cl以及R2是Br。 117A Q2是 4-C1 、3-F-Ph ，R1是Cl以及R2是Cl。 118A Q2是 2-C1 、4-F-Ph ，Rl是Cl以及R2是Me。 119A Q2是 2-C1 、4-F-Ph ，R1是Cl以及R2是CFH2。 120A Q2是 2-C1 、4-F-Ph ，R1是Br以及R2是Me。 121A Q2是 2-C1 、4-F-Ph ，R1是I以及R2是Me。 122A Q2是 2-C1 、4-F-Ph ，R1是Me以及R2是Me。 123A Q2是 2-C1 、4-F-Ph ，R1是Me以及R2是CM。 124A Q2是 2-C1 &gt; 4-F-Ph ，R1是Me以及R2是Br。 125A Q2是 2-C1 、4-F-Ph ，R1是Me以及R2是I。 126A Q2是 2-C1 ' 4-F-Ph ，R1是Br以及R2是Br。 127A Q2是 2-C1 、4-F-Ph ，R1是Br以及R2是Cl。 128A Q2是 2-C1 、4-F-Ph ，R1是Cl以及R2是Br。 129A Q2是 2-C1 、4-F-Ph ，R1是Cl以及R2是α。 130A Q2是 4-F ' 3-Me-Ph ，R1是Cl以及R2是Me。 131A Q2是 4-F、 3-Me-Ph ，R1是Cl以及R2是CFH2。 132A Q2是 4-F、 3-Me-Ph ，R1是Br以及R2是Me。 133A Q2是 4-F、 3-Me-Ph ，R1是I以及R2是Me。 134A Q2是 4-F、 3-Me-Ph ，R1是Me以及R2是Me。 135A Q2是 4-F、 3-Me-Ph ，R1是Me以及R2是CM。 136A Q2是 4-F、 3-Me-Ph ，R1是Me以及R2是Br。 137A Q2是 4-F、 3-Me-Ph ，R1是Me以及R2是I。 138A Q2是 4-F、 3-Me-Ph ，R1是Br以及R2是Br。 139A Q2是 4-F、 3-Me-Ph ，R1是Br以及R2是Cl。 140A Q2是 4-F、 3-Me-Ph ，R1是Cl以及R2是Br。 141A Q2是 4-F，3-Me-Ph， R1是Cl以及R2是Cl。 142A Q2是 3,4-- --F-Ph &gt; R1是Cl以及R2是Me。 143A Q2是 3,4-- --F-Ph &gt; R1是Cl以及R2是CFH2。 144A Q2是 3,4-二-F_Ph， R1是Br以及R2是Me。 145A Q2是 3,4-二-F-Ph， R1是I以及R2是Me。 146A Q2是 3,4-二-F-Ph， R1是Me以及R2是Me。 147A Q2是 3,4-二 --F-Ph - R1是Me以及R2是CM。 148A Q2是 3,4-二-F-Ph， R1是Me以及R2是Br。 •119· 15I284.doc 201117722 表 列標題 149A Q2是 3,4-二 -F-Ph ， R1是Me以及R2是I。 150A Q2是 3,4-二 -F-Ph ’ R1 是Br以及R2是Br。 151A Q2是 3,4-二 -F-Ph ， R1是Br以及R2是Cl。 152A Q2是 3,4-二-F-Ph， R1 是Cl以及R2是Br。 153A Q2是 3,4-二-F-Ph， R1 是Cl以及R2是Cl。 154 A Q2是 3,4-二 -Cl-Ph ，R 是Cl以及R2是Me。 155A Q2是 3,4-二-Cl-Ph ，R 是Cl以及R2是CFH2。 156A Q2是 3,4-二 -Cl-Ph ，R 是Br以及R2是Me。 157A Q2是 3,4-二 -Cl-Ph ，R 是I以及R2是Me。 158A Q2是 3,4-二 -Cl-Ph ，R 是Me以及R2是Me。 159A Q2是 3,4-— -Cl-Ph ，R 是Me以及R2是C卜 160A Q2是 3,4,二 -Cl-Ph ，R 是Me以及R2是Br。 161A Q2是 3,4-二 -Cl-Ph ，R 是Me以及R2是I。 162 A Q2是 3,4-二 -Cl-Ph ，R 是Br以及R2是Br。 163A Q2是 3,4-二 -Cl-Ph ，R 是Br以及R2是C1。 164 A Q2是 3,4-二 -Cl-Ph ，R 是C1以及R2是Br。 165A Q2是 3,4-二 -Cl-Ph ，R 是C1以及R2是C1。 166A Q2是 3,5-二 -MeO-Ph » R1是C1以及R2是Me。 167A Q2是 3,5-二 -MeO_Ph， R1是C1以及R2是CFH2。 168A Q2是 3,5-二 -MeO-Ph * R1是Br以及R2是Me。 169 A Q2是 3,5-二 -MeO-Ph， R1是I以及R2是Me。 170A Q2是 3,5-二 -MeO-Ph， R1是Me以及R2是Me。 171A Q2是 3,5-二 -MeO-Ph， R1是Me以及R2是α。 172A Q2是 3,5-二 -MeO-Ph j R1是Me以及R2是Br。 173A Q2是 3,5-二 -MeO-Ph， R1是Me以及R2是I。 174A Q2是 3,5-二 -MeO-Ph » R1是Br以及R2是Br。 175A Q2是 3,5-二 MeO-Ph， R1是Br以及R2是α。 176A Q2是 3,5-二 -MeO-Ph， R1是C1以及R2是Br。 177A Q2是 3,5-二 -MeO-Ph » R1是C1以及R2是α。 178A Q2是 2-C1 ' 3,5-二 -MeO-Ph，R1 是 Cl 以及 R2 是 Me。 179 A Q2是 2-C1 ' 3，5-二 -MeO-Ph，R1 是 Cl 以及 R2 是 CFH2。 180A Q2是 2-C1 ' 3,5-— -MeO-Ph，R1 是 Br 以及 R2 是 Me。 181A Q2是 2-C1 &gt; 3,5-二 -MeO-Ph，Ri 是 I 以及 R2 是 Me。 182 A Q2是 2-C1 ' 3,5-二 -MeO-Ph，R1 是 Me 以及 R2 是 Me。 183A Q2是 2-C1 ' 3,5-- •MeO-Ph，R1 是 Me 以及 R2 是 Cl。 151284.doc -120- 201117722 表 列標題 184A Q2 是 2-C1、3,5-二-MeO-Ph，R1 是 Me 以及 R2 是 Br。 185A Q2 是 2-α、3,5-二-MeO-Ph，R1 是 Me 以及 R2 是 I。 186A Q2 是 2-α、3,5-二-MeO-Ph，R1 是 Br 以及 R2 是 Br。 187A Q2 是 2-C1、3,5-二-MeO-Ph，R1 是 Br 以及 R2 是 C卜 188A ()2是2-(：卜3,5-二-河6〇-?11，111是（：1以及112是价。 189A Q2 是 2-C卜 3,5-二-MeO-Ph，R1 是 C1 以及 R2 是 C1。 190A Q2 是 4-C1、3,5-二-MeO-Ph，R1 是 C1 以及 R2 是 Me。 191A (52是4-〇、3,5-二-]^^0-?11，111是（：1以及112是〇？出。 192A Q2 是 4-C1、3,5-二-MeO-Ph，R1 是 Br 以及 R2 是 Me。 193A Q2是4-Cl、3,5-二-MeO-Ph，R1是I以及R2是Me。 194A Q2 是 4-C1、3,5-二-MeO-Ph，R1 是 Me 以及 R2 是 Me。 195A Q2是4-Cl、3,5-二-MeO-Ph，R1是Me以及R2是Cl。 196A Q2 是 4-C1、3,5-二-MeO-Ph，R1 是 Me 以及 R2 是 Br。 197A Q2 是 4-a、3,5-二-MeO-Ph，R1 是 Me 以及 R2 是 I。 198A Q2 是 4-C1、3,5-二-MeO-Ph，R1 是 Br 以及 R2 是 Br。 199A Q2是4-C卜3,5-二-MeO-Ph，R1是Br以及R2是Cl。 200A Q2 是 4-C卜 3,5-二-MeO-Ph，R1 是 C1 以及 R2 是 Br。 201A Q2 是 4-C1、3,5-二-MeO-Ph，R1 是 C1 以及 R2 是 C卜 202A Q2 是 4-Cl-Bn，R1 是 C1 以及 R2 是 Me。 203A Q2 是 4-Cl-Bn，R丨是 C1 以及 R2 是 CFH2。 204A Q2 是 4-Cl-Bn，R1 是 Br 以及 R2 是 Me。 205A Q2 是 4-Cl-Bn，R1 是 I 以及 R2 是 Me。 206A Q2 是 4-Cl-Bn，R1 是 Me 以及 R2 是 Me。 207A Q2 是 4-Cl-Bn，R1 是 Me 以及 R2 是 α。 208A Q2 是 4-Cl-Bn，R1 是 Me 以及 R2 是 Br。 209A Q2 是 4-Cl-Bn，R1 是 Me 以及 R2 是 I。 210A Q2 是 4-Cl-Bn，R1 是 Br 以及 R2 是 Br。 211A Q2 是 4-Cl-Bn，R1 是 Br 以及 R2 是 Q。 212A Q2 是 4-Cl-Bn，R1 是 C1 以及 R2 是 Br。 213A Q2 是 4-Cl-Bn，R1 是 C1 以及 R2 是 CH。 214A Q2 是 4-F-Bn，R1 是 Cl 以及 R2 是 Me。 215A Q2 是 4-F-Bn，R1 是 C1 以及 R2 是 CFH2。 216A Q2是4-F-Bn，R丨是Br以及R2是Me。 217A Q2 是 4-F-Bn，R1 是 I 以及 R2 是 Me。 218A Q2 是 4-F-Bn，R1 是 Me 以及 R2 是 Me。 151284.doc -121 - 201117722 表 列標題 219A Q2 是 4-F-Bn，R1 是 Me 以及 R2 是 Cl。 220A Q2 是 4-F-Bn，R1 是 Me 以及 R2 是 Br。 221A Q2 是 4-F-Bn，R1 是 Me 以及 R2 是 I。 222A Q2 是 4-F-Bn，R1 是 Br 以及 R2 是 Br。 223A Q2是4-F-Bn，R1是Br以及R2是C卜 224A Q2 是 4-F-Bn，R1 是 C1 以及 R2 是 Br。 225A Q2 是 4-F-Bn，R1 是 C1 以及 R2 是 Cb 226A Q2是6-C1-3-吡啶基，R1是Cl以及R2是Me。 227A Q2是6-C1-3-吡啶基，R1是C1以及R2是CFH2。 228A Q2是6-C1-3-吡啶基，R1是Br以及R2是Me。 229A Q2是6-C1-3-吡啶基，R1是I以及R2是Me。 230A Q2是6-C1-3-吡啶基，R1是Me以及R2是Me。 231A Q2是6-C1-3-吡啶基，R1是Me以及R2是C卜 232A Q2是6-C1-3-吡啶基，R1是Me以及R2是Br。 233A Q2是6-C1-3-吡啶基，R1是Me以及R2是I。 234A Q2是6-C1-3-吡啶基，R1是Me以及R2是MeO。 235A Q2是6-C1-3-吡啶基，R1是MeO以及R2是Me。 236A Q2是6-C1-3-吡啶基，R1是Br以及R2是Br。 237A Q2是6-C1-3-吡啶基，R1是Br以及R2是Π。 238A Q2是6-C1-3-吡啶基，R1是C1以及R2是Br。 239A Q2是6-C1-3-吡啶基，R1是C1以及R2是C1。 240A Q2是6-C1-3-吡啶基，R1是Me以及R2是MeS。 241A Q2是6-C1-3-吡啶基，R1是MeS以及R2是Me。 242A Q2是6-C1-3-吡啶基，R1是Et以及R2是Br。 243A Q2是6-C1-3-吡啶基，R1是Et以及R2是C卜 244A Q2是6-C1-3-吡啶基，R1是Et以及R2是Me。 245A Q2是6-C1-3-吡啶基，R1是Me以及R2是Et。 246A Q2是6-C1-3-吡啶基，R1是C1以及R2是Et。 247A Q2是6-C1-3-吡啶基，R1是Me以及R2是CN。 248A Q2是6-Me-3-吡啶基，R1是C1以及R2是Me。 249A Q2是6-Me-3-吡啶基，R1是C1以及R2是CFH2。 250A Q2是6-Me-3-°比咬基，R1是Br以及R2是Me。 251A Q2是6-Me-3-吡啶基，R1是I以及R2是Me。 252A Q2是6-Me-3-吡啶基，R1是Me以及R2是Me。 253A Q2是6-Me-3-吡啶基，R1是Me以及R2是C1。 151284.doc -122- 201117722 表 列標題 254A Q2是6-Me-3-n比嗓基， R1是Me以及R2是Br。 255A Q2是6-Me-3-°比咬基， R1是Me以及R2是I。 256A Q2是6-Me-3-°比咬基， R1是Br以及R2是Br。 257A Q2 是 6-Me-3-nit咬基， R1是Br以及R2是C卜 258A Q2 是 6-Me-3-°it咬基， R1是C1以及R2是Br。 259A Q2是6-Me-3-e比咬基， R1是C1以及R2是C卜 260A Q2是6-MeO-3-吡啶基 ，R1是C1以及R2是Me。 261A Q2是6-MeO-3-a比咬基 ，R1是C1以及R2是CFH2。 262A Q2是6-MeO-3-°比咬基 ，R1是Br以及R2是Me。 263A Q2是6-MeO-3-°比咬基 ，R1是I以及R2是Me。 264A Q2是6-MeO-3-吡啶基 ，R1是Me以及R2是Me。 265A Q2是6-MeO-3-n比咬基 ，R1是Me以及R2是C1。 266A Q2是6-MeO-3-°比咬基 ，R1是Me以及R2是Br。 267A Q2是6-MeO-3-D比咬基 ，R1是Me以及R2是I。 268A Q2 是 6-MeO-3-aJt咬基 ，R1是Br以及R2是Br。 269A Q2是6-MeO-3-°比咬基 ，R1是Br以及R2是C1。 270A Q2 是 6-MeO-3-nit咬基 ，R1是C1以及R2是Br » 271A Q2 是 6-MeO-3-wb咬基 ，R1是Cl以及R2是Cl。 272A Q2是6-CF3-3-吡啶基 R1是C1以及R2是Me。 273A Q2是6-CF3-3-吡啶基 R1是C1以及R2是CFH2。 274A Q2是6-CF3-3-吡啶基 R1是Br以及R2是Me。 275A Q2是6-CF3-3-吡啶基 R1是I以及R2是Me。 276A Q2是6-CF3-3-吡啶基 R1是Me以及R2是Me。 277A Q2是6-CF3-3-。比啶基 R1是Me以及R2是α。 278A Q2是6-CF3-3-吡啶基 R1是Me以及R2是Br。 279A Q2是6-CF3-3-吡啶基 R1是Me以及R2是I。 280A Q2 是 6-CF3-3-°tt咬基 R1是Br以及R2是Br。 281A Q2是6-CF3-3-吡啶基 R1是Br以及R2是C卜 282A Q2是6-CF3-3-吡啶基 R1是C1以及R2是Br。 283A Q2是6-CF3-3-吡啶基 R1是C1以及R2是cn。 284A Q2是6-Br-3-吡啶基， R1是Cl以及R2是Me。 285A Q2是6-Br-3-°比咬基， R1是C1以及R2是CFH2。 286A Q2是6-Br-3-吡啶基， R1是Br以及R2是Me。 287A Q2是6-Br-3-吡啶基， R1是I以及R2是Me。 288A Q2 是 咬基， R1是Me以及R2是Me。 151284.doc -123- 201117722 表2-C1,5-CN 2,4-di-F, 5-CN 2- C1, 6-F, 3-MeO 2.6-di-F, 3-NCCH2O 2.6-di-F, 4-NCCH2O The contents also include Tables 1A to 715A, each of which is created in the same manner as Table 1 above, except for the column at the beginning of Table 1 (ie, "Q2 is 4-Cl-Ph, R1 is ci, and R2 is Me"). The other columns are replaced at the beginning. For example, at the beginning of the column of Table 1A, "Q2 is 4-Cl-Ph, R1 is Br and r2 is Me", and (R3) m is defined in Table 1 above. Therefore, the first table value in Table 1A Specifically disclosed is 4-bromo-H4-chlorophenyl)-5-(2,6-difluorophenyl)-iH-mipropene. Tables 2A through 715A are established in a similar manner. The column heading 1A Q疋4-Cl-Ph 'R丨 is Br and R2 is Me. 2A Q2 is 4-Cl-Ph ’ R丨 is Cl and R2 is CFH2. 3A Q is 4-Cl-Ph, Ri is j and R2 is Me. 4A Q2 is 4-Cl-Ph 'R丨 is Me and R2 is Me. 5A Q2 is 4-Cl-Ph 'R丨 is Me and R2 is C1. 6A Q2 is 4-Cl-Ph 'R丨 is Me and R2 is Br. 7A Q2 is 4-Cl-Ph, R丨 is Me and R2 is J. 8A Q2 is 4-Cl-Ph, R1 is Me and R2 is MeO. I51284.doc -115- 201117722 Table Column heading 9A Q2 is 4-Cl-Ph, R1 is MeO and R2 is Me. 10A Q2 is 4-Cl-Ph, R1 is Br and R2 is Br. 11A Q2 is 4-Cl-Ph, R1 is Br and R2 is Cl. 12A Q2 is 4-Cl-Ph, R1 is Cl and R2 is Br. 13A Q2 is 4-Cl-Ph, R1 is Cl and R2 is Cl. 14A Q2 is 4-Cl-Ph, R1 is Me and R2 is MeS. 15A Q2 is 4-Cl-Ph, R1 is MeS and R2 is Me. 16A Q2 is 4-Cl-Ph, R1 is Et and R2 is Br. 17A Q2 is 4-Cl-Ph, R1 is Et and R2 is CM. 18A Q2 is 4-Cl-Ph, R1 is Et and R2 is Me. 19A Q2 is 4-Cl-Ph, R1 is Me and R2 is Et. 20A Q2 is 4-Cl-Ph, R1 is Cl and R2 is Et. 21A Q2 is 4-Cl-Ph, R1 is Me and R2 is CN. 22A Q2 is 3-Cl-Ph, R1 is Cl and R2 is Me. 23A Q2 is 3-Cl-Ph, R1 is Cl and R2 is CFH2. 24A Q2 is 3-Cl-Ph, R1 is Br and R2 is Me. 25A Q2 is 3-Cl-Ph, R1 is I and R2 is Me. 26A Q2 is 3-Cl-Ph, R1 is Me and R2 is Me. 27A Q2 is 3-Cl-Ph, R1 is Me and R2 is Cl. 28A Q2 is 3-Cl-Ph, R1 is Me and R2 is Br. 29A Q2 is 3-Cl-Ph, R1 is Me and R2 is I. 30A Q2 is 3-Cl-Ph, R1 is Br and R2 is Br. 31A Q2 is 3-Cl-Ph, R1 is Br and R2 is a. .32A Q2 is 3-Cl-Ph, R1 is Cl and R2 is Br. 33A Q2 is 3-Cl-Ph, R1 is Cl and R2 is Cl. 34A Q2 is 4-F-Ph, R1 is Cl and R2 is Me. 35A Q2 is 4-F-Ph, R1 is Cl and R2 is CFH2. 36A Q2 is 4-F-Ph, R1 is Br and R2 is Me. 37A Q2 is 4-F-Ph, R1 is I and R2 is Me. 38A Q2 is 4-F-Ph, R1 is Me and R2 is Me. 39A Q2 is 4-F-Ph, R1 is Me and R2 is CBu 40A Q2 is 4-F-Ph, R1 is Me and R2 is Br. 41A Q2 is 4-F-Ph, R1 is Me and R2 is I. 42A Q2 is 4-F-Ph, R1 is Br and R2 is Br. 43A Q2 is 4-F-Ph, R1 is Br and R2 is Cl. 151284.doc -116- 201117722 Table Column heading 44A Q2 is 4-F-Ph, R1 is Cl and R2 is Br. 45A Q2 is 4-F-Ph, R1 is Cl and R2 is Cl. 46A Q2 is 3-F-Ph, R1 is Cl and R2 is Me. 47A Q2 is 3-F-Ph, R1 is Cl and R2 is CFH2. 48A Q2 is 3-F-Ph, R1 is Br and R2 is Me. 49A Q2 is 3-F-Ph, R1 is I and R2 is Me. 50A Q2 is 3-F-Ph, R1 is Me and R2 is Me. 51A Q2 is 3-F-Ph, R1 is Me and R2 is Cb 52A Q2 is 3-F-Ph, R1 is Me and R2 is Br. 53A Q2 is 3-F-Ph, R1 is Me and R2 is I. 54A Q2 is 3-F-Ph, R1 is Br and R2 is Br. 55A Q2 is 3-F-Ph, R1 is Br and R2 is Cl. 56A Q2 is 3-F-Ph, R1 is Cl and R2 is Br. 57A Q2 is 3-F-Ph, R1 is Cl and R2 is Cl. 58A Q2 is 3-CF2HO-Ph, Ri is Cl and R2 is Me. 59A Q2 is 3-CF2HO-Ph, R1 is Cl and R2 is CFH2 · 60A Q2 is 3-CF2HO-Ph, R1 is Br and R2 is Me. 61A Q2 is 3-CF2HO-Ph, R1 is I and R2 is Me. 62A Q2 is 3-CF2HO-Ph, R1 is Me and R2 is Me. 63A Q2 is 3-CF2HO-Ph, R1 is Me and R2 is Cl. 64A Q2 is 3-CF2HO-Ph, R1 is Me and R2 is Br. 65A Q2 is 3-CF2HO-Ph, R1 is Me and R2 is I. 66A Q2 is 3-CF2HO-Ph, R1 is Br and R2 is Br. 67A Q2 is 3-CF2HO-Ph, R1 is Br and R2 is Cl. 68A Q2 is 3-CF2HO-Ph, R1 is Cl and R2 is Br. 69A Q2 is 3-CF2HO-Ph, R1 is Cl and R2 is Cl. 70A Q2 is 4-Me-Ph, R1 is Cl and R2 is Me. 71A Q2 is 4-Me-Ph, R1 is Cl and R2 is CFH2. 72A Q2 is 4-Me-Ph, R1 is Br and R2 is Me. 73A Q2 is 4-Me-Ph, R1 is I and R2 is Me. 74A Q2 is 4-Me-Ph, R1 is Me and R2 is Me. 75A Q2 is 4-Me-Ph, R1 is Me and R2 is a. 76A Q2 is 4-Me-Ph, R1 is Me and R2 is Br. 77A Q2 is 4-Me-Ph, R1 is Me and R2 is I. 78A Q2 is 4-Me-Ph, R1 is Br and R2 is Br. 151284.doc · 117· 201117722 Table Column heading 79A Q2 is 4-Me-Ph, R1 is Br and R2 is Cl. 80A Q2 is 4-Me-Ph, R1 is Cl and R2 is Br. 81A Q2 is 4-Me-Ph, R1 is Cl and R2 is α. 82A Q2 is 3-Me-Ph, R1 is Cl and R2 is Me. 83A Q2 is 3-Me-Ph, R1 is Cl and R2 is CFH2. 84A Q2 is 3-Me-Ph, R丨 is Br and R2 is Me. 85A Q2 is 3-Me-Ph, R1 is I and R2 is Me. 86A Q2 is 3-Me-Ph, R1 is Me and R2 is Me. 87A Q2 is 3-Me-Ph, R1 is Me and R2 is a. 88A Q2 is 3-Me-Ph, R1 is Me and R2 is Br. 89A Q2 is 3-Me-Ph, R1 is Me and R2 is I. 90A Q2 is 3-Me-Ph, R1 is Br and R2 is Br. 91A Q2 is 3-Me-Ph, R1 is Br and R2 is Cl. 92A Q2 is 3-Me-Ph, R1 is Cl and R2 is Br. 93A Q2 is 3-Me-Ph, R1 is Cl and R2 is a. 94A Q2 is 4-Et-Ph, R1 is Cl and R2 is Me. 95A Q2 is 4-Et-Ph, R1 is Cl and R2 is CFH2. 96A Q2 is 4-Et-Ph, R1 is Br and R2 is Me. 97A Q2 is 4-Et-Ph, R1 is I and R2 is Me. 98A Q2 is 4-Et-Ph, R1 is Me and R2 is Me. 99A Q2 is 4-Et-Ph, R1 is Me and R2 is Cl. 100 A Q2 is 4-Et-Ph, R1 is Me and R2 is Br. 101A Q2 is 4-Et-Ph, R1 is Me and R2 is I. 102 A Q2 is 4-Et-Ph, R1 is Br and R2 is Br. 103A Q2 is 4-Et-Ph, R1 is Br and R2 is Q. 104A Q2 is 4-Et-Ph, R1 is Cl and R2 is Br. 105A Q2 is 4-Et-Ph, R1 is Cl and R2 is Cl. 106A Q2 is 4-C1, 3-F-Ph, R1 is Cl and R2 is Me. 107A Q2 is 4-CU, 3-F-Ph, R1 is Cl and R2 is CFH2. 108A Q2 is 4-C1, 3-F-Ph, R1 is Br and R2 is Me. 109A Q2 is 4-C1, 3-F-Ph, R1 is I and R2 is Me. 110A Q2 is 4-C1, 3-F-Ph, R1 is Me and R2 is Me. 111A Q2 is 4-C1, 3-F-Ph, R1 is Me and R2 is Cn. 112A Q2 is 4-C1, 3-F-Ph, R1 is Me and R2 is Br. 113A Q2 is 4-C1, 3-F-Ph, R丨 is Me and R2 is I. 151284.doc -118- 201117722 Table Column heading 114A Q2 is 4-C1, 3-F-Ph, R1 is Br and R2 is Br. 115A Q2 is 4-C1, 3-F-Ph, R1 is Br and R2 is Cl. 116A Q2 is 4-C1, 3-F-Ph, R1 is Cl and R2 is Br. 117A Q2 is 4-C1, 3-F-Ph, R1 is Cl and R2 is Cl. 118A Q2 is 2-C1, 4-F-Ph, Rl is Cl and R2 is Me. 119A Q2 is 2-C1, 4-F-Ph, R1 is Cl and R2 is CFH2. 120A Q2 is 2-C1, 4-F-Ph, R1 is Br and R2 is Me. 121A Q2 is 2-C1, 4-F-Ph, R1 is I and R2 is Me. 122A Q2 is 2-C1, 4-F-Ph, R1 is Me and R2 is Me. 123A Q2 is 2-C1, 4-F-Ph, R1 is Me and R2 is CM. 124A Q2 is 2-C1 &gt; 4-F-Ph, R1 is Me and R2 is Br. 125A Q2 is 2-C1, 4-F-Ph, R1 is Me and R2 is I. 126A Q2 is 2-C1 '4-F-Ph, R1 is Br and R2 is Br. 127A Q2 is 2-C1, 4-F-Ph, R1 is Br and R2 is Cl. 128A Q2 is 2-C1, 4-F-Ph, R1 is Cl and R2 is Br. 129A Q2 is 2-C1, 4-F-Ph, R1 is Cl and R2 is α. 130A Q2 is 4-F ' 3-Me-Ph , R1 is Cl and R2 is Me. 131A Q2 is 4-F, 3-Me-Ph, R1 is Cl and R2 is CFH2. 132A Q2 is 4-F, 3-Me-Ph, R1 is Br and R2 is Me. 133A Q2 is 4-F, 3-Me-Ph, R1 is I and R2 is Me. 134A Q2 is 4-F, 3-Me-Ph, R1 is Me and R2 is Me. 135A Q2 is 4-F, 3-Me-Ph, R1 is Me and R2 is CM. 136A Q2 is 4-F, 3-Me-Ph, R1 is Me and R2 is Br. 137A Q2 is 4-F, 3-Me-Ph, R1 is Me and R2 is I. 138A Q2 is 4-F, 3-Me-Ph, R1 is Br and R2 is Br. 139A Q2 is 4-F, 3-Me-Ph, R1 is Br and R2 is Cl. 140A Q2 is 4-F, 3-Me-Ph, R1 is Cl and R2 is Br. 141A Q2 is 4-F, 3-Me-Ph, R1 is Cl and R2 is Cl. 142A Q2 is 3,4-- --F-Ph &gt; R1 is Cl and R2 is Me. 143A Q2 is 3,4-- --F-Ph &gt; R1 is Cl and R2 is CFH2. 144A Q2 is 3,4-di-F_Ph, R1 is Br and R2 is Me. 145A Q2 is 3,4-di-F-Ph, R1 is I and R2 is Me. 146A Q2 is 3,4-di-F-Ph, R1 is Me and R2 is Me. 147A Q2 is 3,4-di-F-Ph-R1 is Me and R2 is CM. 148A Q2 is 3,4-di-F-Ph, R1 is Me and R2 is Br. • 119· 15I284.doc 201117722 Table Column heading 149A Q2 is 3,4-di-F-Ph, R1 is Me and R2 is I. 150A Q2 is 3,4-di-F-Ph 'R1 is Br and R2 is Br. 151A Q2 is 3,4-di-F-Ph, R1 is Br and R2 is Cl. 152A Q2 is 3,4-di-F-Ph, R1 is Cl and R2 is Br. 153A Q2 is 3,4-di-F-Ph, R1 is Cl and R2 is Cl. 154 A Q2 is 3,4-di-Cl-Ph, R is Cl and R2 is Me. 155A Q2 is 3,4-di-Cl-Ph, R is Cl and R2 is CFH2. 156A Q2 is 3,4-di-Cl-Ph, R is Br and R2 is Me. 157A Q2 is 3,4-di-Cl-Ph, R is I and R2 is Me. 158A Q2 is 3,4-di-Cl-Ph, R is Me and R2 is Me. 159A Q2 is 3,4-—Cl-Ph, R is Me and R2 is CBu 160A Q2 is 3,4, di-Cl-Ph, R is Me and R2 is Br. 161A Q2 is 3,4-di-Cl-Ph, R is Me and R2 is I. 162 A Q2 is 3,4-di-Cl-Ph, R is Br and R2 is Br. 163A Q2 is 3,4-di-Cl-Ph, R is Br and R2 is C1. 164 A Q2 is 3,4-di-Cl-Ph, R is C1 and R2 is Br. 165A Q2 is 3,4-di-Cl-Ph, R is C1 and R2 is C1. 166A Q2 is 3,5-di-MeO-Ph » R1 is C1 and R2 is Me. 167A Q2 is 3,5-di-MeO_Ph, R1 is C1 and R2 is CFH2. 168A Q2 is 3,5-di-MeO-Ph * R1 is Br and R2 is Me. 169 A Q2 is 3,5-di-MeO-Ph, R1 is I and R2 is Me. 170A Q2 is 3,5-di-MeO-Ph, R1 is Me and R2 is Me. 171A Q2 is 3,5-di-MeO-Ph, R1 is Me and R2 is α. 172A Q2 is 3,5-di-MeO-Ph j R1 is Me and R2 is Br. 173A Q2 is 3,5-di-MeO-Ph, R1 is Me and R2 is I. 174A Q2 is 3,5-di-MeO-Ph » R1 is Br and R2 is Br. 175A Q2 is 3,5-di MeO-Ph, R1 is Br and R2 is α. 176A Q2 is 3,5-di-MeO-Ph, R1 is C1 and R2 is Br. 177A Q2 is 3,5-di-MeO-Ph » R1 is C1 and R2 is α. 178A Q2 is 2-C1 '3,5-di-MeO-Ph, R1 is Cl and R2 is Me. 179 A Q2 is 2-C1 '3,5-di-MeO-Ph, R1 is Cl and R2 is CFH2. 180A Q2 is 2-C1 ' 3,5-- -MeO-Ph, R1 is Br and R2 is Me. 181A Q2 is 2-C1 &gt; 3,5-di-MeO-Ph, Ri is I and R2 is Me. 182 A Q2 is 2-C1 '3,5-di-MeO-Ph, R1 is Me and R2 is Me. 183A Q2 is 2-C1 ' 3,5-- •MeO-Ph, R1 is Me and R2 is Cl. 151284.doc -120- 201117722 Table Column heading 184A Q2 is 2-C1,3,5-di-MeO-Ph, R1 is Me and R2 is Br. 185A Q2 is 2-α, 3,5-di-MeO-Ph, R1 is Me and R2 is I. 186A Q2 is 2-α, 3,5-di-MeO-Ph, R1 is Br and R2 is Br. 187A Q2 is 2-C1,3,5-di-MeO-Ph, R1 is Br and R2 is CBu 188A ()2 is 2-(:Bu 3,5-di-he 6〇-?11,111 is (: 1 and 112 are valences. 189A Q2 is 2-C Bu 3,5-di-MeO-Ph, R1 is C1 and R2 is C1. 190A Q2 is 4-C1,3,5-di-MeO-Ph, R1 is C1 and R2 is Me. 191A (52 is 4-〇, 3,5-di-]^^0-?11, 111 is (:1 and 112 are 〇?出. 192A Q2 is 4-C1, 3 , 5-di-MeO-Ph, R1 is Br and R2 is Me. 193A Q2 is 4-Cl, 3,5-di-MeO-Ph, R1 is I and R2 is Me. 194A Q2 is 4-C1, 3 , 5-di-MeO-Ph, R1 is Me and R2 is Me. 195A Q2 is 4-Cl, 3,5-di-MeO-Ph, R1 is Me and R2 is Cl. 196A Q2 is 4-C1, 3 , 5-di-MeO-Ph, R1 is Me and R2 is Br. 197A Q2 is 4-a, 3,5-di-MeO-Ph, R1 is Me and R2 is I. 198A Q2 is 4-C1, 3 , 5-di-MeO-Ph, R1 is Br and R2 is Br. 199A Q2 is 4-CBu 3,5-di-MeO-Ph, R1 is Br and R2 is Cl. 200A Q2 is 4-C Bu 3 ,5-di-MeO-Ph, R1 is C1 and R2 is Br. 201A Q2 is 4-C1,3,5-di-MeO-Ph, R1 is C1 and R2 is CBu 202A Q2 Is 4-Cl-Bn, R1 is C1 and R2 is Me. 203A Q2 is 4-Cl-Bn, R丨 is C1 and R2 is CFH2. 204A Q2 is 4-Cl-Bn, R1 is Br and R2 is Me. 205A Q2 is 4-Cl-Bn, R1 is I and R2 is Me. 206A Q2 is 4-Cl-Bn, R1 is Me and R2 is Me. 207A Q2 is 4-Cl-Bn, R1 is Me and R2 is α 208A Q2 is 4-Cl-Bn, R1 is Me and R2 is Br. 209A Q2 is 4-Cl-Bn, R1 is Me and R2 is I. 210A Q2 is 4-Cl-Bn, R1 is Br and R2 is Br. 211A Q2 is 4-Cl-Bn, R1 is Br and R2 is Q. 212A Q2 is 4-Cl-Bn, R1 is C1 and R2 is Br. 213A Q2 is 4-Cl-Bn, R1 is C1 and R2 is CH. 214A Q2 is 4-F-Bn, R1 is Cl and R2 is Me. 215A Q2 is 4-F-Bn, R1 is C1 and R2 is CFH2. 216A Q2 is 4-F-Bn, R丨 is Br and R2 is Me. 217A Q2 is 4-F-Bn, R1 is I and R2 is Me. 218A Q2 is 4-F-Bn, R1 is Me and R2 is Me. 151284.doc -121 - 201117722 Table Column headings 219A Q2 is 4-F-Bn, R1 is Me and R2 is Cl. 220A Q2 is 4-F-Bn, R1 is Me and R2 is Br. 221A Q2 is 4-F-Bn, R1 is Me and R2 is I. 222A Q2 is 4-F-Bn, R1 is Br and R2 is Br. 223A Q2 is 4-F-Bn, R1 is Br and R2 is CBu 224A Q2 is 4-F-Bn, R1 is C1 and R2 is Br. 225A Q2 is 4-F-Bn, R1 is C1 and R2 is Cb 226A Q2 is 6-C1-3-pyridyl, R1 is Cl and R2 is Me. 227A Q2 is 6-C1-3-pyridyl, R1 is C1 and R2 is CFH2. 228A Q2 is 6-C1-3-pyridyl, R1 is Br and R2 is Me. 229A Q2 is 6-C1-3-pyridyl, R1 is I and R2 is Me. 230A Q2 is 6-C1-3-pyridyl, R1 is Me and R2 is Me. 231A Q2 is 6-C1-3-pyridyl, R1 is Me and R2 is CBu 232A Q2 is 6-C1-3-pyridyl, R1 is Me and R2 is Br. 233A Q2 is 6-C1-3-pyridyl, R1 is Me and R2 is I. 234A Q2 is 6-C1-3-pyridyl, R1 is Me and R2 is MeO. 235A Q2 is 6-C1-3-pyridyl, R1 is MeO and R2 is Me. 236A Q2 is 6-C1-3-pyridyl, R1 is Br and R2 is Br. 237A Q2 is 6-C1-3-pyridyl, R1 is Br and R2 is deuterium. 238A Q2 is 6-C1-3-pyridyl, R1 is C1 and R2 is Br. 239A Q2 is 6-C1-3-pyridyl, R1 is C1 and R2 is C1. 240A Q2 is 6-C1-3-pyridyl, R1 is Me and R2 is MeS. 241A Q2 is 6-C1-3-pyridyl, R1 is MeS and R2 is Me. 242A Q2 is 6-C1-3-pyridyl, R1 is Et and R2 is Br. 243A Q2 is 6-C1-3-pyridyl, R1 is Et and R2 is CBu 244A Q2 is 6-C1-3-pyridyl, R1 is Et and R2 is Me. 245A Q2 is 6-C1-3-pyridyl, R1 is Me and R2 is Et. 246A Q2 is 6-C1-3-pyridyl, R1 is C1 and R2 is Et. 247A Q2 is 6-C1-3-pyridyl, R1 is Me and R2 is CN. 248A Q2 is 6-Me-3-pyridyl, R1 is C1 and R2 is Me. 249A Q2 is 6-Me-3-pyridyl, R1 is C1 and R2 is CFH2. 250A Q2 is a 6-Me-3-° ratio bite, R1 is Br and R2 is Me. 251A Q2 is 6-Me-3-pyridyl, R1 is I and R2 is Me. 252A Q2 is 6-Me-3-pyridyl, R1 is Me and R2 is Me. 253A Q2 is 6-Me-3-pyridyl, R1 is Me and R2 is C1. 151284.doc -122- 201117722 Table Column headings 254A Q2 is 6-Me-3-n than fluorenyl, R1 is Me and R2 is Br. 255A Q2 is a 6-Me-3-° ratio bite, R1 is Me and R2 is I. 256A Q2 is a 6-Me-3-° ratio bite, R1 is Br and R2 is Br. 257A Q2 is a 6-Me-3-nit bite group, R1 is Br and R2 is Cb. 258A Q2 is a 6-Me-3-°it bite group, R1 is C1 and R2 is Br. 259A Q2 is a 6-Me-3-e ratio bite group, R1 is C1 and R2 is CBu 260A Q2 is 6-MeO-3-pyridyl, R1 is C1 and R2 is Me. 261A Q2 is a 6-MeO-3-a ratio bite group, R1 is C1 and R2 is CFH2. 262A Q2 is a 6-MeO-3-° ratio bite group, R1 is Br and R2 is Me. 263A Q2 is a 6-MeO-3-° ratio bite base, R1 is I and R2 is Me. 264A Q2 is 6-MeO-3-pyridyl, R1 is Me and R2 is Me. 265A Q2 is a 6-MeO-3-n ratio bite group, R1 is Me and R2 is C1. 266A Q2 is a 6-MeO-3-° ratio bite base, R1 is Me and R2 is Br. 267A Q2 is a 6-MeO-3-D ratio bite group, R1 is Me and R2 is I. 268A Q2 is a 6-MeO-3-aJt bite group, R1 is Br and R2 is Br. 269A Q2 is a 6-MeO-3-° ratio bite base, R1 is Br and R2 is C1. 270A Q2 is a 6-MeO-3-nit bite group, R1 is C1 and R2 is Br » 271A Q2 is a 6-MeO-3-wb bite group, R1 is Cl and R2 is Cl. 272A Q2 is 6-CF3-3-pyridyl R1 is C1 and R2 is Me. 273A Q2 is 6-CF3-3-pyridyl R1 is C1 and R2 is CFH2. 274A Q2 is 6-CF3-3-pyridyl R1 is Br and R2 is Me. 275A Q2 is 6-CF3-3-pyridyl R1 is I and R2 is Me. 276A Q2 is 6-CF3-3-pyridyl R1 is Me and R2 is Me. 277A Q2 is 6-CF3-3-. The pyridyl group R1 is Me and R2 is α. 278A Q2 is 6-CF3-3-pyridyl R1 is Me and R2 is Br. 279A Q2 is 6-CF3-3-pyridyl R1 is Me and R2 is I. 280A Q2 is a 6-CF3-3-°tt bite. R1 is Br and R2 is Br. 281A Q2 is 6-CF3-3-pyridyl R1 is Br and R2 is C 282A Q2 is 6-CF3-3-pyridyl R1 is C1 and R2 is Br. 283A Q2 is 6-CF3-3-pyridyl R1 is C1 and R2 is cn. 284A Q2 is 6-Br-3-pyridinyl, R1 is Cl and R2 is Me. 285A Q2 is a 6-Br-3-° ratio bite group, R1 is C1 and R2 is CFH2. 286A Q2 is 6-Br-3-pyridyl, R1 is Br and R2 is Me. 287A Q2 is 6-Br-3-pyridyl, R1 is I and R2 is Me. 288A Q2 is a bite base, R1 is Me and R2 is Me. 151284.doc -123- 201117722 Table

289A 290A 291A 292A 293A 294A 295A 296A 297A 298A 299A 300A 301A 302A 303A 304A 305A 306A 307A 308A 309A 310A 311A 312A 313A 314A 315A 316A 317A 318A 319A 320A 321A 322A 323A 列標題 Q2是6-Br-3-吡啶基，R1是Me以及R2是α。 Q2是6-Br-3-吡啶基，R1是Me以及R2是Br。 Q2是6-Br-3-吡啶基，R1是Me以及R2是I。 Q2是6-Br-3-吡啶基，R1是Br以及R2是Br。 Q2是6-ΒΓ-3-吡啶基，R1是Br以及R2是C1。 Q2是6-Br-3-吡啶基，R1是C1以及R2是Br。 Q2是6-Br-3-吡啶基，R1是C1以及R2是C1。 Q2是6-F-3-吡啶基，R1是C1以及R2是Me。 Q2是6-F-3-吡啶基，R1是C1以及R2是CFH2。 Q2是6-F-3-吡啶基，R1是Br以及R2是Me。 Q2是6-F-3-吡啶基，R1是I以及R2是Me。 Q2是6-F-3-吡啶基，R1是Me以及R2是Me。 Q2是6-F-3-吡啶基，R1是Me以及R2是C卜 Q2是6-F-3-吡啶基，R1是Me以及R2是Br。 Q2是6-F-3-吡啶基，R1是Me以及R2是I。 Q2是6-F-3-吡啶基，R1是Br以及R2是Br。 Q2是6-F-3-吡啶基，R1是Br以及R2是CH。 Q2是6-F-3-吡啶基，R1是C1以及R2是Br。 Q2是6-F-3-吡啶基，R1是C1以及R2是C1。 Q2是2-C1、6-Me-4-吡啶基，R1是C1以及R2是Me。 Q2 是 2-Q、6-Me-4-吡啶基，R1 是 C1 以及 R2 是 CFH2。 Q2是2-C1、6-Me-4-吡啶基，R1是Br以及R2是Me。 Q2是2-C1、6-Me-4-吡啶基，R1是I以及R2是Me。 Q2是2-C1、6-Me-4-吡啶基，R1是Me以及R2是Me。 Q2是2-C1、6-Me-4-吡啶基，R1是Me以及R2是C1。 Q2是2-C1、6-Me-4-吡啶基，R1是Me以及R2是Br。 Q2是2-C1、6-Me-4-吡啶基，R1是Me以及R2是I。 Q2是2-Cn、6-Me-4-吡啶基，R1是Br以及R2是Br。 Q2是2-C1、6-Me-4-吡啶基，R1是Br以及R2是α。 Q2是2-C卜6-Me-4-吡啶基，R1是C1以及R2是Br。 Q2是2-C1、6-Me-4-吡啶基，R1是C1以及R2是C1。 Q2 是 2-C1、6-MeO-3-吡啶基，R1 是 C1 以及 R2 是 Me。 Q2 是 2-Q、6-MeO-3-吡啶基，W 是 C1 以及 R2 是 CFH2。 Q2 是 2-C1、6-MeO-3-吡啶基，R1 是 Br 以及 R2 是 Me。 Q2是2-CI、6-MeO-3-吡啶基，R1是I以及R2是Me。 151284.doc •124·289A 290A 291A 292A 293A 294A 295A 296A 297A 298A 299A 300A 301A 302A 303A 304A 305A 306A 307A 308A 309A 310A 311A 312A 313A 314A 315A 316A 317A 318A 319A 320A 321A 322A 323A Column heading Q2 is 6-Br-3-pyridyl, R1 is Me and R2 are α. Q2 is 6-Br-3-pyridyl, R1 is Me and R2 is Br. Q2 is 6-Br-3-pyridyl, R1 is Me and R2 is I. Q2 is 6-Br-3-pyridyl, R1 is Br and R2 is Br. Q2 is 6-fluoren-3-pyridyl, R1 is Br and R2 is C1. Q2 is 6-Br-3-pyridyl, R1 is C1 and R2 is Br. Q2 is 6-Br-3-pyridyl, R1 is C1 and R2 is C1. Q2 is 6-F-3-pyridyl, R1 is C1 and R2 is Me. Q2 is 6-F-3-pyridyl, R1 is C1 and R2 is CFH2. Q2 is 6-F-3-pyridyl, R1 is Br and R2 is Me. Q2 is 6-F-3-pyridyl, R1 is I and R2 is Me. Q2 is 6-F-3-pyridyl, R1 is Me and R2 is Me. Q2 is 6-F-3-pyridyl, R1 is Me and R2 is Cb. Q2 is 6-F-3-pyridyl, R1 is Me and R2 is Br. Q2 is 6-F-3-pyridyl, R1 is Me and R2 is I. Q2 is 6-F-3-pyridyl, R1 is Br and R2 is Br. Q2 is 6-F-3-pyridyl, R1 is Br and R2 is CH. Q2 is 6-F-3-pyridyl, R1 is C1 and R2 is Br. Q2 is 6-F-3-pyridyl, R1 is C1 and R2 is C1. Q2 is 2-C1, 6-Me-4-pyridyl, R1 is C1 and R2 is Me. Q2 is 2-Q, 6-Me-4-pyridyl, R1 is C1 and R2 is CFH2. Q2 is 2-C1, 6-Me-4-pyridyl, R1 is Br and R2 is Me. Q2 is 2-C1, 6-Me-4-pyridyl, R1 is I and R2 is Me. Q2 is 2-C1, 6-Me-4-pyridyl, R1 is Me and R2 is Me. Q2 is 2-C1, 6-Me-4-pyridyl, R1 is Me and R2 is C1. Q2 is 2-C1, 6-Me-4-pyridyl, R1 is Me and R2 is Br. Q2 is 2-C1, 6-Me-4-pyridyl, R1 is Me and R2 is I. Q2 is 2-Cn, 6-Me-4-pyridyl, R1 is Br and R2 is Br. Q2 is 2-C1, 6-Me-4-pyridyl, R1 is Br and R2 is α. Q2 is 2-Cb6-Me-4-pyridyl, R1 is C1 and R2 is Br. Q2 is 2-C1, 6-Me-4-pyridyl, R1 is C1 and R2 is C1. Q2 is 2-C1, 6-MeO-3-pyridyl, R1 is C1 and R2 is Me. Q2 is 2-Q, 6-MeO-3-pyridyl, W is C1 and R2 is CFH2. Q2 is 2-C1, 6-MeO-3-pyridyl, R1 is Br and R2 is Me. Q2 is 2-CI, 6-MeO-3-pyridyl, R1 is I and R2 is Me. 151284.doc •124·

201117722 表 324A 325A 326A 327A 328A 329A 330A 331A 332A 333A 334A 335A 336A 337A 338A 339A 340A 341A 342A 343A 344A 345A 346A 347A 348A 349A 350A 351A 352A 353A 354A 355A 356A 357A 358A 列標題 Q2 是 2-C1、6-MeO-3-吡啶基，R1 是 Me 以及 R2 是 Me。 Q2 是 2-C1、6-MeO-3-吡啶基，R1 是 Me 以及 R2 是 C1。 Q2 是 2-C1、6-MeO-3-吡啶基，R1 是 Me 以及 R2 是 Br。 Q2是2-C1、6-MeO-3-吡啶基，R1是Me以及R2是I。 Q2 是 2-C1、6-MeO-3-吡啶基，R1 是 Br 以及 R2 是 Br。 Q2 是 2-C1、6-MeO-3-吡啶基，R1 是 Br 以及 R2 是 C1。 Q2是2-Q、6-MeO-3-吡啶基，R1是C1以及R2是Br。 Q2 是 2-C1、6-MeO-3-吡啶基，R1 是 C1 以及 R2 是 C1。 Q2 是 2-C1、6-CF3-3-吡啶基，R1 是 C1 以及 R2 是 Me。 Q2 是 2-a、6-CF3-3-吡啶基，R1 是 C1 以及 R2 是 CFH2。 Q2 是 2-C1、6-CF3-3-吡啶基，R1 是 Br 以及 R2 是 Me。 Q2是2-C1、6-CF3-3-吡啶基，R1是I以及R2是Me。 Q2 是 2-C1、6-CF3-3-吡啶基，R1 是 Me 以及 R2 是 Me。 Q2 是 2-C1、6-CF3-3-吡啶基，R1 是 Me 以及 R2 是 C1。 Q2 是 2-C1、6-CF3-3-吡啶基，R1 是 Me 以及 R2 是 Br。 Q2是2-C1、6-CF3-3-吡啶基，R1是Me以及R2是I。 Q2 是 2-C1、6-CF3-3-吡啶基，R1 是 Br 以及 R2 是 Br。 Q2是2-C1、6-CF3-3-吡啶基，R1是Br以及R2是α。 Q2 是 2-C1、6-CF3-3-吡啶基，R1 是 C1 以及 R2 是 Br。 Q2是2-C1、6-CFr3-吡啶基，R1是C1以及R2是C1。 Q2是5-C1-3-吡啶基，R丨是C1以及R2是Me。 Q2是5-C1-3-吡啶基，R1是C1以及R2是CFH2。 Q2是5-C1-3-吡啶基，R1是Br以及R2是Me。 Q2是5-C1-3-吡啶基，R1是I以及R2是Me。 Q2是5-C1-3-吡啶基，R1是Me以及R2是Me。 Q2是5-C1-3-吡啶基，R1是Me以及R2是α。 Q2是5-C1-3-。比啶基，R1是Me以及R2是Br。 Q2是5-C1-3-吡啶基，R1是Me以及R2是I。 Q2是5-C1-3-。比啶基，R1是Br以及R2是Br。 Q2是5-C1-3-吡啶基，R1是Br以及R2是C1。 Q2是5-C1-3-吡啶基，R1是C1以及R2是Br。 Q2是5-C1-3-。比啶基，R1是C1以及R2是C1。 Q2是5-F-3-吡啶基，R1是C1以及R2是Me » Q2是5-F-3-吡啶基，R1是Cl以及R2是CFH2。 Q2是5-F-3-吡啶基，R1是Br以及R2是Me。 151284.doc -125- 201117722 表 列標題 359A Q2是5-F-3-吡啶基，R1是I以及R2是Me。 360A Q2是5-F-3-吡啶基，R1是Me以及R2是Me。 361A Q2是5-F-3-吡啶基，R1是Me以及R2是α。 362A Q2是5-F-3-吡啶基，R1是Me以及R2是Br。 363A Q2是5-F-3-吡啶基，R1是Me以及R2是I。 364A Q2是5-F-3-吡啶基，R1是Br以及R2是Br。 365A Q2是5-F-3-吡啶基，R1是Br以及R2是α。 366A Q2是5-F-3-吡啶基，R1是C1以及R2是Br。 367A Q2是5-F-3-吡啶基，R1是C1以及R2是α。 368A Q2是5-Me-3-吡啶基，R1是Cl以及R2是Me。 369A Q2是5-Me-3-吡啶基，R1是C1以及R2是CFH2。 370A Q2是5-Me-3-吡啶基，R1是Br以及R2是Me。 371A Q2是5-Me-3-吡啶基，R1是I以及R2是Me。 372A Q2是5-Me-3-°比咬基，R1是Me以及R2是Me。 373A Q2是5-Me-3-吡啶基，R1是Me以及R2是α。 374A Q2是5-Me-3-吡啶基，R1是Me以及R2是Br。 375A Q2是5-Me-3-吡啶基，R1是Me以及R2是I。 376A Q2是5-Me-3-吡啶基，R1是Br以及R2是Br。 377A Q2是5-Me-3-吡啶基，R1是Br以及R2是α。 378A Q2是5-Me-3-吡啶基，R1是C1以及R2是Br。 379A Q2是5-Me-3-吡啶基，R1是C1以及R2是C卜 380A Q2是5-MeO-3-吡啶基，R1是C1以及R2是Me·。 381A Q2是5-MeO-3-吡啶基，R1是Cl以及R2是CFH2。 382A Q2是5-MeO-3-吡啶基，R1是Br以及R2是Me。 383A Q2是5-MeO-3-吡啶基，R1是I以及R2是Me。 384A Q2是5-MeO-3-吡啶基，R1是Me以及R2是Me。 385A Q2是5-MeO-3-吡啶基，Ri是Me以及R2是C1。 386A Q2是5-MeO-3-吡啶基，R1是Me以及R2是Br。 387A Q2是5-MeO-3-吡啶基，R1是Me以及R2是I。 388A Q2是5-MeO-3-吡啶基，R1是Br以及R2是Br。 389A Q2是5-MeO-3-吡啶基，R1是Br以及R2是C1。 390A Q2是5-MeO-3-吡啶基，R1是C1以及R2是Br。 391A Q2是5-MeO-3-吡啶基，R1是C1以及R2是C1。 392A Q2 是 6-C1、5-MeO-3-吡啶基，R1 是 C1 以及 R2 是 Me。 393A Q2 是 6-a、5-MeO-3-吡啶基，R1 是 C1 以及 R2 是 CFH2。 151284.doc - 126- 201117722 表 列標題 394A Q2 是 6-C1、5-MeO-3-吡啶基，R1 是 Br 以及 R2 是 Me。 395A Q2是6-C1、5-MeO-3-吡啶基，R1是I以及R2是Me。 396A Q2 是 6-CI、5-MeO-3-吡啶基，R1 是 Me 以及 R2 是 Me。 397A Q2 是 6-C1、5-MeO-3-吡啶基，R1 是 Me 以及 R2 是 C1。 398A Q2 是 6-C1、5-MeO-3-吡啶基，R1 是 Me 以及 R2 是 Br。 399A Q2是6-C1、5-MeO-3-吡啶基，R1是Me以及R2是I。 400A Q2 是 6-C1、5-MeO-3-吡啶基，R1 是 Br 以及 R2 是 Br。 401A Q2是6-C1、5-MeO-3-吡啶基，R1是Br以及R2是α。 402A Q2 是 6-C1、5-MeO-3-吡啶基，R1 是 C1 以及 R2 是 Br。 403A Q2 是 6-C1、5-MeO-3-吡啶基，R1 是 C1 以及 R2 是 C1。 404A Q2是6-CI-3-嗒畊基，R1是C1以及R2是Me。 405A Q2是6-C1-3-嗒畊基，R1是C1以及R2是CFH2。 406A Q2是6-C1-3-嗒畊基，R1是Br以及R2是Me。 407A Q2是6-C1-3-嗒畊基，R1是I以及R2是Me。 408A Q2是6-C1-3-嗒畊基，R1是Me以及R2是Me。 409A Q2是6-C1-3-嗒畊基，R1是Me以及R2是C1。 410A Q2是6-C1-3-嗒畊基，R1是Me以及R2是Br。 411A Q2是6-C1-3-嗒畊基，R1是Me以及R2是I。 412A Q2是6-C1-3-嗒畊基，R1是Br以及R2是Br。 413A Q2是6-C1-3-嗒畊基，R1是Br以及R2是C1。 414A Q2是6-C1-3-嗒畊基，R1是C1以及R2是Br。 415A Q2是6-C1-3-嗒畊基，R1是C1以及R2是C1。 416A Q2是6-Me-3-嗒畊基，R1是C1以及R2是Me。 417A Q2是6-Me-3-嗒畊基，R1是C1以及R2是CFH2。 418A Q2是6-Me-3-嗒p井基，R1是Br以及R2是Me。 419A Q2是6-Me-3-嗒畊基，R1是I以及R2是Me。 420A Q2是6-Me-3-嗒p井基，R1是Me以及R2是Me。 421A Q2是6-Me-3-嗒畊基，R1是Me以及R2是CH。 422A Q2是6-Me-3-嗒》井基，R1是Me以及R2是Br。 423A Q2是6-Me-3-嗒畊基，R1是Me以及R2是I。 424A Q2是6-Me-3-嗒畊基，R1是Br以及R2是Br » 425A Q2是6-Me-3-嗒畊基，R1是Br以及R2是α。 426A Q2是6-Me-3-嗒-井基，R1是C1以及R2是Br。 427A Q2是6-Me-3-嗒畊基，R1是C1以及R2是C1。 428A Q2是6-MeO-3-嗒畊基，R1是C1以及R2是Me。 151284.doc -127- 201117722 表 列標題 429A Q2是6-MeO-3-嗒p井基，R1是Cl以及R2是CFH2 430A Q2是6-MeO-3-嗒畊基，R1是Br以及R2是Me。 431A Q2是6-MeO-3-嗒11井基，R1是I以及R2是Me。 432A Q2是6-MeO-3-嗒畊基，R1是Me以及R2是Me。 433A Q2是6-MeO-3-嗒畊基，R1是Me以及R2是α。 434A Q2是6-MeO-3-嗒畊基，R1是Me以及R2是Br。 435A Q2是6-MeO-3-嗒11井基，R1是Me以及R2是I。 436A Q2是6-MeO-3-嗒畊基，R1是Br以及R2是Br。 437A Q2是6-MeO-3-嗒畊基，R1是Br以及R2是C1。 438A Q2是6-MeO-3-嗒〃井基，R1是C1以及R2是Br。 439A Q2是6-MeO-3-嗒-井基，R1是C1以及R2是α。 440A Q2是6-CF3-3-嗒畊基，R1是C1以及R2是Me。 441A Q2是6-CF3-3-嗒畊基，R1是C1以及R2是CFH2。 442A Q2是6-CF3-3-嗒畊基，R1是Br以及R2是Me。 443A Q2是6-CF3-3-嗒畊基，R1是I以及R2是Me。 444A Q2是6-CF3-3-嗒畊基，R1是Me以及R2是Me。 445A Q2是6-CF3-3-嗒畊基，R1是Me以及R2是C1。 446A Q2是6-CF3-3-嗒畊基，R1是Me以及R2是Br。 447A Q2是6-CF3-3-嗒畊基，R1是Me以及R2是I。 448A Q2是6-CF3-3-嗒畊基，R1是Br以及R2是Br。 449A Q2是6-CF3-3-嗒畊基，R1是Br以及R2是CM。 450A Q2是6-CF3-3-嗒畊基，R1是C1以及R2是Br。 451A Q2是6-CF3-3-嗒畊基，R1是C1以及R2是C1。 452A Q2是5-C1-3-嗒畊基，R1是C1以及R2是Me。 453A Q2是5-C1-3-嗒啩基，R1是C1以及R2是CFH2。 454A Q2是5-C1-3-嗒畊基，R1是Br以及R2是Me。 455A Q2是5-C1-3-嗒井基，R1是I以及R2是Me。 456A Q2是5-C1-3-嗒畊基，R1是Me以及R2是Me。 457A Q2是5-C1-3-嗒畊基，R1是Me以及R2是（：卜 458A Q2是5-C1-3-嗒哨·基，R1是Me以及R2是Br。 459A Q2是5-C1-3-嗒畊基，R1是Me以及R2是I。 460A Q2是5-C1-3-嗒畊基，R1是Br以及R2是Br。 461A Q2是5-C1-3-嗒-井基，R1是Br以及R2是C1。 462A Q2是5-C1-3-嗒〇井基，R1是C1以及R2是Br。 463A Q2是5-C1-3-嗒'井基，R1是C1以及R2是CM。 151284.doc -128- 201117722 表 列標題 464A Q2是5-F-3-嗒啫基，R1是Cl以及R2是Me。 465A Q2是5-F-3-嗒啩基，R1是C1以及R2是CFH2。 466A Q2是5-F-3-嗒畊基，R1是Br以及R2是Me。 467A Q2是5-F-3-嗒畊基，R1是I以及R2是Me。 468A Q2是5-F-3-嗒畊基，R1是Me以及R2是Me。 469A Q2是5-F-3-嗒啩基，R1是Me以及R2是C卜 470A Q2是5-F-3-嗒畊基，R1是Me以及R2是Br。 471A Q2是5-F-3-嗒啩基，R1是Me以及R2是I。 472A Q2是5-F-3-嗒畊基，R1是Br以及R2是Br。 473A Q2是5-F-3-嗒畊基，R1是Br以及R2是C1。 474A Q2是5-F-3-嗒畊基，R1是C1以及R2是Br。 475A Q2是5-F-3-嗒畊基，R1是C1以及R2是C1。 476A Q2是5-MeO-3-嗒畊基，R1是C1以及R2是Me。 477A Q2是5-MeO-3-嗒畊基，R1是C1以及R2是CFH2。 478A Q2是5-MeO-3-嗒畊基，R1是Br以及R2是Me。 479A Q2是5-MeO-3-嗒畊基，R1是I以及R2是Me。 480A Q2是5-MeO-3-嗒-井基，R1是Me以及R2是Me。 481A Q2是5-MeO-3-嗒畊基，R1是Me以及R2是C卜 482A Q2是5-MeO-3-嗒畊基，R1是Me以及R2是Br。 483A Q2是5-MeO-3-嗒p井基，R1是Me以及R2是I。 484A Q2是5-MeO-3-嗒畊基，R1是Br以及R2是Br。 485A Q2是5-MeO-3-嗒啩基，R1是Br以及R2是C1。 486A Q2是5-MeO-3-嗒畊基，R1是C1以及R2是Br。 487A Q2是5-MeO-3-嗒畊基，R1是C1以及R2是C1。 488A Q2是2-C1-5-嘧啶，R1是C1以及R2是Me。 489A Q2是2-C1-5-嘧啶，R1是C1以及R2是CFH2。 490A Q2是2-C1-5-嘧啶，R1是Br以及R2是Me。 491A Q2是2-C1-5-嘧啶，R1是I以及R2是Me。 492A Q2是2-C1-5-嘧啶，R1是Me以及R2是Me。 493A Q2是2-C1-5嘧啶，R1是Me以及R2是C1。 494A Q2是2-C1-5-嘧啶，R1是Me以及R2是Br。 495A Q2是2-C1-5-嘧啶，R1是Me以及R2是I。 496A Q2是2-C1-5-嘧啶，R1是Br以及R2是Br。 497A Q2是2-C1-5-嘧啶，R1是Br以及R2是C1。 498A Q2是2-C1-5-嘧啶，R1是C1以及R2是Br。 151284.doc · 129· 201117722 表 列標題 499A Q2 是 2-C1-5-嘧啶， 是C1以及R2是C卜 500A Q2 是 2-Me-5-嘧啶， R1是C1以及R2是Me。 501A Q2 是 2-Me-5-°^咬， R1是C1以及R2是CFH2。 502A Q2 是 2-Me-5-°^咬， R1是Br以及R2是Me。 503A Q2 是 2-Me-5-嘧啶， R1是I以及R2是Me。 504A Q2 是 2-Me-5-嘧啶， R1是Me以及R2是Me。 505A Q2 是 2-Me-5-嘧啶， R1是Me以及R2是（：卜 506A Q2 是 2-Me-5-°® 咬， R1是Me以及R2是Br。 507A Q2 是 2-Me-5-嘧啶， R1是Me以及R2是I。 508A Q2 是 2-Me-5-°^咬， R1是Br以及R2是Br。 509A Q2 是 2-Me-5-嘧啶， R1是Br以及R2是α。 510A Q2 是 2-Me-5-嘧啶， R1是C1以及R2是Br。 511A Q2 是 2-Me-5-,咬， R1是C1以及R2是C1。 512A Q2 是 2-MeO-5-嘧啶 ，R1是C1以及R2是Me。 513A Q2 是 2-MeO-5-嘧啶 ，R1是C1以及R2是CFH2。 514A Q2 是 2-MeO-5-嘧啶 ，R1是Br以及R2是Me。 515A Q2 是 2-MeO-5-嘧啶 ，R1是I以及R2是Me。 516A Q2 是 2-MeO-5-嘧啶 ，R1是Me以及R2是Me。 517A Q2 是 2-MeO-5-嘧啶 ，R1是Me以及R2是α。 518A Q2 是 2-MeO-5-嘧啶 ，R1是Me以及R2是Br。 519A Q2 是 2-MeO-5-嘧啶 ，R1是Me以及R2是I。 520A Q2是2-MeO-5嘧啶 ，R1是Br以及R2是Br。 521A Q2 是 2-MeO-5-嘧啶 ，R1是Βι•以及R2是C卜 522A Q2 是 2-MeO-5-嘧啶 ，R1是C1以及R2是Br。 523A Q2 是 2-MeO-5-嘧啶 ，R1是C1以及R2是C1。 524A Q2 是 2-CF3-5-嘧啶， R1是C1以及R2是Me。 525A Q2 是 2-CF3-5-嘧啶， R1是C1以及R2是CFH2。 526A Q2 是 2-CF3-5-嘧啶， R1是Br以及R2是Me。 527A Q2 是 2-CF3-5-嘧啶， R1是I以及R2是Me。 528A Q2 是 2-CF3-5-嘧啶， R1是Me以及R2是Me。 529A Q2 是 2-CF3-5-嘧啶， R1是Me以及R2是C卜 530A Q2 是 2-CF3-5-嘧啶， R1是Me以及R2是Br。 531A Q2 是 2-CF3-5-嘧啶， R1是Me以及R2是I。 532A Q2 是 2-CF3-5-嘧啶， R1是Br以及R2是Br。 533A Q2 是 2-CF3-5-嘧啶’ R1是Br以及R2是C1。 151284.doc •130·201117722 Table 324A 325A 326A 327A 328A 329A 330A 331A 332A 333A 334A 335A 336A 337A 338A 339A 340A 341A 342A 343A 344A 345A 346A 347A 348A 349A 350A 351A 352A 353A 354A 355A 356A 357A 358A Column heading Q2 is 2-C1, 6-MeO-3 Pyridyl, R1 is Me and R2 is Me. Q2 is 2-C1, 6-MeO-3-pyridyl, R1 is Me and R2 is C1. Q2 is 2-C1, 6-MeO-3-pyridyl, R1 is Me and R2 is Br. Q2 is 2-C1, 6-MeO-3-pyridyl, R1 is Me and R2 is I. Q2 is 2-C1, 6-MeO-3-pyridyl, R1 is Br and R2 is Br. Q2 is 2-C1, 6-MeO-3-pyridyl, R1 is Br and R2 is C1. Q2 is 2-Q, 6-MeO-3-pyridyl, R1 is C1 and R2 is Br. Q2 is 2-C1, 6-MeO-3-pyridyl, R1 is C1 and R2 is C1. Q2 is 2-C1, 6-CF3-3-pyridyl, R1 is C1 and R2 is Me. Q2 is 2-a, 6-CF3-3-pyridyl, R1 is C1 and R2 is CFH2. Q2 is 2-C1, 6-CF3-3-pyridyl, R1 is Br and R2 is Me. Q2 is 2-C1, 6-CF3-3-pyridyl, R1 is I and R2 is Me. Q2 is 2-C1, 6-CF3-3-pyridyl, R1 is Me and R2 is Me. Q2 is 2-C1, 6-CF3-3-pyridyl, R1 is Me and R2 is C1. Q2 is 2-C1, 6-CF3-3-pyridyl, R1 is Me and R2 is Br. Q2 is 2-C1, 6-CF3-3-pyridyl, R1 is Me and R2 is I. Q2 is 2-C1, 6-CF3-3-pyridyl, R1 is Br and R2 is Br. Q2 is 2-C1, 6-CF3-3-pyridyl, R1 is Br and R2 is α. Q2 is 2-C1, 6-CF3-3-pyridyl, R1 is C1 and R2 is Br. Q2 is 2-C1, 6-CFr3-pyridyl, R1 is C1 and R2 is C1. Q2 is 5-C1-3-pyridyl, R丨 is C1 and R2 is Me. Q2 is 5-C1-3-pyridyl, R1 is C1 and R2 is CFH2. Q2 is 5-C1-3-pyridyl, R1 is Br and R2 is Me. Q2 is 5-C1-3-pyridyl, R1 is I and R2 is Me. Q2 is 5-C1-3-pyridyl, R1 is Me and R2 is Me. Q2 is 5-C1-3-pyridyl, R1 is Me and R2 is α. Q2 is 5-C1-3-. In the case of a pyridinyl group, R1 is Me and R2 is Br. Q2 is 5-C1-3-pyridyl, R1 is Me and R2 is I. Q2 is 5-C1-3-. In the case of a pyridinyl group, R1 is Br and R2 is Br. Q2 is 5-C1-3-pyridyl, R1 is Br and R2 is C1. Q2 is 5-C1-3-pyridyl, R1 is C1 and R2 is Br. Q2 is 5-C1-3-. In the case of a pyridyl group, R1 is C1 and R2 is C1. Q2 is 5-F-3-pyridyl, R1 is C1 and R2 is Me»Q2 is 5-F-3-pyridyl, R1 is Cl and R2 is CFH2. Q2 is 5-F-3-pyridyl, R1 is Br and R2 is Me. 151284.doc -125- 201117722 Table Column heading 359A Q2 is 5-F-3-pyridyl, R1 is I and R2 is Me. 360A Q2 is 5-F-3-pyridyl, R1 is Me and R2 is Me. 361A Q2 is 5-F-3-pyridyl, R1 is Me and R2 is α. 362A Q2 is 5-F-3-pyridyl, R1 is Me and R2 is Br. 363A Q2 is 5-F-3-pyridinyl, R1 is Me and R2 is I. 364A Q2 is 5-F-3-pyridinyl, R1 is Br and R2 is Br. 365A Q2 is 5-F-3-pyridyl, R1 is Br and R2 is alpha. 366A Q2 is 5-F-3-pyridinyl, R1 is C1 and R2 is Br. 367A Q2 is 5-F-3-pyridyl, R1 is C1 and R2 is α. 368A Q2 is 5-Me-3-pyridyl, R1 is Cl and R2 is Me. 369A Q2 is 5-Me-3-pyridyl, R1 is C1 and R2 is CFH2. 370A Q2 is 5-Me-3-pyridyl, R1 is Br and R2 is Me. 371A Q2 is 5-Me-3-pyridyl, R1 is I and R2 is Me. 372A Q2 is a 5-Me-3-° ratio bite base, R1 is Me and R2 is Me. 373A Q2 is 5-Me-3-pyridyl, R1 is Me and R2 is α. 374A Q2 is 5-Me-3-pyridyl, R1 is Me and R2 is Br. 375A Q2 is 5-Me-3-pyridyl, R1 is Me and R2 is I. 376A Q2 is 5-Me-3-pyridyl, R1 is Br and R2 is Br. 377A Q2 is 5-Me-3-pyridyl, R1 is Br and R2 is α. 378A Q2 is 5-Me-3-pyridyl, R1 is C1 and R2 is Br. 379A Q2 is 5-Me-3-pyridyl, R1 is C1 and R2 is CBu 380A Q2 is 5-MeO-3-pyridyl, R1 is C1 and R2 is Me. 381A Q2 is 5-MeO-3-pyridyl, R1 is Cl and R2 is CFH2. 382A Q2 is 5-MeO-3-pyridyl, R1 is Br and R2 is Me. 383A Q2 is 5-MeO-3-pyridyl, R1 is I and R2 is Me. 384A Q2 is 5-MeO-3-pyridyl, R1 is Me and R2 is Me. 385A Q2 is 5-MeO-3-pyridyl, Ri is Me and R2 is C1. 386A Q2 is 5-MeO-3-pyridyl, R1 is Me and R2 is Br. 387A Q2 is 5-MeO-3-pyridyl, R1 is Me and R2 is I. 388A Q2 is 5-MeO-3-pyridyl, R1 is Br and R2 is Br. 389A Q2 is 5-MeO-3-pyridyl, R1 is Br and R2 is C1. 390A Q2 is 5-MeO-3-pyridyl, R1 is C1 and R2 is Br. 391A Q2 is 5-MeO-3-pyridyl, R1 is C1 and R2 is C1. 392A Q2 is 6-C1, 5-MeO-3-pyridyl, R1 is C1 and R2 is Me. 393A Q2 is 6-a, 5-MeO-3-pyridyl, R1 is C1 and R2 is CFH2. 151284.doc - 126- 201117722 Table Column heading 394A Q2 is 6-C1,5-MeO-3-pyridyl, R1 is Br and R2 is Me. 395A Q2 is 6-C1, 5-MeO-3-pyridyl, R1 is I and R2 is Me. 396A Q2 is 6-CI, 5-MeO-3-pyridyl, R1 is Me and R2 is Me. 397A Q2 is 6-C1, 5-MeO-3-pyridyl, R1 is Me and R2 is C1. 398A Q2 is 6-C1, 5-MeO-3-pyridyl, R1 is Me and R2 is Br. 399A Q2 is 6-C1, 5-MeO-3-pyridyl, R1 is Me and R2 is I. 400A Q2 is 6-C1, 5-MeO-3-pyridyl, R1 is Br and R2 is Br. 401A Q2 is 6-C1, 5-MeO-3-pyridyl, R1 is Br and R2 is α. 402A Q2 is 6-C1, 5-MeO-3-pyridyl, R1 is C1 and R2 is Br. 403A Q2 is 6-C1, 5-MeO-3-pyridyl, R1 is C1 and R2 is C1. 404A Q2 is 6-CI-3-嗒 tillage, R1 is C1 and R2 is Me. 405A Q2 is a 6-C1-3-hydroponic group, R1 is C1 and R2 is CFH2. 406A Q2 is 6-C1-3-嗒 tillage, R1 is Br and R2 is Me. 407A Q2 is 6-C1-3-嗒 嗒, R1 is I and R2 is Me. 408A Q2 is 6-C1-3-嗒 基, R1 is Me and R2 is Me. 409A Q2 is 6-C1-3-嗒 tillage, R1 is Me and R2 is C1. 410A Q2 is a 6-C1-3-hydroponic group, R1 is Me and R2 is Br. 411A Q2 is 6-C1-3-嗒 嗒, R1 is Me and R2 is I. 412A Q2 is a 6-C1-3-hydroponic group, R1 is Br and R2 is Br. 413A Q2 is a 6-C1-3-hydroponic group, R1 is Br and R2 is C1. 414A Q2 is 6-C1-3-嗒 嗒, R1 is C1 and R2 is Br. 415A Q2 is 6-C1-3-嗒 嗒, R1 is C1 and R2 is C1. 416A Q2 is 6-Me-3-嗒 tillage, R1 is C1 and R2 is Me. 417A Q2 is 6-Me-3-嗒 tillage, R1 is C1 and R2 is CFH2. 418A Q2 is a 6-Me-3-嗒p well, R1 is Br and R2 is Me. 419A Q2 is 6-Me-3-嗒 tillage, R1 is I and R2 is Me. 420A Q2 is a 6-Me-3-嗒p well base, R1 is Me and R2 is Me. 421A Q2 is a 6-Me-3-嗒 cultivating base, R1 is Me and R2 is CH. 422A Q2 is a 6-Me-3-嗒 well, R1 is Me and R2 is Br. 423A Q2 is 6-Me-3-嗒 tillage, R1 is Me and R2 is I. 424A Q2 is 6-Me-3-嗒 tillage, R1 is Br and R2 is Br » 425A Q2 is 6-Me-3-嗒 tillage, R1 is Br and R2 is α. 426A Q2 is a 6-Me-3-嗒-well group, R1 is C1 and R2 is Br. 427A Q2 is a 6-Me-3-嗒 cultivating base, R1 is C1 and R2 is C1. 428A Q2 is 6-MeO-3-嗒 tillage, R1 is C1 and R2 is Me. 151284.doc -127- 201117722 Table heading 429A Q2 is 6-MeO-3-嗒p well base, R1 is Cl and R2 is CFH2 430A Q2 is 6-MeO-3-嗒 tillage, R1 is Br and R2 is Me. 431A Q2 is a 6-MeO-3-嗒11 well group, R1 is I and R2 is Me. 432A Q2 is a 6-MeO-3-indole, R1 is Me and R2 is Me. 433A Q2 is a 6-MeO-3-嗒 cultivating base, R1 is Me and R2 is α. 434A Q2 is a 6-MeO-3-indole, R1 is Me and R2 is Br. 435A Q2 is a 6-MeO-3-嗒11 well, R1 is Me and R2 is I. 436A Q2 is a 6-MeO-3-indole, R1 is Br and R2 is Br. 437A Q2 is a 6-MeO-3-indole, R1 is Br and R2 is C1. 438A Q2 is a 6-MeO-3-嗒〃 well group, R1 is C1 and R2 is Br. 439A Q2 is a 6-MeO-3-嗒-well group, R1 is C1 and R2 is α. 440A Q2 is a 6-CF3-3-indole, R1 is C1 and R2 is Me. 441A Q2 is a 6-CF3-3-indole, R1 is C1 and R2 is CFH2. 442A Q2 is a 6-CF3-3-indole, R1 is Br and R2 is Me. 443A Q2 is a 6-CF3-3-indole, R1 is I and R2 is Me. 444A Q2 is a 6-CF3-3-indole, R1 is Me and R2 is Me. 445A Q2 is a 6-CF3-3-indole, R1 is Me and R2 is C1. 446A Q2 is a 6-CF3-3-indole, R1 is Me and R2 is Br. 447A Q2 is a 6-CF3-3-indole, R1 is Me and R2 is I. 448A Q2 is a 6-CF3-3-indole, R1 is Br and R2 is Br. 449A Q2 is a 6-CF3-3-indole, R1 is Br and R2 is CM. 450A Q2 is a 6-CF3-3-indole, R1 is C1 and R2 is Br. 451A Q2 is a 6-CF3-3-indole, R1 is C1 and R2 is C1. 452A Q2 is 5-C1-3-嗒 tillage, R1 is C1 and R2 is Me. 453A Q2 is 5-C1-3-fluorenyl, R1 is C1 and R2 is CFH2. 454A Q2 is 5-C1-3-嗒 tillage, R1 is Br and R2 is Me. 455A Q2 is 5-C1-3-嗒 well base, R1 is I and R2 is Me. 456A Q2 is 5-C1-3-嗒 嗒, R1 is Me and R2 is Me. 457A Q2 is 5-C1-3-嗒耕基, R1 is Me and R2 is (: Bu 458A Q2 is 5-C1-3-嗒 · · base, R1 is Me and R2 is Br. 459A Q2 is 5-C1 -3-嗒耕基, R1 is Me and R2 is I. 460A Q2 is 5-C1-3-嗒耕基, R1 is Br and R2 is Br. 461A Q2 is 5-C1-3-嗒-well, R1 is Br and R2 is C1. 462A Q2 is 5-C1-3-嗒〇 well base, R1 is C1 and R2 is Br. 463A Q2 is 5-C1-3-嗒' well base, R1 is C1 and R2 is CM. 151284.doc -128- 201117722 Table heading 464A Q2 is 5-F-3-mercapto, R1 is Cl and R2 is Me. 465A Q2 is 5-F-3-mercapto, R1 is C1 and R2 is CFH2. 466A Q2 is 5-F-3-嗒 tillage, R1 is Br and R2 is Me. 467A Q2 is 5-F-3-嗒 tillage, R1 is I and R2 is Me. 468A Q2 is 5 -F-3-嗒耕基, R1 is Me and R2 is Me. 469A Q2 is 5-F-3-mercapto, R1 is Me and R2 is CBu 470A Q2 is 5-F-3-嗒R1 is Me and R2 is Br. 471A Q2 is 5-F-3-indenyl, R1 is Me and R2 is I. 472A Q2 is 5-F-3-indole, R1 is Br and R2 is Br 473A Q2 is 5-F-3-嗒 tillage, R1 is Br and R2 is C1. 474A Q2 is 5-F-3-嗒 tillage, R1 is C1 and R2 is Br. 475A Q2 is 5-F-3-嗒 tillage, R1 is C1 and R2 is C1. 476A Q2 is 5-MeO-3-嗒 tillage, R1 is C1 and R2 is Me. 477A Q2 is 5 -MeO-3-嗒耕基, R1 is C1 and R2 is CFH2. 478A Q2 is 5-MeO-3-嗒 tillage, R1 is Br and R2 is Me. 479A Q2 is 5-MeO-3-嗒R1 is I and R2 is Me. 480A Q2 is 5-MeO-3-嗒-well, R1 is Me and R2 is Me. 481A Q2 is 5-MeO-3-嗒 tillage, R1 is Me and R2 is C Bu 482A Q2 is 5-MeO-3-嗒 tillage, R1 is Me and R2 is Br. 483A Q2 is 5-MeO-3-嗒p well base, R1 is Me and R2 is I. 484A Q2 is 5- MeO-3-嗒耕基, R1 is Br and R2 is Br. 485A Q2 is 5-MeO-3-fluorenyl, R1 is Br and R2 is C1. 486A Q2 is 5-MeO-3-嗒 arable, R1 is C1 and R2 is Br. 487A Q2 is 5-MeO-3-嗒 tillage, R1 is C1 and R2 is C1. 488A Q2 is 2-C1-5-pyrimidine, R1 is C1 and R2 is Me. 489A Q2 is 2-C1-5-pyrimidine, R1 is C1 and R2 is CFH2. 490A Q2 is 2-C1-5-pyrimidine, R1 is Br and R2 is Me. 491A Q2 is 2-C1-5-pyrimidine, R1 is I and R2 is Me. 492A Q2 is 2-C1-5-pyrimidine, R1 is Me and R2 is Me. 493A Q2 is a 2-C1-5 pyrimidine, R1 is Me and R2 is C1. 494A Q2 is 2-C1-5-pyrimidine, R1 is Me and R2 is Br. 495A Q2 is 2-C1-5-pyrimidine, R1 is Me and R2 is I. 496A Q2 is 2-C1-5-pyrimidine, R1 is Br and R2 is Br. 497A Q2 is 2-C1-5-pyrimidine, R1 is Br and R2 is C1. 498A Q2 is 2-C1-5-pyrimidine, R1 is C1 and R2 is Br. 151284.doc · 129· 201117722 Table Column heading 499A Q2 is 2-C1-5-pyrimidine, is C1 and R2 is CBu 500A Q2 is 2-Me-5-pyrimidine, R1 is C1 and R2 is Me. 501A Q2 is a 2-Me-5-°^ bite, R1 is C1 and R2 is CFH2. 502A Q2 is a 2-Me-5-°^ bite, R1 is Br and R2 is Me. 503A Q2 is 2-Me-5-pyrimidine, R1 is I and R2 is Me. 504A Q2 is 2-Me-5-pyrimidine, R1 is Me and R2 is Me. 505A Q2 is 2-Me-5-pyrimidine, R1 is Me and R2 is (: Bu 506A Q2 is 2-Me-5-°® bite, R1 is Me and R2 is Br. 507A Q2 is 2-Me-5- Pyrimidine, R1 is Me and R2 is I. 508A Q2 is 2-Me-5-° bit, R1 is Br and R2 is Br. 509A Q2 is 2-Me-5-pyrimidine, R1 is Br and R2 is α. 510A Q2 is 2-Me-5-pyrimidine, R1 is C1 and R2 is Br. 511A Q2 is 2-Me-5-, biting, R1 is C1 and R2 is C1. 512A Q2 is 2-MeO-5-pyrimidine, R1 is C1 and R2 is Me. 513A Q2 is 2-MeO-5-pyrimidine, R1 is C1 and R2 is CFH2. 514A Q2 is 2-MeO-5-pyrimidine, R1 is Br and R2 is Me. 515A Q2 is 2 -MeO-5-pyrimidine, R1 is I and R2 is Me. 516A Q2 is 2-MeO-5-pyrimidine, R1 is Me and R2 is Me. 517A Q2 is 2-MeO-5-pyrimidine, R1 is Me and R2 Is α. 518A Q2 is 2-MeO-5-pyrimidine, R1 is Me and R2 is Br. 519A Q2 is 2-MeO-5-pyrimidine, R1 is Me and R2 is I. 520A Q2 is 2-MeO-5 pyrimidine R1 is Br and R2 is Br. 521A Q2 is 2-MeO-5-pyrimidine, R1 is Βι• and R2 is C 522A Q2 is 2-MeO-5-pyrimidine, R1 is C1 and R2 is Br. 523A Q2 Yes 2 -MeO-5-pyrimidine, R1 is C1 and R2 is C1. 524A Q2 is 2-CF3-5-pyrimidine, R1 is C1 and R2 is Me. 525A Q2 is 2-CF3-5-pyrimidine, R1 is C1 and R2 Is CFH 2. 526A Q2 is 2-CF3-5-pyrimidine, R1 is Br and R2 is Me. 527A Q2 is 2-CF3-5-pyrimidine, R1 is I and R2 is Me. 528A Q2 is 2-CF3-5- Pyrimidine, R1 is Me and R2 is Me. 529A Q2 is 2-CF3-5-pyrimidine, R1 is Me and R2 is CBu 530A Q2 is 2-CF3-5-pyrimidine, R1 is Me and R2 is Br. 531A Q2 Is a 2-CF3-5-pyrimidine, R1 is Me and R2 is I. 532A Q2 is 2-CF3-5-pyrimidine, R1 is Br and R2 is Br. 533A Q2 is 2-CF3-5-pyrimidine' R1 is Br and R2 is C1. 151284.doc •130·

201117722 表 534A 535A 536A 537A 538A 539A 540A 541A 542A 543A 544A 545A 546A 547A 548A 549A 550A 551A 552A 553A 554A 555A 556A 557A 558A 559A 560A 561A 562A 563A 564A 565A 566A 567A 568A 列標題 Q2是2-CF3-5-嘧啶，R1是Cl以及R2是Br » Q2是2-CF3-5-嘧啶，R1是Cl以及R2是C卜 Q2是5-C1-2-嘧啶，R1是C1以及R2是Me。 Q2是5-CI-2-嘧啶，R1是C1以及R2是CFH2。 Q2是5-C1-2-嘧啶，R1是Br以及R2是Me。 Q2是5-C1-2-嘧啶，R1是I以及R2是Me。 Q2是5-C1-2-嘧啶，R1是Me以及R2是Me。 Q2是5-C1-2-嘧啶，R1是Me以及R2是α。 Q2是5-C1-2-嘧啶，R1是Me以及R2是Br。 Q2是5-C1-2-嘧啶，R1是Me以及R2是I。 Q2是5-C1-2-嘧啶，R1是Br以及R2是Br。 Q2是5-C1-2-嘧啶，R1是Br以及R2是C1。 Q2是5-C1-2-嘧啶，R1是C1以及R2是Br。 Q2是5-C1-2-嘧啶，R1是C1以及R2是C1。 Q2是5-Me-2-嘧啶 ，R1 是 C1以及R2是Me。 Q2是5-Me-2-嘧咬 ，R1 是 C1以及R2 是 cfh2 Q2是5-Me-2-嘧咬 ，R1 是 Br以及R2是Me。 Q2 是 5-Me-2-°密咬 ，R1 是 I以及R2是Me。 Q2 是 5-Me-2-°® 咬 ，R1 是 Me以及R' !是 Me。 Q2 是 5-Me-2-°^ 咬 ，R1 是 Me以及R: 2是 Cl。 Q2是5-Me-2-鳴咬 ，R1 是 Me以及R: !是 Br。 Q2 是 5-Me-2-°f 咬 ，R1 是 Me以及R2是I。 Q2 是 5-Me-2-°密咬 ，R1 是 Br以及R2 是Br。 Q2是5-Me-2-嘧咬 ，R1 是 Br以及R2 是Cl。 Q2是5-Me-2-嘧啶 &gt; R1 是 Cl以及R2 是Br。 Q2 是 5-Me-2-°^ 咬 ，R1 是 Cl以及R2是Cl。 Q2是5-MeO-2-嘧啶，R1是C1以及R2是Me。 Q2 是 5-MeO-2-嘧啶，R1 是 C1 以及 R2 是 CFH2。 Q2是5-MeO-2-嘧啶，R1是Br以及R2是Me。 Q2是5-MeO-2-嘧啶，R1是I以及R2是Me。 Q2是5-MeO-2-嘧啶，R1是Me以及R2是Me。 Q2是5-MeO-2-嘧啶，R1是Me以及R2是C1。 Q2是5-MeO-2-嘧啶，R1是Me以及R2是Br。 Q2是5-MeO-2-嘧啶，R1是Me以及R2是I。 Q2是5-MeO-2-嘧啶，R1是Br以及R2是Br。 151284.doc -131 201117722 表 列標題 569A Q2是5-MeO-2-嘧啶，R1是Br以及R2是Cl。 570A Q2是5-MeO-2-嘧啶，R1是C1以及R2是Br。 571A Q2是5-MeO-2-嘧啶，R1是C1以及R2是C1。 572A Q2是5-C1-2-嘧啶，R1是C1以及R2是Me。 573A Q2是5-C1-2-嘧啶，R1是C1以及R2是CFH2。 574A Q2是5-C1-2-嘧啶，R1是Br以及R2是Me。 575A Q2是5-C1-2-嘧啶，R1是I以及R2是Me。 576A Q2是5-C1-2-嘧啶，R1是Me以及R2是Me。 577A Q2是5-C1-2-嘧啶，R1是Me以及R2是α。 578A Q2是5-C1-2-嘧啶，R1是Me以及R2是Br。 579A Q2是5-C1-2-嘧啶，R1是Me以及R2是I。 580A Q2是5-C1-2-嘧啶，R1是Br以及R2是Br。 581A Q2是5-C1-2-嘧啶，R1是Br以及R2是α。 582A Q2是5-C1-2-嘧啶，R1是C1以及R2是Br。 583A Q2是5-CI-2-嘧啶，R1是C1以及R2是CH。 584A Q2是5-CF3-2-嘧啶，R1是C1以及R2是Me。 585A Q2 是 5-CF3-2-嘧啶，R1 是 C1 以及 R2 是 CFH2。 586A Q2是5-CF3-2-嘧啶，R1是Br以及R2是Me。 587A Q2是5-CF3-2-嘧啶，R1是I以及R2是Me。 588A Q2是5-CF3-2-嘧啶，R1是Me以及R2是Me。 589A Q2是5-CF3-2-嘧啶，R1是Me以及R2是C卜 590A Q2是5-CF3-2-嘧啶，Ri是Me以及R2是Br。 591A Q2是5-CF3-2-嘧啶，R1是Me以及R2是I。 592A Q2是5-CF3-2-嘧啶，R1是Br以及R2是Br。 593A Q2是5-CF3-2-嘧啶，R1是Br以及R2是C1。 594A Q2是5-CF3-2-嘧啶，R1是C1以及R2是Br。 595A Q2是5-CF3-2-嘧啶，R1是C1以及R2是CU。 596A Q2是5-Me-2-噻吩基，R1是C1以及R2是Me。 597A Q2是5-Me-2-噻吩基，R1是C1以及R2是CFH2。 598A Q2是5-Me-2-噻吩基，R1是Br以及R2是Me。 599A Q2是5-Me-2-噻吩基，R1是I以及R2是Me。 600A Q2是5-Me-2-噻吩基，R1是Me以及R2是Me。 601A Q2是5-Me-2-噻吩基，R1是Me以及R2是C1。 602A Q2是5-Me-2-噻吩基，R1是Me以及R2是Br。 603A Q2是5-Me-2-噻吩基，R1是Me以及R2是I。 151284.doc -132- 201117722 表 列標題 604A Q2是5-Me-2-噻吩基 ，R1是Br以及R2是Br。 605A Q2是5-Me-2-噻吩基 ，R1是Br以及R2是C卜 606A Q2是5-Me-2-噻吩基 ，R1是C1以及R2是Br。 607A Q2是5-Me-2-噻吩基 ，R1是C1以及R2是C卜 608A Q2是5-C1-2-噻吩基 ，R1是C1以及R2是Me。 609A Q2是5-C1-2-噻吩基 ，R1是C1以及R2是CFH2。 610A Q2是5-C1-2-噻吩基 ，R1是Βι•以及R2是Me。 611A Q2是5-C1-2-噻吩基 ，R1是I以及R2是Me。 612A Q2是5-C1-2-噻吩基 R1是Me以及R2是Me。 613A Q2是5-C1-2-噻吩基 R1是Me以及R2是α。 614A Q2是5-C1-2-噻吩基 R1是Me以及R2是Br。 615A Q2是5-C1-2-噻吩基 R1是Me以及R2是I。 616A Q2是5-C1-2-。塞吩基 R1是Br以及R2是Br。 617A Q2是5-C1-2-噻吩基 R1是Br以及R2是C1。 618A Q2是5-C1-2-噻吩基 R1是C1以及R2是Br。 619A Q2是5-C1-2-噻吩基 ，R1是C1以及R2是C卜 620A Q2是5-F-2-噻吩基， R1是C1以及R2是Me。 621A Q2是5-F-2-噻吩基， R1是C1以及R2是CFH2。 622A Q2是5-F-2-噻吩基， R1是Br以及R2是Me。 623A Q2是5-F-2-噻吩基， R1是I以及R2是Me。 624A Q2是5-F-2-噻吩基， R1是Me以及R2是Me。 625A Q2是5-F-2-噻吩基， R1是Me以及R2是C卜 626A Q2是5-F-2-噻吩基， R1是Me以及R2是Br。 627A Q2是5-F-2-噻吩基， R1是Me以及R2是I。 628A Q2是5-F-2-噻吩基， R1是Br以及R2是Br。 629A Q2是5-F-2-噻吩基， R1是Br以及R2是α。 630A Q2是5-F-2-噻吩基， R1是C1以及R2是Br。 631A Q2是5-F-2-噻吩基， R1是C1以及R2是C1。 632A Q2是5-Me-3-噻吩基 ，R1是C1以及R2是Me。 633A Q2是5-Me-3-噻吩基 ，R1是C1以及R2是CFH2。 634A Q2是5-Me-3-噻吩基 ，R1是Br以及R2是Me。 635A Q2是5-Me-3-噻吩基 ，R1是I以及R2是Me。 636A Q2是5-Me-3-噻吩基 ，R1是Me以及R2是Me。 637A Q2是5-Me-3-噻吩基 ，R1是Me以及R2是C卜 638A Q2是5-Me-3-噻吩基 ，R1是Me以及R2是Br。 151284.doc -133- 201117722 表 列標題 639A Q2是5-Me-3-噻吩基 ，R1是Me以及R2是I。 640A Q2是5-Me-3-噻吩基 ，R1是Br以及R2是Br。 641A Q2是5-Me-3-噻吩基 ，R1是Br以及R2是α。 642A Q2是5-Me-3-噻吩基 ，R1是C1以及R2是Br。 643A Q2是5-Me-3-噻吩基 ，R1是C1以及R2是α。 644A Q2是5-C1-3-噻吩基 R1是C1以及R2是Me。 645A Q2是5-C1-3-噻吩基 R1是C1以及R2是CFH2。 646A Q2是5-C1-3-噻吩基 R1是Br以及R2是Me。 647A Q2是5-C1-3-噻吩基 R1是I以及R2是Me。 648A Q2是5-C1-3-噻吩基 R1是Me以及R2是Me。 649A Q2是5-C1-3-噻吩基 R1是Me以及R2是C卜 650A Q2是5-C1-3-噻吩基 R1是Me以及R2是Br。 651A Q2是5-C1-3-噻吩基 R1是Me以及R2是I。 652A Q2是5-C1-3-噻吩基 R1是Br以及R2是Br。 653A Q2是5-C1-3-噻吩基 R1是Br以及R2是C卜 654A Q2是5-C1-3-噻吩基 R1是C1以及R2是Br。 655A Q2是5-C1-3-噻吩基 R1是C1以及R2是cn。 656A Q2是5-F-3-噻吩基， R1是Cl以及R2是Me。 657A Q2是5-F-3-噻吩基， R1是CI以及R2是CFH2。 658A Q2是5-F-3-噻吩基， R1是Br以及R2是Me。 659A Q2是5-F-3-噻吩基， R1是I以及R2是Me。 660A Q2是5-F-3-噻吩基， R1是Me以及R2是Me。 661A Q2是5-F-3-噻吩基， R1是Me以及R2是C卜 662A Q2是5-F-3-噻吩基， R1是Me以及R2是Br。 663A Q2是5-F-3-噻吩基， R1是Me以及R2是I。 664A Q2是5-F-3-噻吩基， R1是Br以及R2是Br。 665A Q2是5-F-3-噻吩基， R1是Br以及R2是α。 666A Q2是5-F-3-噻吩基， R1是C1以及R2是Br。 667A Q2是5-F-3-噻吩基， R1是C1以及R2是C卜 668A Q2是l-Me-ΙΗ-吡唑-3-基，R1是C1以及R2是Me。 669A Q2是卜Me-ΙΗ-吡唑-3-基！ R1是C1以及R2是CFH2。 670A Q2是l-Me-ΙΗ-吡唑-3-基，R1是Br以及R2是Me。 671A Q2是l-Me-ΙΗ-吡唑-3-基，R1是I以及R2是Me。 672A Q2是l-Me-ΙΗ-吡唑-3-基，R1是Me以及R2是Me。 673A Q2是l-Me-ΙΗ-吡唑-3-基，R1是Me以及R2是Q。 151284.doc · 134- 201117722 表 列標題 674A Q2是l-Me-ΙΗ-吡唑-3-基，R1是Me以及R2是Br。 675A Q2是l-Me-ΙΗ-吡唑-3-基，R丨是Me以及R2是I。 676A Q2是卜Me-ΙΗ-吡唑-3-基，R1是Br以及R2是Br。 677A Q2是l-Me-ΙΗ-吡唑-3-基，R1是Br以及R2是C1。 678A Q2是l-Me-ΙΗ-吡唑-3-基，R1是C1以及R2是Br。 679A Q2是l-Me-ΙΗ-吡唑-3-基，R1是C1以及R2是Q。 680A Q2是l-Me-ΙΗ-吡唑-4-基，R1是C1以及R2是Me。 68 ΙΑ Q2 是 l-Me-ΙΗ-吡唑-4-基，R1 是 C1 以及 R2 是 CFH2。 682Α Q2是l-Me-ΙΗ-吡唑-4-基，R1是Br以及R2是Me。 683Α Q2是l-Me-ΙΗ-吡唑-4-基，R1是I以及R2是Me。 684Α Q2是卜Me-1H-吡唑-4-基，R1是Me以及R2是Me。 685Α Q2是l-Me-ΙΗ-吡唑-4-基，R1是Me以及R2是C1。 686Α Q2是l-Me-ΙΗ-吡唑-4-基，R1是Me以及R2是Br。 687Α Q2是l-Me-ΙΗ-吡唑-4-基，R1是Me以及R2是I。 688Α Q2是l-Me-ΙΗ-吡唑-4-基，R1是Br以及R2是Br。 689Α Q2是l-Me-ΙΗ-吡唑-4-基，R1是Br以及R2是Q。 690Α Q2是l-Me-ΙΗ-吡唑-4-基，R1是Cl以及R2是Br。 691Α Q2是卜Me-ΙΗ-吡唑-4-基，R1是C1以及R2是C1。 692Α Q2是2-Me-5-噻唑基，R1是C1以及R2是Me。 693Α Q2是2-Me-5-噻唑基，R1是C1以及R2是CFH2。 694Α Q2是2-Me-5-噻唑基，R1是Br以及R2是Me。 695Α Q2是2-Me-5-噻唑基，R1是I以及R2是Me。 696Α Q2是2-Me-5-噻唑基，R1是Me以及R2是Me。 697Α Q2是2-Me-5-噻唑基，R1是Me以及R2是α。 698Α Q2是2-Me-5-噻唑基，R1是Me以及R2是Br。 699Α Q2是2-Me-5-噻唑基，R1是Me以及R2是I。 700Α Q2是2-Me-5-噻唑基，R1是Br以及R2是Br。 701Α Q2是2-Me-5-噻唑基，R1是Br以及R2是C1。 702Α Q2是2-Me-5-噻唑基，R1是C1以及R2是Br。 703Α Q2是2-Me-5-噻唑基，R1是C1以及R2是α。 704Α Q2是2-C1-5-噻唑基，R1是C1以及R2是Me。 705Α Q2是2-C1-5-噻唑基，R1是C1以及R2是CFH2。 706Α Q2是2-C1-5-噻唑基，R1是Br以及R2是Me。 707Α Q2是2-C1-5-噻唑基，R1是I以及R2是Me。 708Α Q2是2-CI-5-噻唑基，R1是Me以及R2是Me。 15I284.doc 135· 201117722 表 列標題 709A Q2是2-C1-5-噻唑基， R1是Me以及R2是CU。 710A Q2是2-C1-5-噻唑基， R1是Me以及R2是Br。 711A Q2是2-C1-5-噻唑基， R1是Me以及R2是I。 712A Q2是2-C1-5-噻唑基， R1是Br以及R2是Br。 713A Q2是2-C1-5-噻唑基， R1是Br以及R2是Π» 714A Q2是2-C1-5-噻唑基， R1是Cl以及R2是Br。 715A Q2是2-C1-5-噻唑基， R1是C1以及R2是cn。 表2177A 538A 537A 538A 539A 540A 541A Is Cl and R2 is Br » Q2 is 2-CF3-5-pyrimidine, R1 is Cl and R2 is CBu Q2 is 5-C1-2-pyrimidine, R1 is C1 and R2 is Me. Q2 is 5-CI-2-pyrimidine, R1 is C1 and R2 is CFH2. Q2 is 5-C1-2-pyrimidine, R1 is Br and R2 is Me. Q2 is 5-C1-2-pyrimidine, R1 is I and R2 is Me. Q2 is 5-C1-2-pyrimidine, R1 is Me and R2 is Me. Q2 is 5-C1-2-pyrimidine, R1 is Me and R2 is α. Q2 is 5-C1-2-pyrimidine, R1 is Me and R2 is Br. Q2 is 5-C1-2-pyrimidine, R1 is Me and R2 is I. Q2 is 5-C1-2-pyrimidine, R1 is Br and R2 is Br. Q2 is 5-C1-2-pyrimidine, R1 is Br and R2 is C1. Q2 is 5-C1-2-pyrimidine, R1 is C1 and R2 is Br. Q2 is 5-C1-2-pyrimidine, R1 is C1 and R2 is C1. Q2 is 5-Me-2-pyrimidine, R1 is C1 and R2 is Me. Q2 is 5-Me-2-pyrimidine, R1 is C1 and R2 is cfh2 Q2 is 5-Me-2-pyrimidine, R1 is Br and R2 is Me. Q2 is a 5-Me-2-° bite, R1 is I and R2 is Me. Q2 is a 5-Me-2-°® bite, R1 is Me and R'! is Me. Q2 is 5-Me-2-°^ bite, R1 is Me and R: 2 is Cl. Q2 is 5-Me-2-bite, R1 is Me and R: ! is Br. Q2 is a 5-Me-2-°f bite, R1 is Me and R2 is I. Q2 is a 5-Me-2-° bite, R1 is Br and R2 is Br. Q2 is 5-Me-2-pyrimidine, R1 is Br and R2 is Cl. Q2 is 5-Me-2-pyrimidine &gt; R1 is Cl and R2 is Br. Q2 is a 5-Me-2-°^ bite, R1 is Cl and R2 is Cl. Q2 is 5-MeO-2-pyrimidine, R1 is C1 and R2 is Me. Q2 is 5-MeO-2-pyrimidine, R1 is C1 and R2 is CFH2. Q2 is 5-MeO-2-pyrimidine, R1 is Br and R2 is Me. Q2 is 5-MeO-2-pyrimidine, R1 is I and R2 is Me. Q2 is 5-MeO-2-pyrimidine, R1 is Me and R2 is Me. Q2 is 5-MeO-2-pyrimidine, R1 is Me and R2 is C1. Q2 is 5-MeO-2-pyrimidine, R1 is Me and R2 is Br. Q2 is 5-MeO-2-pyrimidine, R1 is Me and R2 is I. Q2 is 5-MeO-2-pyrimidine, R1 is Br and R2 is Br. 151284.doc -131 201117722 Table Column heading 569A Q2 is 5-MeO-2-pyrimidine, R1 is Br and R2 is Cl. 570A Q2 is 5-MeO-2-pyrimidine, R1 is C1 and R2 is Br. 571A Q2 is 5-MeO-2-pyrimidine, R1 is C1 and R2 is C1. 572A Q2 is 5-C1-2-pyrimidine, R1 is C1 and R2 is Me. 573A Q2 is 5-C1-2-pyrimidine, R1 is C1 and R2 is CFH2. 574A Q2 is 5-C1-2-pyrimidine, R1 is Br and R2 is Me. 575A Q2 is 5-C1-2-pyrimidine, R1 is I and R2 is Me. 576A Q2 is 5-C1-2-pyrimidine, R1 is Me and R2 is Me. 577A Q2 is 5-C1-2-pyrimidine, R1 is Me and R2 is α. 578A Q2 is 5-C1-2-pyrimidine, R1 is Me and R2 is Br. 579A Q2 is 5-C1-2-pyrimidine, R1 is Me and R2 is I. 580A Q2 is 5-C1-2-pyrimidine, R1 is Br and R2 is Br. 581A Q2 is 5-C1-2-pyrimidine, R1 is Br and R2 is alpha. 582A Q2 is 5-C1-2-pyrimidine, R1 is C1 and R2 is Br. 583A Q2 is 5-CI-2-pyrimidine, R1 is C1 and R2 is CH. 584A Q2 is 5-CF3-2-pyrimidine, R1 is C1 and R2 is Me. 585A Q2 is 5-CF3-2-pyrimidine, R1 is C1 and R2 is CFH2. 586A Q2 is 5-CF3-2-pyrimidine, R1 is Br and R2 is Me. 587A Q2 is 5-CF3-2-pyrimidine, R1 is I and R2 is Me. 588A Q2 is 5-CF3-2-pyrimidine, R1 is Me and R2 is Me. 589A Q2 is 5-CF3-2-pyrimidine, R1 is Me and R2 is CBu 590A Q2 is 5-CF3-2-pyrimidine, Ri is Me and R2 is Br. 591A Q2 is 5-CF3-2-pyrimidine, R1 is Me and R2 is I. 592A Q2 is 5-CF3-2-pyrimidine, R1 is Br and R2 is Br. 593A Q2 is 5-CF3-2-pyrimidine, R1 is Br and R2 is C1. 594A Q2 is 5-CF3-2-pyrimidine, R1 is C1 and R2 is Br. 595A Q2 is 5-CF3-2-pyrimidine, R1 is C1 and R2 is CU. 596A Q2 is 5-Me-2-thienyl, R1 is C1 and R2 is Me. 597A Q2 is 5-Me-2-thienyl, R1 is C1 and R2 is CFH2. 598A Q2 is 5-Me-2-thienyl, R1 is Br and R2 is Me. 599A Q2 is 5-Me-2-thienyl, R1 is I and R2 is Me. 600A Q2 is 5-Me-2-thienyl, R1 is Me and R2 is Me. 601A Q2 is 5-Me-2-thienyl, R1 is Me and R2 is C1. 602A Q2 is 5-Me-2-thienyl, R1 is Me and R2 is Br. 603A Q2 is 5-Me-2-thienyl, R1 is Me and R2 is I. 151284.doc -132- 201117722 Table Column heading 604A Q2 is 5-Me-2-thienyl, R1 is Br and R2 is Br. 605A Q2 is 5-Me-2-thienyl, R1 is Br and R2 is CBu 606A Q2 is 5-Me-2-thienyl, R1 is C1 and R2 is Br. 607A Q2 is 5-Me-2-thienyl, R1 is C1 and R2 is CBu 608A Q2 is 5-C1-2-thienyl, R1 is C1 and R2 is Me. 609A Q2 is 5-C1-2-thienyl, R1 is C1 and R2 is CFH2. 610A Q2 is 5-C1-2-thienyl, R1 is Βι• and R2 is Me. 611A Q2 is 5-C1-2-thienyl, R1 is I and R2 is Me. 612A Q2 is 5-C1-2-thienyl. R1 is Me and R2 is Me. 613A Q2 is 5-C1-2-thienyl. R1 is Me and R2 is α. 614A Q2 is 5-C1-2-thienyl. R1 is Me and R2 is Br. 615A Q2 is 5-C1-2-thienyl. R1 is Me and R2 is I. 616A Q2 is 5-C1-2-. The thiophene group R1 is Br and R2 is Br. 617A Q2 is 5-C1-2-thienyl R1 is Br and R2 is C1. 618A Q2 is 5-C1-2-thienyl R1 is C1 and R2 is Br. 619A Q2 is 5-C1-2-thienyl, R1 is C1 and R2 is CBu 620A Q2 is 5-F-2-thienyl, R1 is C1 and R2 is Me. 621A Q2 is 5-F-2-thienyl, R1 is C1 and R2 is CFH2. 622A Q2 is 5-F-2-thienyl, R1 is Br and R2 is Me. 623A Q2 is 5-F-2-thienyl, R1 is I and R2 is Me. 624A Q2 is 5-F-2-thienyl, R1 is Me and R2 is Me. 625A Q2 is 5-F-2-thienyl, R1 is Me and R2 is CBu 626A Q2 is 5-F-2-thienyl, R1 is Me and R2 is Br. 627A Q2 is 5-F-2-thienyl, R1 is Me and R2 is I. 628A Q2 is 5-F-2-thienyl, R1 is Br and R2 is Br. 629A Q2 is 5-F-2-thienyl, R1 is Br and R2 is alpha. 630A Q2 is 5-F-2-thienyl, R1 is C1 and R2 is Br. 631A Q2 is 5-F-2-thienyl, R1 is C1 and R2 is C1. 632A Q2 is 5-Me-3-thienyl, R1 is C1 and R2 is Me. 633A Q2 is 5-Me-3-thienyl, R1 is C1 and R2 is CFH2. 634A Q2 is 5-Me-3-thienyl, R1 is Br and R2 is Me. 635A Q2 is 5-Me-3-thienyl, R1 is I and R2 is Me. 636A Q2 is 5-Me-3-thienyl, R1 is Me and R2 is Me. 637A Q2 is 5-Me-3-thienyl, R1 is Me and R2 is CBu 638A Q2 is 5-Me-3-thienyl, R1 is Me and R2 is Br. 151284.doc -133- 201117722 Table Column heading 639A Q2 is 5-Me-3-thienyl, R1 is Me and R2 is I. 640A Q2 is 5-Me-3-thienyl, R1 is Br and R2 is Br. 641A Q2 is 5-Me-3-thienyl, R1 is Br and R2 is α. 642A Q2 is 5-Me-3-thienyl, R1 is C1 and R2 is Br. 643A Q2 is 5-Me-3-thienyl, R1 is C1 and R2 is α. 644A Q2 is 5-C1-3-thienyl R1 is C1 and R2 is Me. 645A Q2 is 5-C1-3-thienyl R1 is C1 and R2 is CFH2. 646A Q2 is 5-C1-3-thienyl R1 is Br and R2 is Me. 647A Q2 is 5-C1-3-thienyl. R1 is I and R2 is Me. 648A Q2 is 5-C1-3-thienyl. R1 is Me and R2 is Me. 649A Q2 is 5-C1-3-thienyl R1 is Me and R2 is CBu 650A Q2 is 5-C1-3-thienyl R1 is Me and R2 is Br. 651A Q2 is 5-C1-3-thienyl. R1 is Me and R2 is I. 652A Q2 is 5-C1-3-thienyl R1 is Br and R2 is Br. 653A Q2 is 5-C1-3-thienyl R1 is Br and R2 is Cb 654A Q2 is 5-C1-3-thienyl R1 is C1 and R2 is Br. 655A Q2 is 5-C1-3-thienyl R1 is C1 and R2 is cn. 656A Q2 is 5-F-3-thienyl, R1 is Cl and R2 is Me. 657A Q2 is 5-F-3-thienyl, R1 is CI and R2 is CFH2. 658A Q2 is 5-F-3-thienyl, R1 is Br and R2 is Me. 659A Q2 is 5-F-3-thienyl, R1 is I and R2 is Me. 660A Q2 is 5-F-3-thienyl, R1 is Me and R2 is Me. 661A Q2 is 5-F-3-thienyl, R1 is Me and R2 is CBu 662A Q2 is 5-F-3-thienyl, R1 is Me and R2 is Br. 663A Q2 is 5-F-3-thienyl, R1 is Me and R2 is I. 664A Q2 is 5-F-3-thienyl, R1 is Br and R2 is Br. 665A Q2 is 5-F-3-thienyl, R1 is Br and R2 is α. 666A Q2 is 5-F-3-thienyl, R1 is C1 and R2 is Br. 667A Q2 is 5-F-3-thienyl, R1 is C1 and R2 is Cb 668A Q2 is l-Me-ΙΗ-pyrazol-3-yl, R1 is C1 and R2 is Me. 669A Q2 is a Me-ΙΗ-pyrazol-3-yl! R1 is C1 and R2 is CFH2. 670A Q2 is l-Me-ΙΗ-pyrazol-3-yl, R1 is Br and R2 is Me. 671A Q2 is l-Me-ΙΗ-pyrazol-3-yl, R1 is I and R2 is Me. 672A Q2 is l-Me-ΙΗ-pyrazol-3-yl, R1 is Me and R2 is Me. 673A Q2 is l-Me-ΙΗ-pyrazol-3-yl, R1 is Me and R2 is Q. 151284.doc · 134- 201117722 Table Column headings 674A Q2 is l-Me-ΙΗ-pyrazol-3-yl, R1 is Me and R2 is Br. 675A Q2 is l-Me-ΙΗ-pyrazol-3-yl, R丨 is Me and R2 is I. 676A Q2 is a Me-ΙΗ-pyrazol-3-yl group, R1 is Br and R2 is Br. 677A Q2 is l-Me-ΙΗ-pyrazol-3-yl, R1 is Br and R2 is C1. 678A Q2 is l-Me-ΙΗ-pyrazol-3-yl, R1 is C1 and R2 is Br. 679A Q2 is l-Me-ΙΗ-pyrazol-3-yl, R1 is C1 and R2 is Q. 680A Q2 is l-Me-ΙΗ-pyrazol-4-yl, R1 is C1 and R2 is Me. 68 ΙΑ Q2 is l-Me-ΙΗ-pyrazol-4-yl, R1 is C1 and R2 is CFH2. 682Α Q2 is l-Me-ΙΗ-pyrazol-4-yl, R1 is Br and R2 is Me. 683Α Q2 is l-Me-ΙΗ-pyrazol-4-yl, R1 is I and R2 is Me. 684Α Q2 is a Me-1H-pyrazol-4-yl group, R1 is Me and R2 is Me. 685Α Q2 is l-Me-ΙΗ-pyrazol-4-yl, R1 is Me and R2 is C1. 686 Α Q2 is l-Me-ΙΗ-pyrazol-4-yl, R1 is Me and R2 is Br. 687Α Q2 is l-Me-ΙΗ-pyrazol-4-yl, R1 is Me and R2 is I. 688Α Q2 is l-Me-ΙΗ-pyrazol-4-yl, R1 is Br and R2 is Br. 689 Α Q2 is l-Me-ΙΗ-pyrazol-4-yl, R1 is Br and R2 is Q. 690 Α Q2 is l-Me-ΙΗ-pyrazol-4-yl, R1 is Cl and R2 is Br. 691Α Q2 is a Me-ΙΗ-pyrazol-4-yl group, R1 is C1 and R2 is C1. 692Α Q2 is 2-Me-5-thiazolyl, R1 is C1 and R2 is Me. 693Α Q2 is 2-Me-5-thiazolyl, R1 is C1 and R2 is CFH2. 694Α Q2 is 2-Me-5-thiazolyl, R1 is Br and R2 is Me. 695 Α Q2 is 2-Me-5-thiazolyl, R1 is I and R2 is Me. 696Α Q2 is 2-Me-5-thiazolyl, R1 is Me and R2 is Me. 697Α Q2 is 2-Me-5-thiazolyl, R1 is Me and R2 is α. 698 Α Q2 is 2-Me-5-thiazolyl, R1 is Me and R2 is Br. 699Α Q2 is 2-Me-5-thiazolyl, R1 is Me and R2 is I. 700 Α Q2 is 2-Me-5-thiazolyl, R1 is Br and R2 is Br. 701Α Q2 is 2-Me-5-thiazolyl, R1 is Br and R2 is C1. 702Α Q2 is 2-Me-5-thiazolyl, R1 is C1 and R2 is Br. 703Α Q2 is 2-Me-5-thiazolyl, R1 is C1 and R2 is α. 704Α Q2 is 2-C1-5-thiazolyl, R1 is C1 and R2 is Me. 705Α Q2 is 2-C1-5-thiazolyl, R1 is C1 and R2 is CFH2. 706Α Q2 is 2-C1-5-thiazolyl, R1 is Br and R2 is Me. 707Α Q2 is 2-C1-5-thiazolyl, R1 is I and R2 is Me. 708Α Q2 is 2-CI-5-thiazolyl, R1 is Me and R2 is Me. 15I284.doc 135· 201117722 Table Column headings 709A Q2 is 2-C1-5-thiazolyl, R1 is Me and R2 is CU. 710A Q2 is 2-C1-5-thiazolyl, R1 is Me and R2 is Br. 711A Q2 is 2-C1-5-thiazolyl, R1 is Me and R2 is I. 712A Q2 is 2-C1-5-thiazolyl, R1 is Br and R2 is Br. 713A Q2 is 2-C1-5-thiazolyl, R1 is Br and R2 is Π» 714A Q2 is 2-C1-5-thiazolyl, R1 is Cl and R2 is Br. 715A Q2 is 2-C1-5-thiazolyl, R1 is C1 and R2 is cn. Table 2

Q1 是 4-Cl-Ph，R1 是 Cl 以及 R2 是 Me。Q1 is 4-Cl-Ph, R1 is Cl and R2 is Me.

(R5) η (R5) n (R5) n (R5) n (R5) n 2,6-二-F 2,4-二-Cl 4-CN，2,6-二 -F 2-CF3, 4-F 2-C1, 4-NO2 2,4,6-三-F 2-C1，4,6-二 -F 2,6-二-F， 4-Me 2-CF2HO, 4-F 2-NO2, 4-F 2,3,6-三-F 2-C1, 6-F 2-C1, 5-CF3 2-CN, 6-F 2,5-二-&lt;：1， 4-F 2,4,5-三-F 2-Br, 6-F 2-C1，4-Me 2,5-二-Cl 2,3-二-Cl， 4-F 2,3,4-三4 2-F, 6-CF3 2-C1，4-MeO 2-CF3, 4-MeO 2-C1, 5-CN 2-C1, 4-F 2-F, 6-CF2HO 2-Br, 4-MeO 2-F, 6-Me 2,4-二-F, 5-CN 2-Br-4-F 2-1, 4-F 2,6-二-F， 3-C1 2,6,二-F， 3-Me 2-C1, 6-F, 3-MeO 2,4-二-F 4-C1，2,6-二 -F 2,6-二-F, 3-CN 2-CF3 2,6-二-F, 3-NCCH2O 151284.doc •136- 201117722(R5) η (R5) n (R5) n (R5) n (R5) n 2,6-di-F 2,4-di-Cl 4-CN,2,6-di-F 2-CF3, 4 -F 2-C1, 4-NO2 2,4,6-tri-F 2-C1,4,6-di-F 2,6-di-F, 4-Me 2-CF2HO, 4-F 2-NO2 , 4-F 2,3,6-Tri-F 2-C1, 6-F 2-C1, 5-CF3 2-CN, 6-F 2,5-di-&lt;:1, 4-F 2, 4,5-tri-F 2-Br, 6-F 2-C1,4-Me 2,5-di-Cl 2,3-di-Cl, 4-F 2,3,4-tris 4 2-F , 6-CF3 2-C1,4-MeO 2-CF3, 4-MeO 2-C1, 5-CN 2-C1, 4-F 2-F, 6-CF2HO 2-Br, 4-MeO 2-F, 6-Me 2,4-di-F, 5-CN 2-Br-4-F 2-1, 4-F 2,6-di-F, 3-C1 2,6,di-F, 3-Me 2-C1, 6-F, 3-MeO 2,4-di-F 4-C1,2,6-di-F 2,6-di-F, 3-CN 2-CF3 2,6-di-F , 3-NCCH2O 151284.doc •136- 201117722

Ql U；)1'Ph，R，^CU^R^Me -Cl 2,6-二-f， 4-Me〇 2-Cl, 6-F, 4- Me〇 2-Cl, 6-F, 5- Me〇Ql U;)1'Ph,R,^CU^R^Me -Cl 2,6-di-f, 4-Me〇2-Cl, 6-F, 4-Me〇2-Cl, 6-F, 5- Me〇

3-MeO 2.6- 二-F， 4-CF2H〇3-MeO 2.6- di-F, 4-CF2H〇

2.6- 二-F， 3-CF2HO 2.6- 二-p 4-N〇2 2.6- 二-f，2.6-di-F, 3-CF2HO 2.6-di-p 4-N〇2 2.6-di-f,

3-EtO3-EtO

(R5) n 2,6·二-F， 4-NCCH2O 本發明揭露的内容亦包含表 表格建立方式與上述表 2相同， 1B到715B，其中每一 「丨 除了表2開頭的列（即 疋4-Cl-Ph ’ R疋C1以及R2是Me」）以下述各別 的列開頭所取代。因此，舉例來說，在表1B列開頭是 「Qi是4-Cl-Ph’ R1是Br以及R2是Me」，以及（R5) η是在上述表2中經定義。表2B到715B以相似的方式 建立。 表 1B Qi 是 4-Cl-Ph ’ 2B Qi 是 4-Cl-Ph， 3B Qi 是 4-Cl-Ph ’ 4B Qi 是 4-Cl-Ph ’ 5B Qi 是 4-Cl-Ph ’ 6B Qi 是 4-Cl-Ph ’ 7B Qi 是 4-Cl-Ph ’ 8B Q1 是 4-Cl-Ph ’ 9B Q1 是 4-Cl-Ph ’ 10B Qi 是 4_C1-Ph ’ 11B Qi 是 4-Cl-Ph ’ 12B Q1 是 4-Cl-Ph， 13B Qi 是 4-Cl-Ph ’ 14B Qi 是 4-Cl-Ph ’ 15B Qi 是 4-Cl-Ph， 16B Qi 是 4-Cl-Ph ’ 列標題 R1是台r以及R2是Me。 R1是C1以及R2是CFH2。 R1是I以及R2是Me。 R1是Me以及R2是Me。 R1是Me以及R2是C1。 R1是Me以及R2是Br 〇 R1是Me以及R2是I。 R1是Me以及R2是MeO。 R1是MeO以及R2是Me。 R1是Br以及R2是Br。 R1是Br以及R2是C卜 R1是C1以及R2是Br。 R1是C1以及R2是C卜 R1是Me以及R2是MeS。 R1是MeS以及R2是Me。 R1是Et以及R2是Br。 I51284.doc • 137- 201117722 表 列標題 17B Q 是 4-Cl-Ph ，R 1是Et以及r2是a。 18B Q 是 4-Cl-Ph » R 1是Et以及R2是Me。 19B Q 是 4-Cl-Ph ，R 1是Me以及R2是Et。 20B Q 是 4-Cl-Ph ，R 1是Cl以及R2是Et。 21B Q 是 4-Cl-Ph ，R 1是Me以及R2是CN。 22B Q 是 3-Cl-Ph ，R 1是Cl以及R2是Me。 23B Q 是 3-Cl-Ph ，R 1是C1以及R2是CFH2。 24B Q 是 3-Cl-Ph ，R 1是Br以及R2是Me。 25B Q 是 3-Cl-Ph ，R 1是I以及R2是Me。 26B Q 是 3-Cl-Ph ，R 1是Me以及R2是Me。 27B Q 是 3-Cl-Ph ，R1是Me以及R2是α。 28B Q 是 3-Cl-Ph ，R 1是Me以及R2是Br。 29B Q 是 3-Cl-Ph ，R 1是Me以及R2是I。 30B Q 是 3-Cl-Ph ，R 1是Br以及R2是Br。 31B Q 是 3-Cl-Ph ，R1是Br以及R2是a。 32B Q 是 3-Cl-Ph ，R 1是C1以及R2是Br。 33B Q 是 3-Cl-Ph ，R 1是C1以及R2是α。 34B Q 是 4-F-Ph， R1 是C1以及R2是Me。 35B Q 是 4-F-Ph ， R1 是C1以及R2是CFH2。 36B Q 是 4-F-Ph， R1 是Br以及R2是Me。 37B Q 是 4-F-Ph &gt; R1 是I以及R2是Me。 38B Q 是 4-F-Ph ， R1 是Me以及R2是Me。 39B Q 是 4-F-Ph ， R1 是Me以及R2是a。 40B Q 是 4-F-Ph ， R1 是Me以及R2是Br。 41B Q 是 4-F-Ph ， R1 是Me以及R2是I。 42B Q 是 4-F-Ph ， R1 是Br以及R2是Br。 43B Q 是 4-F-Ph ， R1 是Br以及R2是C卜 44B Q 是 4-F-Ph ， R1 是C1以及R2是Br。 45B Q 是 4-F-Ph， R1 是C1以及R2是a。 46B Q 是 3-F-Ph ， R1 是C1以及R2是Me。 47B Q 是 3-F-Ph ， R1 是C1以及R2是CFH2。 48B Q 是 3-F-Ph ， R1 是Br以及R2是Me。 49B Q 是 3-F-Ph ， R1 是I以及R2是Me。 50B Q 是 3-F-Ph ， R1 是Me以及R2是Me。 51B Q 是 3-F-Ph - R1 是Me以及R2是CM。 151284.doc - 138- 201117722 表 列標題 52B Q1 是 3-F-Ph ， R1是Me以及R2是Br。 53B Q1 是 3-F-Ph ， R1是Me以及R2是I。 54B Q1 是 3-F-Ph ， R1是Br以及R2是Br。 55B Q1 是 3-F-Ph &gt; R1是Br以及R2是C卜 56B Q1 是 3-F-Ph ， R1是Cl以及R2是Br。 57B Q1 是 3-F-Ph ， r1是ci以及r2是cn。 58B Q1 是 3-CF2HO -Ph ，R1是Cl以及R2是Me。 59B Q1 是 3-CF2HO -Ph ，R1是Cl以及R2是CFH2. 60B Q1 是 3-CF2HO -Ph ，R1是Br以及R2是Me。 61B Q1 是 3-CF2HO-Ph ，R1是I以及R2是Me。 62B Q1 是 3-CF2HO -Ph ，R1是Me以及R2是Me。 63B Q1 是 3-CF2HO -Ph ，R1是Me以及R2是Cl。 64B Q1 是 3-CF2HO -Ph ，R1是Me以及R2是Br。 65B Q1 是 3-CF2HO -Ph ，R1是Me以及R2是I。 66B Q1 是 3-CF2HO-Ph ，R1是Br以及R2是Br。 67B Q1 是 3-CF2HO -Ph ，R1是Br以及R2是Cl。 68B Q1 是 3-CF2HO -Ph ，R1是Cl以及R2是Br。 69B Q1 是 3-CF2HO-Ph ，R1是Cl以及R2是Cl。 70B Q1 是 4-Me-Ph ，R1 是Cl以及R2是Me。 71B Q1 是 4-Me-Ph ，R1 是Cl以及R2是CFH2。 72B Q1 是 4-Me-Ph ，R1 是Br以及R2是Me。 73B Q1 是 4-Me-Ph ，R1 是I以及R2是Me。 74B Q1是 4-Me-Ph ，R1 是Me以及R2是Me。 75B Q1 是 4-Me-Ph ，R1 是Me以及R2是C1。 76B Q1 是 4-Me-Ph ，R1 是Me以及R2是Br。 77B Q1 是 4-Me-Ph ，R1 是Me以及R2是I。 78B Q1 是 4-Me-Ph ，R1 是Br以及R2是Br。 79B Q1 是 4-Me-Ph ，R1 是Br以及R2是C卜 80B Q1 是 4-Me-Ph ，R1 是C1以及R2是Br。 81B Q1 是 4-Me-Ph ，R1 是C1以及R2是α。 82B Q1 是 3-Me-Ph ，R1 是C1以及R2是Me。 83B Q1 是 3-Me-Ph ，R1 是C1以及R2是CFH2。 84B Q1 是 3-Me-Ph ，R1 是Br以及R2是Me。 85B Q1 是 3-Me-Ph ，R1 是I以及R2是Me。 86B Q1 是 3-Me-Ph ，R1是Me以及R2是Me。 151284.doc -139- 201117722 表 列標題 87B Q1 是 3-Me-Ph ，R1是Me以及R2是α。 88B Q1 是 3-Me-Ph ，R1 是Me以及R2是Br。 89B Q1 是 3-Me-Ph ，R1 是Me以及R2是I。 90B Q1 是 3-Me-Ph ，R1 是Br以及R2是Br。 91B Q1 是 3-Me-Ph ，R1 是Br以及R2是Cl。 92B Q1 是 3-Me-Ph ，R1 是Cl以及R2是Br。 93B Q1 是 3-Me-Ph ，R1 是C1以及R2是C卜 94B Q1 是 4-Et-Ph， R1是Cl以及R2是Me。 95B Q1 是 4-Et-Ph &gt; R1是Cl以及R2是CFH2。 96B Q1 是 4-Et-Ph， R1是Br以及R2是Me。 97B Q1 是 4-Et-Ph， R1是I以及R2是Me。 98B Q1 是 4-Et-Ph， R1是Me以及R2是Me。 99B Q1 是 4-Et-Ph &gt; R1是Me以及R2是a。 100B Q1 是 4-Et-Ph， R1是Me以及R2是Br。 101B Q1 是 4-Et-Ph - R1是Me以及R2是I。 102B Q1 是 4-Et-Ph » R1是Br以及R2是Br。 103B Q1 是 4-Et-Ph » R1是Br以及R2是Cl。 104B Q1 是 4-Et-Ph， R1是Cl以及R2是Br。 105B Q1 是 4-Et-Ph， R1是Cl以及R2是Cl。 106B Q1 是 4-C1 ' 3-F-Ph ，R1是C1以及R2是Me。 107B Q1 是 4-C1 ' 3-F-Ph ，R1是C1以及R2是CFH2。 108B Q1 是 4-C1 ' 3-F-Ph ，R1是Br以及R2是Me。 109B Q1 是 4-C1 ' 3-F-Ph ，R1是I以及R2是Me。 110B Q1 是 4-C1 ' 3-F-Ph ，R1是Me以及R2是Me。 111B Q1 是 4-C1 ' 3-F-Ph ，R1是Me以及R2是C卜 112B Q1 是 4-C1 ' 3-F-Ph ，R1是Me以及R2是Br。 113B Q1 是 4-C1 、 3-F-Ph ，R1是Me以及R2是I。 114B Q1 是 4-C1 ' 3-F-Ph ，R1是Br以及R2是Br。 115B Q1 是 4-C1 ' 3-F-Ph ，R1是Br以及R2是C卜 116B Q1 是 4-C1 ' 3-F-Ph ，R1是C1以及R2是Br。 117B Q1 是 4-C1 &gt; 3-F-Ph ，R1是C1以及R2是C1。 118B Q1 是 2-C1 ' 4-F-Ph ，R1是C1以及R2是Me。 119B Q1 是 2-C1 &gt; 4-F-Ph ，R1是C1以及R2是CFH2。 120B Q1 是 2-C1 ' 4-F-Ph ，R1是Br以及R2是Me。 121B Q1 是 2-C1 ' 4-F-Ph ，R1是I以及R2是Me。 151284.doc -140· 201117722 表 列標題 122B Q1 是 2-C1 、4-F-Ph ，R1是Me以及R2是Me。 123B Q1 是 2-C1 、4-F-Ph ，R1是Me以及R2是Π。 124B Q1 是 2-C1 、4-F-Ph ，Ri是Me以及R2是Br。 125B Q1 是 2-C1 、4-F-Ph ，R1是Me以及R2是I。 126B Q1 是 2-C1 ' 4-F-Ph ，R1是Br以及R2是Br。 127B Q1 是 2-C1 ' 4-F-Ph ，R1是Br以及R2是Cl。 128B Q1 是 2-C1 、4-F-Ph ，R1是Cl以及R2是Br。 129B Q1 是 2-C1 、4-F-Ph ，R1是Cl以及R2是a。 130B Q1 是 4-F、 3-Me-Ph ，R1是Cl以及R2是Me。 131B Q1 是 4-F、 3-Me-Ph ，R1是Cl以及R2是CFH2。 132B Q1 是 4-F、 3-Me-Ph ，R1是Br以及R2是Me。 133B Q1 是 4-F、 3-Me-Ph ，R1是I以及R2是Me。 134B Q1 是 4-F、 3-Me-Ph ，R1是Me以及R2是Me。 135B Q1 是 4-F、 3-Me-Ph ，R1是Me以及R2是a。 136B Q1 是 4-F、 3-Me-Ph ，R1是Me以及R2是Br。 137B Q1 是 4-F ' 3-Me-Ph ，R1是Me以及R2是I。 138B Q1 是 4-F、 3-Me-Ph ，R1是Br以及R2是Br。 139B Q1 是 4-F &gt; 3-Me-Ph ，R1是Br以及R2是CM。 140B Q1 是 4-F ' 3-Me-Ph ，R1是Cl以及R2是Br。 141B Q1 是 4-F、 3-Me-Ph ，R1是Cl以及R2是C卜 142B Q1是 3,4-: --F-Ph &gt; R1是Cl以及R2是Me。 143B Q1 是 3,4-二-F-Ph， R1是Cl以及R2是CFH2。 144B Q1 是 3,4-: _-F-Ph &gt; R1是Br以及R2是Me。 145B Q1 是 3,4-二 --F-Ph &gt; R1是I以及R2是Me。 146B Q1 是 3,4-二-F-Ph， R1是Me以及R2是Me。 147B Q1 是 3,4-二 --F-Ph &gt; R1是Me以及R2是a。 148B Q1 是 3,4-二 --F-Ph &gt; R1是Me以及R2是Br。 149B Q1 是 3,4-二 --F-Ph - R1是Me以及R2是I。 150B Q1 是 3,4-二-F-Ph， R1是Br以及R2是Br。 151B Q1 是 3,4-二-F-Ph， R1是Br以及R2是Cl。 152B Q1是 3,4-二-F-Ph， R1是Cl以及R2是Br。 153B Q1 是 3,4-二-F-Ph， R1是Cl以及R2是Cl。 154B Q1 是 3,4-二 --Cl-Ph， R1是Cl以及R2是Me。 155B Q1 是 3,4- --Cl-Ph &gt; R1是Cl以及R2是CFH2。 156B Q1 是 3,4-- --Cl-Ph &gt; R1是Br以及R2是Me。 -141 - 151284.doc 201117722 表 列標題 157B Q1 是 3,4-二-Cl-Ph，R1 是 I 以及 R2 是 Me。 158B Q1 是 3,4-二-Cl-Ph，R1 是 Me 以及 R2 是 Me。 159B Q1 是 3,4-二-Cl-Ph，R1 是 Me 以及 R2 是 C1。 160B Q1 是 3,4-二-Cl-Ph，R1 是 Me 以及 R2 是 Br。 161B Q1 是 3,4-二-Cl-Ph，R1 是 Me 以及 R2 是 I。 162B Q1 是 3,4-二-Cl-Ph，R1 是 Br 以及 R2 是 Br。 163B Q1 是 3,4-二-Cl-Ph，R1 是 Br 以及 R2 是 C1。 164B Q1 是 3,4-二-Cl-Ph，R1 是 C1 以及 R2 是 Br。 165B Q1 是 3,4-二-Cl-Ph，R1 是 C1 以及 R2 是 C1。 166B Q1 是 3,5-二-MeO-Ph，R1 是 C1 以及 R2 是 Me。 167B Q1 是 3,5-二-MeO-Ph，R1 是 C1 以及 R2 是 CFH2。 168B Q1 是 3,5-二-MeO-Ph，R1 是 Br 以及 R2 是 Me。 169B Q1 是 3,5-二-MeO-Ph，R1 是 I 以及 R2 是 Me。 170B Q1 是 3,5-二-MeO-Ph，R1 是 Me 以及 R2 是 Me。 171B (^是3,5-二-1^0-?11，111是厘6以及112是（：1。 172B Q1 是 3,5-二-MeO-Ph，Ri 是 Me 以及 R2 是 Br。 173B Q1 是 3,5-二-MeO-Ph，R1 是 Me 以及 R2 是 I。 174B Q1是3,5-二-MeO-Ph，R1是Br以及R2是Br。 175B Q1是3,5-二-MeO-Ph，R1是Br以及R2是Cl。 176B Q1 是 3,5-二-MeO-Ph，R1 是 C1 以及 R2 是 Br。 177B Q1 是 3,5-二-MeO-Ph，R1 是 C1 以及 R2 是 CH。 178B Q1 是 2-a、3,5-二-MeO-Ph，R1 是 C1 以及 R2 是 Me。 179B Q1是2-Cl、3,5-二-MeO-Ph，R1是Cl以及R2是CFH2。 180B Q1 是 2-CU、3,5-二-MeO-Ph，R1 是 Br 以及 R2 是 Me。 181B Q1 是 2-C1、3,5-二-MeO-Ph，R1 是 I 以及 R2 是 Me。 182B Q1 是 2-C1、3,5-二-MeO-Ph，R丨是 Me 以及 R2 是 Me。 183B Q1 是 2-C1、3,5-二-MeO-Ph，R1 是 Me 以及 R2 是 α。 184B ()1是2-(：1、3,5-二-1^0-?11，111是1^以及112是81·。 185B Q1 是 2-CU、3,5-二-MeO-Ph，R1 是 Me 以及 R2 是 I。 186B Q1 是 2-C1、3,5_二-MeO-Ph，R1 是 Br 以及 R2 是 Br。 187B Q1 是 2-C1、3,5-二-MeO-Ph，R1 是 Br 以及 R2 是 C卜 188B Q1 是 2-C卜 3,5-二-MeO-Ph，R1 是 C1 以及 R2 是 Br。 189B ()1是2-(：卜3,5-二-1^0-?11，111是（：1以及112是（：卜 190B Q1 是 4-C1、3,5-二-MeO-Ph，R1 是 C1 以及 R2 是 Me。 191B Q1 是 4-Cb 3,5-二-MeO-Ph，R1 是 C1 以及 R2 是 CFH2。 151284.doc •142-(R5) n 2,6·2-F, 4-NCCH2O The content disclosed in the present invention also includes the table table being established in the same manner as in Table 2 above, 1B to 715B, wherein each "except the column at the beginning of Table 2 (ie, 疋4-Cl-Ph 'R疋C1 and R2 are Me") are replaced by the following respective columns. Thus, for example, at the beginning of the column of Table 1B, "Qi is 4-Cl-Ph', R1 is Br and R2 is Me", and (R5) η is defined in Table 2 above. Tables 2B through 715B are established in a similar manner. Table 1B Qi is 4-Cl-Ph ' 2B Qi is 4-Cl-Ph, 3B Qi is 4-Cl-Ph ' 4B Qi is 4-Cl-Ph ' 5B Qi is 4-Cl-Ph ' 6B Qi is 4 -Cl-Ph ' 7B Qi is 4-Cl-Ph ' 8B Q1 is 4-Cl-Ph ' 9B Q1 is 4-Cl-Ph ' 10B Qi is 4_C1-Ph ' 11B Qi is 4-Cl-Ph ' 12B Q1 Is 4-Cl-Ph, 13B Qi is 4-Cl-Ph ' 14B Qi is 4-Cl-Ph ' 15B Qi is 4-Cl-Ph, 16B Qi is 4-Cl-Ph ' column heading R1 is a table r and R2 is Me. R1 is C1 and R2 is CFH2. R1 is I and R2 is Me. R1 is Me and R2 is Me. R1 is Me and R2 is C1. R1 is Me and R2 is Br 〇 R1 is Me and R2 is I. R1 is Me and R2 is MeO. R1 is MeO and R2 is Me. R1 is Br and R2 is Br. R1 is Br and R2 is C. R1 is C1 and R2 is Br. R1 is C1 and R2 is CBu. R1 is Me and R2 is MeS. R1 is MeS and R2 is Me. R1 is Et and R2 is Br. I51284.doc • 137- 201117722 Table Column heading 17B Q is 4-Cl-Ph, R 1 is Et and r2 is a. 18B Q is 4-Cl-Ph » R 1 is Et and R 2 is Me. 19B Q is 4-Cl-Ph , R 1 is Me and R 2 is Et. 20B Q is 4-Cl-Ph , R 1 is Cl and R 2 is Et. 21B Q is 4-Cl-Ph , R 1 is Me and R 2 is CN. 22B Q is 3-Cl-Ph , R 1 is Cl and R 2 is Me. 23B Q is 3-Cl-Ph, R 1 is C1 and R 2 is CFH2. 24B Q is 3-Cl-Ph , R 1 is Br and R 2 is Me. 25B Q is 3-Cl-Ph , R 1 is I and R 2 is Me. 26B Q is 3-Cl-Ph , R 1 is Me and R 2 is Me. 27B Q is 3-Cl-Ph, R1 is Me and R2 is α. 28B Q is 3-Cl-Ph, R 1 is Me and R 2 is Br. 29B Q is 3-Cl-Ph, R 1 is Me and R 2 is I. 30B Q is 3-Cl-Ph , R 1 is Br and R 2 is Br. 31B Q is 3-Cl-Ph, R1 is Br and R2 is a. 32B Q is 3-Cl-Ph, R 1 is C1 and R 2 is Br. 33B Q is 3-Cl-Ph , R 1 is C1 and R 2 is α. 34B Q is 4-F-Ph, R1 is C1 and R2 is Me. 35B Q is 4-F-Ph , R1 is C1 and R2 is CFH2. 36B Q is 4-F-Ph, R1 is Br and R2 is Me. 37B Q is 4-F-Ph &gt; R1 is I and R2 is Me. 38B Q is 4-F-Ph , R1 is Me and R2 is Me. 39B Q is 4-F-Ph , R1 is Me and R2 is a. 40B Q is 4-F-Ph, R1 is Me and R2 is Br. 41B Q is 4-F-Ph , R1 is Me and R2 is I. 42B Q is 4-F-Ph, R1 is Br and R2 is Br. 43B Q is 4-F-Ph, R1 is Br and R2 is CBu 44B Q is 4-F-Ph, R1 is C1 and R2 is Br. 45B Q is 4-F-Ph, R1 is C1 and R2 is a. 46B Q is 3-F-Ph , R1 is C1 and R2 is Me. 47B Q is 3-F-Ph, R1 is C1 and R2 is CFH2. 48B Q is 3-F-Ph , R1 is Br and R2 is Me. 49B Q is 3-F-Ph, R1 is I and R2 is Me. 50B Q is 3-F-Ph , R1 is Me and R2 is Me. 51B Q is 3-F-Ph - R1 is Me and R2 is CM. 151284.doc - 138- 201117722 Table Column heading 52B Q1 is 3-F-Ph, R1 is Me and R2 is Br. 53B Q1 is 3-F-Ph, R1 is Me and R2 is I. 54B Q1 is 3-F-Ph, R1 is Br and R2 is Br. 55B Q1 is 3-F-Ph &gt; R1 is Br and R2 is CBu 56B Q1 is 3-F-Ph, R1 is Cl and R2 is Br. 57B Q1 is 3-F-Ph, r1 is ci and r2 is cn. 58B Q1 is 3-CF2HO -Ph , R1 is Cl and R2 is Me. 59B Q1 is 3-CF2HO-Ph, R1 is Cl and R2 is CFH2. 60B Q1 is 3-CF2HO-Ph, R1 is Br and R2 is Me. 61B Q1 is 3-CF2HO-Ph, R1 is I and R2 is Me. 62B Q1 is 3-CF2HO -Ph , R1 is Me and R2 is Me. 63B Q1 is 3-CF2HO -Ph , R1 is Me and R2 is Cl. 64B Q1 is 3-CF2HO -Ph , R1 is Me and R2 is Br. 65B Q1 is 3-CF2HO -Ph , R1 is Me and R2 is I. 66B Q1 is 3-CF2HO-Ph, R1 is Br and R2 is Br. 67B Q1 is 3-CF2HO-Ph, R1 is Br and R2 is Cl. 68B Q1 is 3-CF2HO-Ph, R1 is Cl and R2 is Br. 69B Q1 is 3-CF2HO-Ph, R1 is Cl and R2 is Cl. 70B Q1 is 4-Me-Ph, R1 is Cl and R2 is Me. 71B Q1 is 4-Me-Ph, R1 is Cl and R2 is CFH2. 72B Q1 is 4-Me-Ph, R1 is Br and R2 is Me. 73B Q1 is 4-Me-Ph, R1 is I and R2 is Me. 74B Q1 is 4-Me-Ph, R1 is Me and R2 is Me. 75B Q1 is 4-Me-Ph, R1 is Me and R2 is C1. 76B Q1 is 4-Me-Ph, R1 is Me and R2 is Br. 77B Q1 is 4-Me-Ph, R1 is Me and R2 is I. 78B Q1 is 4-Me-Ph, R1 is Br and R2 is Br. 79B Q1 is 4-Me-Ph, R1 is Br and R2 is CBu 80B Q1 is 4-Me-Ph, R1 is C1 and R2 is Br. 81B Q1 is 4-Me-Ph, R1 is C1 and R2 is α. 82B Q1 is 3-Me-Ph, R1 is C1 and R2 is Me. 83B Q1 is 3-Me-Ph, R1 is C1 and R2 is CFH2. 84B Q1 is 3-Me-Ph, R1 is Br and R2 is Me. 85B Q1 is 3-Me-Ph, R1 is I and R2 is Me. 86B Q1 is 3-Me-Ph, R1 is Me and R2 is Me. 151284.doc -139- 201117722 Table Column heading 87B Q1 is 3-Me-Ph, R1 is Me and R2 is α. 88B Q1 is 3-Me-Ph, R1 is Me and R2 is Br. 89B Q1 is 3-Me-Ph, R1 is Me and R2 is I. 90B Q1 is 3-Me-Ph, R1 is Br and R2 is Br. 91B Q1 is 3-Me-Ph, R1 is Br and R2 is Cl. 92B Q1 is 3-Me-Ph, R1 is Cl and R2 is Br. 93B Q1 is 3-Me-Ph, R1 is C1 and R2 is CBu 94B Q1 is 4-Et-Ph, R1 is Cl and R2 is Me. 95B Q1 is 4-Et-Ph &gt; R1 is Cl and R2 is CFH2. 96B Q1 is 4-Et-Ph, R1 is Br and R2 is Me. 97B Q1 is 4-Et-Ph, R1 is I and R2 is Me. 98B Q1 is 4-Et-Ph, R1 is Me and R2 is Me. 99B Q1 is 4-Et-Ph &gt; R1 is Me and R2 is a. 100B Q1 is 4-Et-Ph, R1 is Me and R2 is Br. 101B Q1 is 4-Et-Ph - R1 is Me and R2 is I. 102B Q1 is 4-Et-Ph » R1 is Br and R2 is Br. 103B Q1 is 4-Et-Ph » R1 is Br and R2 is Cl. 104B Q1 is 4-Et-Ph, R1 is Cl and R2 is Br. 105B Q1 is 4-Et-Ph, R1 is Cl and R2 is Cl. 106B Q1 is 4-C1 ' 3-F-Ph , R1 is C1 and R2 is Me. 107B Q1 is 4-C1 ' 3-F-Ph , R1 is C1 and R2 is CFH2. 108B Q1 is 4-C1 ' 3-F-Ph , R1 is Br and R2 is Me. 109B Q1 is 4-C1 ' 3-F-Ph , R1 is I and R2 is Me. 110B Q1 is 4-C1 ' 3-F-Ph , R1 is Me and R2 is Me. 111B Q1 is 4-C1 ' 3-F-Ph , R1 is Me and R2 is C Bu 112B Q1 is 4-C1 ' 3-F-Ph , R1 is Me and R2 is Br. 113B Q1 is 4-C1, 3-F-Ph, R1 is Me and R2 is I. 114B Q1 is 4-C1 ' 3-F-Ph , R1 is Br and R2 is Br. 115B Q1 is 4-C1 ' 3-F-Ph , R1 is Br and R2 is C Bu 116B Q1 is 4-C1 ' 3-F-Ph , R1 is C1 and R2 is Br. 117B Q1 is 4-C1 &gt; 3-F-Ph, R1 is C1 and R2 is C1. 118B Q1 is 2-C1 ' 4-F-Ph , R1 is C1 and R2 is Me. 119B Q1 is 2-C1 &gt; 4-F-Ph , R1 is C1 and R2 is CFH2. 120B Q1 is 2-C1 '4-F-Ph, R1 is Br and R2 is Me. 121B Q1 is 2-C1 ' 4-F-Ph , R1 is I and R2 is Me. 151284.doc -140· 201117722 Table Column heading 122B Q1 is 2-C1, 4-F-Ph, R1 is Me and R2 is Me. 123B Q1 is 2-C1, 4-F-Ph, R1 is Me and R2 is Π. 124B Q1 is 2-C1, 4-F-Ph, Ri is Me and R2 is Br. 125B Q1 is 2-C1, 4-F-Ph, R1 is Me and R2 is I. 126B Q1 is 2-C1 '4-F-Ph, R1 is Br and R2 is Br. 127B Q1 is 2-C1 '4-F-Ph, R1 is Br and R2 is Cl. 128B Q1 is 2-C1, 4-F-Ph, R1 is Cl and R2 is Br. 129B Q1 is 2-C1, 4-F-Ph, R1 is Cl and R2 is a. 130B Q1 is 4-F, 3-Me-Ph, R1 is Cl and R2 is Me. 131B Q1 is 4-F, 3-Me-Ph, R1 is Cl and R2 is CFH2. 132B Q1 is 4-F, 3-Me-Ph, R1 is Br and R2 is Me. 133B Q1 is 4-F, 3-Me-Ph, R1 is I and R2 is Me. 134B Q1 is 4-F, 3-Me-Ph, R1 is Me and R2 is Me. 135B Q1 is 4-F, 3-Me-Ph, R1 is Me and R2 is a. 136B Q1 is 4-F, 3-Me-Ph, R1 is Me and R2 is Br. 137B Q1 is 4-F ' 3-Me-Ph , R1 is Me and R2 is I. 138B Q1 is 4-F, 3-Me-Ph, R1 is Br and R2 is Br. 139B Q1 is 4-F &gt; 3-Me-Ph, R1 is Br and R2 is CM. 140B Q1 is 4-F ' 3-Me-Ph , R1 is Cl and R2 is Br. 141B Q1 is 4-F, 3-Me-Ph, R1 is Cl and R2 is CBu 142B Q1 is 3,4-: --F-Ph &gt; R1 is Cl and R2 is Me. 143B Q1 is 3,4-di-F-Ph, R1 is Cl and R2 is CFH2. 144B Q1 is 3,4-: _-F-Ph &gt; R1 is Br and R2 is Me. 145B Q1 is 3,4-di-F-Ph &gt; R1 is I and R2 is Me. 146B Q1 is 3,4-di-F-Ph, R1 is Me and R2 is Me. 147B Q1 is 3,4-di-F-Ph &gt; R1 is Me and R2 is a. 148B Q1 is 3,4-di-F-Ph &gt; R1 is Me and R2 is Br. 149B Q1 is 3,4-di-F-Ph - R1 is Me and R2 is I. 150B Q1 is 3,4-di-F-Ph, R1 is Br and R2 is Br. 151B Q1 is 3,4-di-F-Ph, R1 is Br and R2 is Cl. 152B Q1 is 3,4-di-F-Ph, R1 is Cl and R2 is Br. 153B Q1 is 3,4-di-F-Ph, R1 is Cl and R2 is Cl. 154B Q1 is 3,4-di-Cl-Ph, R1 is Cl and R2 is Me. 155B Q1 is 3,4- --Cl-Ph &gt; R1 is Cl and R2 is CFH2. 156B Q1 is 3,4-- --Cl-Ph &gt; R1 is Br and R2 is Me. -141 - 151284.doc 201117722 Table Column headings 157B Q1 is 3,4-di-Cl-Ph, R1 is I and R2 is Me. 158B Q1 is 3,4-di-Cl-Ph, R1 is Me and R2 is Me. 159B Q1 is 3,4-di-Cl-Ph, R1 is Me and R2 is C1. 160B Q1 is 3,4-di-Cl-Ph, R1 is Me and R2 is Br. 161B Q1 is 3,4-di-Cl-Ph, R1 is Me and R2 is I. 162B Q1 is 3,4-di-Cl-Ph, R1 is Br and R2 is Br. 163B Q1 is 3,4-di-Cl-Ph, R1 is Br and R2 is C1. 164B Q1 is 3,4-di-Cl-Ph, R1 is C1 and R2 is Br. 165B Q1 is 3,4-di-Cl-Ph, R1 is C1 and R2 is C1. 166B Q1 is 3,5-di-MeO-Ph, R1 is C1 and R2 is Me. 167B Q1 is 3,5-di-MeO-Ph, R1 is C1 and R2 is CFH2. 168B Q1 is 3,5-di-MeO-Ph, R1 is Br and R2 is Me. 169B Q1 is 3,5-di-MeO-Ph, R1 is I and R2 is Me. 170B Q1 is 3,5-di-MeO-Ph, R1 is Me and R2 is Me. 171B (^ is 3,5-two-1^0-?11, 111 is PCT 6 and 112 is (:1. 172B Q1 is 3,5-di-MeO-Ph, Ri is Me and R2 is Br. 173B Q1 is 3,5-di-MeO-Ph, R1 is Me and R2 is I. 174B Q1 is 3,5-di-MeO-Ph, R1 is Br and R2 is Br. 175B Q1 is 3,5-di- MeO-Ph, R1 is Br and R2 is Cl. 176B Q1 is 3,5-di-MeO-Ph, R1 is C1 and R2 is Br. 177B Q1 is 3,5-di-MeO-Ph, R1 is C1 and R2 is CH. 178B Q1 is 2-a, 3,5-di-MeO-Ph, R1 is C1 and R2 is Me. 179B Q1 is 2-Cl, 3,5-di-MeO-Ph, R1 is Cl and R2 is CFH2. 180B Q1 is 2-CU, 3,5-di-MeO-Ph, R1 is Br and R2 is Me. 181B Q1 is 2-C1, 3,5-di-MeO-Ph, R1 is I and R2 is Me. 182B Q1 is 2-C1, 3,5-di-MeO-Ph, R丨 is Me and R2 is Me. 183B Q1 is 2-C1, 3,5-di-MeO-Ph, R1 is Me And R2 is α. 184B ()1 is 2-(:1,3,5-two-1^0-?11, 111 is 1^ and 112 is 81. 185B Q1 is 2-CU, 3,5- Di-MeO-Ph, R1 is Me and R2 is I. 186B Q1 is 2-C1, 3,5_di-MeO-Ph, R1 is Br and R2 is Br. 187B Q1 is 2-C1,3,5-di-MeO-Ph, R1 is Br and R2 is CBu 188B Q1 is 2-CBu 3,5-di-MeO-Ph, R1 is C1 and R2 is Br. 189B ()1 is 2-(:Bu 3,5-II-1^0-?11,111 is (:1 and 112 are (:Bu 190B Q1 is 4-C1,3,5-di-MeO-Ph , R1 is C1 and R2 is Me. 191B Q1 is 4-Cb 3,5-di-MeO-Ph, R1 is C1 and R2 is CFH2. 151284.doc •142-

201117722 表 192B 193B 194B 195B 196B 197B 198B 199B 200B 201B 202B 203B 204B 205B 206B 207B 208B 209B 210B 211B 212B 213B 214B 215B 216B 217B 218B 219B 220B 221B 222B 223B 224B 225B 226B 列標題 Q1 是 4-CU、3,5-二-MeO-Ph，R1 是 Br 以及 R2 是 Me。 Q1 是 4-C1、3,5-二-MeO-Ph，R1 是 I 以及 R2 是 Me。 Q1 是 4-C1、3,5-二-MeO-Ph，R1 是 Me 以及 R2 是 Me。 Q1 是 4-C1、3,5-二-MeO-Ph，R1 是 Me 以及 R2 是 C卜 Q1是4-C卜3,5-二-MeO-Ph，R1是Me以及R2是Br。 Q1 是 4-C1、3,5-二-MeO-Ph，R1 是 Me 以及 R2 是 I。 Q1 是 4-C1、3,5-二-MeO-Ph，R1 是 Br 以及 R2 是 Br。 Q1 是 4-C卜 3,5-二-MeO-Ph，R1 是 Br 以及 R2 是 C1。 Q1 是 4-C卜 3,5-二-MeO-Ph，R1 是 C1 以及 R2 是 Br。 Q1!4-Cl、3,5-:-MeO-Ph，R1*CUX&amp;R2Sa。 Q1 是 4-Cl-Bn，R1 是 Cl 以及 R2 是 Me。 Q1 是 4-Cl-Bn，R1 是 C1 以及 R2 是 CFH2。 Q1 是 4-Cl-Bn，R1 是 Br 以及 R2 是 Me。 Q1 是 4-Cl-Bn，R1 是 I 以及 R2 是 Me。 Q1 是 4-Cl-Bn，R1 是 Me 以及 R2 是 Me。 Q1 是 4-Cl-Bn，R1 是 Me 以及 R2 是 C1。 Q1 是 4-Cl-Bn，R1 是 Me 以及 R2 是 Br。 Q1 是 4-Cl-Bn，R1 是 Me 以及 R2 是 I。 Q1 是 4-Cl-Bn，R1 是 Br 以及 R2 是 Br。 Q1 是 4-Cl-Bn，R1 是 Br 以及 R2 是 C1。 Q1 是 4-Cl-Bn，R1 是 C1 以及 R2 是 Br。 Q1 是 4-Cl-Bn，R1 是 C1 以及 R2 是 C1。 Q1 是 4-F-Bn，R1 是 C1 以及 R2 是 Me。 Q1 是 4-F-Bn，R1 是 C1 以及 R2 是 CFH2。 Q1 是 4-F-Bn，R1 是 Br 以及 R2 是 Me。 Q1 是 4-F-Bn，R1 是 I 以及 R2 是 Me。 Q1 是 4-F-Bn，R1 是 Me 以及 R2 是 Me。 Q1 是 4-F-Bn，R1 是 Me 以及 R2 是 C1。 Q1 是 4-F-Bn，R1 是 Me 以及 R2 是 Br。 Q1 是 4-F-Bn，R1 是 Me 以及 R2 是 I。 Q1 是 4-F-Bn，R1 是 Br 以及 R2 是 Br。 Q1 是 4-F-Bn，R1 是 Br 以及 R2 是 C1。 Q1 是 4-F-Bn，R1 是 CI 以及 R2 是 Br。 Q1 是 4-F-Bn，R1 是 C1 以及 R2 是 C1。 Q1是6-C1-3-吡啶基，R1是C1以及R2是Me。 151284.doc •143- 201117722 表 列標題 227B Q1是6-C1-3-吡啶基， R1是C1以及R2是CFH2。 228B Q1是6-C1-3-»比啶基， R1是Br以及R2是Me。 229B Q1是6-C1-3-吡啶基， R1是I以及R2是Me。 230B Q1是6-C1-3-吡啶基， R1是Me以及R2是Me。 231B Q1是6-C1-3-吡啶基， R1是Me以及R2是CM。 232B Q1是6-C1-3-吡啶基， R1是Me以及R2是Br。 233B Q1是6-C1-3-吡啶基， R1是Me以及R2是I。 234B Q1是6-01-3-°比啶基， R1是Me以及R2是MeO。 235B Q1是6-C1-3-吡啶基， R1是MeO以及R2是Me。 236B Q1是6-C1-3-。比啶基， R1是Br以及R2是Br。 237B Q1是6-C1-3-吡啶基， R1是Br以及R2是Q。 238B Q1是6-C1-3-吡啶基， R1是C1以及R2是Br。 239B Q1是6-C1-3-。比啶基， R1是C1以及R2是C卜 240B Q1是6-C1-3-吡啶基， R1是Me以及R2是MeS。 241B Q1是6-C1-3-吡啶基， R1是MeS以及R2是Me。 242B Q1是6-C1-3-吡啶基， R1是Et以及R2是Br。 243B Q1是6-C1-3-吡啶基， R1是Et以及R2是α。 244B Q1是6-C1-3-吡啶基， R1是Et以及R2是Me。 245B Q1是6-C1-3-»比啶基， R1是Me以及R2是Et。 246B Q1是6-C1-3-吡啶基， R1是C1以及R2是Et。 247B Q1是6-C1-3-吡啶基， R1是Me以及R2是CN。 248B Q1是6-Me-3-吡啶基 R1是C1以及R2是Me。 249B Q1是6-Me-3-吡啶基 R1是C1以及R2是CFH2。 250B Q1是6-Me-3-。比啶基 R1是Br以及R2是Me。 251B Q1是6-Me-3-吡啶基 R1是I以及R2是Me。 252B Q1是6-Me-3-吡啶基 R1是Me以及R2是Me。 253B Q1是6-Me-3-吡啶基 R1是Me以及R2是Cb 254B Q1是6-Me-3-吡啶基 R1是Me以及R2是Br。 255B Q1是6-Me-3-吡啶基 R1是Me以及R2是I。 256B Q1是6-Me-3-吡啶基 Ri是Br以及R2是Br。 257B Q1是6-Me-3-吡啶基 R1是Br以及R2是CM。 258B Q1是6-Me-3-吡啶基 R1是Cl以及R2是Br。 259B Q1是6-Me-3-e比咬基 R1是C1以及R2是C1。 260B Q1是6-MeO-3-。比啶基 ，R1是C1以及R2是Me。 261B Q1是6-MeO-3-吡啶基 ，R1是C1以及R2是CFH2。 151284.doc -144- 201117722 表 列標題 262B 263B 264B 265B 266B 267B 268B 269B 270B 271B 272B 273B 274B 275B 276B 277B 278B 279B 280B 281B 282B 283B 284B 285B 286B 287B 288B 289B 290B 291B 292B 293B 294B 295B 296B Q1是6-MeO-3-吡啶基，R1是Br以及R2是Me。 Q1是6-MeO-3-吡啶基，R1是I以及R2是Me。 Q1是6-Me〇-3-吡啶基，R1是Me以及R2是Me。 Q1是6-MeO-3-吡啶基，R1是Me以及R2是C卜 Q1是6-MeO-3-吡啶基，R1是Me以及R2是Br。 Q1是6-MeO-3-吡啶基，R1是Me以及R2是I。 Q1是6-MeO-3-吡啶基，R1是Br以及R2是Br。 Q1是6-MeO-3-吡啶基，R1是Br以及R2是C1。 Q1是6-MeO-3-吡啶基，R1是C1以及R2是Br。 Q1是6-MeO-3-吡啶基，R1是C1以及R2是CM。 Q1是6-CF3-3-吡啶基，R1是C1以及R2是Me。 Q1是6-CF3-3-吡啶基，R1是C1以及R2是CFH2。 Q1是6-CF3-3-吡啶基，R1是Br以及R2是Me。 Q1是6-CF3-3-吡啶基，R1是I以及R2是Me。 Q1是6-CF3-3-吡啶基，R1是Me以及R2是Me。 Q1是6-CF3-3-吡啶基，R1是Me以及R2是C1。 Q1是6-CF3-3-吡啶基，R1是Me以及R2是Br。 Q1是6-CF3-3-吡啶基，R1是Me以及R2是I。 Q1是6-CF3-3-吡啶基，R1是Br以及R2是Br。 Q1是6-CF3-3-吡啶基，R1是Br以及R2是C1。 Q1是6-CF3-3-吡啶基，R1是C1以及R2是Br。 Q1是6-CF3-3-吡啶基，R1是C1以及R2是C1。 Q1是6-Br-3-吡啶基，R1是C1以及R2是Me。 Q1是6-Br-3-吡啶基，R1是C1以及R2是CFH2。 Q1是6-Br-3-吡啶基，R1是Br以及R2是Me。 Q1是6-Br-3-吡啶基，R1是I以及R2是Me。 Q1是6-Br-3-吡啶基，R1是Me以及R2是Me。 Q1是6-Br-3-吡啶基，R1是Me以及R2是C1。 Q1是6-Br-3-吡啶基，R1是Me以及R2是Br。 Q1是6-Br-3-吡啶基，R1是Me以及R2是I。 Q1是6-Br-3-吡啶基，R1是Br以及R2是Br。 Q1是6-Br-3-吡啶基，R1是Br以及R2是C1。 Q1是6-ΒΓ-3-吡啶基，R1是C1以及R2是Br。 Q1是6-Br-3-吡啶基，R1是C1以及R2是C1。 Q1是6-F-3-吡啶基，R1是C1以及R2是Me。 151284.doc -145- 201117722 表 列標題 297B Q1是6-F-3-吡啶基，R1是Cl以及R2是CFH2。 298B Q1是6-F-3-吡啶基，R1是Br以及R2是Me。 299B Q1是6-F-3-吡啶基，R1是I以及R2是Me。 300B Q1是6-F-3-吡啶基，R1是Me以及R2是Me。 301B Q1是6-F-3-吡啶基，R1是Me以及R2是α。 302B Q1是6-F-3-吡啶基，R1是Me以及R2是Br。 303B Q1是6-F-3-吡啶基，R1是Me以及R2是I。 304B Q1是6-F-3-吡啶基，R1是Br以及R2是Br。 305B Q1是6-F-3-吡啶基，R1是Br以及R2是C1。 306B Q1是6-F-3-吡啶基，R1是C1以及R2是Br。 307B Q1是6-F-3-吡啶基，R1是C1以及R2是C1。 308B Q1是2-C1、6-Me-4-吡啶基，R1是C1以及R2是Me。 309B Q1 是 2-a、6-Me-4-吡啶基，R1 是 C1 以及 R2 是 CFH2。 310B Q1是2-C1、6-Me-4-吡啶基，Ri是Br以及R2是Me。 311B Q1是2-C1、6-Me-4-吡啶基，R1是I以及R2是Me。 312B Q1是2-C1、6-Me-4-吡啶基，R1是Me以及R2是Me。 313B Q1是2-C1、6-Me-4-吡啶基，R1是Me以及R2是Π。 314B Q1是2-C1、6-Me-4-吡啶基，R1是Me以及R2是Br。 315B Q1是2-C1、6-Me-4-吡啶基，R1是Me以及R2是I。 316B Q1是2-C1、6-Me-4-吡啶基，R1是Br以及R2是Br。 317B Q1是2-C1、6-Me-4-吡啶基，R1是Br以及R2是C卜 318B Q1是2-C1、6-Me-4-吡啶基，R1是C1以及R2是Br。 319B Q1是2-C1、6-Me-4-吡啶基，R1是C1以及R2是C卜 320B Q1 是 2-C1、6-MeO-3-吡啶基，R1 是 C1 以及 R2 是 Me。 321B Q1 是 2-CM、6-MeO-3-吡啶基，R1 是 C1 以及 R2 是 CFH2。 322B Q1 是 2-C1、6-MeO-3-吡啶基，R1 是 Br 以及 R2 是 Me。 323B Q1是2-C1、6-MeO-3-吡啶基，R1是I以及R2是Me。 324B Q1 是 2-C1、6-MeO-3-吡啶基，R1 是 Me 以及 R2 是 Me。 325B Q1 是 2-C1、6-MeO-3-吡啶基，R1 是 Me 以及 R2 是 C1。 326B Q1 是 2-C1、6-MeO-3-吡啶基，R1 是 Me 以及 R2 是 Br。 327B Q1是2-C1、6-MeO-3-吡啶基，R1是Me以及R2是I。 328B Q1 是 2-C1、6-MeO-3-吡啶基，R1 是 Br 以及 R2 是 Br。 329B Q1 是 2-C1、6-MeO-3-吡啶基，R1 是 Br 以及 R2 是 C1。 330B Q】是2-C卜6-MeO-3-吡啶基，R1是C1以及R2是Br。 331B Q1 是 2-C1、6-MeO-3-吡啶基，R1 是 C1 以及 R2 是 C1。 151284.doc -146- 201117722 表 列標題 332B Q1 是 2-C1、6-CF3-3-吡啶基，R1 是 Cl 以及 R2 是 Me。 333B Q1 是 2-Q、6-CF3-3-吡啶基，R1 是 C1 以及 R2 是 CFH2。 334B Q1 是 2-C1、6-CF3-3-吡啶基，R1 是 Br 以及 R2 是 Me。 335B Qi是2-a、6-CF3-3-吡啶基，R1是I以及R2是Me。 336B Q1 是 2-C1、6-CF3-3-吡啶基，R1 是 Me 以及 R2 是 Me。 337B Q1 是 2-C1、6-CF3-3-吡啶基，R1 是 Me 以及 R2 是 C1。 338B Q1 是 2-C1、6-CF3-3-吡啶基，R1 是 Me 以及 R2 是 Br。 339B Q1是2-C16-CF3-3-吡啶基，R1是Me以及R2是I。 340B Q1 是 2-C1、6-CF3-3-吡啶基，R1 是 Br 以及 R2 是 Br。 341B Q1 是 2-C1、6-CF3-3-吡啶基，R1 是 Br 以及 R2 是 C1。 342B Q1 是 2-C1、6-CF3-3-吡啶基，R1 是 C1 以及 R2 是 Br。 343B Q1 是 2-C1、6-CF3-3-吡啶基，R1 是 C1 以及 R2 是 C1。 344B Q1是5-C1-3-吡啶基，R1是C1以及R2是Me。 345B Q1是5-C1-3-吡啶基，R1是C1以及R2是CFH2。 346B Q1是5-CI-3-吡啶基，R1是Br以及R2是Me。 347B Q1是5-C1-3-吡啶基，R1是I以及R2是Me。 348B Q1是5-C1-3-吡啶基，R1是Me以及R2是Me。 349B Q1是5-C1-3-吡啶基，R1是Me以及R2是C1。 350B Q1是5-C1-3-吡啶基，R1是Me以及R2是Br。 351B Q1是5-C1-3-吡啶基，R1是Me以及R2是I。 352B Q1是5-C1-3-吡啶基，R1是Br以及R2是Br。 353B Q1是5-C1-3-吡啶基，R1是Br以及R2是C1。 354B Q1是5-C1-3-吡啶基，R1是C1以及R2是Br。 355B Q1是5-C1-3-吡啶基，R1是C1以及R2是C1。 356B Q1是5-F-3-吡啶基，R1是C1以及R2是Me。 357B Q1是5-F-3-吡啶基，R1是C1以及R2是CFH2。 358B Q1是5-F-3-吡啶基，R1是Br以及R2是Me。 359B Q1是5-F-3-吡啶基，R1是I以及R2是Me。 360B Q1是5-F-3-吡啶基，R1是Me以及R2是Me。 361B Q1是5-F-3-吡啶基，R1是Me以及R2是C1。 362B Q1是5-F-3-吡啶基，R1是Me以及R2是Br。 363B Q1是5-F-3-吡啶基，R1是Me以及R2是I。 364B Q1是5-F-3-吡啶基，R1是Br以及R2是Br。 365B Q1是5-F-3·吡啶基，R1是Br以及R2是C1。 366B Q1是5-F-3-吡啶基，R1是C1以及R2是Br。 151284.doc 147· 201117722 表 列標題 367B Q1是5-F-3-吡啶基，R1是Cl以及R2是CU。 368B Q1是5-Me-3-吡啶基，R1是Cl以及R2是Me。 369B Q1是5-Me-3-吡啶基，R1是C1以及R2是CFH2。 370B Q1是5-Me-3-吡啶基，R1是Br以及R2是Me。 371B Q1是5-Me-3-吡啶基，R1是I以及R2是Me。 372B Q1是5-Me-3-吡啶基，R1是Me以及R2是Me。 373B Q1是5-Me-3-吡啶基，R1是Me以及R2是CM。 374B Q1是5-Me-3-°比咬基，R1是Me以及R2是Br。 375B Q1是5-Me-3-吡啶基，R1是Me以及R2是I。 376B Q1是5-Me-3-吡啶基，R1是Br以及R2是Br。 377B Q1是5-Me-3-吡啶基，R1是Br以及R2是CU。 378B Q1是5-Me-3-吡啶基，R1是C1以及R2是Br。 379B Q1是5-Me-3-吡啶基，R1是C1以及R2是C1。 380B Q1是5-MeO-3-吡啶基，R1是C1以及R2是Me。 381B Q1是5-MeO-3-吡啶基，R1是C1以及R2是CFH2。 382B Q1是5-MeO-3-吡啶基，R1是Br以及R2是Me。 383B Q1是5-MeO-3-吡啶基，R1是I以及R2是Me。 384B Q1是5-MeO-3-吡啶基，R1是Me以及R2是Me。 385B Q1是5-MeO-3-吡啶基，R1是Me以及R2是C卜 386B Q1是5-MeO-3-吡啶基，R1是Me以及R2是Br。 387B Q1是5-MeO-3-吡啶基，R1是Me以及R2是I。 388B Q1是5-MeO-3-吡啶基，R1是Br以及R2是Br。 389B Q1是5-MeO-3-吡啶基，R1是Br以及R2是C卜 390B Q1是5-MeO-3-吡啶基，R1是C1以及R2是Br。 391B Q1是5-MeO-3-吡啶基，R1是C1以及R2是（：卜 392B Q1 是 6-C1、5-MeO-3-吡啶基，R1 是 Cl 以及 R2 是 Me。 393B Q1是6-C卜5-MeO-3-吡啶基，R1是C1以及R2是CFH2。 394B Q1 是 6-C1、5-MeO-3-吡啶基，R1 是 Br 以及 R2 是 Me。 395B Q1是6-C1、5-MeO-3-吡啶基，Ri是I以及R2是Me。 396B Q1 是 6-C1、5-MeO-3-吡啶基，R1 是 Me 以及 R2 是 Me。 397B Q1是6-C1、5-MeO-3-吡啶基，R1是Me以及R2是Q。 398B Q1 是 6-C1、5-MeO-3-吡啶基，R1 是 Me 以及 R2 是 Br。 399B Q1是6-C1、5-MeO-3-吡啶基，R1是Me以及R2是I。 400B Q1 是 6-C1、5-MeO-3-吡啶基，R1 是 Br 以及 R2 是 Br。 401B Q1 是 6-C1、5-MeO-3-吡啶基，R1 是 Br 以及 R2 是 C1。 151284.doc -148- 201117722 表 列標題 402B Q1 是 6_C1、5-MeO-3-吡啶基，R1 是 Cl 以及 R2 是 Br。 403B Q1 是 6-a、5-MeO-3- &quot;比啶基，R1是C1以及R2是C1。 404B Q1是6-C1-3-嗒-井基， R1是C1以及R2是Me。 405B Q1是6-C1-3-嗒'井基， R1是C1以及R2是CFH2。 406B Q1是6-C1-3-嗒畊基， R1是Br以及R2是Me。 407B Q1是6-C1-3-嗒畊基， R1是I以及R2是Me。 408B Q1是6-C1-3-嗒畊基， R1是Me以及R2是Me。 409B Q1是6-C1-3-嗒畊基， R1是Me以及R2是C1。 410B Q1是6-CI-3-嗒畊基， R1是Me以及R2是Br。 411B Q1是6-C1-3-嗒畊基， R1是Me以及R2是I。 412B Q1是6-C1-3-嗒》井基， R1是Br以及R2是Br。 413B Q1是6-C1-3-嗒畊基， R1是Br以及R2是α。 414B Q1是6-C1-3-嗒畊基， R1是C1以及R2是Br。 415B Q1是6-C1-3-嗒畊基， R1是C1以及R2是α。 416B Q1是6-Me-3-嗒畊基， R1是C1以及R2是Me。 417B Q1是6-Me-3-嗒畊基， R1是C1以及R2是CFH2。 418B Q1是6-Me-3-嗒&quot;井基， R1是Br以及R2是Me。 419B Q1是6-Me-3-嗒畊基， R1是I以及R2是Me。 420B Q1是6-Me-3-嗒畊基， R1是Me以及R2是Me。 421B Q1是6-Me-3-嗒畊基， R1是Me以及R2是C卜 422B Q1是6-Me-3-嗒η井基， R1是Me以及R2是Br。 423B Q1是6-Me-3-嗒啩基， R1是Me以及R2是I。 424B Q1是6-Me-3-嗒畊基， R1是Br以及R2是Br。 425B Q1是6-Me-3-嗒畊基， R1是Br以及R2是C1。 426B Q1是6-Me-3-嗒嗜基， R1是C1以及R2是Br。 427B Q1是6-Me-3-嗒哨基， R1是C1以及R2是C1。 428B Q1是6-MeO-3-嗒啫基 ，R1是C1以及R2是Me。 429B Q1是6-MeO-3-嗒嗜基 ，R1是C1以及R2是CFH2。 430B Q1是6-MeO-3-嗒畊基 ，R1是Br以及R2是Me。 431B Q1是6-MeO-3-嗒畊基 ，R1是I以及R2是Me。 432B Q1是6-MeO-3-嗒畊基 ，R1是Me以及R2是Me。 433B Q1是6-MeO-3-嗒畊基 ，R1是Me以及R2是C1。 434B Q1是6-MeO-3-嗒井基 ，R1是Me以及R2是Br。 435B Q1是6-MeO-3-嗒哨·基 ，R1是Me以及R2是I。 436B Q1是6-MeO-3-嗒呼基 ，R1是Βι•以及R2是Br。 151284.doc -149- 201117722 表 列標題 437B Q1是6-MeO-3-嗒畊基，R1是Br以及R2是Cl。 438B Q1是6-MeO-3-嗒畊基，R1是C1以及R2是Br。 439B Q1是6-MeO-3-嗒哨·基，R1是C1以及R2是C1。 440B Q1是6-CF3-3-嗒畊基，R1是C1以及R2是Me。 441B Q1是6-CF3-3·嗒'井基，R1是C1以及R2是CFH2。 442B Q1是6-CF3-3-嗒井基，R1是Br以及R2是Me。 443B Q1是6-CF3-3-嗒畊基，R1是I以及R2是Me。 444B Q1是6-CF3-3-嗒畊基，R1是Me以及R2是Me。 445B Q1是6-CF3-3-嗒畊基，R1是Me以及R2是C1。 446B Q1是6-CF3-3-嗒畊基，R1是Me以及R2是Br。 447B Q1是6-CF3-3-嗒畊基，R1是Me以及R2是I。 448B Q1是6-CF3-3-嗒井基，Ri是Br以及R2是Br。 449B Q1是6-CF3-3-嗒哨基，Ri是Br以及R2是C卜 450B Q1是6-CF3-3-嗒喷基，R1是C1以及R2是Br。 451B Q1是6-CF3-3-嗒嗜基，R1是C1以及R2是α。 452B Q1是5-C1-3-嗒啡基，R1是C1以及R2是Me。 453B Q1是5-C1-3-嗒畊基，R1是C1以及R2是CFH2。 454B Q1是5-C1-3-嗒畊基，R1是Br以及R2是Me。 455B Q1是5-C1-3-嗒啩基，R1是I以及R2是Me。 456B Q1是5-C1-3-嗒畊基，R1是Me以及R2是Me。 457B Q1是5-C1-3-嗒畊基，R1是Me以及R2是C1。 458B Q1是5-C1-3-嗒畊基，R1是Me以及R2是Br。 459B Q1是5-C1-3-嗒畊基，R1是Me以及R2是I。 460B Q1是5-C1-3-嗒畊基，R1是Br以及R2是Br。 461B Q1是5-C1-3-嗒啩基，R1是Br以及R2是α。 462B Q1是5-C1-3-嗒畊基，R1是C1以及R2是Br。 463B Q1是5-C1-3-嗒畊基，R1是C1以及R2是α。 464B Q1是5-F-3-嗒畊基，R1是C1以及R2是Me。 465B Q1是5-F-3-嗒畊基，R1是C1以及R2是CFH2。 466B Q1是5-F-3-嗒畊基，R1是Br以及R2是Me。 467B Q1是5-F-3-嗒畊基，R1是I以及R2是Me。 468B Q1是5-F-3-嗒畊基，R1是Me以及R2是Me。 469B Q1是5-F-3-嗒呼基，R1是Me以及R2是C1。 470B Q1是5-F-3-嗒畊基，R1是Me以及R2是Br。 471B Q1是5-F-3-嗒畊基，R1是Me以及R2是I » 151284.doc -150- 201117722 表 列標題 472B 473B 474B 475B 476B 477B 478B 479B 480B 481B 482B 483B 484B 485B 486B 487B 488B 489B 490B 491B 492B 493B 494B 495B 496B 497B 498B 499B 500B 501B 502B 503B 504B 505B 506B Q1是5-F-3-嗒p井基，R1是Br以及R2是Br。 Q1是5-F-3-嗒畊基，R1是Br以及R2是C1。 Q1是5-F-3-嗒》井基，R1是C1以及R2是Br。 Q1是5-F-3-嗒畊基，R1是C1以及R2是C1。 Q1是5-MeO-3-嗒畊基，R1是C1以及R2是Me。 Q1是5-MeO-3-嗒啩基，R1是C1以及R2是CFH2。 Q1是5-MeO-3-嗒畊基，R1是Br以及R2是Me。 Q1是5-MeO-3-嗒畊基，R1是I以及R2是Me。 Q1是5-MeO-3-嗒畊基，R1是Me以及R2是Me。 Q1是5-MeO-3-嗒畊基，R1是Me以及R2是C1。 Q1是5-MeO-3-嗒畊基，R1是Me以及R2是Br。 Q1是5-MeO-3-嗒畊基，R1是Me以及R2是I。 Q1是5-MeO-3-嗒畊基，R1是Br以及R2是Br。 Q1是5-MeO-3-嗒畊基，R1是Br以及R2是C1。 Q1是5-MeO-3-嗒&quot;井基，R1是C1以及R2是Br。 Q1是5-MeO-3-嗒畊基，R1是C1以及R2是C1。 Q1是2-C1-5-嘧啶，R1是C1以及R2是Me。 Q1是2-C1-5-嘧啶，R1是C1以及R2是CFH2。 Q1是2-C1-5-嘧啶，R1是Br以及R2是Me。 Q1是2-C1-5-嘧啶，R1是I以及R2是Me。 Q1是2-C1-5-嘧啶，R1是Me以及R2是Me。 Q1是2-C1-5嘧啶，R1是Me以及R2是C1。 Q1是2-C1-5-嘧啶，R1是Me以及R2是Br。 Q1是2-C1-5-嘧啶，R1是Me以及R2是I。 Q1是2-C1-5-嘧啶，R1是Br以及R2是Br。 Q1是2-C1-5-嘧啶，R1是Br以及R2是C1。 Q1是2-C1-5-嘧啶，R1是C1以及R2是Br。 Q1是2-C1-5-嘧啶，R1是C1以及R2是CI。 Q1是2-Me-5-嘧啶，R1是C1以及R2是Me。 Q1是2-Me-5-嘧啶，R1是C1以及R2是CFH2。 Q1是2-Me-5-嘧啶，R1是Br以及R2是Me。 Q1是2-Me-5-嘧啶，R1是I以及R2是Me。 Q1是2-Me-5-嘧啶，R1是Me以及R2是Me。 Q1是2-Me-5-嘧啶，R1是Me以及R2是C1。 Q1是2-Me-5-嘧啶，R1是Me以及R2是Br。 151284.doc -151 - 201117722 表 列標題 507B Q1是2-Me-5-嘧啶，R1是Me以及R2是I。 508B Q1是2-Me-5-嘧啶，R1是Br以及R2是Br。 509B Q1是2-Me-5-嘧啶，R1是Br以及R2是α。 510B Q1是2-Me-5-嘧啶，R1是C1以及R2是Br。 511B Q1是2-Me-5-嘧啶，R1是C1以及R2是C1。 512B Q1是2-MeO-5-嘧啶，R1是C1以及R2是Me。 513B Q1 是 2-MeO-5-嘧啶，R1 是 C1 以及 R2 是 CFH2。 514B Q1是2-MeO-5-嘧啶，R1是Br以及R2是Me。 515B Q1是2-MeO-5-嘧啶，R1是I以及R2是Me。 516B Q1是2-MeO-5-嘧啶，R1是Me以及R2是Me。 517B Q1是2-MeO-5-嘧啶，R1是Me以及R2是C1。 518B Q1是2-MeO-5-嘧啶，R1是Me以及R2是Br。 519B Q1是2-MeO-5-嘧啶，R1是Me以及R2是I。 520B Q1是2-MeO-5嘧啶，R丨是Br以及R2是Br。 521B Q1是2-MeO-5-嘧啶，R1是Br以及R2是C1。 522B Q1是2-MeO-5-嘧啶，R1是C1以及R2是Br。 523B Q1是2-MeO-5-嘧啶，R1是C1以及R2是C1。 524B Q1是2-CF3-5-嘧啶，R1是C1以及R2是Me。 525B Q1 是 2-CF3-5-嘧啶，R1 是 C1 以及 R2 是 CFH2。 526B Q1是2-CF3-5-嘧啶，R1是Br以及R2是Me。 527B Q1是2-CF3-5-嘧啶，R1是I以及R2是Me。 528B Q1是2-CF3-5-嘧啶，R1是Me以及R2是Me。 529B Q1是2-CF3-5-嘧啶，R1是Me以及R2是C1。 530B Q1是2-CF3-5-嘧啶，R1是Me以及R2是Br。 531B Q1是2-CF3-5-嘧啶，R1是Me以及R2是I。 532B Q1是2-CF3-5-嘧啶，R1是Br以及R2是Br。 533B Q1是2-CF3-5-嘧啶，R1是Br以及R2是C1。 534B Q1是2-CF3-5-嘧啶，R1是C1以及R2是Br。 535B Q1是2-CF3-5-嘧啶，R1是C1以及R2是C1。 536B Q1是5-C1-2-嘧啶，R1是C1以及R2是Me。 537B Q1是5-C1-2-嘧啶，R1是C1以及R2是CFH2。 538B Q1是5-C1-2-嘧啶，R1是Br以及R2是Me。 539B Q1是5-C1-2-嘧啶，R1是I以及R2是Me。 540B Q1是5-C1-2-嘧啶，R1是Me以及R2是Me。 541B Q1是5-C1-2-嘧啶，R1是Me以及R2是α。 151284.doc -152- 201117722 表 列標題 542B Q1 是 5-C1-2-嘧啶， R1是Me以及R2是Br。 543B Q1 是 5-C1-2-嘧啶， R1是Me以及R2是I。 544B Q1 是 5-C1-2-嘧啶， R1是Br以及R2是Br。 545B Q1 是 5-C1-2-嘧啶， R1是Br以及R2是α。 546B Q1 是 5-C1-2-嘧啶， R1是Cl以及R2是Br。 547B Q1 是 5-C1-2-嘧啶， R1是C1以及R2是α。 548B Q1 是 5-Me-2-嘧啶， R1是C1以及R2是Me。 549B Q1 是 5-Me-2-°S咬， R1是C1以及R2是CFH2。 550B Q1 是 5-Me-2-°§咬， R1是Br以及R2是Me。 551B Q1 是 5-Me-2-°^咬， R1是I以及R2是Me。 552B Q1 是 5-Me-2-嘧啶， R1是Me以及R2是Me。 553B Q1 是 5-Me-2-嘧啶， R1是Me以及R2是C1。 554B Q1 是 5-Me-2-嘧啶， R1是Me以及R2是Br。 555B Q1 是 5-Me-2-嘧啶， R1是Me以及R2是I。 556B Q1 是 5-Me-2-嘧啶， R1是Br以及R2是Br。 557B Q1 是 5-Me-2-嘧啶， R1是Br以及R2是α。 558B Q1 是 5-Me-2-嘧啶， R1是C1以及R2是Br。 559B Q1 是 5-Me-2-嘧啶， R1是C1以及R2是C1。 560B Q1 是 5-MeO-2-嘧啶 ，R1是C1以及R2是Me。 561B Q1 是 5-MeO-2-嘧啶 ，R1是C1以及R2是CFH2。 562B Q1 是 5-MeO-2-嘧啶 ，R1是Br以及R2是Me。 563B Q1 是 5-MeO-2-嘧啶 ，R1是I以及R2是Me。 564B Q1 是 5-MeO-2-嘧啶 ，R1是Me以及R2是Me。 565B Q1 是 5-MeO-2-嘧啶 ，R1是Me以及R2是C卜 566B Q1 是 5-MeO-2-嘧啶 ，R1是Me以及R2是Br。 567B Q1 是 5-MeO-2-°^咬 ，R1是Me以及R2是I。 568B Q1 是 5-MeO-2-嘧啶 ，R1是Br以及R2是Br。 569B Q1 是 5-MeO-2-嘧啶 ，R1是Br以及R2是α。 570B Q1 是 ，R1是C1以及R2是Br。 571B Q1 是 5-MeO-2-嘧啶 ，R1是C1以及R2是C1。 572B Q1 是 5-C1-2-嘧啶， R1是C1以及R2是Me。 573B Q1 是 5-C1-2-嘧啶， R1是C1以及R2是CFH2。 574B Q1 是 5-C1-2-嘧啶， R1是Br以及R2是Me。 575B Q1 是 5-C1-2-嘧啶， R1是I以及R2是Me。 576B Q1 是 5-C1-2-嘧啶， R1是Me以及R2是Me。 I51284.doc - 153 - 201117722 表 列標題 577B Q1是5-C1-2-嘧啶，R1是Me以及R2是CM。 578B Q1是5-C1-2-嘧啶，R1是Me以及R2是Br。 579B Q1是5-C1-2-嘧啶，R1是Me以及R2是I。 580B Q1是5-C1-2-嘧啶，R1是Br以及R2是Br。 581B Q1是5-C1-2-嘧啶，R1是Br以及R2是C1。 582B Q1是5-C1-2-嘧啶，R1是C1以及R2是Br。 583B Q1是5-C1-2-嘧啶，R1是C丨以及R2是CM。 584B Q1是5-CF3-2-嘧啶，R1是Cl以及R2是Me。 585B Q1 是 5-CF3-2-嘧啶，R1 是 C1 以及 R2 是 CFH2。 586B Q1是5-CF3-2-嘧啶，R1是Br以及R2是Me。 587B Q1是5-CF3-2-嘧啶，R1是I以及R2是Me。 588B Q1是5-CF3-2-嘧啶，R1是Me以及R2是Me。 589B Q1是5-CF3-2-嘧啶，R1是Me以及R2是C卜 590B Q1是5-CF3-2-嘧啶，R1是Me以及R2是Br。 591B Q1是5-CF3-2-嘧啶，R1是Me以及R2是I。 592B Q1是5-CF3-2-嘧啶，R1是Br以及R2是Br。 593B Q1是5-CF3-2-嘧啶，R1是Br以及R2是CH。 594B Q1是5-CF3-2-嘧啶，R1是C1以及R2是Br。 595B Q1是5-CF3-2-嘧啶，R1是C1以及R2是 &lt;：卜 596B Q1是5-Me-2-噻吩基，R1是Cl以及R2是Me。 597B Q1是5-Me-2-噻吩基，R1是C1以及R2是CFH2。 598B Q1是5-Me-2-噻吩基，R1是Br以及R2是Me。 599B Q1是5-Me-2-噻吩基，R1是I以及R2是Me。 600B Q1是5-Me-2-噻吩基，R1是Me以及R2是Me。 601B Q1是5-Me-2-噻吩基，R1是Me以及R2是C1。 602B Q1是5-Me-2-噻吩基，R1是Me以及R2是Br。 603B Q1是5-Me-2-噻吩基，R1是Me以及R2是I。 604B Q1是5-Me-2-噻吩基，R1是Br以及R2是Br。 605B Q1是5-Me-2-噻吩基，R1是Br以及R2是C1。 606B Q1是5-Me-2-噻吩基，R1是C1以及R2是Br。 607B Q1是5-Me-2-噻吩基，R1是C1以及R2是C1。 608B Q1是5-C1-2-噻吩基，R1是C1以及R2是Me。 609B Q1是5-C1-2-噻吩基，R1是C1以及R2是CFH2。 610B Q1是5-C1-2-噻吩基，R1是Br以及R2是Me。 611B Q1是5-C1-2-噻吩基，R1是I以及R2是Me。 151284.doc -154- 201117722 表 列標題 612B Q1是5-C1-2-噻吩基，R1是Me以及R2是Me。 613B Q1是5-C1-2-噻吩基，R1是Me以及R2是C1。 614B Q1是5-C1-2-噻吩基，R1是Me以及R2是Br。 615B Q1是5-C1-2-噻吩基，R1是Me以及R2是I。 616B Q1是5-C1-2-噻吩基，R1是Br以及R2是Br。 617B Q1是5-C1-2-噻吩基，R1是Br以及R2是C1。 618B Q1是5-C1-2-噻吩基，R1是C1以及R2是Br。 619B Q1是5-C1-2-噻吩基，R1是C1以及R2是C1。 620B Q1是5-F-2-噻吩基，R1是C1以及R2是Me。 621B Q1是5-F-2-噻吩基，R1是C1以及R2是CFH2。 622B Q1是5-F-2-噻吩基，R1是Br以及R2是Me。 623B Q1是5-F-2-噻吩基，R1是I以及R2是Me。 624B Q1是5-F-2-噻吩基，R1是Me以及R2是Me。 625B Q1是5-F-2-噻吩基，R1是Me以及R2是α。 626B Q1是5-F-2-噻吩基，R1是Me以及R2是Br。 627B Q1是5-F-2-噻吩基，R1是Me以及R2是I。 628B Q1是5-F-2-噻吩基，R1是Br以及R2是Br。 629B Q1是5-F-2-噻吩基，R1是Br以及R2是CM。 630B Q1是5-F-2-噻吩基，R1是C1以及R2是Br。 631B Q1是5-F-2-噻吩基，R1是C1以及R2是C1。 632B Q1是5-Me-3-噻吩基，R1是C1以及R2是Me。 633B Q1是5-Me-3-噻吩基，R1是C1以及R2是CFH2。 634B Q1是5-Me-3-噻吩基，R1是Br以及R2是Me。 635B Q1是5-Me-3-噻吩基，R1是I以及R2是Me。 636B Q1是5-Me-3-噻吩基，R1是Me以及R2是Me。 637B Q1是5-Me-3-噻吩基，R1是Me以及R2是C1。 638B Q1是5-Me-3-噻吩基，R1是Me以及R2是Br。 639B Q1是5-Me-3-噻吩基，R1是Me以及R2是I。 640B Q1是5-Me-3-噻吩基，R1是Br以及R2是Br。 641B Q1是5-Me-3-噻吩基，R1是Br以及R2是C1。 642B Q1是5-Me-3-噻吩基，R1是C1以及R2是Br。 643B Q1是5-Me-3-噻吩基，R1是C1以及R2是α。 644B Q1是5-C1-3-噻吩基，R1是C1以及R2是Me。 645B Q1是5-C1-3-噻吩基，R1是C1以及R2是CFH2。 646B Q1是5-C1-3-噻吩基，R1是Br以及R2是Me。 151284.doc •155· 201117722 表 列標題 647B Q1是5-C1-3-噻吩基，R1是I以及R2是Me。 648B Q1是5-C1-3-噻吩基，R1是Me以及R2是Me。 649B Q1是5-C1-3-噻吩基，R1是Me以及R2是Q。 650B Q1是5-C1-3-噻吩基，R1是Me以及R2是Br。 651B Q1是5-C1-3-噻吩基，R1是Me以及R2是I。 652B Q1是5-C1-3-噻吩基，R1是Br以及R2是Br。 653B Q1是5-C1-3-噻吩基，R1是Br以及R2是C1。 654B Q1是5-C1-3-噻吩基，R1是C1以及R2是Br。 655B Q1是5-C1-3-噻吩基，R1是C1以及R2是C1。 656B Q1是5-F-3-噻吩基，R1是C1以及R2是Me。 657B Q1是5-F-3-噻吩基，R1是C1以及R2是CFH2。 658B Q1是5-F-3-噻吩基，R1是Br以及R2是Me。 659B Q1是5-F-3-噻吩基，R1是I以及R2是Me。 660B Q1是5-F-3-噻吩基，R1是Me以及R2是Me。 661B Q1是5-F-3-噻吩基，R1是Me以及R2是α。 662B Q1是5-F-3-噻吩基，R1是Me以及R2是Br。 663B Q1是5-F-3-噻吩基，R1是Me以及R2是I。 664B Q1是5-F-3-噻吩基，R1是Br以及R2是Br。 665B Q1是5-F-3-噻吩基，R1是Br以及R2是Q。 666B Q1是5-F-3-噻吩基，R1是C1以及R2是Br。 667B Q1是5-F-3-噻吩基，R1是C1以及R2是α。 668B Q1是l-Me-ΙΗ-吡唑-3-基，R1是C1以及R2是Me。 669B Q1 是 l-Me-ΙΗ-吡唑-3-基，R1 是 C1 以及 R2 是 CFH2。 670B Q1是l-Me-ΙΗ-吡唑-3-基，Ri是Br以及R2是Me。 671B Q1是l-Me-ΙΗ-吡唑-3-基，R1是I以及R2是Me。 672B Q1是l-Me-ΙΗ-吡唑-3-基，R1是Me以及R2是Me。 673B Q1是l-Me-ΙΗ-吡唑-3-基，R1是Me以及R2是α。 674B Q1是l-Me-ΙΗ-吡唑-3-基，R1是Me以及R2是Br。 675B Q1是l-Me-ΙΗ-吡唑-3-基，R1是Me以及R2是I。 676B Q1是l-Me-ΙΗ-吡唑-3-基，R1是Br以及R2是Br。 677B Q1是l-Me-ΙΗ-吡唑-3-基，R1是Br以及R2是C1。 678B Q1是l-Me-ΙΗ-吡唑-3-基，R1是C1以及R2是Br。 679B Q1是l-Me-ΙΗ-吡唑-3-基，R1是C1以及R2是C1。 680B Q1是l-Me-ΙΗ-吡唑-4-基，R1是C1以及R2是Me。 681B Q1 是 l-Me-ΙΗ-吡唑-4-基，R1 是 C1 以及 R2 是 CFH2。 151284.doc -156- 201117722 表 列標題 682B Q1是l-Me-ΙΗ-吡唑-4-基，R1是Br以及R2是Me。 683B Q1是l-Me-ΙΗ-吡唑-4-基，R1是I以及R2是Me。 684B Q1是l-Me-ΙΗ-吡唑-4-基，R1是Me以及R2是Me。 685B Q1是l-Me-ΙΗ-吡唑-4-基，R1是Me以及R2是C1。 686B Q1是l-Me-ΙΗ-吡唑-4-基，R1是Me以及R2是Br。 687B Q1是l-Me-ΙΗ-吡唑-4-基，R1是Me以及R2是I。 688B Q1是卜Me-ΙΗ-吡唑-4-基，R1是Br以及R2是Br。 689B Q1是l-Me-ΙΗ-吡唑-4-基，R1是Br以及R2是C1。 690B Q1是l-Me-ΙΗ-吡唑-4-基，R1是C1以及R2是Br。 691B Q1是l-Me-ΙΗ-吡唑-4-基，R1是C1以及R2是C1。 692B Q1是2-Me-5-噻唑基 ，R1是C1以及R2是Me。 693B Q1是2-Me-5-噻唑基 ，R1是C1以及R2是CFH2。 694B Q1是2-Me-5-噻唑基 ，R1是Βι以及R2是Me。 695B Q1是2-Me-5-噻唑基 ，R1是I以及R2是Me。 696B Q1是2-Me-5-噻唑基 ，R1是Me以及R2是Me。 697B Q1是2-Me-5-噻唑基 ，R1是Me以及R2是α。 698B Q1是2-Me-5-噻唑基 ，R1是Me以及R2是Br。 699B Q1是2-Me-5-噻唑基 ，R1是Me以及R2是I。 700B Q1是2-Me-5-噻唑基 ，R1是Br以及R2是Br。 701B Q1是2-Me-5-噻唑基 ，R1是Br以及R2是α。 702B Q1是2-Me-5-噻唑基 ，Ri是Cl以及R2是Br。 703B Q1是2-Me-5-噻唑基 ，R1是C1以及R2是C卜 704B Q1是2-C1-5-噻唑基， R1是C1以及R2是Me。 705B Q1是2-C1-5-噻唑基， R1是C1以及R2是CFH2。 706B Q1是2-C1-5-噻唑基， R1是Br以及R2是Me。 707B Q1是2-C1-5-噻唑基， R1是I以及R2是Me。 708B Q1是2-C1-5-噻唑基， R1是Me以及R2是Me。 709B Q1是2-C1-5-噻唑基， R1是Me以及R2是α。 710B Q1是2-C1-5-噻唑基， R1是Me以及R2是Br。 711B Q1是2-C1-5-噻唑基， R1是Me以及R2是I。 712B Q1是2-C1-5-噻唑基， R1是Br以及R2是Br。 713B Q1是2-C1-5-噻唑基， R1是Br以及R2是Q。 714B Q1是2-C1-5-噻唑基， R1是C1以及R2是Br。 715B Q1是2-C1-5-噻唑基， R1是C1以及R2是C1。 151284.doc -157- 201117722 表3201117722 Table 192B 193B 194B 195B 196B 197B 198B 199B 200B 201B 202B 203B 204B 205B 206B 207B 208B 209B 210B 211B 212B 213B 214B 215B 216B 217B 218B 219B 220B 221B 222B 223B 224B 225B 226B Column heading Q1 is 4-CU, 3,5-two -MeO-Ph, R1 is Br and R2 is Me. Q1 is 4-C1, 3,5-di-MeO-Ph, R1 is I and R2 is Me. Q1 is 4-C1, 3,5-di-MeO-Ph, R1 is Me and R2 is Me. Q1 is 4-C1,3,5-di-MeO-Ph, R1 is Me and R2 is CBu Q1 is 4-CBu 3,5-di-MeO-Ph, R1 is Me and R2 is Br. Q1 is 4-C1, 3,5-di-MeO-Ph, R1 is Me and R2 is I. Q1 is 4-C1,3,5-di-MeO-Ph, R1 is Br and R2 is Br. Q1 is 4-C Bu 3,5-di-MeO-Ph, R1 is Br and R2 is C1. Q1 is 4-CBu 3,5-di-MeO-Ph, R1 is C1 and R2 is Br. Q1!4-Cl, 3,5-:-MeO-Ph, R1*CUX&amp;R2Sa. Q1 is 4-Cl-Bn, R1 is Cl and R2 is Me. Q1 is 4-Cl-Bn, R1 is C1 and R2 is CFH2. Q1 is 4-Cl-Bn, R1 is Br and R2 is Me. Q1 is 4-Cl-Bn, R1 is I and R2 is Me. Q1 is 4-Cl-Bn, R1 is Me and R2 is Me. Q1 is 4-Cl-Bn, R1 is Me and R2 is C1. Q1 is 4-Cl-Bn, R1 is Me and R2 is Br. Q1 is 4-Cl-Bn, R1 is Me and R2 is I. Q1 is 4-Cl-Bn, R1 is Br and R2 is Br. Q1 is 4-Cl-Bn, R1 is Br and R2 is C1. Q1 is 4-Cl-Bn, R1 is C1 and R2 is Br. Q1 is 4-Cl-Bn, R1 is C1 and R2 is C1. Q1 is 4-F-Bn, R1 is C1 and R2 is Me. Q1 is 4-F-Bn, R1 is C1 and R2 is CFH2. Q1 is 4-F-Bn, R1 is Br and R2 is Me. Q1 is 4-F-Bn, R1 is I and R2 is Me. Q1 is 4-F-Bn, R1 is Me and R2 is Me. Q1 is 4-F-Bn, R1 is Me and R2 is C1. Q1 is 4-F-Bn, R1 is Me and R2 is Br. Q1 is 4-F-Bn, R1 is Me and R2 is I. Q1 is 4-F-Bn, R1 is Br and R2 is Br. Q1 is 4-F-Bn, R1 is Br and R2 is C1. Q1 is 4-F-Bn, R1 is CI and R2 is Br. Q1 is 4-F-Bn, R1 is C1 and R2 is C1. Q1 is 6-C1-3-pyridyl, R1 is C1 and R2 is Me. 151284.doc •143- 201117722 Table Column heading 227B Q1 is 6-C1-3-pyridyl, R1 is C1 and R2 is CFH2. 228B Q1 is 6-C1-3-»bipyridyl, R1 is Br and R2 is Me. 229B Q1 is 6-C1-3-pyridyl, R1 is I and R2 is Me. 230B Q1 is 6-C1-3-pyridyl, R1 is Me and R2 is Me. 231B Q1 is 6-C1-3-pyridyl, R1 is Me and R2 is CM. 232B Q1 is 6-C1-3-pyridyl, R1 is Me and R2 is Br. 233B Q1 is 6-C1-3-pyridyl, R1 is Me and R2 is I. 234B Q1 is 6-01-3-° pyridine group, R1 is Me and R2 is MeO. 235B Q1 is 6-C1-3-pyridyl, R1 is MeO and R2 is Me. 236B Q1 is 6-C1-3-. In the case of a pyridinyl group, R1 is Br and R2 is Br. 237B Q1 is 6-C1-3-pyridyl, R1 is Br and R2 is Q. 238B Q1 is 6-C1-3-pyridyl, R1 is C1 and R2 is Br. 239B Q1 is 6-C1-3-. Pyridyl, R1 is C1 and R2 is CBu 240B Q1 is 6-C1-3-pyridyl, R1 is Me and R2 is MeS. 241B Q1 is 6-C1-3-pyridyl, R1 is MeS and R2 is Me. 242B Q1 is 6-C1-3-pyridyl, R1 is Et and R2 is Br. 243B Q1 is 6-C1-3-pyridyl, R1 is Et and R2 is α. 244B Q1 is 6-C1-3-pyridyl, R1 is Et and R2 is Me. 245B Q1 is 6-C1-3-»bipyridyl, R1 is Me and R2 is Et. 246B Q1 is 6-C1-3-pyridyl, R1 is C1 and R2 is Et. 247B Q1 is 6-C1-3-pyridyl, R1 is Me and R2 is CN. 248B Q1 is 6-Me-3-pyridyl R1 is C1 and R2 is Me. 249B Q1 is 6-Me-3-pyridyl R1 is C1 and R2 is CFH2. 250B Q1 is 6-Me-3-. The pyridyl group R1 is Br and R2 is Me. 251B Q1 is 6-Me-3-pyridyl R1 is I and R2 is Me. 252B Q1 is 6-Me-3-pyridyl R1 is Me and R2 is Me. 253B Q1 is 6-Me-3-pyridyl R1 is Me and R2 is Cb 254B Q1 is 6-Me-3-pyridyl R1 is Me and R2 is Br. 255B Q1 is 6-Me-3-pyridyl R1 is Me and R2 is I. 256B Q1 is 6-Me-3-pyridyl Ri is Br and R2 is Br. 257B Q1 is 6-Me-3-pyridyl R1 is Br and R2 is CM. 258B Q1 is 6-Me-3-pyridyl R1 is Cl and R2 is Br. 259B Q1 is a 6-Me-3-e ratio bite base R1 is C1 and R2 is C1. 260B Q1 is 6-MeO-3-. Pyridyl, R1 is C1 and R2 is Me. 261B Q1 is 6-MeO-3-pyridyl, R1 is C1 and R2 is CFH2. 151284.doc -144- 201117722 Table headings 262B 263B 264B 265B 266B 267B 268B 269B 270B 271B 272B 273B 274B 275B 276B 277B 278B 279B 280B 281B 282B 283B 284B 285B 286B 287B 288B 289B 290B 291B 292B 293B 294B 295B 296B Q1 is 6-MeO -3-pyridyl, R1 is Br and R2 is Me. Q1 is 6-MeO-3-pyridyl, R1 is I and R2 is Me. Q1 is 6-Me〇-3-pyridyl, R1 is Me and R2 is Me. Q1 is 6-MeO-3-pyridyl, R1 is Me and R2 is Cb. Q1 is 6-MeO-3-pyridyl, R1 is Me and R2 is Br. Q1 is 6-MeO-3-pyridyl, R1 is Me and R2 is I. Q1 is 6-MeO-3-pyridyl, R1 is Br and R2 is Br. Q1 is 6-MeO-3-pyridyl, R1 is Br and R2 is C1. Q1 is 6-MeO-3-pyridyl, R1 is C1 and R2 is Br. Q1 is 6-MeO-3-pyridyl, R1 is C1 and R2 is CM. Q1 is 6-CF3-3-pyridyl, R1 is C1 and R2 is Me. Q1 is 6-CF3-3-pyridyl, R1 is C1 and R2 is CFH2. Q1 is 6-CF3-3-pyridyl, R1 is Br and R2 is Me. Q1 is 6-CF3-3-pyridyl, R1 is I and R2 is Me. Q1 is 6-CF3-3-pyridyl, R1 is Me and R2 is Me. Q1 is 6-CF3-3-pyridyl, R1 is Me and R2 is C1. Q1 is 6-CF3-3-pyridyl, R1 is Me and R2 is Br. Q1 is 6-CF3-3-pyridyl, R1 is Me and R2 is I. Q1 is 6-CF3-3-pyridyl, R1 is Br and R2 is Br. Q1 is 6-CF3-3-pyridyl, R1 is Br and R2 is C1. Q1 is 6-CF3-3-pyridyl, R1 is C1 and R2 is Br. Q1 is 6-CF3-3-pyridyl, R1 is C1 and R2 is C1. Q1 is 6-Br-3-pyridyl, R1 is C1 and R2 is Me. Q1 is 6-Br-3-pyridyl, R1 is C1 and R2 is CFH2. Q1 is 6-Br-3-pyridyl, R1 is Br and R2 is Me. Q1 is 6-Br-3-pyridyl, R1 is I and R2 is Me. Q1 is 6-Br-3-pyridyl, R1 is Me and R2 is Me. Q1 is 6-Br-3-pyridyl, R1 is Me and R2 is C1. Q1 is 6-Br-3-pyridyl, R1 is Me and R2 is Br. Q1 is 6-Br-3-pyridyl, R1 is Me and R2 is I. Q1 is 6-Br-3-pyridyl, R1 is Br and R2 is Br. Q1 is 6-Br-3-pyridyl, R1 is Br and R2 is C1. Q1 is 6-fluoren-3-pyridyl, R1 is C1 and R2 is Br. Q1 is 6-Br-3-pyridyl, R1 is C1 and R2 is C1. Q1 is 6-F-3-pyridyl, R1 is C1 and R2 is Me. 151284.doc -145- 201117722 Table Column heading 297B Q1 is 6-F-3-pyridyl, R1 is Cl and R2 is CFH2. 298B Q1 is 6-F-3-pyridyl, R1 is Br and R2 is Me. 299B Q1 is 6-F-3-pyridyl, R1 is I and R2 is Me. 300B Q1 is 6-F-3-pyridyl, R1 is Me and R2 is Me. 301B Q1 is 6-F-3-pyridyl, R1 is Me and R2 is α. 302B Q1 is 6-F-3-pyridyl, R1 is Me and R2 is Br. 303B Q1 is 6-F-3-pyridyl, R1 is Me and R2 is I. 304B Q1 is 6-F-3-pyridyl, R1 is Br and R2 is Br. 305B Q1 is 6-F-3-pyridyl, R1 is Br and R2 is C1. 306B Q1 is 6-F-3-pyridyl, R1 is C1 and R2 is Br. 307B Q1 is 6-F-3-pyridyl, R1 is C1 and R2 is C1. 308B Q1 is 2-C1, 6-Me-4-pyridyl, R1 is C1 and R2 is Me. 309B Q1 is 2-a, 6-Me-4-pyridyl, R1 is C1 and R2 is CFH2. 310B Q1 is 2-C1, 6-Me-4-pyridyl, Ri is Br and R2 is Me. 311B Q1 is 2-C1, 6-Me-4-pyridyl, R1 is I and R2 is Me. 312B Q1 is 2-C1, 6-Me-4-pyridyl, R1 is Me and R2 is Me. 313B Q1 is 2-C1, 6-Me-4-pyridyl, R1 is Me and R2 is Π. 314B Q1 is 2-C1, 6-Me-4-pyridyl, R1 is Me and R2 is Br. 315B Q1 is 2-C1, 6-Me-4-pyridyl, R1 is Me and R2 is I. 316B Q1 is 2-C1, 6-Me-4-pyridyl, R1 is Br and R2 is Br. 317B Q1 is 2-C1, 6-Me-4-pyridyl, R1 is Br and R2 is Cb 318B Q1 is 2-C1, 6-Me-4-pyridyl, R1 is C1 and R2 is Br. 319B Q1 is 2-C1, 6-Me-4-pyridyl, R1 is C1 and R2 is CBu 320B Q1 is 2-C1, 6-MeO-3-pyridyl, R1 is C1 and R2 is Me. 321B Q1 is 2-CM, 6-MeO-3-pyridyl, R1 is C1 and R2 is CFH2. 322B Q1 is 2-C1, 6-MeO-3-pyridyl, R1 is Br and R2 is Me. 323B Q1 is 2-C1, 6-MeO-3-pyridyl, R1 is I and R2 is Me. 324B Q1 is 2-C1, 6-MeO-3-pyridyl, R1 is Me and R2 is Me. 325B Q1 is 2-C1, 6-MeO-3-pyridyl, R1 is Me and R2 is C1. 326B Q1 is 2-C1, 6-MeO-3-pyridyl, R1 is Me and R2 is Br. 327B Q1 is 2-C1, 6-MeO-3-pyridyl, R1 is Me and R2 is I. 328B Q1 is 2-C1, 6-MeO-3-pyridyl, R1 is Br and R2 is Br. 329B Q1 is 2-C1, 6-MeO-3-pyridyl, R1 is Br and R2 is C1. 330B Q] is 2-Cb 6-MeO-3-pyridyl, R1 is C1 and R2 is Br. 331B Q1 is a 2-C1, 6-MeO-3-pyridyl group, R1 is C1 and R2 is C1. 151284.doc -146- 201117722 Table Column heading 332B Q1 is 2-C1, 6-CF3-3-pyridyl, R1 is Cl and R2 is Me. 333B Q1 is 2-Q, 6-CF3-3-pyridyl, R1 is C1 and R2 is CFH2. 334B Q1 is 2-C1, 6-CF3-3-pyridyl, R1 is Br and R2 is Me. 335B Qi is 2-a, 6-CF3-3-pyridyl, R1 is I and R2 is Me. 336B Q1 is 2-C1, 6-CF3-3-pyridyl, R1 is Me and R2 is Me. 337B Q1 is 2-C1, 6-CF3-3-pyridyl, R1 is Me and R2 is C1. 338B Q1 is 2-C1, 6-CF3-3-pyridyl, R1 is Me and R2 is Br. 339B Q1 is 2-C16-CF3-3-pyridyl, R1 is Me and R2 is I. 340B Q1 is 2-C1, 6-CF3-3-pyridyl, R1 is Br and R2 is Br. 341B Q1 is 2-C1, 6-CF3-3-pyridyl, R1 is Br and R2 is C1. 342B Q1 is 2-C1, 6-CF3-3-pyridyl, R1 is C1 and R2 is Br. 343B Q1 is 2-C1, 6-CF3-3-pyridyl, R1 is C1 and R2 is C1. 344B Q1 is 5-C1-3-pyridyl, R1 is C1 and R2 is Me. 345B Q1 is 5-C1-3-pyridyl, R1 is C1 and R2 is CFH2. 346B Q1 is 5-CI-3-pyridyl, R1 is Br and R2 is Me. 347B Q1 is 5-C1-3-pyridyl, R1 is I and R2 is Me. 348B Q1 is 5-C1-3-pyridyl, R1 is Me and R2 is Me. 349B Q1 is 5-C1-3-pyridyl, R1 is Me and R2 is C1. 350B Q1 is 5-C1-3-pyridyl, R1 is Me and R2 is Br. 351B Q1 is 5-C1-3-pyridyl, R1 is Me and R2 is I. 352B Q1 is 5-C1-3-pyridyl, R1 is Br and R2 is Br. 353B Q1 is 5-C1-3-pyridyl, R1 is Br and R2 is C1. 354B Q1 is 5-C1-3-pyridyl, R1 is C1 and R2 is Br. 355B Q1 is 5-C1-3-pyridyl, R1 is C1 and R2 is C1. 356B Q1 is 5-F-3-pyridyl, R1 is C1 and R2 is Me. 357B Q1 is 5-F-3-pyridyl, R1 is C1 and R2 is CFH2. 358B Q1 is 5-F-3-pyridyl, R1 is Br and R2 is Me. 359B Q1 is 5-F-3-pyridyl, R1 is I and R2 is Me. 360B Q1 is 5-F-3-pyridyl, R1 is Me and R2 is Me. 361B Q1 is 5-F-3-pyridyl, R1 is Me and R2 is C1. 362B Q1 is 5-F-3-pyridyl, R1 is Me and R2 is Br. 363B Q1 is 5-F-3-pyridyl, R1 is Me and R2 is I. 364B Q1 is 5-F-3-pyridyl, R1 is Br and R2 is Br. 365B Q1 is 5-F-3·pyridyl, R1 is Br and R2 is C1. 366B Q1 is 5-F-3-pyridyl, R1 is C1 and R2 is Br. 151284.doc 147· 201117722 Table Column heading 367B Q1 is 5-F-3-pyridyl, R1 is Cl and R2 is CU. 368B Q1 is 5-Me-3-pyridyl, R1 is Cl and R2 is Me. 369B Q1 is 5-Me-3-pyridyl, R1 is C1 and R2 is CFH2. 370B Q1 is 5-Me-3-pyridyl, R1 is Br and R2 is Me. 371B Q1 is 5-Me-3-pyridyl, R1 is I and R2 is Me. 372B Q1 is 5-Me-3-pyridyl, R1 is Me and R2 is Me. 373B Q1 is 5-Me-3-pyridyl, R1 is Me and R2 is CM. 374B Q1 is a 5-Me-3-° ratio bite base, R1 is Me and R2 is Br. 375B Q1 is 5-Me-3-pyridyl, R1 is Me and R2 is I. 376B Q1 is 5-Me-3-pyridyl, R1 is Br and R2 is Br. 377B Q1 is 5-Me-3-pyridyl, R1 is Br and R2 is CU. 378B Q1 is 5-Me-3-pyridyl, R1 is C1 and R2 is Br. 379B Q1 is 5-Me-3-pyridyl, R1 is C1 and R2 is C1. 380B Q1 is 5-MeO-3-pyridyl, R1 is C1 and R2 is Me. 381B Q1 is 5-MeO-3-pyridyl, R1 is C1 and R2 is CFH2. 382B Q1 is 5-MeO-3-pyridyl, R1 is Br and R2 is Me. 383B Q1 is 5-MeO-3-pyridyl, R1 is I and R2 is Me. 384B Q1 is 5-MeO-3-pyridyl, R1 is Me and R2 is Me. 385B Q1 is 5-MeO-3-pyridyl, R1 is Me and R2 is CBu 386B Q1 is 5-MeO-3-pyridyl, R1 is Me and R2 is Br. 387B Q1 is 5-MeO-3-pyridyl, R1 is Me and R2 is I. 388B Q1 is 5-MeO-3-pyridyl, R1 is Br and R2 is Br. 389B Q1 is 5-MeO-3-pyridyl, R1 is Br and R2 is Cb 390B Q1 is 5-MeO-3-pyridyl, R1 is C1 and R2 is Br. 391B Q1 is 5-MeO-3-pyridyl, R1 is C1 and R2 is (: 392B Q1 is 6-C1, 5-MeO-3-pyridyl, R1 is Cl and R2 is Me. 393B Q1 is 6- Cb 5-MeO-3-pyridyl, R1 is C1 and R2 is CFH2. 394B Q1 is 6-C1, 5-MeO-3-pyridyl, R1 is Br and R2 is Me. 395B Q1 is 6-C1 5-MeO-3-pyridyl, Ri is I and R2 is Me. 396B Q1 is 6-C1, 5-MeO-3-pyridyl, R1 is Me and R2 is Me. 397B Q1 is 6-C1, 5- MeO-3-pyridyl, R1 is Me and R2 is Q. 398B Q1 is 6-C1, 5-MeO-3-pyridyl, R1 is Me and R2 is Br. 399B Q1 is 6-C1, 5-MeO- 3-pyridyl, R1 is Me and R2 is I. 400B Q1 is 6-C1, 5-MeO-3-pyridyl, R1 is Br and R2 is Br. 401B Q1 is 6-C1, 5-MeO-3- Pyridyl, R1 is Br and R2 is C1. 151284.doc -148- 201117722 Table heading 402B Q1 is 6_C1, 5-MeO-3-pyridyl, R1 is Cl and R2 is Br. 403B Q1 is 6-a, 5-MeO-3- &quot; pyridine group, R1 is C1 and R2 is C1. 404B Q1 is 6-C1-3-嗒-well, R1 is C1 and R2 is Me. 405B Q1 is 6-C1-3 -嗒' well base, R1 is C1 And R2 is CFH2. 406B Q1 is 6-C1-3-嗒耕基, R1 is Br and R2 is Me. 407B Q1 is 6-C1-3-嗒 tillage, R1 is I and R2 is Me. 408B Q1 is 6-C1-3-嗒耕基, R1 is Me and R2 is Me. 409B Q1 is 6-C1-3-嗒 tillage, R1 is Me and R2 is C1. 410B Q1 is 6-CI-3-嗒Base, R1 is Me and R2 is Br. 411B Q1 is 6-C1-3-嗒耕基, R1 is Me and R2 is I. 412B Q1 is 6-C1-3-嗒" well base, R1 is Br and R2 Is Br. 413B Q1 is 6-C1-3-嗒耕基, R1 is Br and R2 is α. 414B Q1 is 6-C1-3-嗒 tillage, R1 is C1 and R2 is Br. 415B Q1 is 6- C1-3-嗒耕基, R1 is C1 and R2 is α. 416B Q1 is 6-Me-3-嗒 tillage, R1 is C1 and R2 is Me. 417B Q1 is 6-Me-3-嗒 tillage, R1 is C1 and R2 is CFH2. 418B Q1 is a 6-Me-3-嗒&quot; well base, R1 is Br and R2 is Me. 419B Q1 is 6-Me-3-嗒 tillage, R1 is I and R2 is Me. 420B Q1 is 6-Me-3-嗒 tillage, R1 is Me and R2 is Me. 421B Q1 is 6-Me-3-嗒 tillage, R1 is Me and R2 is CBu 422B Q1 is a 6-Me-3-嗒n well group, R1 is Me and R2 is Br. 423B Q1 is 6-Me-3-fluorenyl, R1 is Me and R2 is I. 424B Q1 is 6-Me-3-嗒 tillage, R1 is Br and R2 is Br. 425B Q1 is 6-Me-3-嗒 tillage, R1 is Br and R2 is C1. 426B Q1 is 6-Me-3-oxime, R1 is C1 and R2 is Br. 427B Q1 is a 6-Me-3-嗒 whistle, R1 is C1 and R2 is C1. 428B Q1 is 6-MeO-3-fluorenyl, R1 is C1 and R2 is Me. 429B Q1 is 6-MeO-3-oxime, R1 is C1 and R2 is CFH2. 430B Q1 is 6-MeO-3-嗒 tillage, R1 is Br and R2 is Me. 431B Q1 is 6-MeO-3-嗒 tillage, R1 is I and R2 is Me. 432B Q1 is 6-MeO-3-嗒 tillage, R1 is Me and R2 is Me. 433B Q1 is 6-MeO-3-嗒 tillage, R1 is Me and R2 is C1. 434B Q1 is a 6-MeO-3-嗒 well base, R1 is Me and R2 is Br. 435B Q1 is 6-MeO-3-嗒 · base, R1 is Me and R2 is I. 436B Q1 is 6-MeO-3-嗒 基, R1 is Βι• and R2 is Br. 151284.doc -149- 201117722 Table Column heading 437B Q1 is 6-MeO-3-嗒 tillage, R1 is Br and R2 is Cl. 438B Q1 is a 6-MeO-3-indole, R1 is C1 and R2 is Br. 439B Q1 is a 6-MeO-3-嗒 · base, R1 is C1 and R2 is C1. 440B Q1 is a 6-CF3-3-indole, R1 is C1 and R2 is Me. 441B Q1 is a 6-CF3-3·嗒' well base, R1 is C1 and R2 is CFH2. 442B Q1 is a 6-CF3-3-嗒 well group, R1 is Br and R2 is Me. 443B Q1 is a 6-CF3-3-indole, R1 is I and R2 is Me. 444B Q1 is 6-CF3-3-嗒 tillage, R1 is Me and R2 is Me. 445B Q1 is a 6-CF3-3-indole, R1 is Me and R2 is C1. 446B Q1 is a 6-CF3-3-indole, R1 is Me and R2 is Br. 447B Q1 is a 6-CF3-3-indole, R1 is Me and R2 is I. 448B Q1 is a 6-CF3-3-嗒 well group, Ri is Br and R2 is Br. 449B Q1 is a 6-CF3-3-fluorene whistle, Ri is Br and R2 is CBu 450B Q1 is 6-CF3-3-fluorenyl, R1 is C1 and R2 is Br. 451B Q1 is 6-CF3-3-indolyl, R1 is C1 and R2 is α. 452B Q1 is 5-C1-3-quinoneyl, R1 is C1 and R2 is Me. 453B Q1 is 5-C1-3-嗒 tillage, R1 is C1 and R2 is CFH2. 454B Q1 is 5-C1-3-嗒 基, R1 is Br and R2 is Me. 455B Q1 is 5-C1-3-fluorenyl, R1 is I and R2 is Me. 456B Q1 is 5-C1-3-嗒 tillage, R1 is Me and R2 is Me. 457B Q1 is 5-C1-3-嗒 tillage, R1 is Me and R2 is C1. 458B Q1 is 5-C1-3-嗒 嗒, R1 is Me and R2 is Br. 459B Q1 is 5-C1-3-嗒 tillage, R1 is Me and R2 is I. 460B Q1 is 5-C1-3-嗒 tillage, R1 is Br and R2 is Br. 461B Q1 is 5-C1-3-fluorenyl, R1 is Br and R2 is α. 462B Q1 is 5-C1-3-嗒 嗒, R1 is C1 and R2 is Br. 463B Q1 is 5-C1-3-嗒 嗒, R1 is C1 and R2 is α. 464B Q1 is a 5-F-3-indole, R1 is C1 and R2 is Me. 465B Q1 is a 5-F-3-indole, R1 is C1 and R2 is CFH2. 466B Q1 is 5-F-3-嗒 tillage, R1 is Br and R2 is Me. 467B Q1 is 5-F-3-indole, R1 is I and R2 is Me. 468B Q1 is 5-F-3-嗒 tillage, R1 is Me and R2 is Me. 469B Q1 is 5-F-3-嗒 基, R1 is Me and R2 is C1. 470B Q1 is a 5-F-3-indole, R1 is Me and R2 is Br. 471B Q1 is 5-F-3-嗒 tillage, R1 is Me and R2 is I » 151284.doc -150- 201117722 Table headings 472B 473B 474B 475B 476B 477B 478B 479B 480B 481B 482B 483B 484B 485B 486B 487B 488B 489B 490B 491B 492B 493B 494B 495B 496B 497B 498B 499B 500B 501B 502B 503B 504B 505B 506B Q1 is a 5-F-3-嗒p well base, R1 is Br and R2 is Br. Q1 is 5-F-3-indole, R1 is Br and R2 is C1. Q1 is a 5-F-3-嗒 well, R1 is C1 and R2 is Br. Q1 is a 5-F-3-indole, R1 is C1 and R2 is C1. Q1 is 5-MeO-3-indole, R1 is C1 and R2 is Me. Q1 is 5-MeO-3-indenyl, R1 is C1 and R2 is CFH2. Q1 is 5-MeO-3-indole, R1 is Br and R2 is Me. Q1 is 5-MeO-3-indole, R1 is I and R2 is Me. Q1 is 5-MeO-3-indole, R1 is Me and R2 is Me. Q1 is 5-MeO-3-indole, R1 is Me and R2 is C1. Q1 is 5-MeO-3-indole, R1 is Me and R2 is Br. Q1 is 5-MeO-3-indole, R1 is Me and R2 is I. Q1 is 5-MeO-3-indole, R1 is Br and R2 is Br. Q1 is 5-MeO-3-indole, R1 is Br and R2 is C1. Q1 is a 5-MeO-3-嗒&quot; well base, R1 is C1 and R2 is Br. Q1 is 5-MeO-3-indole, R1 is C1 and R2 is C1. Q1 is 2-C1-5-pyrimidine, R1 is C1 and R2 is Me. Q1 is 2-C1-5-pyrimidine, R1 is C1 and R2 is CFH2. Q1 is 2-C1-5-pyrimidine, R1 is Br and R2 is Me. Q1 is 2-C1-5-pyrimidine, R1 is I and R2 is Me. Q1 is 2-C1-5-pyrimidine, R1 is Me and R2 is Me. Q1 is a 2-C1-5 pyrimidine, R1 is Me and R2 is C1. Q1 is 2-C1-5-pyrimidine, R1 is Me and R2 is Br. Q1 is 2-C1-5-pyrimidine, R1 is Me and R2 is I. Q1 is 2-C1-5-pyrimidine, R1 is Br and R2 is Br. Q1 is 2-C1-5-pyrimidine, R1 is Br and R2 is C1. Q1 is 2-C1-5-pyrimidine, R1 is C1 and R2 is Br. Q1 is 2-C1-5-pyrimidine, R1 is C1 and R2 is CI. Q1 is 2-Me-5-pyrimidine, R1 is C1 and R2 is Me. Q1 is 2-Me-5-pyrimidine, R1 is C1 and R2 is CFH2. Q1 is 2-Me-5-pyrimidine, R1 is Br and R2 is Me. Q1 is 2-Me-5-pyrimidine, R1 is I and R2 is Me. Q1 is 2-Me-5-pyrimidine, R1 is Me and R2 is Me. Q1 is 2-Me-5-pyrimidine, R1 is Me and R2 is C1. Q1 is 2-Me-5-pyrimidine, R1 is Me and R2 is Br. 151284.doc -151 - 201117722 Table Column heading 507B Q1 is 2-Me-5-pyrimidine, R1 is Me and R2 is I. 508B Q1 is 2-Me-5-pyrimidine, R1 is Br and R2 is Br. 509B Q1 is 2-Me-5-pyrimidine, R1 is Br and R2 is α. 510B Q1 is 2-Me-5-pyrimidine, R1 is C1 and R2 is Br. 511B Q1 is 2-Me-5-pyrimidine, R1 is C1 and R2 is C1. 512B Q1 is 2-MeO-5-pyrimidine, R1 is C1 and R2 is Me. 513B Q1 is 2-MeO-5-pyrimidine, R1 is C1 and R2 is CFH2. 514B Q1 is 2-MeO-5-pyrimidine, R1 is Br and R2 is Me. 515B Q1 is 2-MeO-5-pyrimidine, R1 is I and R2 is Me. 516B Q1 is 2-MeO-5-pyrimidine, R1 is Me and R2 is Me. 517B Q1 is 2-MeO-5-pyrimidine, R1 is Me and R2 is C1. 518B Q1 is 2-MeO-5-pyrimidine, R1 is Me and R2 is Br. 519B Q1 is 2-MeO-5-pyrimidine, R1 is Me and R2 is I. 520B Q1 is 2-MeO-5 pyrimidine, R丨 is Br and R2 is Br. 521B Q1 is 2-MeO-5-pyrimidine, R1 is Br and R2 is C1. 522B Q1 is 2-MeO-5-pyrimidine, R1 is C1 and R2 is Br. 523B Q1 is 2-MeO-5-pyrimidine, R1 is C1 and R2 is C1. 524B Q1 is 2-CF3-5-pyrimidine, R1 is C1 and R2 is Me. 525B Q1 is a 2-CF3-5-pyrimidine, R1 is C1 and R2 is CFH2. 526B Q1 is 2-CF3-5-pyrimidine, R1 is Br and R2 is Me. 527B Q1 is 2-CF3-5-pyrimidine, R1 is I and R2 is Me. 528B Q1 is 2-CF3-5-pyrimidine, R1 is Me and R2 is Me. 529B Q1 is 2-CF3-5-pyrimidine, R1 is Me and R2 is C1. 530B Q1 is 2-CF3-5-pyrimidine, R1 is Me and R2 is Br. 531B Q1 is 2-CF3-5-pyrimidine, R1 is Me and R2 is I. 532B Q1 is 2-CF3-5-pyrimidine, R1 is Br and R2 is Br. 533B Q1 is 2-CF3-5-pyrimidine, R1 is Br and R2 is C1. 534B Q1 is 2-CF3-5-pyrimidine, R1 is C1 and R2 is Br. 535B Q1 is 2-CF3-5-pyrimidine, R1 is C1 and R2 is C1. 536B Q1 is 5-C1-2-pyrimidine, R1 is C1 and R2 is Me. 537B Q1 is 5-C1-2-pyrimidine, R1 is C1 and R2 is CFH2. 538B Q1 is 5-C1-2-pyrimidine, R1 is Br and R2 is Me. 539B Q1 is 5-C1-2-pyrimidine, R1 is I and R2 is Me. 540B Q1 is 5-C1-2-pyrimidine, R1 is Me and R2 is Me. 541B Q1 is 5-C1-2-pyrimidine, R1 is Me and R2 is α. 151284.doc -152- 201117722 Table Column heading 542B Q1 is 5-C1-2-pyrimidine, R1 is Me and R2 is Br. 543B Q1 is 5-C1-2-pyrimidine, R1 is Me and R2 is I. 544B Q1 is 5-C1-2-pyrimidine, R1 is Br and R2 is Br. 545B Q1 is 5-C1-2-pyrimidine, R1 is Br and R2 is α. 546B Q1 is 5-C1-2-pyrimidine, R1 is Cl and R2 is Br. 547B Q1 is 5-C1-2-pyrimidine, R1 is C1 and R2 is α. 548B Q1 is 5-Me-2-pyrimidine, R1 is C1 and R2 is Me. 549B Q1 is a 5-Me-2-°S bite, R1 is C1 and R2 is CFH2. 550B Q1 is a 5-Me-2-° § bite, R1 is Br and R2 is Me. 551B Q1 is 5-Me-2-°^ bite, R1 is I and R2 is Me. 552B Q1 is 5-Me-2-pyrimidine, R1 is Me and R2 is Me. 553B Q1 is 5-Me-2-pyrimidine, R1 is Me and R2 is C1. 554B Q1 is 5-Me-2-pyrimidine, R1 is Me and R2 is Br. 555B Q1 is 5-Me-2-pyrimidine, R1 is Me and R2 is I. 556B Q1 is 5-Me-2-pyrimidine, R1 is Br and R2 is Br. 557B Q1 is 5-Me-2-pyrimidine, R1 is Br and R2 is α. 558B Q1 is 5-Me-2-pyrimidine, R1 is C1 and R2 is Br. 559B Q1 is 5-Me-2-pyrimidine, R1 is C1 and R2 is C1. 560B Q1 is 5-MeO-2-pyrimidine, R1 is C1 and R2 is Me. 561B Q1 is 5-MeO-2-pyrimidine, R1 is C1 and R2 is CFH2. 562B Q1 is 5-MeO-2-pyrimidine, R1 is Br and R2 is Me. 563B Q1 is 5-MeO-2-pyrimidine, R1 is I and R2 is Me. 564B Q1 is 5-MeO-2-pyrimidine, R1 is Me and R2 is Me. 565B Q1 is 5-MeO-2-pyrimidine, R1 is Me and R2 is CBu 566B Q1 is 5-MeO-2-pyrimidine, R1 is Me and R2 is Br. 567B Q1 is a 5-MeO-2-°^ bite, R1 is Me and R2 is I. 568B Q1 is 5-MeO-2-pyrimidine, R1 is Br and R2 is Br. 569B Q1 is 5-MeO-2-pyrimidine, R1 is Br and R2 is α. 570B Q1 Yes, R1 is C1 and R2 is Br. 571B Q1 is 5-MeO-2-pyrimidine, R1 is C1 and R2 is C1. 572B Q1 is 5-C1-2-pyrimidine, R1 is C1 and R2 is Me. 573B Q1 is 5-C1-2-pyrimidine, R1 is C1 and R2 is CFH2. 574B Q1 is 5-C1-2-pyrimidine, R1 is Br and R2 is Me. 575B Q1 is 5-C1-2-pyrimidine, R1 is I and R2 is Me. 576B Q1 is 5-C1-2-pyrimidine, R1 is Me and R2 is Me. I51284.doc - 153 - 201117722 Table Column heading 577B Q1 is 5-C1-2-pyrimidine, R1 is Me and R2 is CM. 578B Q1 is 5-C1-2-pyrimidine, R1 is Me and R2 is Br. 579B Q1 is 5-C1-2-pyrimidine, R1 is Me and R2 is I. 580B Q1 is 5-C1-2-pyrimidine, R1 is Br and R2 is Br. 581B Q1 is 5-C1-2-pyrimidine, R1 is Br and R2 is C1. 582B Q1 is 5-C1-2-pyrimidine, R1 is C1 and R2 is Br. 583B Q1 is 5-C1-2-pyrimidine, R1 is C丨 and R2 is CM. 584B Q1 is 5-CF3-2-pyrimidine, R1 is Cl and R2 is Me. 585B Q1 is 5-CF3-2-pyrimidine, R1 is C1 and R2 is CFH2. 586B Q1 is 5-CF3-2-pyrimidine, R1 is Br and R2 is Me. 587B Q1 is 5-CF3-2-pyrimidine, R1 is I and R2 is Me. 588B Q1 is 5-CF3-2-pyrimidine, R1 is Me and R2 is Me. 589B Q1 is 5-CF3-2-pyrimidine, R1 is Me and R2 is CBu 590B Q1 is 5-CF3-2-pyrimidine, R1 is Me and R2 is Br. 591B Q1 is 5-CF3-2-pyrimidine, R1 is Me and R2 is I. 592B Q1 is 5-CF3-2-pyrimidine, R1 is Br and R2 is Br. 593B Q1 is 5-CF3-2-pyrimidine, R1 is Br and R2 is CH. 594B Q1 is 5-CF3-2-pyrimidine, R1 is C1 and R2 is Br. 595B Q1 is 5-CF3-2-pyrimidine, R1 is C1 and R2 is &lt;:Bu 596B Q1 is 5-Me-2-thienyl, R1 is Cl and R2 is Me. 597B Q1 is 5-Me-2-thienyl, R1 is C1 and R2 is CFH2. 598B Q1 is 5-Me-2-thienyl, R1 is Br and R2 is Me. 599B Q1 is 5-Me-2-thienyl, R1 is I and R2 is Me. 600B Q1 is 5-Me-2-thienyl, R1 is Me and R2 is Me. 601B Q1 is 5-Me-2-thienyl, R1 is Me and R2 is C1. 602B Q1 is 5-Me-2-thienyl, R1 is Me and R2 is Br. 603B Q1 is 5-Me-2-thienyl, R1 is Me and R2 is I. 604B Q1 is 5-Me-2-thienyl, R1 is Br and R2 is Br. 605B Q1 is 5-Me-2-thienyl, R1 is Br and R2 is C1. 606B Q1 is 5-Me-2-thienyl, R1 is C1 and R2 is Br. 607B Q1 is 5-Me-2-thienyl, R1 is C1 and R2 is C1. 608B Q1 is 5-C1-2-thienyl, R1 is C1 and R2 is Me. 609B Q1 is 5-C1-2-thienyl, R1 is C1 and R2 is CFH2. 610B Q1 is 5-C1-2-thienyl, R1 is Br and R2 is Me. 611B Q1 is 5-C1-2-thienyl, R1 is I and R2 is Me. 151284.doc -154- 201117722 Table Column heading 612B Q1 is 5-C1-2-thienyl, R1 is Me and R2 is Me. 613B Q1 is 5-C1-2-thienyl, R1 is Me and R2 is C1. 614B Q1 is 5-C1-2-thienyl, R1 is Me and R2 is Br. 615B Q1 is 5-C1-2-thienyl, R1 is Me and R2 is I. 616B Q1 is 5-C1-2-thienyl, R1 is Br and R2 is Br. 617B Q1 is 5-C1-2-thienyl, R1 is Br and R2 is C1. 618B Q1 is 5-C1-2-thienyl, R1 is C1 and R2 is Br. 619B Q1 is 5-C1-2-thienyl, R1 is C1 and R2 is C1. 620B Q1 is 5-F-2-thienyl, R1 is C1 and R2 is Me. 621B Q1 is 5-F-2-thienyl, R1 is C1 and R2 is CFH2. 622B Q1 is 5-F-2-thienyl, R1 is Br and R2 is Me. 623B Q1 is 5-F-2-thienyl, R1 is I and R2 is Me. 624B Q1 is 5-F-2-thienyl, R1 is Me and R2 is Me. 625B Q1 is 5-F-2-thienyl, R1 is Me and R2 is α. 626B Q1 is 5-F-2-thienyl, R1 is Me and R2 is Br. 627B Q1 is 5-F-2-thienyl, R1 is Me and R2 is I. 628B Q1 is 5-F-2-thienyl, R1 is Br and R2 is Br. 629B Q1 is 5-F-2-thienyl, R1 is Br and R2 is CM. 630B Q1 is 5-F-2-thienyl, R1 is C1 and R2 is Br. 631B Q1 is 5-F-2-thienyl, R1 is C1 and R2 is C1. 632B Q1 is 5-Me-3-thienyl, R1 is C1 and R2 is Me. 633B Q1 is 5-Me-3-thienyl, R1 is C1 and R2 is CFH2. 634B Q1 is 5-Me-3-thienyl, R1 is Br and R2 is Me. 635B Q1 is 5-Me-3-thienyl, R1 is I and R2 is Me. 636B Q1 is 5-Me-3-thienyl, R1 is Me and R2 is Me. 637B Q1 is 5-Me-3-thienyl, R1 is Me and R2 is C1. 638B Q1 is 5-Me-3-thienyl, R1 is Me and R2 is Br. 639B Q1 is 5-Me-3-thienyl, R1 is Me and R2 is I. 640B Q1 is 5-Me-3-thienyl, R1 is Br and R2 is Br. 641B Q1 is 5-Me-3-thienyl, R1 is Br and R2 is C1. 642B Q1 is 5-Me-3-thienyl, R1 is C1 and R2 is Br. 643B Q1 is 5-Me-3-thienyl, R1 is C1 and R2 is α. 644B Q1 is 5-C1-3-thienyl, R1 is C1 and R2 is Me. 645B Q1 is 5-C1-3-thienyl, R1 is C1 and R2 is CFH2. 646B Q1 is 5-C1-3-thienyl, R1 is Br and R2 is Me. 151284.doc •155· 201117722 Table Column heading 647B Q1 is 5-C1-3-thienyl, R1 is I and R2 is Me. 648B Q1 is 5-C1-3-thienyl, R1 is Me and R2 is Me. 649B Q1 is 5-C1-3-thienyl, R1 is Me and R2 is Q. 650B Q1 is 5-C1-3-thienyl, R1 is Me and R2 is Br. 651B Q1 is 5-C1-3-thienyl, R1 is Me and R2 is I. 652B Q1 is 5-C1-3-thienyl, R1 is Br and R2 is Br. 653B Q1 is 5-C1-3-thienyl, R1 is Br and R2 is C1. 654B Q1 is 5-C1-3-thienyl, R1 is C1 and R2 is Br. 655B Q1 is 5-C1-3-thienyl, R1 is C1 and R2 is C1. 656B Q1 is 5-F-3-thienyl, R1 is C1 and R2 is Me. 657B Q1 is 5-F-3-thienyl, R1 is C1 and R2 is CFH2. 658B Q1 is 5-F-3-thienyl, R1 is Br and R2 is Me. 659B Q1 is 5-F-3-thienyl, R1 is I and R2 is Me. 660B Q1 is 5-F-3-thienyl, R1 is Me and R2 is Me. 661B Q1 is 5-F-3-thienyl, R1 is Me and R2 is α. 662B Q1 is 5-F-3-thienyl, R1 is Me and R2 is Br. 663B Q1 is 5-F-3-thienyl, R1 is Me and R2 is I. 664B Q1 is 5-F-3-thienyl, R1 is Br and R2 is Br. 665B Q1 is 5-F-3-thienyl, R1 is Br and R2 is Q. 666B Q1 is 5-F-3-thienyl, R1 is C1 and R2 is Br. 667B Q1 is 5-F-3-thienyl, R1 is C1 and R2 is α. 668B Q1 is l-Me-ΙΗ-pyrazol-3-yl, R1 is C1 and R2 is Me. 669B Q1 is l-Me-ΙΗ-pyrazol-3-yl, R1 is C1 and R2 is CFH2. 670B Q1 is l-Me-ΙΗ-pyrazol-3-yl, Ri is Br and R2 is Me. 671B Q1 is l-Me-ΙΗ-pyrazol-3-yl, R1 is I and R2 is Me. 672B Q1 is l-Me-ΙΗ-pyrazol-3-yl, R1 is Me and R2 is Me. 673B Q1 is l-Me-ΙΗ-pyrazol-3-yl, R1 is Me and R2 is α. 674B Q1 is l-Me-ΙΗ-pyrazol-3-yl, R1 is Me and R2 is Br. 675B Q1 is l-Me-ΙΗ-pyrazol-3-yl, R1 is Me and R2 is I. 676B Q1 is l-Me-ΙΗ-pyrazol-3-yl, R1 is Br and R2 is Br. 677B Q1 is l-Me-ΙΗ-pyrazol-3-yl, R1 is Br and R2 is C1. 678B Q1 is l-Me-ΙΗ-pyrazol-3-yl, R1 is C1 and R2 is Br. 679B Q1 is l-Me-ΙΗ-pyrazol-3-yl, R1 is C1 and R2 is C1. 680B Q1 is l-Me-ΙΗ-pyrazol-4-yl, R1 is C1 and R2 is Me. 681B Q1 is l-Me-ΙΗ-pyrazol-4-yl, R1 is C1 and R2 is CFH2. 151284.doc -156- 201117722 Table Column heading 682B Q1 is l-Me-ΙΗ-pyrazol-4-yl, R1 is Br and R2 is Me. 683B Q1 is l-Me-ΙΗ-pyrazol-4-yl, R1 is I and R2 is Me. 684B Q1 is l-Me-ΙΗ-pyrazol-4-yl, R1 is Me and R2 is Me. 685B Q1 is l-Me-ΙΗ-pyrazol-4-yl, R1 is Me and R2 is C1. 686B Q1 is l-Me-ΙΗ-pyrazol-4-yl, R1 is Me and R2 is Br. 687B Q1 is l-Me-ΙΗ-pyrazol-4-yl, R1 is Me and R2 is I. 688B Q1 is a Me-ΙΗ-pyrazol-4-yl group, R1 is Br and R2 is Br. 689B Q1 is l-Me-ΙΗ-pyrazol-4-yl, R1 is Br and R2 is C1. 690B Q1 is l-Me-ΙΗ-pyrazol-4-yl, R1 is C1 and R2 is Br. 691B Q1 is l-Me-ΙΗ-pyrazol-4-yl, R1 is C1 and R2 is C1. 692B Q1 is 2-Me-5-thiazolyl, R1 is C1 and R2 is Me. 693B Q1 is 2-Me-5-thiazolyl, R1 is C1 and R2 is CFH2. 694B Q1 is 2-Me-5-thiazolyl, R1 is Βι and R2 is Me. 695B Q1 is 2-Me-5-thiazolyl, R1 is I and R2 is Me. 696B Q1 is 2-Me-5-thiazolyl, R1 is Me and R2 is Me. 697B Q1 is 2-Me-5-thiazolyl, R1 is Me and R2 is α. 698B Q1 is 2-Me-5-thiazolyl, R1 is Me and R2 is Br. 699B Q1 is 2-Me-5-thiazolyl, R1 is Me and R2 is I. 700B Q1 is 2-Me-5-thiazolyl, R1 is Br and R2 is Br. 701B Q1 is 2-Me-5-thiazolyl, R1 is Br and R2 is α. 702B Q1 is 2-Me-5-thiazolyl, Ri is Cl and R2 is Br. 703B Q1 is 2-Me-5-thiazolyl, R1 is C1 and R2 is CBu 704B Q1 is 2-C1-5-thiazolyl, R1 is C1 and R2 is Me. 705B Q1 is 2-C1-5-thiazolyl, R1 is C1 and R2 is CFH2. 706B Q1 is 2-C1-5-thiazolyl, R1 is Br and R2 is Me. 707B Q1 is 2-C1-5-thiazolyl, R1 is I and R2 is Me. 708B Q1 is 2-C1-5-thiazolyl, R1 is Me and R2 is Me. 709B Q1 is 2-C1-5-thiazolyl, R1 is Me and R2 is α. 710B Q1 is 2-C1-5-thiazolyl, R1 is Me and R2 is Br. 711B Q1 is 2-C1-5-thiazolyl, R1 is Me and R2 is I. 712B Q1 is 2-C1-5-thiazolyl, R1 is Br and R2 is Br. 713B Q1 is 2-C1-5-thiazolyl, R1 is Br and R2 is Q. 714B Q1 is 2-C1-5-thiazolyl, R1 is C1 and R2 is Br. 715B Q1 is 2-C1-5-thiazolyl, R1 is C1 and R2 is C1. 151284.doc -157- 201117722 Table 3

R1 是 C卜 R2 是 Me 以及（R3) m 是 2,6-二-F，4-MeNH(CH2)3〇 Q2 Q2 Q2 4-Cl-Ph 4-F-Ph 4-Br-Ph 4-Me-Ph 4-Et-Ph 4-Cl-Bn 4-F-Bn 3-Cl-Ph 3-F-Ph 3-Br-Ph 3-Me-Ph 3- Et-Ph 3-F、 4- Me-Ph 4-C1' 3-F-Ph 2-C1'4-F-Ph 3,5-二 -MeO-Ph 3.4- 二-F-Ph 3.4- 二-Cl-Ph 2-C卜 3,5-二 -MeO-Ph 4- C卜 3,5-二 -MeO-Ph 5- MeO-3-B 比咬 基 6- MeO-3-e 比咬 基 S-Me-S-1»比咬基 6-F-3-0比咬基 6-CF3-3-。比咬基 2-Cn、6-CF3-3-0 比啶 基 2-C卜 6-MeO-3-吡 啶基 2-C1、6-Me-3-吡啶 基 6-MeO-3-e比咬基 6-Br-3-°比咬基 2-CF3_5-B比咳基 咬基 5-Me-3^5&quot;&quot; 基 5-F-3-吡啶基 6-Me-3-° 比咬 基 6-C1-3-吡啶 基 5- C1-3-吡啶 基 6-CF3_3_ B 比1^ 基 2-C1-5-吡啶 基 6- C1-3-吡啶 基 2-MeO-5_0比 啶基 本發明揭露的内容亦包括表1C到62C，每一表格 建立方式與上述表3相同，除了表3開頭的列（即「R1是 Cl· R2 是 Me 以及(R3)m 是 2,6-二-F、4-MeNH(CH2)30」）是以下述各別的列開頭所取代。因此，舉例來說，在表 1C列開頭是「R1是Cl，R2是C1以及(R3)m是2,6_二·F、 151284.doc •158- 201117722 4-ΜεΝίί((：Ιί2)30」，以及Q2是在上述表3中經定義。表 2C到62C以相似的方式建立。 列標題 表格代號R1 is C, R2 is Me and (R3) m is 2,6-di-F, 4-MeNH(CH2)3〇Q2 Q2 Q2 4-Cl-Ph 4-F-Ph 4-Br-Ph 4-Me -Ph 4-Et-Ph 4-Cl-Bn 4-F-Bn 3-Cl-Ph 3-F-Ph 3-Br-Ph 3-Me-Ph 3- Et-Ph 3-F, 4- Me- Ph 4-C1' 3-F-Ph 2-C1'4-F-Ph 3,5-di-MeO-Ph 3.4-di-F-Ph 3.4-di-Cl-Ph 2-C Bu 3,5- Di-MeO-Ph 4-CBu 3,5-di-MeO-Ph 5-MeO-3-B than bite 6-MeO-3-e than bite-based S-Me-S-1» than bite 6 -F-3-0 is more than a bite 6-CF3-3-. Than 2-Cn, 6-CF3-3-0, pyridyl 2-C, 6-MeO-3-pyridyl 2-C1, 6-Me-3-pyridyl 6-MeO-3-e Base 6-Br-3-° ratio biting base 2-CF3_5-B than cough base bite 5-Me-3^5&quot;&quot; base 5-F-3-pyridyl 6-Me-3-° ratio bite base 6-C1-3-pyridyl 5-C1-3-pyridyl 6-CF3_3_ B ratio 1^-yl 2-C1-5-pyridyl 6-C1-3-pyridyl 2-MeO-5_0 pyridine The contents also include Tables 1C to 62C. Each table is created in the same manner as Table 3 above, except for the column at the beginning of Table 3 (ie, "R1 is Cl· R2 is Me and (R3)m is 2,6-di-F, 4-MeNH(CH2)30") is replaced by the beginning of each of the following columns. So, for example, at the beginning of the table in Table 1C, "R1 is Cl, R2 is C1, and (R3)m is 2,6_2·F, 151284.doc •158-201117722 4-ΜεΝίί((:Ιί2)30 "," and Q2 are defined in Table 3 above. Tables 2C through 62C are established in a similar manner. Column heading table code

1C 2C 3C 4C 5C 6C 7C 8C 9C 10C 11C 12C 13C 14C 15C 16C 17C 18C 19C 20C 21C 22C 23C 24C 25C 26C 27C 28C 29C 30C 31C 32C 33C R1 是 α，R2 是 C1 以及（R3)m 是 2,6-二-F、4-MeNH(CH2)30。 R1 是 a，R2 是 Br 以及(R3)m 是 2,6-二-F、4-MeNH(CH2)30。 R1 是 Br，R2 是 Me 以及（R3)m 是 2,6·二-F、4-MeNH(CH2)30。 R1 是 Br，R2 是 C1 以及(R3)m 是 2,6-二-F、4-MeNH(CH2)30。 R1 是 Me，R2 是 Me 以及(R3)m 是 2,6-二-F、4-MeNH(CH2)30。 R1 是 Br，R2 是 Br 以及（R3)m 是 2,6-二-F、4-MeNH(CH2)30。 R1 是 Cl，R2 是 Me 以及（R3)m 是 2,6-二-F、4-Me2N(CH2)30。 R1 是 Cl，R2 是 C1 以及（R3)m 是 2,6-二-F、4-Me2N(CH2)30。 R1 是 CL· R2 是 Br 以及（尺巧爪是 2,6-二-F、4-Me2N(CH2)30。 R1 是 Br，R2 是 Me 以及（R3)m 是 2,6-二-F、4-Me2N(CH2)30。 R1 是 Br，R2 是 C1 以及（R3)m 是 2,6-二-F、4-Me2N(CH2)30。 R1 是 Me，R2 是 Me 以及(R3)m 是 2,6-二-F、4-Me2N(CH2)30。 R1 是 Br，R2 是 Br 以及（R3)m 是 2,6-二-F、4-Me2N(CH2)30。 R1 是 Cl，R2 是 Me 以及（R3)m 是 2,6-二-F、4-Me0(CH2)30。 R1 是 Cl，R2 是 C1 以及（R3)m 是 2,6-二-F、4-Me0(CH2)30。 R1 是 Cl，R2 是 Br 以及（R3)m 是 2,6-二-F、4-Me0(CH2)30。 R1 是 Br，R2 是 Me 以及（R3)m 是 2,6-二-F、4-MecT(CH2)30。 R1 是 Br，R2 是 C1 以及（R3)m! 2,6-二-F、4-Me0(CH2)30。 R1 是 Me，R2 是 Me 以及（R3)m 是 2,6-二-F、4-Me0(CH2)30。 R1 是 Br，R2 是 Br 以及（R3)m 是 2,6-二-F、4-Me0(CH2)30。 R1 是 C卜 R2 是 Me 以及(R3)m 是 2-C1-6-F、4-MeNH(CH2)30。 R1 是 CP R2 是 C1 以及（R3)m 是 2-C1-6-F、4-MeNH(CH2)30。 R1 是 Cl，R2 是 Br 以及（R3)m 是 2-C1-6-F、4-MeNH(CH2)30。 R1 是 Br，R2 是 Me 以及（R3)m 是 2-C1-6-F、4-MeNH(CH2)30。 R1 是 Br，R2 是 C1 以及（R3)m* 2-C1-6-F、4-MeNH(CH2)30。 R1 是 Me，R2 是 Me 以及(R3)m 是 2-C1-6-F、4-MeNH(CH2)30。 R1 是 Br，R2 是 Br 以及（R3)m 是 2-C1-6-F、4-MeNH(CH2)30。 R1 是 CL· R2 是 Me 以及（R3)m 是 2,6-二-F、3-MeNH(CH2)30。 R1 是 Cl，R2 是 C1 以及（R3)m 是 2,6-二-F、3-MeNH(CH2)30。 R1 是 Cl，R2 是 Br 以及（R3)m 是 2,6-二-F、3-MeNH(CH2)3〇。 R1 是 Br，R2 是 Me 以及(R3)m 是 2,6·二-F、3-MeNH(CH2)30。 R1 是 Br，R2 是 C1 以及（R3)m 是 2,6-二-F、3-MeNH(CH2)30。 R1 是 Me，R2 是 Me 以及(R3)m 是 2,6-二-F、3-MeNH(CH2)30。 151284.doc -159- 201117722 表格代號 列標題1C 2C 3C 4C 5C 6C 7C 8C 9C 10C 11C 12C 13C 14C 15C 16C 17C 18C 19C 20C 21C 22C 23C 24C 25C 26C 27C 28C 29C 30C 31C 32C 33C R1 is α, R2 is C1 and (R3)m is 2,6- Di-F, 4-MeNH(CH2)30. R1 is a, R2 is Br and (R3)m is 2,6-di-F, 4-MeNH(CH2)30. R1 is Br, R2 is Me and (R3)m is 2,6·di-F, 4-MeNH(CH2)30. R1 is Br, R2 is C1 and (R3)m is 2,6-di-F, 4-MeNH(CH2)30. R1 is Me, R2 is Me and (R3)m is 2,6-di-F, 4-MeNH(CH2)30. R1 is Br, R2 is Br and (R3)m is 2,6-di-F, 4-MeNH(CH2)30. R1 is Cl, R2 is Me and (R3)m is 2,6-di-F, 4-Me2N(CH2)30. R1 is Cl, R2 is C1 and (R3)m is 2,6-di-F, 4-Me2N(CH2)30. R1 is CL· R2 is Br and (the ruler is 2,6-di-F, 4-Me2N(CH2)30. R1 is Br, R2 is Me and (R3)m is 2,6-di-F, 4-Me2N(CH2)30. R1 is Br, R2 is C1 and (R3)m is 2,6-di-F, 4-Me2N(CH2)30. R1 is Me, R2 is Me and (R3)m is 2,6-di-F, 4-Me2N(CH2)30. R1 is Br, R2 is Br and (R3)m is 2,6-di-F, 4-Me2N(CH2)30. R1 is Cl, R2 Yes Me and (R3)m are 2,6-di-F, 4-Me0(CH2)30. R1 is Cl, R2 is C1 and (R3)m is 2,6-di-F, 4-Me0(CH2 30. R1 is Cl, R2 is Br and (R3)m is 2,6-di-F, 4-Me0(CH2)30. R1 is Br, R2 is Me and (R3)m is 2,6-two -F, 4-MecT(CH2)30. R1 is Br, R2 is C1 and (R3)m! 2,6-di-F, 4-Me0(CH2)30. R1 is Me, R2 is Me and (R3 m is 2,6-di-F, 4-Me0(CH2)30. R1 is Br, R2 is Br and (R3)m is 2,6-di-F, 4-Me0(CH2)30. R1 is C is R2 is Me and (R3)m is 2-C1-6-F, 4-MeNH(CH2)30. R1 is CP R2 is C1 and (R3)m is 2-C1-6-F, 4-MeNH (CH2)30. R1 is Cl, R2 is Br and (R3)m is 2-C1-6- F, 4-MeNH(CH2)30. R1 is Br, R2 is Me and (R3)m is 2-C1-6-F, 4-MeNH(CH2)30. R1 is Br, R2 is C1 and (R3) m* 2-C1-6-F, 4-MeNH(CH2)30. R1 is Me, R2 is Me and (R3)m is 2-C1-6-F, 4-MeNH(CH2)30. R1 is Br , R2 is Br and (R3)m is 2-C1-6-F, 4-MeNH(CH2)30. R1 is CL· R2 is Me and (R3)m is 2,6-di-F, 3-MeNH (CH2) 30. R1 is Cl, R2 is C1 and (R3)m is 2,6-di-F, 3-MeNH(CH2)30. R1 is Cl, R2 is Br and (R3)m is 2,6-di-F, 3-MeNH(CH2)3〇. R1 is Br, R2 is Me and (R3)m is 2,6·di-F, 3-MeNH(CH2)30. R1 is Br, R2 is C1 and (R3)m is 2,6-di-F, 3-MeNH(CH2)30. R1 is Me, R2 is Me and (R3)m is 2,6-di-F, 3-MeNH(CH2)30. 151284.doc -159- 201117722 Table Code Column Heading

34C 35C 36C 37C 38C 39C 40C 41C 42C 43C 44C 45C 46C 46C 48C 49C 50C 51C 52C 53C 54C 55C 56C 57C 58C 59C 60C 61C 62C R1 是 Br，R2 是 Br 以及(R3)m 是 2,6-二-F、3-MeNH(CH2)30。 R1 是 CP R2 是 Me 以及(以“是 2,6-二-F、3-Me2N(CH2)30。 R1 是 CP R2 是 C1 以及（R3)m 是 2,6-二-F、3-Me2N(CH2)30。 R1 是 CP R2 是 Br 以及({^爪是 2,6-二-F、3-Me2N(CH2)30。 R1 是 Br，R2 是 Me 以及(“一是 2,6-二-F、3-Me2N(CH2)30。 R1 是 Br，R2 是 C1 以及⑺巧阳是 2,6-二-F、3-Me2N(CH2)30。 R1 是 Me，R2 是 Me 以及(^、是 2,6-二-F、3-Me2N(CH2)30。 R1 是 Br，R2 是 Br 以及(R3)m 是 2,6-二-F、3-Me2N(CH2)30。 R1 是 CL· R2 是 Me,以及(R3)m 是 2,6-二-F、3-Me0(CH2)30。 R1 是 CM，R2 是 C1 以及(R3)m 是 2,6-二-F、3-Me0(CH2)30。 R1 是 Q，R2 是 Br 以及（R3)m 是 2,6-二-F、3-Me0(CH2)30。 R1 是 Br，R2 是 Me 以及（R3)m 是 2,6-二-F、3-Me0(CH2)30。 R1 是 Br，R2 是 C1 以及（尺巧阳是 2,6-二-F、3-Me0(CH2)30。 R1 是 Me，R2 是 Me 以及（R3)m 是 2,6-二-F、3-Me0(CH2)30。 R1 是 Br，R2 是 Br 以及(R3)m 是 2,6-二-F、3-Me0(CH2)30。 R1 是 CU，R2 是 Me 以及(“、是 2-C1-6-F、3-MeNH(CH2)30。 R1 是 a，R2 是 C1 以及（R3)m 是 2-C1-6-F、3-MeNH(CH2)30。 R1 是 CU，R2 是 Br 以及（R3)m 是 2-C1-6-F、3-MeNH(CH2)30。 R1 是 Br，R2 是 Me 以及(以‘是 2-C1-6-F、3-MeNH(CH2)30。 R1 是 Br，R2 是 C1 以及(R3)m 是 2-C1-6-F、3-MeNH(CH2)30。 R1 是 Me，R2 是 Me 以及（R3)m 是 6-C1-6-F、3-MeNH(CH2)30。 R1 是 Br，R2 是 Br 以及（R3)m 是 2-C1-6-F、3-MeNH(CH2)30。 R1 是 Cl，R2 是 Me 以及（R3)m 是 6-C1-2-F、3-MeNH(CH2)30。 R1 是 Cl，R2 是 C1 以及（R3)m 是 6-C1-2-F、3-MeNH(CH2)30。 R1 是 Cl，R2 是 Br 以及(R3)m 是 6-C1-2-F、3-MeNH(CH2)30。 R1 是 Br，R2 是 Me 以及（“、是 6-C1-2-F、3-MeNH(CH2)30。 R1 是 Br，R2 是 C1 以及（R3)m 是 6-C1-2-F、3-MeNH(CH2)30。 R1 是 Me，R2 是 Me 以及(R3)m 是 6-C1-2-F、3-MeNH(CH2)30。 R1 是 Br，R2 是 Br 以及（^一是 6-C1-2-F、3-MeNH(CH2)30。 表4 151284.doc -160- 201117722 R134C 35C 36C 37C 38C 39C 40C 41C 42C 43C 44C 45C 46C 46C 48C 49C 50C 51C 52C 53C 54C 55C 56C 57C 58C 59C 60C 61C 62C R1 is Br, R2 is Br and (R3)m is 2,6-di-F, 3-MeNH(CH2)30. R1 is CP R2 is Me and ("is 2,6-di-F, 3-Me2N(CH2)30. R1 is CP R2 is C1 and (R3)m is 2,6-di-F, 3-Me2N (CH2)30. R1 is CP R2 is Br and ({^claw is 2,6-di-F, 3-Me2N(CH2)30. R1 is Br, R2 is Me and ("One is 2,6-two -F, 3-Me2N(CH2)30. R1 is Br, R2 is C1 and (7) Qiaoyang is 2,6-di-F, 3-Me2N(CH2)30. R1 is Me, R2 is Me and (^, It is 2,6-di-F, 3-Me2N(CH2)30. R1 is Br, R2 is Br and (R3)m is 2,6-di-F, 3-Me2N(CH2)30. R1 is CL· R2 is Me, and (R3)m is 2,6-di-F, 3-Me0(CH2)30. R1 is CM, R2 is C1 and (R3)m is 2,6-di-F, 3-Me0 (CH2)30. R1 is Q, R2 is Br and (R3)m is 2,6-di-F, 3-Me0(CH2)30. R1 is Br, R2 is Me and (R3)m is 2,6 -Di-F, 3-Me0(CH2)30. R1 is Br, R2 is C1 and (Jiaoqiaoyang is 2,6-di-F, 3-Me0(CH2)30. R1 is Me, R2 is Me and (R3)m is 2,6-di-F, 3-Me0(CH2)30. R1 is Br, R2 is Br and (R3)m is 2,6-di-F, 3-Me0(CH2)30. R1 is CU, R2 is Me and (", is 2-C1-6-F, 3-MeNH(C H2)30. R1 is a, R2 is C1 and (R3)m is 2-C1-6-F, 3-MeNH(CH2)30. R1 is CU, R2 is Br and (R3)m is 2-C1- 6-F, 3-MeNH(CH2)30. R1 is Br, R2 is Me and (is '2-C1-6-F, 3-MeNH(CH2)30. R1 is Br, R2 is C1 and (R3) m is 2-C1-6-F, 3-MeNH(CH2)30. R1 is Me, R2 is Me and (R3)m is 6-C1-6-F, 3-MeNH(CH2)30. R1 is Br, R2 is Br and (R3)m is 2-C1-6-F, 3-MeNH(CH2)30. R1 is Cl, R2 is Me and (R3)m is 6-C1-2-F, 3-MeNH(CH2)30. R1 is Cl, R2 is C1 and (R3)m is 6-C1-2-F, 3-MeNH(CH2)30. R1 is Cl, R2 is Br and (R3)m is 6-C1-2-F, 3-MeNH(CH2)30. R1 is Br, R2 is Me and (", is 6-C1-2-F, 3-MeNH(CH2)30. R1 is Br, R2 is C1 and (R3)m is 6-C1-2-F, 3 -MeNH(CH2)30. R1 is Me, R2 is Me and (R3)m is 6-C1-2-F, 3-MeNH(CH2)30. R1 is Br, R2 is Br and (^ is 6- C1-2-F, 3-MeNH(CH2)30. Table 4 151284.doc -160- 201117722 R1

R1 是 C1， Q1 R2是Me以及（R5 Q1 )n 是 2,6-二_F、4_ Q1 MeNH(CH2)3〇 ° 〇! Q1 4-Cl-Ph 3-F-Ph 3,4-二-F_ph 6-CF3-3-吡啶基 5-Me-3-0 比咬 基 4-F-Ph 3-Br-Ph 3,4-—Cl-Ph 2-C1 ' 6-CF3-3- 5-F-3-吡啶 0比咬基 基 4-Br-Ph 3-Me-Ph 2-C卜 3,5-二 2-C1 ' 6-MeO-3- 6-Me-3-e 比咬 -Me〇-Ph -比咬基 基 4-Me-Ph 3-Et-Ph 4-cl、3,5-二 2-C1 ' 6-Me-3- 6-C1-3-吡啶 -MeO-Ph &quot;比咬基 基 4-Et-Ph 3-F、4-Me-Ph 5-MeO-3_a 比咬 6-McO-3 5-C1-3-吡啶 基 基 基 4-Cl-Bn 4-a、3-F-Ph 6-MeO-3 比咬 6-Br-3-°比咬基 6-CF3*3 - 基 啶基 4-F-Bn 2-C1 &gt; 4-F-Ph 2-Me-5-〇比咬基 2-CF3-5-吡啶基 2-C1-5·11 比咬 3-Cl-Ph 3,5-二-MeO-Ph 6-F-3-吡啶基 6-Me-3-°比咬基 基 基 2-MeO-5-口比 啶基 本發明揭露的内容亦包含表ID到62D，每一表格 建立方式與上述表4相同，除了表4開頭的列（即「Ri 疋 C1，R2 是 Me 以及(R5)n 是 2,6-二-F、4-MeNH(CH2)3〇」） 疋以下述各別的列開頭所取代。因此，舉例來說，在表 1D列開頭是「R1是Cl，R2是C1以及(R5)n是2,6_:F、 4-MeNH(CH2)3〇j，以及Q1是在上述表i中經定義。表 2D到62D以相似的方式建立。 151284.doc • 161 - 201117722 表格代號 列標題R1 is C1, Q1 R2 is Me and (R5 Q1 )n is 2,6-di_F, 4_ Q1 MeNH(CH2)3〇° 〇! Q1 4-Cl-Ph 3-F-Ph 3,4-two -F_ph 6-CF3-3-pyridyl 5-Me-3-0 butyl 4-F-Ph 3-Br-Ph 3,4-Cl-Ph 2-C1 '6-CF3-3- 5- F-3-pyridine 0 to bite base 4-Br-Ph 3-Me-Ph 2-C b 3,5-di 2-C1 '6-MeO-3- 6-Me-3-e ratio bite-Me 〇-Ph-Bit base 4-Me-Ph 3-Et-Ph 4-cl, 3,5-di 2-C1 '6-Me-3- 6-C1-3-pyridine-MeO-Ph &quot; Specific bite base 4-Et-Ph 3-F, 4-Me-Ph 5-MeO-3_a ratio 6-McO-3 5-C1-3-pyridyl 4-cl-Bn 4-a, 3 -F-Ph 6-MeO-3 than bite 6-Br-3-° ratio bite 6-CF3*3 - pyridine group 4-F-Bn 2-C1 &gt; 4-F-Ph 2-Me-5 - 〇 咬 2- 2-CF3-5-pyridyl 2-C1-5·11 than 3-Cl-Ph 3,5-di-MeO-Ph 6-F-3-pyridyl 6-Me-3- The content of the basic invention disclosed in the basic invention also includes Table ID to 62D, and each table is created in the same manner as Table 4 above, except for the column at the beginning of Table 4 (ie, "Ri 疋 C1" , R2 is Me and (R5)n is 2,6-di-F, 4-MeNH(CH2)3〇") 疋 replaced by the following respective columns . So, for example, at the beginning of the column in Table 1D is "R1 is Cl, R2 is C1, and (R5)n is 2,6_:F, 4-MeNH(CH2)3〇j, and Q1 is in the above table i By definition, Tables 2D through 62D are created in a similar manner. 151284.doc • 161 - 201117722 Table Code Column Headings

1D 2D 3D 4D 5D 6D 7D 8D 9D 10D 11D 12D 13D 14D 15D 16D 17D 18D 19D 20D 21D 22D 23D 24D 25D 26D 27D 28D 29D 30D 31D 32D 33D 34D 35D 36D R1 是 C卜 R2 是 C1 以及（R5)n 是 2,6-二-F、4-MeNH(CH2)30。 R1 是 Q，R2 是 Br 以及（R5)n 是 2,6-二-F、4-MeNH(CH2)30。 R1 是 Br，R2 是 Me 以及(R5)n 是 2,6-二-F、4-MeNH(CH2)30。 R1 是 Br，R2 是 C1 以及(R5)n 是 2,6-二-F、4-MeNH(CH2)30。 R】是 Me，R2 是 Me 以及(R5)n 是 2,6-二-F、4-MeNH(CH2)30。 R1 是 Br，R2 是 Br 以及（R5)n 是 2,6-二-F、4-MeNH(CH2)30。 R1 是 a，R2 是 Me 以及(R5)n 是 2,6-二-F、4-Me2N(CH2)30。 R1 是 CP R2 是 C1 以及（R5)n 是 2,6-二-F、4-Me2N(CH2)3〇。 R1 是 C卜 R2 是 Br 以及（R5)n 是 2,6-二-F、4-Me2N(CH2)30。 R1 是 Br，R2 是 Me 以及（R5)n 是 2,6-二-F、4-Me2N(CH2)30。 R1 是 Br，R2 是 C1 以及（R5)n 是 2,6-二-F、4-Me2N(CH2)30。 R1 是 Me，R2 是 Me 以及（R5)n 是 2,6-二-F、4-Me2N(CH2)30。 R1 是 Br，R2 是 Br 以及（R5)n 是 2,6-二-F、4-Me2N(CH2)30。 R1 是 C卜 R2 是 Me，以及（R5)n 是 2,6-二-F、4-Me0(CH2)30。 R1 是 CL· R2 是 C1 以及(R5)n 是 2,6-二-F、4-Me0(CH2)30。 R1 是 a，R2 是 Br 以及（R5)n 是 2,6-二-F、4-Me0(CH2)30。 R1 是 Br，R2 是 Me 以及（R5)n 是 2,6-二-F、4-Me0(CH2)30。 R1 是 Br，R2 是 C1 以及（R5)n 是 2,6-二-F、4-Me0(CH2)30。 R1 是 Me，R2 是 Me 以及(R5)n 是 2,6-二-F、4-Me0(CH2)30。 R1 是 Br，R2 是 Br 以及(R5)n 是 2,6-二-F、4-Me0(CH2)30。 R1 是 C卜 R2 是 Me 以及（R5)n 是 2-C1-6-F、4-MeNH(CH2)30。 R1 是 CU，R2 是 C1 以及（R5)n 是 2-C1-6-F、4-MeNH(CH2)30。 R1 是 a，R2 是 Br 以及(R5)n 是 2-C1-6-F、4-MeNH(CH2)30。 R1 是 Br，R2 是 Me 以及(R5)n 是 2-C1-6-F、4-MeNH(CH2)30。 是 Br，R2 是 C1 以及(R5)n 是 2-C1-6-F、4-MeNH(CH2)30。 R1 是 Me，R2 是 Me 以及(R5)n 是 2-C1-6-F、4-MeNH(CH2)30。 R1 是 Br，R2 是 Br 以及（R5)n 是 2-C1-6-F、4-MeNH(CH2)30。 R1 是 C卜 R2 是 Me 以及(R5)n 是 2,6-二-F、3-MeNH(CH2)30。 R1 是 Q，R2 是 C1 以及(R5)n 是 2,6-二-F、3-MeNH(CH2)30。 R1 是 a，R2 是 Br 以及（R5)n 是 2,6-二-F、3-MeNH(CH2)30。 R1 是 Br，R2 是 Me 以及(R5)n 是 2,6-二-F、3-MeNH(CH2)30。 R1 是 Br，R2 是 C1 以及（R5)n 是 2,6-二-F、3-MeNH(CH2)30。 R1 是 Me，R2 是 Me 以及(R5)n 是 2,6-二-F、3-MeNH(CH2)30。 R1 是 Br，R2 是 Br 以及（R5)n 是 2,6-二-F、3-MeNH(CH2)30。 R1 是 a，R2 是 Me 以及(R5)n 是 2,6-二-F、3-Me2N(CH2)30。 R1 是 C卜 R2 是 C1 以及（R5)n 是 2,6-二-F、3-Me2N(CH2)3〇。 151284.doc -162- 201117722 表格代號 列標題1D 2D 3D 4D 5D 6D 7D 8D 9D 10D 11D 12D 13D 14D 15D 16D 17D 18D 19D 20D 21D 22D 23D 24D 25D 26D 27D 28D 29D 30D 31D 32D 33D 34D 35D 36D R1 is C Bu R2 is C1 and (R5)n is 2 , 6-di-F, 4-MeNH(CH2)30. R1 is Q, R2 is Br and (R5)n is 2,6-di-F, 4-MeNH(CH2)30. R1 is Br, R2 is Me and (R5)n is 2,6-di-F, 4-MeNH(CH2)30. R1 is Br, R2 is C1 and (R5)n is 2,6-di-F, 4-MeNH(CH2)30. R] is Me, R2 is Me and (R5)n is 2,6-di-F, 4-MeNH(CH2)30. R1 is Br, R2 is Br and (R5)n is 2,6-di-F, 4-MeNH(CH2)30. R1 is a, R2 is Me and (R5)n is 2,6-di-F, 4-Me2N(CH2)30. R1 is CP R2 is C1 and (R5)n is 2,6-di-F, 4-Me2N(CH2)3〇. R1 is C, R2 is Br and (R5)n is 2,6-di-F, 4-Me2N(CH2)30. R1 is Br, R2 is Me and (R5)n is 2,6-di-F, 4-Me2N(CH2)30. R1 is Br, R2 is C1 and (R5)n is 2,6-di-F, 4-Me2N(CH2)30. R1 is Me, R2 is Me and (R5)n is 2,6-di-F, 4-Me2N(CH2)30. R1 is Br, R2 is Br and (R5)n is 2,6-di-F, 4-Me2N(CH2)30. R1 is CBu, R2 is Me, and (R5)n is 2,6-di-F, 4-Me0(CH2)30. R1 is CL· R2 is C1 and (R5)n is 2,6-di-F, 4-Me0(CH2)30. R1 is a, R2 is Br and (R5)n is 2,6-di-F, 4-Me0(CH2)30. R1 is Br, R2 is Me and (R5)n is 2,6-di-F, 4-Me0(CH2)30. R1 is Br, R2 is C1 and (R5)n is 2,6-di-F, 4-Me0(CH2)30. R1 is Me, R2 is Me and (R5)n is 2,6-di-F, 4-Me0(CH2)30. R1 is Br, R2 is Br and (R5)n is 2,6-di-F, 4-Me0(CH2)30. R1 is C, R2 is Me, and (R5)n is 2-C1-6-F, 4-MeNH(CH2)30. R1 is CU, R2 is C1 and (R5)n is 2-C1-6-F, 4-MeNH(CH2)30. R1 is a, R2 is Br and (R5)n is 2-C1-6-F, 4-MeNH(CH2)30. R1 is Br, R2 is Me and (R5)n is 2-C1-6-F, 4-MeNH(CH2)30. Is Br, R2 is C1 and (R5)n is 2-C1-6-F, 4-MeNH(CH2)30. R1 is Me, R2 is Me and (R5)n is 2-C1-6-F, 4-MeNH(CH2)30. R1 is Br, R2 is Br and (R5)n is 2-C1-6-F, 4-MeNH(CH2)30. R1 is C, R2 is Me and (R5)n is 2,6-di-F, 3-MeNH(CH2)30. R1 is Q, R2 is C1 and (R5)n is 2,6-di-F, 3-MeNH(CH2)30. R1 is a, R2 is Br and (R5)n is 2,6-di-F, 3-MeNH(CH2)30. R1 is Br, R2 is Me and (R5)n is 2,6-di-F, 3-MeNH(CH2)30. R1 is Br, R2 is C1 and (R5)n is 2,6-di-F, 3-MeNH(CH2)30. R1 is Me, R2 is Me and (R5)n is 2,6-di-F, 3-MeNH(CH2)30. R1 is Br, R2 is Br and (R5)n is 2,6-di-F, 3-MeNH(CH2)30. R1 is a, R2 is Me and (R5)n is 2,6-di-F, 3-Me2N(CH2)30. R1 is CBu R2 is C1 and (R5)n is 2,6-di-F, 3-Me2N(CH2)3〇. 151284.doc -162- 201117722 Table Code Column Heading

37D 38D 39D 40D 41D 42D 43D 44D 45D 3-Me2N(CH2)3〇。 3-Me2N(CH2)3〇 0 3-Me2N(CH2)30。 、3-Me2N(CH2)30 3-Me2N(CH2)30。 3-Me0(CH2)30。 3-Me0(CH2)30。 3-Me0(CH2)30。 3-Me0(CH2)30。 R1 是 CL· R2 是 Br 以及（R5)n 是 2,6-二-F、 R1 是 Br，R2 是 Me 以及（R5)n 是 2,6-二-F R1 是 Br，R2 是 C1 以及（R5)n 是 2,6-二-F、 R1 是 Me，R2 是 Me 以及（R5)n 是 2,6-二-F R1 是 Br，R2 是 Br 以及（R5)n 是 2,6-二-F、 R1 是 CL· R2 是 Me，以及（R5)n! 2,6-二-F ' R1 是 α，R2 是 C1 以及（R5)n 是 2,6-二-F、 R1 是 CL· R2 是 Br 以及（R5)n 是 2,6-二-F、 R1 是 Br，R2 是 Me 以及(R5)n* 2,6-二-F，37D 38D 39D 40D 41D 42D 43D 44D 45D 3-Me2N(CH2)3〇. 3-Me2N(CH2)3〇 0 3-Me2N(CH2)30. 3-Me2N(CH2)30 3-Me2N(CH2)30. 3-Me0(CH2)30. 3-Me0(CH2)30. 3-Me0(CH2)30. 3-Me0(CH2)30. R1 is CL· R2 is Br and (R5)n is 2,6-di-F, R1 is Br, R2 is Me and (R5)n is 2,6-di-F R1 is Br, R2 is C1 and R5)n is 2,6-di-F, R1 is Me, R2 is Me and (R5)n is 2,6-di-F R1 is Br, R2 is Br and (R5)n is 2,6-di -F, R1 is CL· R2 is Me, and (R5)n! 2,6-di-F ' R1 is α, R2 is C1 and (R5)n is 2,6-di-F, and R1 is CL· R2 is Br and (R5)n is 2,6-di-F, R1 is Br, R2 is Me and (R5)n* 2,6-di-F,

46D 46D 48D 49D 50D 51D 52D 53D 54D 55D 56D 57D 58D 59D 60D 61D 62D R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 是Br 是Me 是Br 是Cl 是Cl 是Cl 是Br 是Br 是Me 是Br 是Cl 是Cl 是Cl 是Br 是Br 是Me 是Br R2 是 Cl 以及（R5)n 是 2,6-二-F、 ，R2 是 Me 以及（R5)n 是 2,6-二-F R2 是 Br 以及（R5)n 是 2,6-二-F、 R2 是 Me 以及（R5)n 是 2-C1-6-F R2 是 Cl 以及（R5)n 是 2-C1-6-F、 R2 是 Br 以及（R5)n 是 2-C1-6-F、 R2 是 Me 以及（R5)n 是 2-C1-6-F R2 是 Cl 以及（R5)n 是 2-C1-6-F、 R2 是 Me 以及（R5)n 是 6-C1-6-F R2 是 Br 以及（R5)n 是 2-C1-6-F、 R2 是 Me 以及(R5)n 是 6-C1-2-F R2 是 Cl 以及（R5)n 是 6-C1-2-F、 R2 是 Br 以及（R5)n 是 6-C1-2-F、 R2 是 Me 以及（R5)n 是 6-C1-2-F R2 是 Cl 以及（R5)n 是 6-C1-2-F、 R2 是 Me 以及(R5)n 是 6-C1-2-F R2 是 Br 以及（R5)n 是 6-C1-2-F、 3-Me0(CH2)30。 、3-Me0(CH2)30。 3-Me0(CH2)30。 '3-MeNH(CH2)30。 3-MeNH(CH2)30。 3-MeNH(CH2)30。 ‘ 3-MeNH(CH2)3〇。 3-MeNH(CH2)30。 、3-MeNH(CH2)30。 3-MeNH(CH2)30。 3-MeNH(CH2)30。 3-MeNH(CH2)30。 3-MeNH(CH2)30。 • 3-MeNH(CH2)30。 3-MeNH(CH2)30。 、3-MeNH(CH2)30。 3-MeNH(CH2)30。 製劑/效用 一個選自式1化合物、其N-氧化物及其鹽類的化 合物，或是一個混合物（即組合物），包含具有至少一 個在發明内容中描述的額外殺真菌化合物之化合物（即 殺真菌劑），將主要地用來提供進一步組合物的殺真菌 活性成分，即配方，其具有至少一種選自由以下所組成 之群組的成分：表面活性劑、固體稀釋劑以及液體稀釋 151284.doc •163- 201117722 :體，活性成分的生物性質，使 用模式以及认因子例如土壤類型、溼度以及溫度符合 一致的配方或組成成分。 M OU即至少i式卜N_氧化物、或其鹽類 的化合物）與!且分⑴（例如，選自前述之（Μ)到（Μ6) 以及其鹽類）以及/或-個或更多其他的生物活性化合 物或藥劑（即殺蟲劑、其他殺真菌劑、殺線蟲劑、殺螨 劑、除草劑以及其他生物藥劑）可以數種方式來調配， 包括： (1)組分（a)、組分（b)以及/或一個或更多其他 的生物活性化合物或藥劑可以適當的重量比 經分別調配以及分別應用或同時應用，例如， 槽混合；或 (ii)組分（a)、組分（b)以及/或一個或更多其他 的生物活性化合物或藥劑可以適當的重量比 一起進行調配。 可用的配方包括液體及固體組合物^液體組合物包 括溶液（包括乳劑）、懸浮液、乳液（包括微乳液和/或 懸浮乳液（suspoemulsions))等等，並可選擇地將其增 濃成凝膠。含水液體組合物的一般類型為可溶劑 (soluble concentrate )、水懸劑（suspension concentrate)、膠囊懸著劑（capsule suspension)、濃縮 乳液、微乳液和懸浮乳液。非水液體組合物的一般類型 為乳劑、微乳劑、水分散性乳劑（dispersible concentrate ) 及水分散性油懸劑（oil dispersion)。 151284.doc * 164 - 201117722 體、'且5物的一般類型為塵粉（dusts )、粉劑、粒 齊I 丸M (pdlets)、珠劑（prills)、錠劑（pastilles)、 片劑^ (fllledfllms)(包括種子塗覆物）等等，其 可^水刀政性（「可濕性」）或水溶性。從成膜溶液劑或 可a動懸’形成的薄膜和塗層在種子處理上特別有 二性成分可以經（微）膠囊包裹著以及進一步形成 /«lw字體或固體配方；或者整個活性物質的配方可以經 膠囊，裹著（或「保護層包裹著」）。膠囊包裹可以防治 或減緩居性成分的釋放。乳粒劑結合了乳劑配方與乾粒 狀配方的優點。高強度組合物主要用作進一步配方的中 間物。 值知&gt;主意的是一個組合物實施例，其中一個固體組 合物的粒狀體其包括一個式1的化合物（或一個N-氧 化物或其鹽類）與包括組分（b)的固體組合物的粒狀 體一起混合。這些混何物可以進一步與包括額外農業用 保護劑的粒狀物做混合。或者，兩個或更多的農業用保 護劑（例如，一個組分（a)(式丨）化合物、一個組分 (b)化合物、一個非組分或的農業用保護 劑）可以經結合在一組粒狀體的固體組合物，其之後經 與包括一個或多個附加的農業用保護劑之固體組合物 之一組或多組的粒狀體所混合。這些粒狀體混合物可與 在PCT專利公開號WO 94/24861中揭露的一般粒狀體 混合物一致’或較佳的是，美國專利號6,022,552的同 質粒狀體混合物教學中揭露的一般粒狀體混合物一致。 可喷灑配方通常在喷麗前會先在適合的介質中擴 展。將這樣的液體及固體配方配製成可容易稀釋於噴灑 151284.doc -165· 201117722 介質（通常是水）中。噴灑的量可從每公頃約 公升’但更通常為從每公頃約十到數百公升。 方可在槽中與水或其他適合的介質混合，藉由 从 面施用而運騎葉治療，或施用於植物的生 5 體配方和乾配方可在播㈣，直接計量加4流文 統或舉溝。液體和冊配方可以施麟農作物和其他所 欲植物的種子，作為_前種子處理之用，/系 吸收以保護發育中的根及其它地下的植物部分及/或 遠配方通常含有有效量在下列近似範圍中的活性 成分、稀釋劑和界面活性劑，其重量加起來會等於百分 之百。 重量百分比 活性 水分散性粒劑及水溶性粒劑，片劑 及粉劑 成分 0.001-90 稀釋劑 0-99.999 界面活性劑 0-15 水分散性油懸劑、懸浮液、乳液、 溶液（包括乳劑） 1-50 40-99 〇~5〇 粉塵 1-25 70-99 〇-5 細粒及顆粒 高強度組合物 0.001-99 5-99.999 0-15 90-99 0—10 0-2 固體稀釋劑包括例如，像是膨土、微 晶商嶺石、， 帖浦石及商嶺土的黏土 、石膏、 纖維素、 一氧化欽、. 氧 化鋅、澱粉、糊精、糠（例如乳糖、蔗糖）、矽石、滑 石、雲母、矽藻土、尿素、碳酸鈣、碳酸鈉及碳酸氫鈉 以及硫酸鈉。典型的固體稀釋劑在Watkinsetal的著作 15l284.doc 201117722 中已、經描述，Handbook of Insecticide Dust Diluents and Carriers，2nd Ed., Dorland Books，Caldwell, New Jersey。 液體稀釋劑包含，例如，水、N，N-二曱基烧醯胺（例 如，N，N-二曱基曱醯胺）、葶烯、二曱基亞砜、N-烷吡 咯啶酮（例如，N-曱基吡咯烷酮）、乙二醇、三乙烯乙 二醇、丙烯乙二醇、二丙烯甘醇、聚丙烯乙二醇、丙烯 碳酸鹽、伸丁基碳酸酯、鏈烧烴（例如，白色礦物油、 正構烷烴、異烷烴）、烷基苯、烷基萘、甘油、甘油三 醋酸、山梨糖醇、三乙醯甘油、芳香族化合物烴類、脫 芳脂肪族化合物、烷基苯、烷基萘、酮類例如環己酮、 2-庚酮、異佛酮以及4-經基-4-甲基-2-戊酮、醋酸鹽、 例如乙酸異戊酯、乙酸己酯、乙酸庚酯、乙酸辛酯、乙 酸壬酯、十三基醋酸鹽以及乙酸異莰酯、其他酯類，例 如烷基化乳酸鹽酯類、二元酯類以及γ_ 丁内酯，以及 醇’其可以疋直鍵、支鍵、飽和或不飽和，例如曱醇、 乙醇、正丙醇、異丙醇、正丁醇、異丁醇、正己醇、2_ 乙基己醇、正辛醇、癸醇、異癸醇、異十八醇、鯨蠟醇、 月桂醇、十三醇、油醇、環己醇、四氫糠醇、二丙酮醇 以及节基醇。液體稀釋劑也包括飽和以及不飽和脂肪酸 的甘油醋類（典型為C6_C22)，例如植物種子以及水果 油（例如’橄欖油、萬麻、亞麻仁、芝麻、玉米、花生、 向曰葵、葡萄籽油、紅花、棉籽、黃豆、油菜、椰子以 及棕櫚仁）、動物性脂肪（例如，牛油、豬肉獸脂、豬 油、鱈魚肝油、魚油）’以及其混合物。液體稀釋劑也 包括烷化脂肪酸（例如甲基化、乙基化、丁基化），其 中該脂肪酸可藉由水解來自植物和動物來源的甘油醋 151284.doc -167- 201117722 而獲得’並可用蒸餾純化。典型的液體稀釋劑已經描述 在 Marsden，Solvents Guide，2nd Ed.，lnterscience, New46D 46D 48D 49D 50D 51D 52D 53D 54D 55D 56D 57D 58D 59D 60D 61D 62D R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 R1 Yes Br is Me Yes Br is Cl Yes Cl is Cl Yes Br is Br Is Me is Br is Cl is Cl is Cl is Cl is Br is Br is Mer is Br R2 is Cl and (R5)n is 2,6-di-F, R2 is Me and (R5)n is 2,6-two -F R2 is Br and (R5)n is 2,6-di-F, R2 is Me and (R5)n is 2-C1-6-F R2 is Cl and (R5)n is 2-C1-6- F, R2 is Br and (R5)n is 2-C1-6-F, R2 is Me and (R5)n is 2-C1-6-F R2 is Cl and (R5)n is 2-C1-6- F, R2 is Me and (R5)n is 6-C1-6-F R2 is Br and (R5)n is 2-C1-6-F, R2 is Me and (R5)n is 6-C1-2- F R2 is Cl and (R5)n is 6-C1-2-F, R2 is Br and (R5)n is 6-C1-2-F, R2 is Me and (R5)n is 6-C1-2- F R2 is Cl and (R5)n is 6-C1-2-F, R2 is Me and (R5)n is 6-C1-2-F R2 is Br and (R5)n is 6-C1-2-F , 3-Me0(CH2)30. , 3-Me0(CH2)30. 3-Me0(CH2)30. '3-MeNH(CH2)30. 3-MeNH(CH2)30. 3-MeNH(CH2)30. ‘ 3-MeNH(CH2)3〇. 3-MeNH(CH2)30. , 3-MeNH(CH2)30. 3-MeNH(CH2)30. 3-MeNH(CH2)30. 3-MeNH(CH2)30. 3-MeNH(CH2)30. • 3-MeNH(CH2)30. 3-MeNH(CH2)30. , 3-MeNH(CH2)30. 3-MeNH(CH2)30. Formulation / Utility A compound selected from the group consisting of a compound of formula 1, an N-oxide thereof and a salt thereof, or a mixture (ie, a composition) comprising a compound having at least one additional fungicidal compound described in the Summary of the Invention (ie, A fungicide) will be used primarily to provide a fungicidal active ingredient of a further composition, ie a formulation having at least one ingredient selected from the group consisting of surfactants, solid diluents, and liquid dilutions 151284. Doc •163- 201117722 : Body, the biological properties of the active ingredients, the mode of use and the factors such as soil type, humidity and temperature are consistent with the formula or composition. M OU is a compound of at least i-type N_oxide, or a salt thereof) and is divided into (1) (for example, selected from the foregoing (Μ) to (Μ6) and its salts) and/or - or more Many other biologically active compounds or agents (ie, insecticides, other fungicides, nematicides, acaricides, herbicides, and other biological agents) can be formulated in a number of ways, including: (1) Components (a And component (b) and/or one or more other biologically active compounds or agents may be separately formulated and applied separately or simultaneously, for example, in tank mixing; or (ii) component (a). Component (b) and/or one or more other biologically active compounds or agents may be formulated together in suitable weight ratios. Useful formulations include liquid and solid compositions. Liquid compositions include solutions (including emulsions), suspensions, emulsions (including microemulsions and/or suspoemulsions), and the like, and optionally thickened to a condensate. gum. Typical types of aqueous liquid compositions are soluble concentrates, suspension concentrates, capsule suspensions, concentrated emulsions, microemulsions, and suspension emulsions. Typical types of non-aqueous liquid compositions are emulsions, microemulsions, dispersible concentrates and water-dispersible oil dispersions. 151284.doc * 164 - 201117722 The general type of body, 'and 5 things are dusts, powders, pdlets, prills, pastilles, tablets ^ ( Flulledfllms) (including seed coatings), etc., which can be water-jetted ("wettable") or water soluble. Films and coatings formed from film-forming solutions or can be suspended and treated, in particular, the amphoteric component can be encapsulated by (micro)capsules and further formed into a «lw font or solid formulation; or the entire active substance The formula can be encapsulated (or "protected"). Capsules can prevent or slow the release of cohabiting ingredients. The granules combine the advantages of an emulsion formulation with a dry granule formulation. The high strength composition is primarily used as a intermediate for further formulation. The value of the present invention is a composition embodiment in which the granule of a solid composition comprises a compound of formula 1 (or an N-oxide or a salt thereof) and a solid comprising component (b) The granules of the composition are mixed together. These blends can be further mixed with granules including additional agricultural protectants. Alternatively, two or more agricultural protective agents (for example, one component (a) (formula) compound, one component (b) compound, one non-component or agricultural protective agent) may be combined A set of granulated solid compositions which are thereafter combined with one or more sets of granules comprising one or more additional solid compositions of agricultural protective agents. These granulated body mixtures may be identical to the general granulated body mixture disclosed in PCT Patent Publication No. WO 94/24861 or, preferably, the general granules disclosed in the teaching of the same mixture of plasmids of U.S. Patent No. 6,022,552. The mixture is consistent. Sprayable formulations are usually extended in a suitable medium before spraying. Such liquid and solid formulations can be formulated to be easily diluted in a spray 151284.doc -165· 201117722 medium (usually water). The amount sprayed can be from about liters per hectare but more typically from about ten to hundreds of liters per hectare. It can be mixed with water or other suitable medium in the tank, and can be treated by surface application, or the raw and dry formula applied to the plant can be broadcasted (4), directly metered plus 4 streams or Lift the ditch. Liquid and proprietary formulations can be used as seeds for crops and other desired plants, as a pre-seed treatment, / for absorption to protect developing roots and other subterranean plant parts and/or far formulas usually containing an effective amount in the following The active ingredients, diluents and surfactants in the approximate range will add up to one hundred percent by weight. Weight percent active water-dispersible granules and water-soluble granules, tablets and powder ingredients 0.001-90 Thinner 0-99.999 Surfactant 0-15 Water-dispersible oil suspensions, suspensions, emulsions, solutions (including emulsions) 1-50 40-99 〇~5〇Dust 1-25 70-99 〇-5 Fine granule and granule high strength composition 0.001-99 5-99.999 0-15 90-99 0—10 0-2 Solid diluent includes For example, such as bentonite, microcrystalline kaolinite, clay, gypsum, cellulose, oxidized chin, zinc oxide, starch, dextrin, bismuth (such as lactose, sucrose), Vermiculite, talc, mica, diatomaceous earth, urea, calcium carbonate, sodium carbonate and sodium bicarbonate, and sodium sulfate. Typical solid diluents are described in the work of Watkinsetal, 15l284.doc 201117722, Handbook of Insecticide Dust Diluents and Carriers, 2nd Ed., Dorland Books, Caldwell, New Jersey. The liquid diluent comprises, for example, water, N,N-dimercaptoalkylamine (for example, N,N-didecylguanamine), terpene, dimercaptosulfoxide, N-alkylpyrrolidone ( For example, N-mercaptopyrrolidone), ethylene glycol, triethylene glycol, propylene glycol, dipropylene glycol, polypropylene glycol, propylene carbonate, butyl carbonate, chain burned hydrocarbons (eg , white mineral oil, normal paraffin, isoalkane, alkylbenzene, alkylnaphthalene, glycerin, triacetin, sorbitol, triethylene glycol glycerol, aromatic hydrocarbons, dearomatized aliphatic compounds, alkyl Benzene, alkylnaphthalene, ketones such as cyclohexanone, 2-heptanone, isophorone, and 4-pyridyl-4-methyl-2-pentanone, acetate, for example, isoamyl acetate, hexyl acetate, Heptyl acetate, octyl acetate, decyl acetate, tridecyl acetate and isodecyl acetate, other esters such as alkylated lactate esters, dibasic esters and γ-butyrolactone, and alcohols Can be straight, bond, saturated or unsaturated, such as decyl alcohol, ethanol, n-propanol, isopropanol, n-butanol, isobutanol, hexane Alcohol, 2-ethylhexanol, n-octanol, nonanol, isodecyl alcohol, isostearyl alcohol, cetyl alcohol, lauryl alcohol, tridecyl alcohol, oleyl alcohol, cyclohexanol, tetrahydrofurfuryl alcohol, diacetone alcohol and Alkyl alcohol. Liquid diluents also include glycerols of saturated and unsaturated fatty acids (typically C6_C22), such as plant seeds and fruit oils (eg 'olive oil, marijuana, linseed, sesame, corn, peanuts, hollyhocks, grape seeds Oil, safflower, cottonseed, soybean, canola, coconut and palm kernel), animal fat (eg, butter, pork fat, lard, cod liver oil, fish oil) and mixtures thereof. Liquid diluents also include alkylated fatty acids (eg, methylated, ethylated, butylated), wherein the fatty acids are obtained by hydrolyzing glycerin 151284.doc-167-201117722 from plant and animal sources. Purified by distillation. Typical liquid diluents have been described in Marsden, Solvents Guide, 2nd Ed., lnterscience, New

York, 1950。 ’ 本發明的固體和液體組合物通常包括一個或多個 界面活性劑。當加至液體中時，界面活性劑（也經稱為 「表面活性劑」）通常會改變（最常的是減少）液體的 表面張力。根據界面活性劑分子中親水性和親油性基的 性質’界面活性劑可用作為潤濕劑、分散劑、乳化&amp;或 界面活性劑可以分為非離子性、陰離子性或陽 性。對本組合物有用之非離子表面活性劑，其包括作 不限於：酒精烧氧基，例如基於自如及合成的 酒精烧氧基（其可料分核_)以及㈣精以及产 氧5烧、丙烯氧化物、伸丁基氧化物或其混合物所製二 ^于’胺乙氧酸鹽、燒醇酿胺以及乙氧基烧醇酿胺；广 二基化甘油二酯，例如乙氧基黃豆、缝麻以及油菜： 乙=、二壬基苯紛、乙氧酸鹽以及十二燒基:：、 酚類以及環氧乙烷、丙烯氧化物、伸丁 ，化物或其混合物所製備);嵌段聚合 :： 化物製備而來’从反向嵌段聚合物，其= 由丙稀氧化物製傷而得;乙氧基化脂肪酸;= 三桂皮苯齡（包括那些由^甲基貞，乙氧基化 基氧化物或其混合物製備、丙烯氧化物、伸丁 羊毛脂基礎衍生物、旨肪義、甘油醋類、 151284.doc 基酯類，例如聚乙氧基化山York, 1950. The solid and liquid compositions of the present invention typically comprise one or more surfactants. Surfactants (also known as "surfactants") typically change (and most often reduce) the surface tension of a liquid when added to a liquid. Depending on the nature of the hydrophilic and lipophilic groups in the surfactant molecule, the surfactant can be used as a wetting agent, dispersant, emulsification &amp; or surfactant to be classified as nonionic, anionic or positive. Nonionic surfactants useful in the present compositions include, but are not limited to, alcoholic alkoxy groups, such as alcohol-based alkoxy groups based on free and synthetic (which can be deuterated) and (iv) fine and oxygen-producing 5, propylene An oxide, a butyl oxide or a mixture thereof, prepared from an amine oxyacid salt, an oxy-alcoholic amine, and an ethoxylated alcoholic amine; a broad-based diglyceride, such as an ethoxylated soybean, Sesame and rapeseed: B =, dimercaptobenzene, ethoxylate and dodecapine::, phenols and ethylene oxide, propylene oxide, butyl, or mixtures thereof; Stage polymerization:: The compound is prepared from 'inverse block polymer, which is derived from acryl oxide; ethoxylated fatty acid; = tricotyl benzene age (including those from ^ methyl hydrazine, B Preparation of oxylated base oxides or mixtures thereof, propylene oxides, base derivatives of butyl lanolin, glycerides, glycerides, 151284.doc esters, such as polyethoxylated mountains

)C 201117722 乙氣基化甘、、ft聚乙氧基化山梨糖醇脂肪酸酯以及聚 梨醇軒s旨類:旨’·其他山梨醇酐衍生物 ，例如山 段共聚物、♦聚Γ的表面活性劑’例如隨機共聚物、丧 聚合物’乙—醇_、接枝或梳狀聚合物以及星狀 聚石夕4其1乙烯—醇類（pegs);聚乙二醇脂肪酸醋； 類，表面活性劑；以及糖衍生物，例如綱 儿暴多糖苷以及烷基多醣。 基；^用的陰離子表面活性劑，包括，但不限於：烧芳 酸:二以及其鹽類；幾化醇或烧基紛乙氧酸鹽；聯苯績 二·-订生物；木質素以及木質素衍生物，例如木質磺酸 順丁缔二酸或琥珀酸或其酐；烯烴磺酸鹽；磷酸鹽 酉曰類’例如酒精的磷酸鹽酯類，烷基酚的磷酸鹽酯類以 及笨乙烯基苯酚聚氧乙烯醚的磷酸鹽酯類；蛋白質基礎 表面活性劑；肌胺酸衍生物；酚醚硫酸鹽；油及脂肪酸 之磺酸鹽以及硫酸鹽；乙氧基烷基酚之磺酸鹽以及硫酸 鹽；醇之硫酸鹽；乙氧基醇之硫酸鹽；胺類以及醯胺之 續酸鹽’例如n，n-烷牛磺酸酯；苯、異丙苯、曱苯、 茬，以及十二烷基苯及十三烷基苯；濃縮萘的磺酸鹽； 萘以及烷基萘的磺酸鹽；分餾石油的磺酸鹽；磺琥珀醯 胺酸鹽；以及橫琥珀酸鹽以及其衍生物，例如二烧基磺 基琥珀酸酯鹽類。 有用之陽離子表面活性劑，包括，但不限於：醯胺 以及乙氧基醯胺；胺類’例如Ν·烷基丙二胺、三丙烯 二胺以及二丙烯四胺、以及乙氧基胺類、乙氧基二胺以 及丙氧基胺類（從胺類以及環氧乙烷、丙烯氧化物、伸 丁基氧化物及其混合物製備）；胺鹽，例如胺醋酸以及 151284.doc -169- 201117722 二胺鹽類；四級氨鹽，例如四級鹽類、乙氧基四級鹽類 以及雙四級鹽類；以及胺氧化物，例如烷二曱胺氧化物 以及雙-(2-羥乙基)-烷基胺氧化物。 可用於本發明組合物的還有非離子界面活性劑與 陰離子界面活性劑的混合物，或是非離子界面活性劑與 陽離子界面活性劑的混合物。非離子、陰離子以及陽離 子表面活性劑，以及其使用建議在許多的出版參考文獻 中已經揭露，包括 McCutcheon’s Emulsifiers and Detergents, annual American and International Editions published by McCutcheon’s Division，The Manufacturing Confectioner Publishing Co. ; Sisely and Wood, Encyclopedia of Surface Active Agents, Chemical Publ.C 201117722 Ethylene-based glycan, ft polyethoxylated sorbitan fatty acid ester and polysorbate Xuan s intended: 'Other sorbitan derivatives, such as mountain copolymer, ♦ poly Surfactant 'for example, a random copolymer, a damaging polymer 'e-alcohol _, a graft or comb polymer, and a stellate polyglycol 4 1 ethylene-alcohol (pegs); a polyethylene glycol fatty acid vinegar; Classes, surfactants; and sugar derivatives, such as the genus polyglycosides and alkyl polysaccharides. Anionic surfactants, including, but not limited to, succinic acid: two and its salts; polyhydric alcohols or alkyl ethoxylates; biphenyl bismuth--scheduled organisms; lignin and Lignin derivatives, such as lignin sulfosuccinate or succinic acid or anhydrides thereof; olefin sulfonates; phosphate oximes such as phosphate esters of alcohols, phosphate esters of alkyl phenols and stupid Phosphate esters of vinyl phenol ethoxylates; protein based surfactants; creatinine derivatives; phenol ether sulfates; sulfonates and sulfates of oils and fatty acids; sulfonic acid ethoxylated alkyl phenols Salts and sulfates; sulfates of alcohols; sulfates of ethoxylated alcohols; amines and hydrochlorides of guanamines such as n, n-alkyl taurates; benzene, cumene, toluene, hydrazine, And laurylbenzene and tridecylbenzene; sulfonate of concentrated naphthalene; sulfonate of naphthalene and alkylnaphthalene; fractionated petroleum sulfonate; sulfosuccinamide; and trans-succinate and Its derivatives, such as dialkyl sulfosuccinate salts. Useful cationic surfactants, including, but not limited to, decylamine and ethoxylated decylamine; amines such as hydrazine alkyl propylene diamine, tripropylene diamine, and dipropylene tetramine, and ethoxy amines , ethoxydiamines and propoxyamines (prepared from amines and ethylene oxide, propylene oxides, butyl oxides and mixtures thereof); amine salts such as amine acetic acid and 151284.doc -169- 201117722 Diamine salts; fourth-grade ammonium salts, such as quaternary salts, ethoxylated quaternary salts, and quaternary salts; and amine oxides such as alkanediamine oxides and bis-(2-hydroxyl Ethyl)-alkylamine oxide. Also useful in the compositions of the present invention are mixtures of nonionic surfactants with anionic surfactants, or mixtures of nonionic surfactants with cationic surfactants. Nonionic, anionic, and cationic surfactants, as well as their use recommendations, have been disclosed in numerous published references, including McCutcheon's Emulsifiers and Detergents, annual American and International Editions published by McCutcheon's Division, The Manufacturing Confectioner Publishing Co.; Sisely and Wood. , Encyclopedia of Surface Active Agents, Chemical Publ.

Co.，Inc.，New York，1964; and A S. Davidson and B. Milwidsky, Synthetic Detergents, Seventh Edition, John Wiley and Sons, New York, 1987。 本發明組合物亦可包含製劑輔助物及添加劑，及本 技藝中熟知之製劑助劑（其中部分亦可視為提供固體稀 釋劑、液體稀釋液或界面活性劑之功能）。這些配方辅 劑以及添加劑可能防治：pH (緩衝溶液）、處理過程中 的發泡（防止這些聚有機石夕氧烧發泡）、活性成份的沉 積（懸浮劑）、黏滯性（觸變增稠劑）、容器中之微生物 生長（抗菌劑）、產物的凍結（抗凍劑）、染色（染劑/ 顏料分散劑）、洗除（成膜劑或黏著劑）、蒸發（蒸發延 緩劑）、以及其他配方特性。成膜劑包括例如聚乙酸乙 烯、聚乙酸乙烯共聚物、聚乙烯吡咯烷酮·乙酸乙烯共 聚物、聚乙烯醇、聚乙烯醇共聚物及蠟。配方輔劑以及 151284.doc Ί70- 201117722 添加劑的實例，包含那些列於]VIcCutcheon’s Volume 2 : Functional Materials, annual International and NorthCo., Inc., New York, 1964; and A S. Davidson and B. Milwidsky, Synthetic Detergents, Seventh Edition, John Wiley and Sons, New York, 1987. The compositions of the present invention may also contain formulation aids and additives, as well as formulation auxiliaries well known in the art (some of which may also be considered to provide a function as a solid diluent, liquid diluent or surfactant). These formulation adjuvants and additives may be controlled: pH (buffer solution), foaming during processing (preventing these polyorganisms, foaming), deposition of active ingredients (suspension), viscosity (thixotropy) Thickener), microbial growth in containers (antibacterial agents), freezing of products (antifreeze), dyeing (dye/pigment dispersant), washing (film former or adhesive), evaporation (evaporation retardant) And other recipe features. Film formers include, for example, polyvinyl acetate, polyvinyl acetate copolymers, polyvinylpyrrolidone-vinyl acetate copolymers, polyvinyl alcohol, polyvinyl alcohol copolymers, and waxes. Formulation adjuvants and examples of additives 151284.doc Ί70- 201117722, including those listed in] VIcCutcheon’s Volume 2 : Functional Materials, annual International and North

American editions published by McCutcheon，s Division， The Manufacturing Confectioner Publishing Co.;以及 PCT公開號WO 03/024222其中之實例。 式1的化合物以及任何其他活性物質經典型地整 合進目前的組合物中，藉由在溶劑中溶解活性成分或在 一液體或乾性稀釋劑中磨碎。藉由簡單混合成分可製備 出液劑，包括乳劑。若打算用作為乳劑的液體組合物之 溶劑與水不互溶，則通常會在用水稀釋時，加入乳化劑 以乳化該含活性成分之溶劑。使用介質研磨機濕磨粒子 直徑達到2,000 μιη的活性成分漿體，以獲得平均直徑 在3 μιη以下的粒子。含水漿體可製成成品水懸劑（參 見如U.S. 3,060,084)或藉由喷霧乾燥進一步加工成水 分散粒劑。乾配方通常需要乾磨製程，其產生的平均粒 子直徑在2到10 μιη的範圍内。粉塵及粉末製備方式係 採取摻合，且通常加上研磨（如以錘磨或液能研磨機）。 細粒及顆粒製備方式則透過將活性材料喷灑於預先形 成之粒狀載體或以黏聚技術製成。見Browning， “Agglomeration”，Chemical Engineering, December 4, 1967, pp 147-48, Perry’s Chemical Engineer’s Handbook, 4th Ed.，McGraw-Hill, New York，1963, 8-57 頁以及之 後，以及WO 91/13546。微丸劑可以經製備如U.S. 4,172,714所述。水分散性以及水溶性粒狀體可以經製 備如 U.S. 4,144,050、U.S. 3,920,442 以及 DE 3,246,493 所教示。片劑可以經製備如U.S. 5，180,587、U.S. 151284.doc -171 - 201117722 5,232,701以及U.S. 5,208,030所教示。膜料可以經製備 如 GB 2,095,558 以及 U.S. 3,299,566 所教示。 有關製劑技術之進一步資訊，見T. S. Woods，“The Formulator’s Toolbox - Product Forms for Modern Agriculture” in Pesticide Chemistry and Bioscience，The Food-Environment Challenge, T. Brooks 和 T. R. Roberts， Eds., Proceedings of the 9th International Congress on Pesticide Chemistry, The Royal Society of Chemistry, Cambridge，1999, pp· 120-133。亦請參見 U.S. 3,235,361， Col. 6第16行至Col. 7第19行與實例10-41 ; U.S. 3,309，192, Col. 5,第 43 行至 Col. 7 第 62 行及實例 8、 12、15、39、4卜 52、53、58、132、138-140、162-164、 166、167 及 169-182 ; U.S. 2,891,855, Col. 3 第 66 行至 Col. 5 第 217 行及實例 1-4 ; Klingman，Weed Control as a Science, John Wiley and Sons, Inc., New York, 1961, pp 81-96 ； Hance et al., Weed Control Handbook, 8th Ed., Blackwell Scientific Publications, Oxford, 1989 ;及 Developments in formulation technology, PJB Publications，Richmond, UK, 2000。 在下面的實例中，所有的百分比均為按重量計且所 有的配方均以常規方式製備。化合物號碼則參照索引表 A中的化合物。即使沒有進一步的闡述，相信使用上述 說明的熟習該領域之技藝人士仍能夠最大程度地利用 本發明。因此，以下實例僅為說明之用，而絕非用於限 制本發明之揭露内容。除非另有說明，百分比為按重量 計。 151284.doc •172· 201117722 實例A 高強度濃縮物 化合物517 49.3% 吡噻菌胺 49.2% 矽氣凝膠 0.5% 合成的非晶質細緻矽石 1.0% 實例B 可濕性粉末 化合物536 43.0% 快諾芬 22.0% 十二烷笨酚聚乙二醇醚 2.0% 鈉木素磺酸鹽 4.0% 鈉化矽鋁鹽 6.0% 微晶高嶺石（煆燒） 23.0% 實例c 細粒 化合物525 7.5% 依普座 2.5% 厄帖浦石粒狀體（低揮發物， 0.71/0.30 mm ； U.S. S. No. 25-50 β ) 90.0% 壓出顆粒 實例D 化合物529 8.0% 葚孢菌素 17.0% 無水硫酸鈉 10.0% 原油鈣木素磺酸鹽 5.0% 鈉烷基萘磺酸 1.0% 鈣/鎂漿土 59.0% 151284.doc • 173- 201117722American editions published by McCutcheon, s Division, The Manufacturing Confectioner Publishing Co.; and PCT Publication No. WO 03/024222, examples thereof. The compound of Formula 1 and any other active substance are classically incorporated into the present compositions by dissolving the active ingredient in a solvent or by grinding in a liquid or dry diluent. The liquid preparation, including the emulsion, can be prepared by simply mixing the ingredients. If the solvent of the liquid composition intended to be used as an emulsion is immiscible with water, an emulsifier is usually added to dilute the solvent containing the active ingredient when diluted with water. The active ingredient slurry having a diameter of 2,000 μm was wet-milled using a media mill to obtain particles having an average diameter of 3 μηη or less. The aqueous slurry can be made into a finished aqueous suspension (see, e.g., U.S. 3,060,084) or further processed into a water-dispersible granule by spray drying. Dry formulations typically require a dry milling process which produces an average particle diameter in the range of 2 to 10 μηη. Dust and powder preparation methods are blended and usually added with grinding (e.g., with a hammer or liquid energy mill). The fines and granules are prepared by spraying the active material onto a pre-formed granular carrier or by cohesive techniques. See Browning, "Agglomeration", Chemical Engineering, December 4, 1967, pp 147-48, Perry's Chemical Engineer's Handbook, 4th Ed., McGraw-Hill, New York, 1963, pages 8-57 and later, and WO 91/13546 . Pellets can be prepared as described in U.S. Patent 4,172,714. The water-dispersible and water-soluble granules can be prepared as described in U.S. Patent No. 4,144,050, U.S. Tablets can be prepared as described in U.S. Patent No. 5,180,587, U.S. Pat. The film material can be prepared as taught in GB 2,095,558 and U.S. Patent 3,299,566. For further information on formulation technology, see TS Woods, "The Formulator's Toolbox - Product Forms for Modern Agriculture" in Pesticide Chemistry and Bioscience, The Food-Environment Challenge, T. Brooks and TR Roberts, Eds., Proceedings of the 9th International Congress On Pesticide Chemistry, The Royal Society of Chemistry, Cambridge, 1999, pp. 120-133. See also US 3,235,361, Col. 6 line 16 to Col. 7 line 19 and example 10-41; US 3,309,192, Col. 5, line 43 to Col. 7 line 62 and examples 8, 12, 15, 39, 4, 52, 53, 58, 132, 138-140, 162-164, 166, 167, and 169-182; US 2,891,855, Col. 3 Line 66 to Col. 5 Line 217 and Example 1- 4; Klingman, Weed Control as a Science, John Wiley and Sons, Inc., New York, 1961, pp 81-96; Hance et al., Weed Control Handbook, 8th Ed., Blackwell Scientific Publications, Oxford, 1989; Developments in formulation technology, PJB Publications, Richmond, UK, 2000. In the examples below, all percentages are by weight and all formulations are prepared in a conventional manner. For compound numbers, refer to the compounds in Index Table A. Even without further elaboration, it is believed that those skilled in the art using the above description will be able to make the most of the invention. Therefore, the following examples are for illustrative purposes only and are not intended to limit the disclosure of the invention. The percentages are by weight unless otherwise stated. 151284.doc •172· 201117722 Example A High-intensity concentrate compound 517 49.3% penthiopyramine 49.2% helium gel 0.5% synthetic amorphous fine vermiculite 1.0% Example B wettable powder compound 536 43.0% Fen 22.0% Dodecane phenol polyglycol ether 2.0% Sodium lignin sulfonate 4.0% Sodium strontium sulphate 6.0% Microcrystalline kaolinite (smoked) 23.0% Example c Fine granules 525 7.5% 依普2.5% ergium granules (low volatiles, 0.71/0.30 mm; USS No. 25-50 β) 90.0% extruded particles Example D Compound 529 8.0% Fusarium 17.0% anhydrous sodium sulfate 10.0% Crude oil calcium lignin sulfonate 5.0% sodium alkyl naphthalene sulfonic acid 1.0% calcium / magnesium pulp 59.0% 151284.doc • 173- 201117722

實例E 化合物520 5.0% 亞托敏 5.0% 聚氧乙稀山梨糖醇hexoleate 20.0% C6-C10脂肪酸甲酯 70.0% 實例F 微乳液 化合物516 3.3% 咬氧菌酯 1.7% 聚乙烯吡咯烷酮乙烯基醋酸鹽共聚物 30.0% 烷基聚葡萄糖苷 30.0% 單油酸甘油S旨 15.0% 水 20.0% 實例G 種子處理 化合物526 4.00% 異菌脲 16.00% 聚乙烯吡咯烷酮乙烯基醋酸鹽共聚物 5.00% 褐煤蠟酸蠟 5.00% 鈣木素磺酸鹽 1.00% 聚氧乙烯/聚氧丙烯嵌段共聚物 1.00% 硬脂醇（P0E 20) 2.00% 聚有機矽烷 0.20% 著色劑紅色素 0.05% 水 65.75% 151284.doc -174- 201117722 通常在施用前，會將那些在配方表中的配方以水稀 釋以形成含水組合物。水性組合物用以直接應用於植物 或其部分組織（例如，噴灑槽組合物）典型地包括至少 約1 ppm或更多（例如，從1 ppm到100 ppm )的殺真 菌有效化合物，其根據本發明所示。 組分（b)殺真菌化合物的實例（即殺真菌劑）包 括阿拉酸式苯-S-甲基、殺螟丹、辛唑嘧菌胺、吲唑磺 菌胺、敵菌靈、阿扎康唑、亞托敏、本達樂、本達樂-M、 麥鏽靈、苯菌靈、苯噻菌胺、苯噻菌胺-異丙基、貝殺 新、百蟎克、聯苯、比多農、百殺芬、保米黴素、白克 列、溴克座、布瑞莫、萎鏽靈、加普胺、四氣丹、卡普 坦、多菌靈、氯甲氧苯、百菌清、克氣得、克霉π坐、銅 鹽，例如波多混合液（三元硫酸銅）、銅氫氧化物以及 銅氧氯化物、氰霜唑、環氟菌胺、霜脲氰、環克座、賽 普洛、抑菌靈、雙氯氰菌胺、達滅淨、氯硝胺、乙黴威、 待克利、氟嘧菌胺、二曱嘧酚、達滅芬、醚菌胺、達克 利、達克利-Μ、敵蟎普、二噻農、嗎菌靈、多果定、護 粒松、烯肟菌酯、依普座、噻唑菌胺、依瑞莫、依得利、 凡殺同、咪唑菌酮、芬瑞莫、芬克座、曱呋醯胺、環醯 菌胺、氰菌胺、半種咯、苯鏽啶、丁苯嗎啉、芬派殺、 三苯醋錫、三苯氣錫、三苯羥錫、二甲胺甲硫羥羰酸鐵、 富米綜、扶吉胺、洛菌酯、氟酿菌胺、氟嗎琳、氟D比菌 胺（亦稱picobenzamid)、氟°比菌醯胺、唾咬草、氟《密 菌酯、氟喹唑、護矽得、氟硫滅、福提泥（2-[[2-氟-5-(三 氟甲基)苯基]硫基]·2_[3-(2-甲氧苯基)-2-四氫噻唑亞基] 乙腈）、福多寧、護汰芬、福批殺、滅菌丹、三乙膦酸 151284.doc -175- 201117722 鋁、麥穗寧、霜靈、福拉比、菲克利、殺紋寧、雙胍鹽、 依滅列、易胺座、雙胍辛胺、碘代丙炔基丁基甲胺酸酯、 種菌嗤、丙基喜樂松、異眺、丙森辞、亞賜圃、異派 來桑、異。塞菌胺、嘉賜黴素、克收欣、鋅猛乃浦、雙块 醯菌胺、代森鐘、滅普寧、氧乙酸基白粉克、滅達樂、 滅達樂-M、滅特座、續菌胺、代森聯殺菌劑、苯氧菌胺、 喊菌胺、滅芬農、邁克尼、那夫梯芬、甲胂鐵銨（甲基 月申酸鐵）、尼瑞莫、辛侧、甲伽胺、賴菌胺、殴 殺斯、f索林酸、惡咪吐、氧化萎鏽靈、經四環素、平 ，座賓克隆、派福芬（Ν·[2_(1，3_二甲基丁基)苯基]巧· 氣比唾_4彻胺）吻㈣胺、披扶座、 2磷^^鹽類、熱必斯、錄菌s|、粉病靈、 =殺=撲克拉、腐黴利、普拔克、普拔克鹽酸鹽 2二鋅、曝啉、丙硫菌唾、百克敏、唑胺 菌Sa坐菌酯、白粉松、防霉丹、裨草芒、比落雄 霉胺、派芬農、百快隆，各尼群、滅蜗猛、:：芬喷 ::基二、赛得先、石夕嗔菌胺、錢唾、 =那芬、四克利、腐絕、赛氣滅、多保淨1 ί芬褐3隆領菌胺、甲二立_、對甲抑菌 維利黴素t λ 致唾、 士鬧二(及瓦务)、乙烯菌核利、代森銼 口闌、座赛胺、N，_f4林氣·3_(:鑫 '森鋅、 151284.doc 土 7(4甲基六氫η比咬小基犯糾三唾[喷= doc Λ m • 176- 201117722 (BAS600)、N_[2-[4-[[3-(4-氯苯基)-2-丙炔_1-基]氧]-3-甲氧苯基]乙基]-3-曱基-2-[(曱磺醯基）胺基]丁醯胺、 N-[2-[4-[[3-(4-氣苯基)-2-丙炔-1-基]氧]-3-曱氧苯基]乙 基]-3-甲基-2-[(乙基硫基)胺基]丁醯胺、2-丁氧基-6-碘基 -3-丙基-4H-1-苯并哌喃-4-酮、3-[5-(4-氯苯基)-2,3-二曱 基-3-異噁唑烷基]吼啶、4-氟苯基N-[l-[[[l-(4-氰基苯基) 乙基]磺醯基]甲基]丙基]胺曱酸鹽、N-[[(環丙基曱氧基) 胺基][6-(二氟甲氧基)-2,3-二氟苯基]亞甲基]苯醯胺α-甲氧亞胺基)-Ν-曱基-2-[[[1·[3-(三氟甲基）苯基]乙氧基] 亞胺基]甲基]苯醯胺、Ν’-[4-[4-氯-3-(三氟曱基）笨氧 基]-2,5-二曱苯基]-N-乙基-N-雙曱脒、N-(4-氣-2-硝基 苯)-N-乙基-4-曱基苯磺醯胺、2-[[[[3-(2,6-二氣苯基)-1-曱基-2-丙烯-1-亞基]胺基]氧]甲基]-α-(曱氧亞胺基)-N-曱基苯乙醯胺、l-[(2-丙烯硫基）羰基]-2-(卜甲基乙 基）-4-(2-甲苯基）-5-胺基-1Η-η比唑-3-酮、乙基-6-辛基 -[1,2,4]***[1，5-小密啶-7-基胺、戊基&gt;^[4-[[[[(1-曱基 -1H-四唑-5-基）苯基亞曱基]胺基]氧]曱基]_2-噻唑基]胺 曱酸鹽以及戊基N-[6-[[[[(l-曱基-1H-四唑-5-基）苯基亞 曱基]胺基]氧]曱基]-2-吼啶基]胺曱酸鹽。值得注意的是 前述列表不包括芬派殺、福批殺、α坐胺菌S旨、。坐菌醋、 派芬農、泰伏勤以及瓦芬耐。 值得注意的，本組合物中的組分（b)之殺真菌化 合物是亞托敏、克收欣、三氟敏、百克敏、β坐胺菌S旨、 唑菌酯、啶氧菌酯、醚菌胺、苯氧菌胺/芬諾米特賓 (fenominostrobin )、多菌靈、百菌清、快諾芬、滅芬農、 派芬農、環氟菌胺、苯鑛σ定、丁苯嗎淋、溴克座、環克 151284.doc -177- 201117722 座、待克利、依普座、芬克座、護矽得、福批殺、菲克 利、種菌唑、滅特座、邁克尼、平克座、普克利、丙氧 喹啉、丙硫菌唑、得克利、滅菌唑、凡殺同、撲克拉、 吡噻菌胺以及白克列（nicobifen)。值得進一步注意的 是前述列表不包括唑胺菌酯、唑菌酯、派芬農以及福批 殺。 一般對於由真菌類植物致病原所造成的植物疾病 (例如，對於植物致病原防治具有較低使用率或較廣的 範圍）以及抗藥性管理之較好的防治是由式1、其N_ 氧化物、或其鹽類的化合物與選自下列群組的殺真菌化 合物之混合：亞托敏、克收欣、三氟敏、百克敏、唑胺 菌酯、唑菌酯、啶氧菌酯、醚菌胺、笨氧菌胺 /fenominostrobin、快諾芬、滅芬農、環氟菌胺、苯鏽啶、 丁苯嗎淋、環克座、待克利、依普座、護矽得、滅特座、 邁克尼、普克利、丙氧喹啉、丙硫菌唑、派芬農、得克 利、滅菌唑、凡殺同以及吡噻菌胺。值得注意的是前述 列表不包括σ坐胺菌酯、°坐菌酯以及派芬農。 本發明的殺真菌組合物中，組分（a)(即至少一種 化合物選自式1化合物、其N_氧化物、以及其鹽類） 以及組分（b)以殺真菌有效劑量存在。組分的重 量比（即一個或更多附加的殺黴化合物）與組分（a) 之重量比一般來說介於約1:3〇〇〇到約3〇〇〇:1，以及更 典型上來說介於約1:5〇〇以及約5〇〇:卜表m列出關於 組分（b)之殺真菌化合物的典翌，更典型以及最典型 的比例範圍。表A1到A27以及ci到C27例示殺真菌 化合物的特殊組合之重量比例。值得注意的組合物，其 151284.doc •178· 201117722 與組分⑴之重量比是從約125:1到約1:125。 由於/、有許夕組分⑴之殺難成分，這些组入 菌類，病原所造成的植物疾病具有特別良 ’。值付進一步注意的組合物，其組分（a)與 組分⑴之重量比是從約25:1到約ι 25，或從約$」 ^ = °熟習此技藝人士可藉由簡單的實驗來輕易的 1比以及對於所欲達成的殺額保護以及控制 靶=之必需的殺真菌化合物之使用比例。很顯然的，在 、、且刀（b)中包含附加的殺真菌化合物可能較單獨使用 組分（a)可擴張對於植物疾病的控制範圍。 特定的混合物（化合物的編號關於在索引表A的化 合物）列於表AbjA27。在表，每個在欄位開 員’、且刀（a)」以及「組分（b)」之下的行特定地揭露 組分（a)，其為化合物⑻，與一個組分⑴殺真菌化 合物。標題「說雜比率」下的項目揭露3個該揭露混 合物中’組分⑴比上組分（a)的具财量百分比。 舉例來說’表A1的第-行揭露—個具有阿拉酸式苯-s_ 甲基之化合物181的混合物，以及列出阿拉酸式苯各 甲基與化合物181之重量比，其為1:1、1:4或1:18。 組分（a) 化合物181 化合物181 化合物181 化合物181 化合物181 組分（b) 拉酸式苯-S-甲基 巴丹 辛唑嘧菌胺 吲唑磺菌胺 敵菌靈 表Α1 1:1 7:1 3:1 1:1 22:1 1:18 4:1 I51284.doc -179- 201117722 化合物181 敵菌靈 2:1 1:2 1 4 化合物181 亞托敏 3:1 1:1 1 3 化合物181 本達樂 1:1 1:2 1 6 化合物181 本達樂-M 1:1 1:3 1 8 化合物181 麥鏽靈 4:1 2:1 1 2 化合物181 免賴得 11:1 4:1 1 1 化合物181 苯噻菌胺 1:1 1:4 1:12 化合物181 異丙基苯噻菌胺 1:1 1:4 1: 12 化合物181 貝殺新 15:1 5:1 2 1 化合物181 百蟎克 15:1 5:1 2 1 化合物181 聯苯基 15:1 5:1 2 1 化合物181 比多農 3:1 1:1 1 2 化合物181 百殺芬 2:1 1:1 1 3 化合物181 保米徽素 1:4 1:12 1:30 化合物181 波爾多混合劑（三元硫酸銅） 45:1 15:1 5 1 化合物181 白克列 4:1 2:1 1 2 化合物181 溴克座 3:1 1:1 1 3 化合物181 布瑞莫 1:3 1:10 1:30 化合物181 敵菌丹 15:1 5:1 2 1 化合物181 克菌丹 15:1 5:1 2 1 化合物181 貝芬替 11:1 4:1 2 1 化合物181 萎銹靈 4:1 2:1 1 2 化合物181 加普胺 3:1 1:1 1 3 化合物181 地茂丹 100:1 35:1 14:1 化合物181 四氣異苯腈 15:1 5:1 2 1 化合物181 克氣得 11:1 4:1 2 1 化合物181 克黴唑 3:1 1:1 1 3 化合物181 氫氧化銅 45:1 15:1 5 1 化合物181 賊性氣氧化銅 45:1 15:1 5 1 化合物181 赛座滅 1:1 1:2 1 6 化合物181 赛芬胺 1:2 1:6 1:24 化合物181 克絕 1:1 1:2 1 5 化合物181 環克座 1:1 1:2 1 6 化合物181 赛普洛 4:1 2:1 1 2 151284.doc -180 - 201117722 化合物181 益發靈 15:1 5:1 2 1 化合物181 雙氯氰菌胺 15:1 5:1 2 1 化合物181 &quot;达菌酮 3:1 1:1 1 3 化合物181 大克爛 15:1 5:1 2 1 化合物181 乙霉威 7:1 2:1 1 2 化合物181 待克利 1:1 1:3 1:12 化合物181 二氟林 15:1 5:1 2:1 化合物181 二曱嘧酚 1:3 1:8 1:30 化合物181 達滅芬 3:1 1:1 1 2 化合物181 醚菌胺 2:1 1:1 1 4 化合物181 達克利 1:1 1:3 1 8 化合物181 達克利-M (達克利-M) 1:1 1:3 1:12 化合物181 白粉克 2:1 1:1 1 3 化合物181 腈硫醌 5:1 2:1 1 2 化合物181 十二環嗎琳 7:1 3:1 1 1 化合物181 多寧 10:1 4:1 2 1 化合物181 護粒松 3:1 1:1 1 3 化合物181 烯肟菌酯 2:1 1:1 1 4 化合物181 依普座 1:1 1:3 1 7 化合物181 坐菌胺 2:1 1:1 1 3 化合物181 依瑞莫（ethirimol) 7:1 3:1 1 1 化合物181 依得利 7:1 2:1 1 2 化合物181 凡殺同 2:1 1:1 1 4 化合物181 **米D坐菌酮 2:1 1:1 1 4 化合物181 芬瑞莫 1:2 1:7 1:24 化合物181 腈苯嗤 1:1 1:3 1:10 化合物181 甲呋醯胺 4:1 1:1 1 2 化合物181 環醯菌胺 10:1 4:1 2 1 化合物181 氰菌胺 15:1 4:1 1 1 化合物181 半種咯 15:1 5:1 2 1 化合物181 苯鏽咬 7:1 2:1 1 1 化合物181 芬普福 7:1 2:1 1 1 化合物181 芬派殺 3:1 1:1 1 3 151284.doc •181 201117722 化合物181 像是三苯醋錫（三苯醋錫）、三 苯氣化錫（三苯氣錫）或三苯經 錫（三苯經錫）的三苯鹽錫 3:1 1 1 化合物181 福美鐵 30:1 10:1 化合物181 富米綜 7:1 2 1 化合物181 扶吉胺 3:1 1 1 化合物181 咯菌酯 2:1 1 1 化合物181 氟醯菌胺 3:1 1 1 化合物181 氟嗎啦 3:1 1 1 化合物181 氟0比菌胺 1:1 1 2 化合物181 氟0比菌醯胺 3:1 1 1 化合物181 唑呋草 37:1 14:1 化合物181 氟嘧菌酯 1:1 1 2 化合物181 氟啥°坐 1:1 1 2 化合物181 護矽得 3:1 1 1 化合物181 氟硫滅 15:1 5 1 化合物181 福提泥 1:1 1 2 化合物181 福多寧 4:1 1 1 化合物181 護汰芬 1:1 1 2 化合物181 福批殺 2:1 1 1 化合物181 福爾培 15:1 5 1 化合物181 福赛得 30:1 12:1 化合物181 苯并咪唑 11:1 4 1 化合物181 呋霜靈 1:1 1 2 化合物181 福拉比 15:1 5 1 化合物181 克熱淨 15:1 5 1 化合物181 菲克利 1:1 1 2 化合物181 殺紋寧 75:1 25:1 化合物181 依滅列 1:1 1 2 化合物181 易胺座 1:1 1 2 化合物181 克熱淨 15:1 4 1 化合物181 碘代丙炔基丁基曱胺酸酯 15:1 5 1 化合物181 種菌唑 1:1 1 2 化合物181 丙基喜樂松 15:1 5 1 •182· 151284.doc 201117722 化合物181 依普同 15:1 5:1 2 1 化合物181 異丙菌胺 2:1 1:1 1 3 化合物181 亞賜圃 45:1 15:1 5 1 化合物181 異派來桑 2:1 1:1 1 3 化合物181 異噻菌胺 2:1 1:1 1 3 化合物181 嘉賜黴素 1:2 1:7 1:24 化合物181 克收欣 2:1 1:1 1 4 化合物181 鋅錳乃浦 22:1 7:1 3 1 化合物181 曼普胺 2:1 1:1 1 4 化合物181 錳乃浦 22:1 7:1 3 1 化合物181 嘧菌胺 6:1 2:1 1 1 化合物181 甲呋醯胺 1:1 1:2 1 6 化合物181 氧乙酸基白粉克 2:1 1:1 1 3 化合物181 滅達樂 1:1 1:2 1 6 化合物181 滅達樂-M 1:1 1:4 1:12 化合物181 葉菌唑 1:1 1:2 1 6 化合物181 滅速克 15:1 5:1 2 1 化合物181 免得爛 15:1 5:1 2 1 化合物181 苯氧菌胺 3:1 1:1 1 3 化合物181 滅芬農 2:1 1:1 1 4 化合物181 邁克尼 1:1 1:3 1 8 化合物181 那夫梯芬 15:1 5:1 2 1 化合物181 鐵甲砷酸銨 15:1 5:1 2 1 化合物181 尼瑞莫 3:1 1:1 1 3 化合物181 辛噻酮 15:1 4:1 1 1 化合物181 甲呋醯胺 1:1 1:2 1 6 化合物181 肟醚菌胺 3:1 1:1 1 3 化合物181 毆殺斯 1:1 1:2 1 6 化合物181 歐索林酸 7:1 2:1 1 2 化合物181 富馬酸惡咪唑 1:1 1:2 1 5 化合物181 氧萎銹靈 4:1 1:1 1 2 化合物181 經四環素 3:1 1:1 1 3 化合物181 彼扶座 15:1 5:1 2 1 化合物181 平克座 1:2 1:6 1: 15 151284.doc -183· 201117722 化合物181 賓克隆 11 :1 4:1 2 1 化合物181 派福芬（N-[2-(l，3-二曱基丁基） 2:1 1:1 1:3 苯基]-5-氟-1，3-二曱基-1H-吡唑 -4-羧醯胺） 化合物181 吡噻菌胺 2 1 1:1 1 3 化合物181 亞磷酸或其鹽類 15:1 6:1 2 1 化合物181 熱必斯 15:1 6:1 2 1 化合物181 咬氧菌酯 1 1 1:2 1 5 化合物181 粉病靈 3 1 1:1 1 3 化合物181 多氧菌素 3 1 1:1 1 3 化合物181 撲殺熱 3 1 1:1 1 3 化合物181 撲克拉 7 1 2:1 1 2 化合物181 撲滅寧 11 :1 4:1 2 1 化合物181 普拔克（propamocarb)或普拔 10:1 4:1 2 1 克鹽酸鹽 (propamocarb-hydrochloride ) 化合物181 普克利 1 1 1:2 1 5 化合物181 曱基鋅乃浦 11:1 4:1 2 1 化合物181 丙氧喹琳 1 1 1:3 1:12 化合物181 硫菌威（prothiocarb ) 3 1 1:1 1 3 化合物181 丙硫菌。坐 1 1 1:2 1 5 化合物181 百克敏 2 1 1:1 1 4 化合物181 唑胺菌酯 2 1 1:1 1 4 化合物181 唾菌酯 2 1 1:1 1 4 化合物181 白粉松 15:1 4:1 1 1 化合物181 防霉丹 4:1 1:1 1 2 化合物181 稗草畏 15:1 4:1 1 1 化合物181 比芬諾 3 1 1:1 1 3 化合物181 嘧霉胺 3 1 1:1 1 2 化合物181 派芬農 2 1 1:1 1 4 化合物181 百快隆 3 1 1:1 1 3 化合物181 石肖0比D各菌素 15:1 5:1 2 1 化合物181 滅蟎猛 15:1 5:1 2 1 化合物181 快諾芬 1 1 1:2 1 6 化合物181 五氣硝苯 15:1 5:1 2 1 151284.doc .184- 201117722 化合物181 矽噻菌胺 2:1 1 1 1:4 化合物181 矽氟唑 1:1 1 2 1:5 化合物181 螺旋胺 5:1 2 1 1:2 化合物181 鏈黴素 3:1 1 1 1:3 化合物181 硫 75:1 25:1 9:1 化合物181 得克利 1:1 1 2 1:5 化合物181 泰伏勤 3:1 1 1 1:3 化合物181 克枯爛 15:1 5 1 2:1 化合物181 四氣硝基苯 15:1 5 1 2:1 化合物181 特比那芬 15:1 5 1 2:1 化合物181 四克利 1:1 1 2 1:5 化合物181 。塞苯咪嗤 11:1 4 1 2:1 化合物181 賽氟滅 3:1 1 1 1:3 化合物181 多保淨 11:1 4 1 2:1 化合物181 甲基多保淨 11:1 4 1 2:1 化合物181 得恩地 37:1 14:1 5:1 化合物181 噻醯菌胺 2:1 1 1 1:3 化合物181 甲基立枯磷 37:1 14 :1 5:1 化合物181 甲苯氟磺胺 15:1 5 1 2:1 化合物181 三°坐酮 1:1 1 2 1:5 化合物181 ***醇 1:1 1 2 1:5 化合物181 三。坐氧化物 15:1 5 1 2:1 化合物181 三賽唑 3:1 1 1 1:3 化合物181 十三嗎淋 7:1 2 1 1:1 化合物181 三氟敏 2:1 1 1 1:4 化合物181 賽福座 3:1 1 1 1:3 化合物181 賽福寧 3:1 1 1 1:3 化合物181 三形醯胺 7:1 2 1 1:2 化合物181 滅菌11 坐 1:1 1 2 1:5 化合物181 稀效嗤 1:1 1 2 1:5 化合物181 維利黴素 3:1 1 1 1:3 化合物181 及瓦芬财（valifenalate (valiphenal)) 2:1 1 1 1:4 化合物181 免克寧 15:1 6:1 2:1 151284.doc - 185- 201117722 化合物181 鋅乃浦 37:1 14:1 5:1 化合物181 福美鋅 37:1 14:1 5:1 化合物181 座赛胺 2:1 1:1 1:4 化合物181 5-氣-6-(2,4,6-三氟苯基)-7-(4-甲 基六氫&quot;比啶-1-基）[1，2,4]*** [l，5-a]°S&gt;^ 1:1 1:2 1:6 化合物181 N-[2-[4-[[3-(4-氣苯基)-2-丙炔 -1-基]氧]-3-甲氧苯基]乙基]-3-曱基-2-[(曱磺醯基)胺基]丁醯胺 2:1 1:1 1:4 化合物181 N-[2-[4-[[3-(4-氣苯基)-2-丙炔 -1-基]氧]-3-曱氧苯基]乙基]-3_ 曱基-2-[(乙基硫基）胺基]丁醯胺 2:1 1:1 1:4 化合物181 2-丁氧基-6-峨基-3-丙基-4H-1· 苯并哌喃-4-酮 1:1 1:3 1:12 化合物181 3-[5-(4-氣苯基)-2,3-二甲基-3-異噁唑啶基]吡啶 3:1 1:1 1:3 化合物181 4-氟苯基N-[l-[[[l-(4-氱苯基）乙 基]磺醯基]曱基]丙基]胺甲酸鹽 2:1 1:1 1:4 化合物181 N-[[(環丙曱氧基)胺基][6-(二氟 曱氧基)-2,3-二氟苯基]亞曱基] 苯醯胺 1:2 1:7 1:24 化合物181 α-[甲氧亞胺基]-N-甲基 -2-[[[1-[3-(三氟甲基）笨基]乙氧 基]亞胺基]曱基]苯醯胺 3:1 1:1 1:3 化合物181 Ν'-[4-[4-氣-3-(三氟曱基）苯氧 基]-2,5-二甲苯基]-N-乙基-N-雙 甲脒 3:1 1:1 1:3 化合物181 N-(4-氣-2-硝基苯)-N-乙基-4-甲 基苯磺酿胺 3:1 1:1 1:3 化合物181 2-[[p-(2,6-二氣苯基)-1-甲基-2-丙烯-1-亞基]胺基]氧]曱 基]-α-(曱氧亞胺基)-N-曱基笨乙 醯胺 3:1 1:1 1:3 化合物181 N-[4-[[[[(l-甲基-1H-四唑-5-基） 苯基亞甲基]胺基]氧]曱基]-2-噻 唑基]胺曱酸戊酯 3:1 1:1 1:3 化合物181 戊基N-[6-[[[[(l-曱基-1H-四唑 -5-基）苯基亞f基]胺基]氧]甲 基]-2-吡啶基]胺甲酸鹽 3:1 1:1 1:3 151284.doc -186· 201117722 (*)組分（b )相對於組分（a)之重量比例。 表A2至A27除了「組分（a)」欄標題係以下列各 組分（a)欄位名稱代替之外，各與上述表A1架構相同。 因此，舉例來說，在表A2中，在「組分（a)」標題下 的項目都意指「化合物292」，以及在表A2之欄標題下 的第一行特定的揭露一個具有阿拉酸式苯-S-甲基的化 合物292之混合物。表A3至A27係類似架構。 表格代號 組分（a)欄位名稱 表格代號 組分（a)欄位名稱 A2 化合物292 A15 化合物524 A3 化合物469 A16 化合物525 A4 化合物513 A17 化合物526 A5 化合物514 A18 化合物527 A6 化合物515 A19 化合物528 A7 化合物516 A20 化合物529 A8 化合物517 A21 化合物530 A9 化合物518 A22 化合物531 A10 化合物519 A23 化合物532 All 化合物520 A24 化合物533 A12 化合物521 A25 化合物534 A13 化合物522 A26 化合物535 A14 化合物523 A27 化合物536 表B1列出說明本發明混合物、組合物及方法之組 分（b)化合物與組分（a)之特定組合。表B1的第一 欄列出特定組分（b)化合物（例如：第一行的「阿拉 酸式苯-S-曱基（acibenzolar-S-methyl)」）。表 B1 的第 二、三和四攔列出通常在應用於農地生長作物時，組分 (b)化合物相對於組分（a)之重量比範圍（例如：阿 •187- 151284.doc 201117722 拉酸式苯-S-甲基相對於組分（a)的重量為「2.1至 1:180」）。因此，例如表B1第一行具體揭露阿拉酸式苯 -S-甲基（acibenzolar-S-methyl)與組分（a )係通常以 重量比介於2:1至1··180之間的比例施用。表B1其餘 行的架構則與其類似。表Β1其餘行的架構則與其類 似。值得注意的是一個列於實施例38中的任一組成分 與列於表Β1且根據表Β1揭露之重量比之組合物的混 合物。表Β1因此對這些組合以一定比例範圍來補充在 表Α1到Α27中揭露的特定比例。 組分（b) 通常 重量比 -------- 更典型 重量比 最典型 重量比 阿拉酸式苯-S-曱基 2:1 至 1:180 1:1 至 1:60 1:1 至 1:18 巴丹 30:1 至 1:3 10:1 至 1:1 7:1 至 1:1 辛唑嘧菌胺（巴斯夫***并嘧 9:1 至 1:18 唑類化合物） 3:1 至 1:6 3:1 至 1:3 吲唑磺菌胺 6:1 至 1:18 2:1 至 1:6 1:1 至 1:6 敵菌靈 ----- 90:1 至 2:1 30:1 至 4:1 22:1 至 4:1 敵菌靈 7:1 至 1:18 2:1 至 1:6 2:1 至 1:4 亞托敏 — 9:1 至 1:12 3:1 至 1:4 3:1 至 1:3 本達樂 4:1 至 1:18 1:1 至 1:6 1:1 至 1:6 本達樂-M 4:1 至 1:36 1:1 至 1:12 1:1 至 1:8 麥鏽靈 Wl 至 1:6 6:1 至 1:2 4:1 至 1:2 免賴得 45:1 至 1:4 15:1 至 1:1 11:1 至 1:1 苯噻菌胺或苯噻菌胺異丙基 2:1 至 1:36 1:1 至 1:12 1:1 至 1:12 貝殺新 15〇:1 至 1:36 50:1 至 1:12 15:1 至 2:1 百蟎克 15〇:1 至 1:36 50:1 至 1:12 15:1 至 2:1 151284.doc -188- 201117722 組分（b) 通常 重量比 更典型 重量比 最典型 重量比 聯笨基 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 比多農 15:1 至 1:5 5:1 至 1:2 3:1 至 1:2 百殺芬 12:1 至 1:9 4:1 至 1:3 2:1 至 1:3 保米黴素 3:1 至 1:90 1:1 至 1:30 1:4 至 1:30 白克列 18:1 至 1:6 6:1 至 1:2 4:1 至 1:2 溴克座 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 布瑞莫 3:1 至 1:90 1:1 至 1:30 1:3 至 1:30 敵菌丹 90:1 至 1:4 30:1 至 1:2 15:1 至 2:1 克菌丹 90:1 至 1:4 30:1 至 1:2 15:1 至 2:1 貝芬替 45:1 至 1:4 15:1 至 1:2 11:1 至 2:1 萎銹靈 18:1 至 1:6 6:1 至 1:2 4:1 至 1:2 加普胺 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 地茂丹 300:1 至 2:1 100:1 至 4:1 100:1 至 14:1 四氣異苯腈 90:1 至 1:4 30:1 至 1:2 15:1 至 2:1 克氯得 45:1 至 1:2 15:1 至 2:1 11:1 至 2:1 克黴唑 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 銅鹽像是波爾多混合液（三元 硫酸銅）、氣氧化銅、硫酸銅 及氫氧化銅 450:1 至 1:1 150:1 至 4:1 45··1 至 5:1 賽座滅 4:1 至 1:18 1:1 至 1:6 1:1 至 1:6 賽芬胺 1:1 至 1:90 1:2 至 1:30 1:2 至 1:24 克絕 6:1 至 1:18 2:1 至 1:6 1:1 至 1:5 環克座 4:1 至 1:18 1:1 至 1:6 1:1 至 1:6 赛普洛 22:1 至 1:9 7:1 至 1:3 4:1 至 1:2 益發靈 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 雙氣氰菌胺 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 σ达菌嗣 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 151284.doc •189- 201117722 組分（b ) 通常 重量比 更典型 重量比 最典型 重量比 大克爛 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 乙霉威 22:1 至 1:9 7:1 至 1:3 7:1 至 1:2 待克利 4:1 至 1:36 1:1 至 1:12 1:1 至 1:12 二氟林 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 二曱嘧酚 3:1 至 1:90 1:1 至 1:30 1:3 至 1:30 達滅芬 9:1 至 1:6 3:1 至 1:2 3:1 至 1:2 醚菌胺 9:1 至 1:18 3:1 至 1:6 2:1 至 1:4 達克利 3:1 至 1:36 1:1 至 1:12 1:1 至 1:8 達克利Μ 3:1 至 1:90 1:1 至 1:30 1:1 至 1:12 白粉克 7:1 至 1:9 2:1 至 1:3 2:1 至 1:3 腈硫醌 15:1 至 1:4 5:1 至 1:2 5:1 至 1:2 十二環嗎琳 30:1 至 1:3 10:1 至 1:1 7:1 至 1:1 多寧 30:1 至 1:2 10:1 至 2:1 10:1 至 2:1 護粒松 30:1 至 1:9 10:1 至 1:3 3:1 至 1:3 烯肟菌酯 9:1 至 1:18 3:1 至 1:6 2:1 至 1:4 依普座 3:1 至 1:36 1:1 至 1:12 1:1 至 1:7 噻唑菌胺 7:1 至 1:9 2:1 至 1:3 2:1 至 1:3 依瑞莫（ethirimol) 30:1 至 1:3 10:1 至 1:1 7:1 至 1:1 依得利 30:1 至 1:9 10:1 至 1:3 7:1 至 1:2 凡殺同 9:1 至 1:18 3:1 至 1:6 2:1 至 1:4 °米α坐菌酿I 6:1 至 1:18 2:1 至 1:6 2:1 至 1:4 芬瑞莫 3:1 至 1:90 1:1 至 1:30 1:2 至 1:24 腈苯唑 3:1 至 1:30 1:1 至 1:10 1:1 至 1:10 甲呋醯胺 18:1 至 1:6 6:1 至 1:2 4:1 至 1:2 環醯菌胺 30:1 至 1:2 10:1 至 2:1 10:1 至 2:1 11菌胺 150:1 至 1:36 50:1 至 1:12 15:1 至 1:1 151284.doc •190- 201117722 組分（b ) 通常 重量比 更典型 重量比 最典型 重量比 半種咯 75:1 至 1:9 25:1 至 1:3 15:1 至 2:1 苯鑛咬 30:1 至 1:3 10:1 至 1:1 7:1 至 1:1 芬普福 30:1 至 1:3 10:1 至 1:1 7:1 至 1:1 三苯鹽錫，像是醋酸鹽、氣化 物或經化物三苯鹽錫 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 福美鐵 300:1 至 1:2 100:1 至 2:1 30:1 至 4:1 富米綜 30:1 至 1:5 10:1 至 1:2 7:1 至 1:2 扶吉胺 22:1 至 1:5 7:1 至 1:2 3:1 至 1:2 咯菌酯 7:1 至 1:12 2:1 至 1:4 2:1 至 1:4 氟醢菌胺 9:1 至 1:6 3:1 至 1:2 3:1 至 1:2 氟嗎琳 9:1 至 1:18 3:1 至 1:6 3:1 至 1:3 氟°比菌胺 3:1 至 1:18 1:1 至 1:6 1:1 至 1:6 氟'比菌醯胺 15:1 至 1:90 5:1 至 1:30 3:1 至 1:3 氣氣菌核利 150·_1 至 2:1 50:1 至 4··1 37·· 1 至 5:1 氟嘧菌酯 4:1 至 1:18 1:1 至 1:6 1:1 至 1:6 氟喧α坐 4:1 至 1:12 1:1 至 1:4 1:1 至 1:4 護矽得 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 氟硫滅 90:1 至 1:2 30:1 至 2:1 15:1 至 2:1 福提泥 7:1 至 1:36 2:1 至 1:12 1:1 至 1:6 福多寧 18:1 至 1:6 6:1 至 1:2 4:1 至 1:2 護汰芬 4:1 至 1:12 1:1 至 1:4 1:1 至 1:4 福批殺 12:1 至 1:9 4:1 至 1:3 2:1 至 1:3 福爾培 90:1 至 1:4 30:1 至 1:2 15:1 至 2:1 福赛得 225:1 至 2:1 75:1 至 5:1 30:1 至 5:1 苯并咪唑 45:1 至 1:4 15:1 至 1:2 11:1 至 2:1 呋霜靈 15:1 至 1:45 5:1 至 1:15 1:1 至 1:6 151284.doc -191 - 201117722 組分（b) 通常 重量比 更典型 重量比 最典型 重量比 福拉比 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 克熱淨或克熱淨 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 菲克利 15:1 至 1:36 5:1 至 1:12 1:1 至 1:5 殺紋寧 225:1 至 2:1 75:1 至 4:1 75:1 至 9:1 依滅列 7:1 至 1:18 2:1 至 1:6 1:1 至 1:5 易胺座 15:1 至 1:36 5:1 至 1:12 1:1 至 1:5 碘代丙炔基丁基曱胺酸酯 (iodocarb) 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 種菌唑 15:1 至 1:36 5:1 至 1:12 1:1 至 1:5 丙基喜樂松 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 依普同 120:1 至 1:2 40:1 至 2:1 15:1 至 2:1 異丙菌胺 9:1 至 1:9 3:1 至 1:3 2:1 至 1:3 亞賜圃 150:1 至 2:1 50:1 至 4:1 45:1 至 5:1 異派來桑 12:1 至 1:9 4:1 至 1:3 2:1 至 1:3 異噻菌胺 12:1 至 1:9 4:1 至 1:3 2:1 至 1:3 嘉賜黴素 7:1 至 1:90 2:1 至 1:30 1:2 至 1:24 克收欣 7:1 至 1:18 2:1 至 1:6 2:1 至 1:4 鋅錳乃浦 180:1 至 1:3 60:1 至 2:1 22:1 至 3:1 曼普胺 6:1 至 1:18 2:1 至 1:6 2:1 至 1:4 錳乃浦 180:1 至 1:3 60:1 至 2:1 22:1 至 3:1 嘧菌胺 18:1 至 1:3 6:1 至 1:1 6:1 至 1:1 甲呋醯胺 7:1 至 1:36 2:1 至 1:12 1:1 至 1:6 氧乙酸基白粉克 7:1 至 1:9 2:1 至 1:3 2:1 至 1:3 滅達樂 15:1 至 1:45 5:1 至 1:15 1:1 至 1:6 滅達樂-M 7:1 至 1:90 2:1 至 1:30 1:1 至 1:12 葉菌唑 3:1 至 1:18 1:1 至 1:6 1:1 至 1:6 151284.doc •192- 201117722 組分（b) 通常 重量比 更典型 重量比 最典型 重量比 滅速克 150:1 至 1:36 50:1 至 1:12 15:1 至 1:1 免得爛 150:1 至 1:36 50:1 至 1:12 15:1 至 1:1 苯氧菌胺 9:1 至 1:12 3:1 至 1:4 3:1 至 1:3 滅芬農 6:1 至 1:12 2:1 至 1:4 2:1 至 1:4 邁克尼 5:1 至 1:26 1:1 至 1:9 1:1 至 1:8 那夫梯芬 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 鐵甲砷酸銨（甲基砷酸鐵） 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 尼瑞莫 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 辛α塞酮 150:1 至 1:36 50:1 至 1:12 15:1 至 1:1 甲呋醯胺 15:1 至 1:45 5:1 至 1:15 1:1 至 1:6 肟醚菌胺 9:1 至 1:12 3:1 至 1:4 3:1 至 1:3 毆殺斯 15:1 至 1:45 5:1 至 1:15 1:1 至 1:6 歐索林酸 30:1 至 1:9 10:1 至 1:3 7:1 至 1:2 富馬酸惡°米峻 15:1 至 1:36 5:1 至 1:12 1:1 至 1:5 氧萎銹靈 18:1 至 1:6 6:1 至 1:2 4:1 至 1:2 經四環素 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 彼扶座 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 平克座 1:1 至 1:45 1:2 至 1:15 1:2 至 1:15 賓克隆 150:1 至 1:2 50:1 至 2:1 11:1 至 2:1 派福芬（N-[2-(l,3-二曱基丁 基）苯基]-5-氟-1,3-二曱基-1Η-吡唑-4-羧醯胺） 12:1 至 1:9 4:1 至 1··3 2:1 至 1:3 吡噻菌胺 12:1 至 1:9 4:1 至 1:3 2:1 至 1:3 亞磷酸及其鹽類 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 熱必斯 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 咬氧菌酯 7:1 至 1:18 2:1 至 1:6 1:1 至 1:5 粉病靈 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 151284.doc -193- 201117722 組分（b) 通常 重量比 更典型 重量比 最典型 重量比 多氧菌素 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 撲殺熱 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 撲克拉 22:1 至 1:4 7:1 至 1:1 7:1 至 1:2 撲滅寧 45:1 至 1:3 15:1 至 1:1 11:1 至 2:1 普拔克或普拔克鹽酸鹽 30:1 至 1:2 10:1 至 2:1 10:1 至 2:1 普克利 4:1 至 1:18 1:1 至 1:6 1:1 至 1:5 甲基鋅乃浦 45:1 至 1:2 15:1 至 2:1 11:1 至 2:1 丙氧喹淋 3:1 至 1:36 1:1 至 1:12 1:1 至 1:12 硫菌威 9:1 至 1:18 3:1 至 1:6 3:1 至 1:3 丙硫菌。坐 6:1 至 1:18 2:1 至 1:6 1:1 至 1:5 百克敏 9:1 至 1:18 3:1 至 1:6 2:1 至 1:4 唑胺菌酯 9:1 至 1:18 3:1 至 1:6 2:1 至 1:4 唑菌酯 9:1 至 1:18 3:1 至 1:6 2:1 至 1:4 白粉松 150:1 至 1:36 50:1 至 1:12 15:1 至 1:1 防霉丹 15:1 至 1:6 5:1 至 1:2 4:1 至 1:2 比芬諾 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 嘧霉胺 30:1 至 1:6 10:1 至 1:2 3:1 至 1:2 派芬農 6:1 至 1:12 2:1 至 1:4 2:1 至 1:4 百快隆 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 硝0比咯菌素 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 滅蟎猛 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 快諾芬 4:1 至 1:18 1:1 至 1:6 1:1 至 1:6 五氣硝苯 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 矽噻菌胺 7:1 至 1:18 2:1 至 1:6 2:1 至 1:4 矽氟唑 15:1 至 1:36 5:1 至 1:12 1:1 至 1:5 螺旋胺 22:1 至 1:4 7:1 至 1:2 5:1 至 1:2 151284.doc -194- 201117722 組分（b) 通常 重量比 更典型 重量比 最典型 重量比 鏈黴素 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 硫 300:1 至 3:1 100:1 至 9:1 75:1 至 9:1 得克利 7:1 至 1:18 2:1 至 1:6 1:1 至 1:5 泰伏勤 100:1 至 1:100 10:1 至 1:10 3:1 至 1:3 克枯爛 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 四氣硝基笨 150:1 至 1:36 50:1 至 1:12 15··1 至 2_1 特比那芬 150:1 至 1:36 50:1 至 1:12 15··1 至 2:1 四克利 15:1 至 1:36 5:1 至 1:12 1:1 至 1:5 噻苯咪唑 45:1 至 1:4 15:1 至 1:2 11:1 至 2:1 賽氟滅 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 多保淨 45:1 至 1:3 15:1 至 2:1 11:1 至 2:1 甲基多保淨 45:1 至 1:3 15:1 至 2:1 11:1 至 2:1 付恩地 150:1 至 1:2 50:1 至 2:1 37:1 至 5:1 噻醯菌胺 12:1 至 1:9 4:1 至 1:3 2:1 至 1:3 甲基立枯磷 150:1 至 1:2 50:1 至 2:1 37:1 至 5:1 甲苯氟磺胺 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 三嗤酮 15:1 至 1:36 5:1 至 1:12 1:1 至 1:5 ***醇 15:1 至 1:36 5:1 至 1:12 1:1 至 1:5 三0坐氧化物 150:1 至 1:36 50:1 至 1:12 15:1 至 2:1 三赛唑 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 十三嗎嚇· 30:1 至 1:3 10:1 至 1:1 7:1 至 1:1 三氟敏 6:1 至 1··18 2:1 至 1:6 2:1 至 1:4 賽福座 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 賽福寧 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 三形醯胺 45:1 至 1:9 15:1 至 1:3 7:1 至 1:2 滅菌嗤 15:1 至 1:36 5:1 至 1:12 1:1 至 1:5 151284.doc •195- 201117722 組分（b ) 通常 重量比 更典型 重量比 最典型 重量比 稀效°坐 15:1 至 1:36 5:1 至 1:12 1:1 至 1:5 維利黴素 150:1 至 1:36 50:1 至 1:12 3:1 至 1:3 及瓦芬财（valifenalate (valiphenal)) 6:1 至 1:18 2:1 至 1:6 2:1 至 1:4 免克寧 120:1 至 1:2 40:1 至 2:1 15:1 至 2:1 鋅乃浦 150:1 至 1:2 50:1 至 2:1 37:1 至 5:1 福美鋅 150:1 至 1:2 50:1 至 2:1 37:1 至 5:1 座赛胺 6:1 至 1:18 2:1 至 1:6 2:1 至 1:4 5-氣-6-(2,4,6-三 1 苯基）-7-(4-甲基六氫吡啶-1-基）[1，2,4]三 。坐[l，5-a]°^ 咬 15:1 至 1:36 5:1 至 1:12 1:1 至 1:6 N-[2-[4-[[3-(4-氣苯基)-2-丙炔 -1-基]氧]-3-曱氧苯基]乙 基]-3-曱基-2-[(甲磺醯基)胺 基]丁醯胺 6:1 至 1:18 2:1 至 1:6 2:1 至 1:4 N-[2-[4-[[3-(4-氣苯基)-2-丙炔 -1-基]氧]-3-曱氧苯基]乙 基]-3-甲基-2-[(乙基硫基)胺 基]丁醯胺 6:1 至 1:18 2:1 至 1:6 2:1 至 1:4 2 - 丁氧基-6-峨-3 -丙基- 4H-1 -苯并派喃_4_酮 3:1 至 1:36 1:1 至 1:12 1:1 至 1:12 3-[5-(4-氣苯基)-2,3-二曱基-3-異17惡°坐咬基]°比咬 15:1 至 1:9 5:1 至 1:3 3:1 至 1:3 4-氟苯基N-[l-[[[l-(4-氰基苯 基）乙基]磺醯基]甲基]丙基]胺 曱酸鹽 6:1 至 1:18 2:1 至 1:6 2:1 至 1:4 N-[[(環丙基曱氧基）胺 基][6-(二氟曱氧基)-2,3-二氟 苯基]亞曱基]苯醯胺 1:1 至 1:90 1:2 至 1:30 1:2 至 1:24 α-[甲氧亞胺基]-N-甲基 -2-[[[1-[3-(三氟甲基）苯基]乙 氧基]亞胺基]甲基]苯醯胺 9:1 至 1:18 3:1 至 1:6 3:1 至 1:3 151284.doc •196· 201117722 組分（b) 通常 重量比 更典型 重量比 最典型 \Γ_Γ/ί ΓΑ 备 —甚讲讨、纪备 --—--- Ϊ重比 二氣 Τ 巷）本氧 基]-2,5-二甲苯基]-1^-乙基-：^- 雙甲脒 15:1 至 1:18 5:1 至 1:6 3:1 至 1:3 N-(4-氣-2-硝笨基)-N-乙基-4- 甲基苯磺醯胺 15:1 至 1:18 5:1 至 1:6 3:1 至 1:3 2-[[[3-(2,6-二氣苯基)-1-曱基 -2-丙烯-1-亞基]胺基]氧]甲 基]-α-(甲氧亞胺基)-N-甲基苯 乙醯胺 9:1 至 1:18 3:1 至 1:6 3:1 至 1:3 N-[4-[[[[(l-甲基-1H-四唑-5-基）苯基亞曱基]胺基]氧]曱 基]-2-噻唑基]胺甲酸戊酯 9:1 至 1_18 --〜--- 3··1 至 1:6 ------ 3:1 至 1:3 Ν·[6-[[[[(1-甲基-1H-四唑-5-基）苯基亞甲基]胺基]氧]甲 基]-2-吡啶基]胺f酸戊酯 9:1 至 1:18 3:1 至 1:6 3:1 至 1:3 如上所述，本發明包括其中之組合物含組分（a) 及⑴之實施例，其中組分⑴包含至少一種來自於 選自（b!)至（b46)之兩群組各一的殺真菌劑。表〇 至C27列出特定混合物（化合物編號參見索引表a中 化合物）以說明實施例，其中組分（b)包括至少一種 來自於選自（M)至（b46)之兩群組各一的殺真菌劑。 在表ci中，於欄標題「組分（a)」及「組分（b)」下 每一行係具體揭露一種組分（a)之混合物，其係化合 物181 ’併有至少兩種組分（b )殺真菌劑。在標題「說 明比例」下的項目依揭露之混合物順序揭露組分（a) 相對於各組分（b)殺真菌劑三種特定重量比。例如， 第一行揭露一種化合物181與環克座（cypr〇c〇naz〇le) 及亞托敏（azoxystrobin)之混合物，並列出1:1:卜2:1:1 151284.doc •197- 201117722 或3.1 · 1的化合物181比環克座（cyproconazole )比亞 托敏（azoxystrobin)之重量比。 表C1 組分（a) 組分（b) 說明實例比例（*) 化合物181 環克座 亞托敏 1:1:1 2:1:1 3:1:1 化合物181 環克座 克收欣 1:1:1 2:1:1 3:1:1 化合物181 環克座 啶氧菌酯 1:1:1 2:1:1 3:1:1 化合物181 環克座 百克敏 1:1:1 2:1:1 3:1:1 化合物181 環克座 唑胺菌酯 1:1:1 2:1:1 3:1:1 化合物181 環克座 唑菌酯 1:1:1 2:1:1 3:1:1 化合物181 環克座 三氟敏 1:1:1 2:1:1 3:1:1 化合物181 環克座 百殺芬 1:1:2 2:1:2 3:1:2 化合物181 環克座 白克列 1:1:2 2:1:2 3:1:2 化合物181 環克座 赛芬胺 1:2:1 2:2:1 3:2:1 化合物181 環克座 氟吡菌醯胺 1:1:2 2:1:2 3:1:2 化合物181 環克座 異派來桑 1:1:2 2:1:2 3:1:2 化合物181 環克座 滅芬農 1:1:2 2:1:2 3:1:2 化合物181 環克座 吡噻菌胺 1:1:2 2:1:2 3:1:2 化合物181 環克座 丙氧喹嚇· 1:1:1 2:1:1 3:1:1 化合物181 環克座 派芬農 1:1:2 2:1:2 3:1:2 化合物181 環克座 快諾芬 1:1:1 2:1:1 3:1:1 化合物181 環克座 先正達 1:1:2 2:1:2 3:1:2 化合物181 環克座 啶氧菌酯 丙氧喹啉 1:1:1:1 2:1:1:1 3:1:1:1 化合物181 環克座 三氟敏 丙氧喹啉 1:1:1:1 2:1:1:1 3:1:1:1 待克利 2:1:1 3:1:1 化合物181 (difenconazole )亞托敏 1:1:1 化合物181 待克利 克收欣 1:1:1 2:1:1 3:1:1 化合物181 待克利 啶氧菌酯 1:1:1 2:1:1 3:1:1 化合物181 待克利 百克敏 1:1:1 2:1:1 3:1:1 化合物181 待克利 唑胺菌酯 1:1:1 2:1:1 3:1:1 化合物181 待克利 。坐菌S旨 1:1:1 2:1:1 3:1:1 151284.doc -198- 201117722 組分（a ) 組分（b ) 說明實例比例 (” 化合物181 待克利 三氟敏 1:1:1 2:1:1 3:1:1 化合物181 待克利 百殺芬 1:1:2 2:1:2 3:1:2 化合物181 待克利 白克列 1:1:2 2:1:2 3:1:2 化合物181 待克利 賽芬胺 1:2:1 2:2:1 3:2:1 化合物181 待克利 氟11比菌醯胺 1:1:2 2:1:2 3:1:2 化合物181 待克利 異派來桑 1:1:2 2:1:2 3:1:2 化合物181 待克利 滅芬農 1:1:2 2:1:2 3:1:2 化合物181 待克利 。比噻菌胺 1:1:2 2:1:2 3:1:2 化合物181 待克利 丙氧淋 1:1:1 2:1:1 3:1:1 化合物181 待克利 派芬農 1:1:2 2:1:2 3:1:2 化合物181 待克利 快諾芬 1:1:1 2:1:1 3:1:1 化合物181 待克利 先正達 1:1:2 2:1:2 3:1:2 化合物181 待克利 啶氧菌酯 丙氧啥琳 1:1:1:1 2:1:1:1 3:1:1:1 化合物181 待克利 三氟敏 丙氧1#琳 1:1:1:1 2:1:1:1 3:1:1:1 化合物181 依普座 亞托敏 1:1:1 2:1:1 3:1:1 化合物181 依普座 克收欣 1:1:1 2:1:1 3:1:1 化合物181 依普座 啶氧菌酯 1:1:1 2:1:1 3:1:1 化合物181 依普座 百克敏 1:1:1 2:1:1 3:1:1 化合物181 依普座 唑胺菌酯 1:1:1 2:1:1 3:1:1 化合物181 依普座 唑菌酯 1:1:1 2:1:1 3:1:1 化合物181 依普座 三氟敏 1:1:1 2:1:1 3:1:1 化合物181 依普座 百殺芬 1:1:2 2:1:2 3:1:2 化合物181 依普座 白克列 1:1:2 2:1:2 3:1:2 化合物181 依普座 賽芬胺 1:2:1 2:2:1 3:2:1 化合物181 依普座 氟吼菌醯胺 1:1:2 2:1:2 3:1:2 化合物181 依普座 異派來桑 1:1:2 2:1:2 3:1:2 化合物181 依普座 滅芬農 1:1:2 2:1:2 3:1:2 化合物181 依普座 °比°塞菌胺 1:1:2 2:1:2 3:1:2 化合物181 依普座 丙氧0i琳 1:1:1 2:1:1 3:1:1 化合物181 依普座 派芬農 1:1:2 2:1:2 3:1:2 化合物181 依普座 快諾芬 1:1:1 2:1:1 3:1:1 化合物181 依普座 先正達 1:1:2 2:1:2 3:1:2 151284.doc -199- 201117722 組分（a) 組分（b ) 說明實例比例 (*) 化合物181 依普座 咬氧菌酯 丙氧011# 1:1:1:1 2:1:1:1 3:1:1:1 化合物181 依普座 三氟敏 丙氧喹琳 1:1:1:1 2:1:1:1 3:1:1:1 化合物181 葉菌唑 亞托敏 1:1:1 2:1:1 3:1:1 化合物181 葉菌唑 克收欣 1:1:1 2:1:1 3:1:1 化合物181 葉菌D坐 啶氧菌酯 1:1:1 2:1:1 3:1:1 化合物181 葉菌唑 百克敏 1:1:1 2:1:1 3:1:1 化合物181 葉菌。坐 唑胺菌酯 1:1:1 2:1:1 3:1:1 化合物181 葉菌唑 α坐菌酯 1:1:1 2:1:1 3:1:1 化合物181 葉菌唑 三氟敏 1:1:1 2:1:1 3:1:1 化合物181 葉菌唑 百殺芬 1:1:2 2:1:2 3:1:2 化合物181 葉菌唑 白克列 1:1:2 2:1:2 3:1:2 化合物181 葉菌唑 赛芬胺 1:2:1 2:2:1 3:2:1 化合物181 葉菌唑 氟吼菌醯胺 1:1:2 2:1:2 3:1:2 化合物181 葉菌峻 異派來桑 1:1:2 2:1:2 3:1:2 化合物181 葉菌'•坐 滅芬農 1:1:2 2:1:2 3:1:2 化合物181 葉菌唑 吡噻菌胺 1:1:2 2:1:2 3:1:2 化合物181 葉菌唑 丙氧喹琳 1:1:1 2:1:1 3:1:1 化合物181 葉菌唑 派芬農 1:1:2 2:1:2 3:1:2 化合物181 葉菌唑 快諾芬 1:1:1 2:1:1 3:1:1 化合物181 葉菌唑 先正達 1:1:2 2:1:2 3:1:2 化合物181 葉菌°坐 啶氧菌酯 丙氧喹琳 1:1:1:1 2:1:1:1 3:1:1:1 化合物181 葉菌唑 三氟敏 丙氧喹嘛 1:1:1:1 2:1:1:1 3:1:1:1 化合物181 邁克尼 亞托敏 1:1:1 2:1:1 3:1:1 化合物181 邁克尼 克收欣 1:1:1 2:1:1 3:1:1 化合物181 邁克尼 咬氧菌酯 1:1:1 2:1:1 3:1:1 化合物181 邁克尼 百克敏 1:1:1 2:1:1 3:1:1 化合物181 邁克尼 唑胺菌酯 1:1:1 2:1:1 3:1:1 化合物181 邁克尼 唑菌酯 1:1:1 2:1:1 3:1:1 化合物181 邁克尼 三氟敏 1:1:1 2:1:1 3:1:1 化合物181 邁克尼 百殺芬 1:1:2 2:1:2 3:1:2 化合物181 邁克尼 白克列 1:1:2 2:1:2 3:1:2 化合物181 邁克尼 赛芬胺 1:2:1 2:2:1 3:2:1 151284.doc •200· 201117722 組分（a) 組分（b ) 說明實例比例 (” 化合物181 邁克尼 氟°比菌醯胺 1:1:2 2:1:2 3:1:2 化合物181 邁克尼 異派來桑 1:1:2 2:1:2 3:1:2 化合物181 邁克尼 滅芬農 1:1:2 2:1:2 3:1:2 化合物181 邁克尼 吡噻菌胺 1:1:2 2:1:2 3:1:2 化合物181 邁克尼 丙氧啥淋 1:1:1 2:1:1 3:1:1 化合物181 邁克尼 派芬農 1:1:2 2:1:2 3:1:2 化合物181 邁克尼 快諾芬 1:1:1 2:1:1 3:1:1 化合物181 邁克尼 先正達 1:1:2 2:1:2 3:1:2 化合物181 邁克尼 咬氧菌酯 丙氧啥琳 1:1:1:1 2:1:1:1 3:1:1:1 化合物181 邁克尼 三氟敏 丙氧啥琳 1:1:1:1 2:1:1:1 3:1:1:1 化合物181 丙硫菌。坐 亞托敏 1:1:1 2:1:1 3:1:1 化合物181 丙硫菌。坐 克收欣 1:1:1 2:1:1 3:1:1 化合物181 丙硫菌嗤 咬氧菌酯 1:1:1 2:1:1 3:1:1 化合物181 丙硫菌D坐 百克敏 1:1:1 2:1:1 3:1:1 化合物181 丙硫菌。坐 唑胺菌酯 1:1:1 2:1:1 3:1:1 化合物181 丙硫菌α坐 唑菌酯 1:1:1 2:1:1 3:1:1 化合物181 丙硫菌唆 三氟敏 1:1:1 2:1:1 3:1:1 化合物181 丙硫菌唾 百殺芬 1:1:2 2:1:2 3:1:2 化合物181 丙硫菌唾 白克列 1:1:2 2:1:2 3:1:2 化合物181 丙硫菌。坐 赛芬胺 1:2:1 2:2:1 3:2:1 化合物181 丙硫菌嗤 氟°比菌醯胺 1:1:2 2:1:2 3:1:2 化合物181 丙硫菌唾 異派來桑 1:1:2 2:1:2 3:1:2 化合物181 丙硫菌'•坐 滅芬農 1:1:2 2:1:2 3:1:2 化合物181 丙硫菌。坐 吡噻菌胺 1:1:2 2:1:2 3:1:2 化合物181 丙硫菌嗤 丙氧喹琳 1:1:1 2:1:1 3:1:1 化合物181 丙硫菌。坐 派芬農 1:1:2 2:1:2 3:1:2 化合物181 丙硫菌嗤 快諾芬 1:1:1 2:1:1 3:1:1 化合物181 丙硫菌β坐 先正達 1:1:2 2:1:2 3:1:2 化合物181 丙硫菌。坐 啶氧菌酯 丙氧喹琳 1:1:1:1 2:1:1:1 3:1:1:1 化合物181 丙硫菌α坐 三氟敏 丙氧啥淋 1:1:1:1 2:1:1:1 3:1:1:1 化合物181 得克利 亞托敏 1:1:1 2:1:1 3:1:1 化合物181 得克利 克收欣 1:1:1 2:1:1 3:1:1 151284.doc •201 - 201117722 組分（a) 組分（b) 說明實例比例（*) 化合物181 得克利 啶氧菌酯 1:1:1 2:1:1 3:1:1 化合物181 得克利 百克敏 1:1:1 2:1:1 3:1:1 化合物181 得克利 唑胺菌酯 1:1:1 2:1:1 3:1:1 化合物181 得克利 唑菌酯 1:1:1 2:1:1 3:1:1 化合物181 得克利 三氟敏 1:1:1 2:1:1 3:1:1 化合物181 得克利 百殺芬 1:1:2 2:1:2 3:1:2 化合物181 得克利 白克列 1:1:2 2:1:2 3:1:2 化合物181 得克利 赛芬胺 1:2:1 2:2:1 3:2:1 化合物181 得克利 氟&quot;比菌醯胺 1:1:2 2:1:2 3:1:2 化合物181 得克利 異派來桑 1:1:2 2:1:2 3:1:2 化合物181 得克利 滅芬農 1:1:2 2:1:2 3:1:2 化合物181 得克利 0比嘆菌胺 1:1:2 2:1:2 3:1:2 化合物181 得克利 丙氧啥咐 1:1:1 2:1:1 3:1:1 化合物181 得克利 派芬農 1:1:2 2:1:2 3:1:2 化合物181 得克利 快諾芬 1:1:1 2:1:1 3:1:1 化合物181 得克利 先正達 1:1:2 2:1:2 3:1:2 化合物181 得克利 啶氧菌酯 丙氧喹啉 1:1:1:1 2:1:1:1 3:1:1:1 化合物181 得克利 三氟敏 丙氧喹琳 1:1:1:1 2:1:1:1 3:1:1:1 (*)依序之組分（a)相對於成分（b)重量比。 表C2至C27除了「組分（a)」棚標題下項目分別 依下列組分（a)欄位名稱代替之外，其餘各以同上述 表C1之方式架構。因此，例如在表C2中，在「組分 (a)」欄標題下項目均列示為r化合物292」，在表C2 欄標題下第一行具體揭露一種化合物292與環克座 (cyproconazole)及亞托敏（azoXyStr〇bin)之混合物， 且化合物292 .環克座：亞托敏的例示重量比為m、 2.1.1及3.1.1。表C3至C27架構類似。 151284.doc -202- 201117722 表格代號 組分（a )搁位名稱 表格代號 組分（a)欄位名稱 C2 化合物292 C15 化合物524 C3 化合物469 C16 化合物525 C4 化合物513 C17 化合物526 C5 化合物514 C18 化合物527 C6 化合物515 C19 化合物528 C7 化合物516 C20 化合物529 C8 化合物517 C21 化合物530 C9 化合物518 C22 化合物531 C10 化合物519 C23 化合物532 C11 化合物520 C24 化合物533 C12 化合物521 C25 化合物534 C13 化合物522 C26 化合物535 C14 化合物523 C27 化合物536 值得注意的是本發明的一個組合物，其包含一個式 1的化合物（或一其N-氧化物或其鹽類），以及至少一 個與式1的化合物具有不同作用位的其他殺真菌化合 物。在此實例中，一個至少一種具有相同控制範圍但不 同作用位的殺真菌化合物組成對於抗藥性管理將有特 別的益處。因此，本發明的一個組合物可優越的包含至 少一種殺真菌活性化合物，其選自於前述由（bl)到 (b46)所組成的群組，其具有相同的控制範圍但不同 的作用位。 組分（a)與組分（b)的組合物可進一步與一個或 多個其他生物活性化合物或藥劑混合，包含殺蟲劑、殺 線蟲劑、殺菌劑、殺蜗劑、除草劑、除草安全劑、生長 調控劑例如昆蟲蜆皮抑製劑以及生根刺激劑、化學滅菌 劑、訊息化學物質、驅轰劑、吸引劑、信息激素、慑食 刺激劑、植物營養素、其他生物活性化合物或昆蟲病原 151284.doc - 203 - 201117722 細菌、病毒或真菌，以形成一多組分殺蟲劑其提供更廣 泛的農業保護範圍。因此本發明亦關於一組合物其包含 一殺真菌有效劑量之組分（a)與組分（b)之混合物與 一生物有效劑量之至少一種附加的生物活性化合物或 藥劑，且可進一步包括至少一種界面活性劑、一種固體 稀釋劑或一種液體稀釋劑。其他生物活性化合物或藥劑 亦可經分別調配於包含至少一個界面活性劑、一個固體 或液體的稀釋劑的組合物之中。關於本發明的組合物， 一個或多個其他生物活性化合物或藥劑可以與組分（a) 以及（b)中的一個或兩者一起調配，以形成一個預混 物，或一個或多個其他生物活性化合物或藥劑可經分別 從組分（a)以及（b)中調配出來，以及該配方在應用 前先行結合（例如，在一個喷灑槽）或是，在使用中時 結合，兩者擇一。 此些生物活性化合物或藥劑的實例，其組分（a ) 及組分（b)的子組合物可經調配如下：殺蟲劑如阿巴 美丁、乙醯曱胺磷、啶蟲脒、亞滅培、愛撕特普羅 (acetoprole )、碳盤、阿蜜多福昧（amidoflumet)、阿 米曲拉、除虫菌素、印楝素、穀硫填、聯苯菊S旨、聯苯 肼酯、必斯其福隆（bistrifluron)、。塞嗓酮、克百威、殺 螟丹、滅蟎猛、溴蟲腈、氟啶脲、氯蟲醯胺、毒死蜱、 曱基毒死蜱、乙酯殺蟎醇、環蟲醯肼、可尼丁、氰特破 (3-溴基小（3-氯-2-«比啶基）-N-[4-氰基-2-曱基 -6-[(methylamino)叛基]苯基]-1Η-°比哇-5-叛醯胺）、丁 氟虫茜s旨、氣氣氮lijs旨、南效氟j氣乱勒s旨、格林奈、精南 效氯氟氰菊酯、高效氯氟氰菊酯、環己錫、氯氰菊酯、 151284.doc -204· 201117722 環丙三氨三啤、溴氰菊酯、丁醚脲、二嗪農、開樂散、 地特靈、除蟎靈、除虫脲、四氟曱醚菊酯、樂果、呋蟲 胺、苯蟲謎、依馬菌素、硫丹、高效氰戊菊酯、乙蟲清、 乙蟎嗤、克線磷、喹蟎醚、苯丁錫氧化物、苯硫威芬硫 克、芬諾克、甲氰菊酯、唑蟎酯、芬化利、芬普尼、氟 尼胺、氟蟲醯胺、護賽寧、氟胺氰菊酯、福翻雅寧 (flufenerim )、氟芬隆、福諾佛（f〇n〇ph〇s )、氣蟲醯肼、 六伏隆、嗟蜗酮、愛美松、新煙驗類（imiCyaf〇s )、益 達胺、因得克、異柳磷、祿芬隆、馬拉硫磷、美派寧、 美氟綜、四聚乙醛、甲胺磷、殺撲磷、納乃得、美賜平、 曱氧滴滴涕、滅芬諾、甲氧苄氟菊酯、久效磷、烯啶蟲 胺、尼权赛、諾伐隆、諾米福馬林（n〇vi£|urnur〇n )、殴 殺滅、對硫磷、對硫磷-曱基、氣菊酯、曱拌磷、裕必 松、益滅松、磷胺、抗蚜威、丙溴磷、丙氟菊酯、克蟎 特、胺丙威、破陸翻不特（pr〇trjfenbute)、派滅淨、〇比 唤氣蟲腈、除蟲菊、畢達本、啶蟲丙醚、皮難福歸納總 (pyrifluquinazon)、吡啶氟美腈、百利普芬、魚藤酮、 魚尼丁、賜托拉、賜諾殺、撕霹靂的可分（spiridicl〇fen )、 螺甲蜗知、螺蟲乙酯、劉州·佛（sulfoxaflor )、硫丙填、 得芬諾、吡蟎胺、伏蟲隆、七氟菊酯、特丁硫磷、殺蟲 威、四氟醚菊酯、赛果培、赛速安、硫歒克、殺蟲單、 脫芬瑞、泰滅寧、唑蚜威、敵百蟲、三福隆；殺線蟲劑 如涕滅威、新煙鹼類（hnicyaf〇s)、毆殺滅及笨線磷； 殺菌劑如鏈黴素；殺蟎劑如三亞蹣、滅蟎猛、乙酯殺蟎 醇、殺蟎劑（Cyen0pyrafen)、三環錫、開樂散、除蟎靈、 乙蟎唑、喹蟎醚、殺蟎錫、甲氰菊酯、唑蟎酯、噻蟎酮、 I51284.doc -205 · 201117722 克蜗特、畢達本及吡蟎胺；及生物藥劑包括昆蟲病原體 細菌’如蘇力菌 aizavvai、蘇力菌（Bacillus thuringiensis subsp. kurstaki)及囊封的蘇力菌δ-内毒素（例如，細胞 冠（Cellcap)、MPV、MPVII);昆蟲病原體黴，如綠色 僵菌，及昆蟲病原體病毒，包括桿狀病毒、核多角體病 毒（NPV)，如美洲棉鈴蟲核型多角體病毒（HzNPV)、 安那葛福核多角體病毒（AfNPV);及顆粒體病毒（GV) 如卷葉蛾顆粒體病毒（CpGV)。 一般參考之農業保護劑（即殺蟲劑、殺真菌劑、殺 線蟲劑、殺蟎劑、除草劑及生物藥劑）包括The Pesticide Manual, 13th Edition, C. D. S. Tomlin, Ed., British Crop Protection Council, Farnham, Surrey, U.K., 2003 and TheExample E Compound 520 5. 0% Atomin 5. 0% polyoxyethylene sorbitol hexoleate 20. 0% C6-C10 fatty acid methyl ester 70. 0% Example F Microemulsion Compound 516 3. 3% oxycephala ester 1. 7% polyvinylpyrrolidone vinyl acetate copolymer 30. 0% alkyl polyglucoside 30. 0% monooleic acid glycerin S. 0% water 20. 0% Example G Seed Treatment Compound 526 4. 00% isourea 16. 00% polyvinylpyrrolidone vinyl acetate copolymer 5. 00% montan wax wax 5. 00% calcium lignin sulfonate 1. 00% polyoxyethylene/polyoxypropylene block copolymer 1. 00% stearyl alcohol (P0E 20) 2. 00% polyorganodecane 0. 20% colorant red pigment 0. 05% water 65. 75% 151284. Doc-174-201117722 Typically, those formulations in the formula list are diluted with water to form an aqueous composition prior to application. The aqueous composition for direct application to a plant or a portion thereof (eg, a spray tank composition) typically includes at least about 1 ppm or more (eg, from 1 ppm to 100 ppm) of a fungicidal effective compound, according to the present invention. The invention is shown. Examples of component (b) fungicidal compounds (ie fungicides) include arsenic acid Benzene-S-methyl, chlorpyrifos, cyfluazin, carbazolam, carbendazim, Azacon Azole, Atmomin, Bendula, Bendula-M, Mai Rustling, Benomyl, Benzolid, Benzolidin-Isopropyl, Bezoxin, Baikeke, Biphenyl, Bis Duo Nong, Baishenfen, Baommycin, Baikelie, Bromo, Bramo, Brassin, Gupamine, Tetra-tan, Captan, Carbendazim, Chloromethoxybenzene, Hundred Bacterial clear, gram gas, ketone π sitting, copper salt, such as a mixture of potassium (tribasic copper sulfate), copper hydroxide and copper oxychloride, cyanosin, cycloflufenamide, cymoxanil, ring Kezu, 赛普洛, bacteriostatic, chloramphenicol, chlorhexidine, chloramine, carbendazim, chlorhexidine, fluzalazine, dipyridamole, daxen, dexamethasone, Dakley, Dakli-Μ, Enemy, Dithianon, carbendazim, Polydatin, Pleurotus ostreatus, enestrobin, Epto, Ethaboxam, Erimene, Edeli, Van Killing, Imidazolidone, Fenrimimo, Fenke, 曱Indoleamine, cycloheximide, cyanamide, saponin, fenpropidin, butyl morpholine, fentanyl, triphenyl vinegar, triphenyl sulphur, triphenyl hydroxy tin, dimethyl methoxide Iron carboxylate, Fumi, gibberellin, tromethamine, flubendiamide, fluocinine, fluoride D bismuth (also known as picobenzamid), fluoropyridinium amide, salivary grass, fluoride Bacteriocin, fluoroquinazole, oxime, fluorosulfuron, fudi mud (2-[[2-fluoro-5-(trifluoromethyl)phenyl]thio]] 2_[3-(2- Oxyphenyl)-2-tetrahydrothiazole subunit] acetonitrile), pentandine, dimethoate, chlorpyrifos, sterilized dan, triethylphosphonic acid 151284. Doc -175- 201117722 Aluminium, Mai Sui Ning, Clining, Furabi, Fickley, Killing Ning, Bismuth Salt, Ignition, Amine, Dioctylamine, Iodopropynylbutyl Methacrylate, Inoculation of sputum, propyl philazone, sputum, propyl sin, sin, sang, and sang. Cefixamide, carnitamicin, kexinxin, zinc mannep, diammonium, daisenzhong, cumin, oxyacetic acid white powder, nectar, halal-M, extant , sulphate, dexamethasone, phenoxystrobin, chlorfenapyr, fentanyl, micney, naftifen, formazan (methyl monthly iron), nyrim, xin Side, methamine, lysine, scorpion, f-sormine, smear, oxidized rust, tetracycline, ping, budbin, pefufen (Ν·[2_(1,3_二) Methyl butyl) phenyl] Qiao · gas than sal _ 4 enamine) kiss (four) amine, pedestal, 2 phosphorus ^ salt, hot bis, bacterium s |, powder disease, = kill = poker Pull, procymidone, plucker, plucker hydrochloride 2 bis zinc, protoporphyrin, prothiophene saliva, baikemin, oxazolamide Sa sinensis, white pine, anti-mildew, valerian Compared with the drop maleol, propionin, Baikulong, each nirvana, destroying the fierce, :: Fen spray:: base two, Saide first, aspartame, money saliva, = Nafon, Sikhli , rot, qi qi, more than 1 ί 芬 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 t λ to saliva, 士二二 (and 瓦务), 乙菌核, 代森锉 阑, 赛赛amine, N, _f4林气·3_(: Xin 'sen zinc, 151284. Doc soil 7 (4 methyl hexahydro η than the bite of the small base swearing three saliva [spray = doc Λ m • 176- 201117722 (BAS600), N_[2-[4-[[3-(4-chlorophenyl)) 2-propyne-1-yl]oxy]-3-methoxyphenyl]ethyl]-3-indolyl-2-[(indolyl)amino]butanamine, N-[2- [4-[[3-(4-Phenylphenyl)-2-propyn-1-yl]oxy]-3-indolyloxyphenyl]ethyl]-3-methyl-2-[(ethyl thio Amino]butanamine, 2-butoxy-6-iodo-3-propyl-4H-1-benzopipen-4-one, 3-[5-(4-chlorophenyl) -2,3-dimercapto-3-isoxazole alkyl]acridine, 4-fluorophenyl N-[l-[[[l-(4-cyanophenyl)ethyl]sulfonyl] Methyl]propyl]amine decanoate, N-[[(cyclopropyldecyloxy)amino][6-(difluoromethoxy)-2,3-difluorophenyl]methylene] Phenylguanamine α-methoxyimino)-fluorenyl-fluorenyl-2-[[[1·[3-(trifluoromethyl)phenyl]ethoxy]imino]methyl]phenyl hydrazide ,Ν'-[4-[4-Chloro-3-(trifluoromethyl)phenyloxy]-2,5-diphenylene]-N-ethyl-N-biguanide, N-(4 - gas-2-nitrophenyl)-N-ethyl-4-mercaptobenzenesulfonamide, 2-[[[[3-(2,6-diphenyl)-1-indolyl-2- Propylene-1-ylidene]amino]oxy]methyl]-α-(nonoxyimino)-N-mercaptophenylamine, 1-[(2-propenylthio) Carbonyl]-2-(b-methylethyl)-4-(2-methylphenyl)-5-amino-1Η-η-pyrazol-3-one, ethyl-6-octyl-[1,2,4] Triazole [1,5-small pyridin-7-ylamine, pentyl&gt;^[4-[[[[(1-]-yl-1H-tetrazol-5-yl)phenylarylene]amine Alkyl]oxy]indolyl]_2-thiazolyl]amine decanoate and pentyl N-[6-[[[[(l-indolyl-1H-tetrazol-5-yl)phenylarylene]amine Alkyloxy]indolyl-2-pyridinyl]amine decanoate. It is worth noting that the above list does not include Finnish killing, Foster killing, and A. sinensis. Sputum vinegar, Phenfenong, Taifuqin and Waffenai. It is noted that the fungicidal compound of component (b) in the present composition is atramine, kexinxin, trifluoro-sensitive, baikemin, beta-sodium acetaminophen, pyraclostrobin, picoxystrobin, Ethionamide, phenoxybenzamine/fennominostrobin, carbendazim, chlorothalonil, vinofen, fenfennon, phenanthin, cycloflufenamide, benzene ore, butylbenzene Lin, bromo, ring grams 151284. Doc -177- 201117722 Block, Waiting Klee, Epp, Fink, Guardian, Foster, Fickley, Oxazole, Gator, McKinney, Pink, Pkke, Propoxyquinoline , prothioconazole, dexamethasone, sterilized azole, mortal, poker, pirimipen and nicobifen. It is worth noting that the above list does not include carbazinamide, pyraclostrobin, phenanthrene and chlorpyrifos. Generally, the plant diseases caused by fungal plant pathogens (for example, having a low usage rate or a wide range for plant pathogen control) and the better control of drug resistance management are by Formula 1, and their N_ oxidation. a mixture of a compound, or a salt thereof, with a fungicidal compound selected from the group consisting of azotoxin, kexinxin, trifluoro-sensitive, baikemin, zogolide, pyraclostrobin, picoxystrobin, Ethoxystrobin, phenoxybenzamine/fenominostrobin, vinofenol, fentanyl, cycloflufenamide, fenpropidin, butyl benzoate, cyclazone, holly, yipu, 矽 矽, 灭, McKinney, Puckley, propoxyquinoline, prothioconazole, phenanthrene, dextran, sterilized azole, chlorpyrifos and thifen. It is worth noting that the above list does not include scutellarin, guanosin, and phenanthrene. In the fungicidal composition of the present invention, component (a) (i.e., at least one compound selected from the group consisting of the compound of formula 1, its N-oxide, and salts thereof) and component (b) are present in a fungicidally effective amount. The weight ratio of the components (i.e., one or more additional fungicide compounds) to the weight ratio of component (a) is generally from about 1:3 Torr to about 3 Torr:1, and more typically. Above is about 1:5 〇〇 and about 5 〇〇: Table m lists the typical, most typical and most typical range of ratios for the fungicidal compounds of component (b). Tables A1 to A27 and ci to C27 exemplify the weight ratio of a particular combination of fungicidal compounds. A noteworthy composition, 151284. Doc •178· 201117722 The weight ratio to component (1) is from about 125:1 to about 1:125. Due to the fact that there are catastrophic components of the component (1), these are incorporated into the fungus, and the plant diseases caused by the pathogen are particularly good. A composition for further attention, wherein the weight ratio of component (a) to component (1) is from about 25:1 to about ι 25, or from about $"^ = °, which is familiar to those skilled in the art by simple experimentation. The ratio of the use of the fungicidal compound necessary for the protection of the target and the control of the target is determined. It is apparent that the inclusion of additional fungicidal compounds in the knives (b) may be more restrictive for the control of plant diseases than the use of component (a) alone. The specific mixture (the numbering of the compound with respect to the compound in the index table A) is shown in Table AbjA27. In the table, each row under the column opening ', and the knife (a) and the component (b) specifically exposes component (a), which is compound (8), and one component (1) is killed. Fungal compounds. The item under the heading "Roughness ratio" reveals the financial percentage of 'component (1) to the upper component (a) in the three disclosed mixtures. For example, the first row of Table A1 discloses a mixture of a compound 181 having a phenyl-s-methyl group of araic acid, and a weight ratio of a benzyl group of arlic acid to a compound 181, which is 1:1. , 1:4 or 1:18. Component (a) Compound 181 Compound 181 Compound 181 Compound 181 Compound 181 Component (b) Lactic acid benzene-S-methyl batamine octazolam oxazolamide carbendazim Α 1 1:1 7 :1 3:1 1:1 22:1 1:18 4:1 I51284. Doc -179- 201117722 Compound 181 carbendazim 2:1 1:2 1 4 Compound 181 Atomin 3:1 1:1 1 3 Compound 181 Bunda 1:1 1:2 1 6 Compound 181 Bunda - M 1:1 1:3 1 8 Compound 181 Mai rusting 4:1 2:1 1 2 Compound 181 Freedom 11:1 4:1 1 1 Compound 181 Bethicil 1:1 1:4 1:12 Compound 181 Isopropyl thiazide 1:1 1:4 1: 12 Compound 181 Beast new 15:1 5:1 2 1 Compound 181 Baikeke 15:1 5:1 2 1 Compound 181 Biphenyl 15 :1 5:1 2 1 Compound 181 Bidanon 3:1 1:1 1 2 Compound 181 Baishenfen 2:1 1:1 1 3 Compound 181 Baume Huisu 1:4 1:12 1:30 Compound 181 Bordeaux mixture (tribasic copper sulfate) 45:1 15:1 5 1 Compound 181 White column 4:1 2:1 1 2 Compound 181 Bromogram 3:1 1:1 1 3 Compound 181 Breimo 1: 3 1:10 1:30 Compound 181 Capitamin 15:1 5:1 2 1 Compound 181 Captan 15:1 5:1 2 1 Compound 181 Beffene 11:1 4:1 2 1 Compound 181 Spirit 4:1 2:1 1 2 Compound 181 Gypamine 3:1 1:1 1 3 Compound 181 Dimodan 100:1 35:1 14:1 Compound 181 Tetraisophthalonitrile 15:1 5:1 2 1 Compound 181 g gas obtained 11:1 4:1 2 1 compound 181 clotrimazole 3:1 1:1 1 3 compound 181 copper hydroxide 45:1 15:1 5 1 compound 181 thief gas copper oxide 45:1 15:1 5 1 Compound 181 Racer 1:1 1:2 1 6 Compound 181 Safinamide 1:2 1:6 1:24 Compound 181 克 1:1 1:2 1 5 Compound 181 Ring gram 1 :1 1:2 1 6 Compound 181 Siplow 4:1 2:1 1 2 151284. Doc -180 - 201117722 Compound 181 Yifaling 15:1 5:1 2 1 Compound 181 Diclofenac 15:1 5:1 2 1 Compound 181 &quot;Dactoxone 3:1 1:1 1 3 Compound 181 Large克烂15:1 5:1 2 1 Compound 181 Methanecarb 7:1 2:1 1 2 Compound 181 Waiting Kelly 1:1 1:3 1:12 Compound 181 Diflurane 15:1 5:1 2:1 Compound 181 Dipyridamole 1:3 1:8 1:30 Compound 181 Damethorin 3:1 1:1 1 2 Compound 181 Ethionamide 2:1 1:1 1 4 Compound 181 Dakley 1:1 1: 3 1 8 Compound 181 Dakli-M (Dakli-M) 1:1 1:3 1:12 Compound 181 White powder 2:1 1:1 1 3 Compound 181 Nitrile sulfonium 5:1 2:1 1 2 Compound 181 Twelve Rings Lynch 7:1 3:1 1 1 Compound 181 Doning 10:1 4:1 2 1 Compound 181 Pleurotus ostreatus 3:1 1:1 1 3 Compound 181 Enoxacin 2:1 1: 1 1 4 Compound 181 Eptrix 1:1 1:3 1 7 Compound 181 Coccidia 2:1 1:1 1 3 Compound 181 ethirimol 7:1 3:1 1 1 Compound 181 edeli 7:1 2:1 1 2 Compound 181 Wherein 2:1 1:1 1 4 Compound 181 **M D ketal 2:1 1:1 1 4 Compound 181 Fenrimo 1:2 1:7 1 :24 Compound 181 Benzoquinone 1:1 1:3 1:10 Compound 181 mefenamide 4:1 1:1 1 2 Compound 181 Cyclosporin 10:1 4:1 2 1 Compound 181 Cyanamide 15:1 4:1 1 1 Compound 181 Semi-species 15:1 5:1 2 1 Compound 181 Benzene rust bite 7:1 2:1 1 1 Compound 181 Fenford 7:1 2:1 1 1 Compound 181 Fenpai 3:1 1 :1 1 3 151284. Doc •181 201117722 Compound 181 is like triphenylacetate (triphenyltin), triphenyltin (triphenyltin) or triphenyltin (triphenyltin) triphenyl salt 3:1 1 1 Compound 181 Fame iron 30:1 10:1 Compound 181 Fumi sum 7:1 2 1 Compound 181 Cougiamine 3:1 1 1 Compound 181 Flavulin 2:1 1 1 Compound 181 Fluorizine 3:1 1 1 Compound 181 Fluorine 3:1 1 1 Compound 181 Fluorine 0 bacteriocin 1:1 1 2 Compound 181 Fluorine 0 bismuthamide 3:1 1 1 Compound 181 Oxafura 37:1 14:1 Compound 181 Fluoxacillin 1:1 1 2 Compound 181 Fluorine 啥 Sitting 1:1 1 2 Compound 181 Hydrating 3:1 1 1 Compound 181 Fluorine Sulphur 15:1 5 1 Compound 181 Futi Mud 1:1 1 2 Compound 181 Fodonin 4:1 1 1 Compound 181 Difen 1:1 1 2 Compound 181 Fenicide 2:1 1 1 Compound 181 Forte 15:1 5 1 Compound 181 Forsyth 30:1 12: 1 Compound 181 Benzimidazole 11:1 4 1 Compound 181 Furosemide 1:1 1 2 Compound 181 Furabi 15:1 5 1 Compound 181 gram heat 15:1 5 1 Compound 181 Fickley 1:1 1 2 Compound 181 Killing Ning 75:1 25:1 Compound 181 SEQ ID NO: 1:1 1 2 Compound 181 Easy amine 1:1 1 2 Compound 181 gram heat 15:1 4 1 Compound 181 Iodopropynyl butyl phthalate 15:1 5 1 Compound 181 Inosine 1:1 1 2 Compound 181 propyl chelsson 15:1 5 1 •182· 151284. Doc 201117722 Compound 181 Ep 15:1 5:1 2 1 Compound 181 Isoprofen 2:1 1:1 1 3 Compound 181 Affluent 45:1 15:1 5 1 Compound 181 Isolate 2: 1 1:1 1 3 Compound 181 Isotianil 2:1 1:1 1 3 Compound 181 Catherine 1:2 1:7 1:24 Compound 181 Gram 2:1 1:1 1 4 Compound 181 Zinc Manganese 22:1 7:1 3 1 Compound 181 Manpamine 2:1 1:1 1 4 Compound 181 Manganese 22:1 7:1 3 1 Compound 181 Azoxystrobin 6:1 2:1 1 1 Compound 181 mesofuramide 1:1 1:2 1 6 Compound 181 Oxyacetic acid based white powder 2:1 1:1 1 3 Compound 181 Destroy 1:1 1:2 1 6 Compound 181 Destroy-M 1:1 1:4 1:12 Compound 181 Xanthomol 1:1 1:2 1 6 Compound 181 Desiccant 15:1 5:1 2 1 Compound 181 Free rotten 15:1 5:1 2 1 Compound 181 Benzene Oxystrobin 3:1 1:1 1 3 Compound 181 Defenfen 2:1 1:1 1 4 Compound 181 McNea 1:1 1:3 1 8 Compound 181 Naftifen 15:1 5:1 2 1 Compound 181 Ammonium iron arsenate 15:1 5:1 2 1 Compound 181 Nerimo 3:1 1:1 1 3 Compound 181 Octyl ketone 15:1 4:1 1 1 Compound 181 Mesofuramide 1:1 1:2 1 6 Compound 181 Epothilone 3:1 1:1 1 3 Compound 181 殴 斯 1:1 1:2 1 6 Compound 181 Oxalolin 7:1 2:1 1 2 Compound 181 Fumar Acid imidazole 1:1 1:2 1 5 Compound 181 Oxygen rust 4:1 1:1 1 2 Compound 181 Tetracycline 3:1 1:1 1 3 Compound 181 Pituitary 15:1 5:1 2 1 Compound 181 gram seat 1:2 1:6 1: 15 151284. Doc -183· 201117722 Compound 181 Bin clone 11 :1 4:1 2 1 Compound 181 Penfufen (N-[2-(l,3-dimerylbutyl) 2:1 1:1 1:3 phenyl ]-5-fluoro-1,3-dimercapto-1H-pyrazole-4-carboxyguanamine) Compound 181 Lapidillin 2 1 1:1 1 3 Compound 181 Phosphorous acid or a salt thereof 15:1 6 :1 2 1 Compound 181 Hotbis 15:1 6:1 2 1 Compound 181 Oxygenate 1 1 1:2 1 5 Compound 181 Powder Disease 3 1 1:1 1 3 Compound 181 Polyoxin 3 1 1:1 1 3 Compound 181 Sweat Heat 3 1 1:1 1 3 Compound 181 Poker Pull 7 1 2:1 1 2 Compound 181 Fighting Ning 11 :1 4:1 2 1 Compound 181 Propamocarb or Propa 10:1 4:1 2 1 g of hydrochloride (propamocarb-hydrochloride) Compound 181 Puckley 1 1 1:2 1 5 Compound 181 Mercapto Zinc Napu 11:1 4:1 2 1 Compound 181 Propoxyquine 1 1 1:3 1:12 Compound 181 Prothiocarb 3 1 1:1 1 3 Compound 181 Propionibacterium. Sit 1 1 1:2 1 5 Compound 181 Bai Kemin 2 1 1:1 1 4 Compound 181 Zymosillus 2 1 1:1 1 4 Compound 181 Sputum 2 1 1:1 1 4 Compound 181 White Pine 15: 1 4:1 1 1 Compound 181 Mold inhibitor 4:1 1:1 1 2 Compound 181 Drosophila 15:1 4:1 1 1 Compound 181 Bifenol 3 1 1:1 1 3 Compound 181 Pyrimethanil 3 1 1:1 1 2 Compound 181 Phenfenone 2 1 1:1 1 4 Compound 181 Baikulong 3 1 1:1 1 3 Compound 181 Shi Xiao 0 to D each bacteriocin 15:1 5:1 2 1 Compound 181螨 螨 15:1 5:1 2 1 Compound 181 Fastin 1 1 1:2 1 6 Compound 181 Five gas benzene 15:1 5:1 2 1 151284. Doc . 184- 201117722 Compound 181 Thiabendamide 2:1 1 1 1:4 Compound 181 Hydrazine 1:1 1 2 1:5 Compound 181 Spiramine 5:1 2 1 1:2 Compound 181 Streptomycin 3:1 1 1 1:3 Compound 181 Sulfur 75:1 25:1 9:1 Compound 181 Dekley 1:1 1 2 1:5 Compound 181 Taifuqin 3:1 1 1 1:3 Compound 181 g rot 15:1 5 1 2:1 Compound 181 Tetranitrobenzene 15:1 5 1 2:1 Compound 181 Tebinafin 15:1 5 1 2:1 Compound 181 Sikhli 1:1 1 2 1:5 Compound 181. Benzene oxime 11:1 4 1 2:1 Compound 181 cyprofen 3:1 1 1 1:3 Compound 181 Multi-purity 11:1 4 1 2:1 Compound 181 Methyl multi-purity 11:1 4 1 2:1 Compound 181 Dean Land 37:1 14:1 5:1 Compound 181 Thiabendamide 2:1 1 1 1:3 Compound 181 Methylphosphorus 37:1 14 :1 5:1 Compound 181 Toluene Fluoride Sulfonamide 15:1 5 1 2:1 Compound 181 Tris-one ketone 1:1 1 2 1:5 Compound 181 Triazole alcohol 1:1 1 2 1:5 Compound 181 III. Sitting oxide 15:1 5 1 2:1 Compound 181 Trimethoazole 3:1 1 1 1:3 Compound 181 Thirteen lining 7:1 2 1 1:1 Compound 181 Trifluoro-sensitive 2:1 1 1 1: 4 Compound 181 Ceflon 3:1 1 1 1:3 Compound 181 Safranine 3:1 1 1 1:3 Compound 181 Triformin 7:1 2 1 1:2 Compound 181 Sterilization 11 Sit 1:1 1 2 1:5 Compound 181 Dilute 嗤1:1 1 2 1:5 Compound 181 Wielimycin 3:1 1 1 1:3 Compound 181 and valifenalate (valiphenal) 2:1 1 1 1: 4 Compound 181 Bian Ning 15:1 6:1 2:1 151284. Doc - 185- 201117722 Compound 181 Zinc Napo 37:1 14:1 5:1 Compound 181 Famine Zinc 37:1 14:1 5:1 Compound 181 Cathamide 2:1 1:1 1:4 Compound 181 5- Gas-6-(2,4,6-trifluorophenyl)-7-(4-methylhexahydro&quot;bipyridin-1-yl)[1,2,4]triazole [l,5-a ]°S&gt;^ 1:1 1:2 1:6 Compound 181 N-[2-[4-[[3-(4-Phenylphenyl)-2-propyn-1-yl]oxy]-3- Methoxyphenyl]ethyl]-3-mercapto-2-[(oxasulfonyl)amino]butanamine 2:1 1:1 1:4 Compound 181 N-[2-[4-[[ 3-(4-Phenylphenyl)-2-propyn-1-yl]oxy]-3-indolyloxyphenyl]ethyl]-3_indolyl-2-[(ethylthio)amino]butyl Indoleamine 2:1 1:1 1:4 Compound 181 2-butoxy-6-mercapto-3-propyl-4H-1·benzopipen-4-one 1:1 1:3 1:12 Compound 181 3-[5-(4-Phenylphenyl)-2,3-dimethyl-3-isoxazolidinyl]pyridine 3:1 1:1 1:3 Compound 181 4-fluorophenyl N- [l-[[l-(4-Phenylphenyl)ethyl]sulfonyl]indolyl]propyl]amine formate 2:1 1:1 1:4 Compound 181 N-[[(cyclopropane曱oxy)amino][6-(difluorodecyloxy)-2,3-difluorophenyl]indenyl]benzamide 1:2 1:7 1:24 Compound 181 α-[methoxy Imino]-N-methyl-2-[[[1-[3-(trifluoromethyl) Styrene]ethoxy]imino]mercapto]benzamide 3:1 1:1 1:3 Compound 181 Ν'-[4-[4-Ga-3-(trifluoromethyl)phenoxy ]-2,5-Dimethylphenyl]-N-ethyl-N-dimethylhydrazine 3:1 1:1 1:3 Compound 181 N-(4-Gas-2-nitrophenyl)-N-ethyl -4-Methylbenzenesulfonamide 3:1 1:1 1:3 Compound 181 2-[[p-(2,6-Diphenyl)-1-methyl-2-propene-1-ylidene Amino]oxy]indolyl]-α-(nonoxyimino)-N-mercaptoethylamine 3:1 1:1 1:3 Compound 181 N-[4-[[[[(l -methyl-1H-tetrazol-5-yl)phenylmethylene]amino]oxy]indolyl]-2-thiazolyl]ammonium decanoate 3:1 1:1 1:3 Compound 181 N-[6-[[[[(l-indolyl-1H-tetrazol-5-yl)phenyl]f-yl]amino]oxy]methyl]-2-pyridyl]amine formate 3 :1 1:1 1:3 151284. Doc -186· 201117722 (*) The weight ratio of component (b) to component (a). Tables A2 to A27 are the same as the above-mentioned Table A1 except that the title of "Component (a)" is replaced by the column names of the following components (a). Thus, for example, in Table A2, the items under the heading "Component (a)" all mean "Compound 292", and the first line under the heading of Table A2 specifically discloses a aralic acid. A mixture of compounds 292 of the formula Benzene-S-methyl. Tables A3 to A27 are similar architectures. Table Code Component (a) Field Name Table Code Component Component (a) Field Name A2 Compound 292 A15 Compound 524 A3 Compound 469 A16 Compound 525 A4 Compound 513 A17 Compound 526 A5 Compound 514 A18 Compound 527 A6 Compound 515 A19 Compound 528 A7 Compound 516 A20 Compound 529 A8 Compound 517 A21 Compound 530 A9 Compound 518 A22 Compound 531 A10 Compound 519 A23 Compound 532 All Compound 520 A24 Compound 533 A12 Compound 521 A25 Compound 534 A13 Compound 522 A26 Compound 535 A14 Compound 523 A27 Compound 536 Table B1 Specific combinations of components of component (b) and component (a) illustrating mixtures, compositions and methods of the invention are set forth. The first column of Table B1 lists the specific component (b) compound (for example, the first row of "acibenzolar-S-methyl"). The second, third and fourth blocks of Table B1 list the weight ratio range of component (b) to component (a), usually applied to agricultural crops (eg: A • 187- 151284. Doc 201117722 The weight of the benzene-S-methyl group relative to the component (a) is "2. 1 to 1:180"). Thus, for example, the first row of Table B1 specifically discloses that acibenzolar-S-methyl and component (a) are usually in a weight ratio of between 2:1 and 1.180. Proportional application. The architecture of the remaining rows in Table B1 is similar. The structure of the remaining rows of Table 1 is similar. Of note is a mixture of any of the components listed in Example 38 and the compositions listed in Table 1 and disclosed in Table 1 by weight ratio. Table 1 therefore supplements these combinations with a certain proportion range to the specific ratios disclosed in Tables 1 to 27. Component (b) Normal weight ratio -------- More typical weight ratio Most typical weight ratio arsenic acid Benzene-S-fluorenyl 2:1 to 1:180 1:1 to 1:60 1:1 To 1:18 Bataan 30:1 to 1:3 10:1 to 1:1 7:1 to 1:1 octazolam (BASF triazolopyrimidine 9:1 to 1:18 azole compound) 3 :1 to 1:6 3:1 to 1:3 Oxazone 6:1 to 1:18 2:1 to 1:6 1:1 to 1:6 Enzyme----- 90:1 To 2:1 30:1 to 4:1 22:1 to 4:1 carbendazim 7:1 to 1:18 2:1 to 1:6 2:1 to 1:4 Atomin - 9:1 to 1:12 3:1 to 1:4 3:1 to 1:3 Bunda 4:1 to 1:18 1:1 to 1:6 1:1 to 1:6 Bunda-M 4:1 to 1:36 1:1 to 1:12 1:1 to 1:8 Wheat Rust Wl to 1:6 6:1 to 1:2 4:1 to 1:2 Freedom 45:1 to 1:4 15 :1 to 1:1 11:1 to 1:1 phenothimethamine or phenothimethamine isopropyl 2:1 to 1:36 1:1 to 1:12 1:1 to 1:12 〇:1 to 1:36 50:1 to 1:12 15:1 to 2:1 Baikeke 15〇:1 to 1:36 50:1 to 1:12 15:1 to 2:1 151284. Doc -188- 201117722 Component (b) Normal weight ratio more typical weight ratio most typical weight ratio 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 Bidan 15: 1 to 1:5 5:1 to 1:2 3:1 to 1:2 Baifenfen 12:1 to 1:9 4:1 to 1:3 2:1 to 1:3 Baumemycin 3:1 To 1:90 1:1 to 1:30 1:4 to 1:30 White Column 18:1 to 1:6 6:1 to 1:2 4:1 to 1:2 Bromo Block 15:1 to 1 :9 5:1 to 1:3 3:1 to 1:3 Bremer 3:1 to 1:90 1:1 to 1:30 1:3 to 1:30 Enemy 90:1 to 1:4 30:1 to 1:2 15:1 to 2:1 Captan 80:1 to 1:4 30:1 to 1:2 15:1 to 2:1 Beffinte 45:1 to 1:4 15: 1 to 1:2 11:1 to 2:1 rusting spirit 18:1 to 1:6 6:1 to 1:2 4:1 to 1:2 gupamine 15:1 to 1:9 5:1 to 1:3 3:1 to 1:3 Dimuda 300:1 to 2:1 100:1 to 4:1 100:1 to 14:1 Four-isophthalonitrile 90:1 to 1:4 30:1 to 1:2 15:1 to 2:1 gram of chlorine 45:1 to 1:2 15:1 to 2:1 11:1 to 2:1 Clotrimazole 15:1 to 1:9 5:1 to 1: 3 3:1 to 1:3 Copper salt is like Bordeaux mixture (tribasic copper sulfate), copper oxide, copper sulfate and copper hydroxide 450:1 to 1: 1 150:1 to 4:1 45··1 to 5:1 Race off 4:1 to 1:18 1:1 to 1:6 1:1 to 1:6 Safinamide 1:1 to 1:90 1:2 to 1:30 1:2 to 1:24 gram 6:1 to 1:18 2:1 to 1:6 1:1 to 1:5 Circus 4:1 to 1:18 1:1 To 1:6 1:1 to 1:6 Cypress 22:1 to 1:9 7:1 to 1:3 4:1 to 1:2 Yifaling 150:1 to 1:36 50:1 to 1: 12 15:1 to 2:1 cyanidin 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 σ达菌嗣15:1 to 1:9 5:1 to 1 :3 3:1 to 1:3 151284. Doc •189- 201117722 Component (b) Normal weight ratio is more typical weight ratio Most typical weight ratio is 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1. 1 to 1:9 7:1 to 1:3 7:1 to 1:2 Waiting for Klee 4:1 to 1:36 1:1 to 1:12 1:1 to 1:12 Teflon 150:1 to 1 :36 50:1 to 1:12 15:1 to 2:1 Dipyridamole 3:1 to 1:90 1:1 to 1:30 1:3 to 1:30 Dafenfen 9:1 to 1: 6 3:1 to 1:2 3:1 to 1:2 Ethionamide 9:1 to 1:18 3:1 to 1:6 2:1 to 1:4 Dakley 3:1 to 1:36 1: 1 to 1:12 1:1 to 1:8 DakliΜ 3:1 to 1:90 1:1 to 1:30 1:1 to 1:12 White powder 7:1 to 1:9 2:1 to 1 :3 2:1 to 1:3 Nitrile sulfonium 15:1 to 1:4 5:1 to 1:2 5:1 to 1:2 Twelve Rings 30:1 to 1:3 10:1 to 1 :1 7:1 to 1:1 Doning 30:1 to 1:2 10:1 to 2:1 10:1 to 2:1 granules 30:1 to 1:9 10:1 to 1:3 3 :1 to 1:3 Enoxalate 9:1 to 1:18 3:1 to 1:6 2:1 to 1:4 Epp 3:1 to 1:36 1:1 to 1:12 1: 1 to 1:7 Ethaboxam 7:1 to 1:9 2:1 to 1:3 2:1 to 1:3 ethirimol 30:1 to 1:3 10:1 to 1:1 7 :1 to 1 :1 Dependence 30:1 to 1:9 10:1 to 1:3 7:1 to 1:2 Where murder is 9:1 to 1:18 3:1 to 1:6 2:1 to 1:4 °m α sitting bacteria I 6:1 to 1:18 2:1 to 1:6 2:1 to 1:4 Fenrimo 3:1 to 1:90 1:1 to 1:30 1:2 to 1 :24 Nitrile benzophenone 3:1 to 1:30 1:1 to 1:10 1:1 to 1:10 formazanamide 18:1 to 1:6 6:1 to 1:2 4:1 to 1: 2 Cyclosporin 30:1 to 1:2 10:1 to 2:1 10:1 to 2:1 11 mytamine 150:1 to 1:36 50:1 to 1:12 15:1 to 1:1 151284. Doc •190- 201117722 Component (b) Normal weight ratio more typical weight ratio Most typical weight ratio half 75:1 to 1:9 25:1 to 1:3 15:1 to 2:1 Benzoite bite 30: 1 to 1:3 10:1 to 1:1 7:1 to 1:1 Fenford 30:1 to 1:3 10:1 to 1:1 7:1 to 1:1 Triphenyl salt, like Acetate, vapor or hydride triphenyl salt 15:1 to 1:9 5:1 to 1:3 3:1 to 1:3 thiram 300:1 to 1:2 100:1 to 2:1 30 :1 to 4:1 Fumi Comprehensive 30:1 to 1:5 10:1 to 1:2 7:1 to 1:2 Cougiamine 22:1 to 1:5 7:1 to 1:2 3:1 To 1:2 oxybdate 7:1 to 1:12 2:1 to 1:4 2:1 to 1:4 flufenamide 9:1 to 1:6 3:1 to 1:2 3:1 to 1:2 Fluorine 9:1 to 1:18 3:1 to 1:6 3:1 to 1:3 Fluorine than bacteriocin 3:1 to 1:18 1:1 to 1:6 1:1 to 1:6 Fluorine bismuthamide 15:1 to 1:90 5:1 to 1:30 3:1 to 1:3 gas sclerotia 150._1 to 2:1 50:1 to 4··1 37·· 1 to 5:1 fluoxastrobin 4:1 to 1:18 1:1 to 1:6 1:1 to 1:6 Fluorine 坐α 4:1 to 1:12 1:1 to 1: 4 1:1 to 1:4 Guards 15:1 to 1:9 5:1 to 1:3 3:1 to 1:3 sulphur sulphur 90:1 to 1:2 30:1 to 2 :1 15:1 to 2:1 Fouti Mud 7:1 to 1:36 2:1 to 1:12 1:1 to 1:6 Fudonin 18:1 to 1:6 6:1 to 1:2 4:1 to 1:2 Refining 4:1 to 1:12 1:1 to 1:4 1:1 to 1:4 Blessing and killing 12:1 to 1:9 4:1 to 1:3 2: 1 to 1:3 Forepe 90:1 to 1:4 30:1 to 1:2 15:1 to 2:1 Forsyth 225:1 to 2:1 75:1 to 5:1 30:1 to 5:1 Benzimidazole 45:1 to 1:4 15:1 to 1:2 11:1 to 2:1 Furosemide 15:1 to 1:45 5:1 to 1:15 1:1 to 1: 6 151284. Doc -191 - 201117722 Component (b) Normal weight ratio more typical weight ratio Typical typical weight ratio Folah 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 gram heat or gram Hot 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 Fickley 15:1 to 1:36 5:1 to 1:12 1:1 to 1:5 Killing Ning 225 :1 to 2:1 75:1 to 4:1 75:1 to 9:1 Dependent column 7:1 to 1:18 2:1 to 1:6 1:1 to 1:5 Easy amine seat 15:1 To 1:36 5:1 to 1:12 1:1 to 1:5 Iodocarbinyl phthalate (iodocarb) 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 carbazole 15:1 to 1:36 5:1 to 1:12 1:1 to 1:5 propyl chelsone 150:1 to 1:36 50:1 to 1:12 15:1 to 2: 1 Yiputong 120:1 to 1:2 40:1 to 2:1 15:1 to 2:1 Isoprofen 9:1 to 1:9 3:1 to 1:3 2:1 to 1:3圃 圃 150:1 to 2:1 50:1 to 4:1 45:1 to 5:1 派来来桑 12:1 to 1:9 4:1 to 1:3 2:1 to 1:3 Thiamin 12:1 to 1:9 4:1 to 1:3 2:1 to 1:3 Catherine 7:1 to 1:90 2:1 to 1:30 1:2 to 1:24 g Receiving Xin 7:1 to 1:18 2:1 to 1:6 2:1 to 1:4 Zinc Manganese 180:1 to 1:3 60:1 to 2:1 22:1 to 3:1 Manpamine 6:1 to 1:18 2:1 to 1:6 2:1 to 1:4 Manganese Pool 180:1 to 1:3 60:1 to 2:1 22: 1 to 3:1 Azoxystrobin 18:1 to 1:3 6:1 to 1:1 6:1 to 1:1 formazanamide 7:1 to 1:36 2:1 to 1:12 1:1 To 1:6 Oxyacetic acid based white powder 7:1 to 1:9 2:1 to 1:3 2:1 to 1:3 Destroy 15:1 to 1:45 5:1 to 1:15 1:1 To 1:6 Destroy-M 7:1 to 1:90 2:1 to 1:30 1:1 to 1:12 Xanthozol 3:1 to 1:18 1:1 to 1:6 1:1 To 1:6 151284. Doc •192- 201117722 Component (b) Normal weight ratio is more typical weight ratio The most typical weight ratio is 150:1 to 1:36 50:1 to 1:12 15:1 to 1:1 to avoid rotten 150:1 To 1:36 50:1 to 1:12 15:1 to 1:1 phenoxystrobin 9:1 to 1:12 3:1 to 1:4 3:1 to 1:3 Defennon 6:1 to 1:12 2:1 to 1:4 2:1 to 1:4 McKenna 5:1 to 1:26 1:1 to 1:9 1:1 to 1:8 Naftifen 150:1 to 1: 36 50:1 to 1:12 15:1 to 2:1 Ammonium iron arsenate (iron methyl arsenate) 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 Nerimo 15:1 to 1:9 5:1 to 1:3 3:1 to 1:3 αα-saidone 150:1 to 1:36 50:1 to 1:12 15:1 to 1:1 mezamide 15:1 to 1:45 5:1 to 1:15 1:1 to 1:6 Oxypyramine 9:1 to 1:12 3:1 to 1:4 3:1 to 1:3 Killing 15 :1 to 1:45 5:1 to 1:15 1:1 to 1:6 Oxalic acid 30:1 to 1:9 10:1 to 1:3 7:1 to 1:2 Fumaric acid ° Mi Jun 15:1 to 1:36 5:1 to 1:12 1:1 to 1:5 Oxygen rustling 18:1 to 1:6 6:1 to 1:2 4:1 to 1:2 Tetracycline 15:1 to 1:9 5:1 to 1:3 3:1 to 1:3 Hejiao 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 gram seat 1:1 to 1:45 1:2 to 1:15 1:2 to 1:15 Bin clone 150:1 to 1:2 50:1 to 2:1 11:1 to 2:1 Piperfin (N-[2-(l,3-dimercaptobutyl)phenyl]-5-fluoro-1,3-didecyl-1Η-pyrazole-4-carboxamide) 12:1 To 1:9 4:1 to 1··3 2:1 to 1:3 Pyridillium 12:1 to 1:9 4:1 to 1:3 2:1 to 1:3 Phosphorous acid and its salts 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 Hots 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 Acetate 7 :1 to 1:18 2:1 to 1:6 1:1 to 1:5 Powder disease 15:1 to 1:9 5:1 to 1:3 3:1 to 1:3 151284. Doc -193- 201117722 Component (b) Normal weight ratio more typical weight ratio Most typical weight ratio polyoxin 15:1 to 1:9 5:1 to 1:3 3:1 to 1:3 Fighting heat 15: 1 to 1:9 5:1 to 1:3 3:1 to 1:3 Poker Pull 22:1 to 1:4 7:1 to 1:1 7:1 to 1:2 Fighting Ning 45:1 to 1: 3 15:1 to 1:1 11:1 to 2:1 Pumper or Propk Hydrochloride 30:1 to 1:2 10:1 to 2:1 10:1 to 2:1 Pushley 4: 1 to 1:18 1:1 to 1:6 1:1 to 1:5 methyl zinc is a 45:1 to 1:2 15:1 to 2:1 11:1 to 2:1 propoxyquinol 3 :1 to 1:36 1:1 to 1:12 1:1 to 1:12 Thiocarbazone 9:1 to 1:18 3:1 to 1:6 3:1 to 1:3 Propionibacterium. Sit 6:1 to 1:18 2:1 to 1:6 1:1 to 1:5 Bai Kemin 9:1 to 1:18 3:1 to 1:6 2:1 to 1:4 Zymosillus 9 :1 to 1:18 3:1 to 1:6 2:1 to 1:4 pyraclostrobin 9:1 to 1:18 3:1 to 1:6 2:1 to 1:4 White Pine 150:1 to 1:36 50:1 to 1:12 15:1 to 1:1 Mold proof 15:1 to 1:6 5:1 to 1:2 4:1 to 1:2 Tefino 15:1 to 1: 9 5:1 to 1:3 3:1 to 1:3 Pyrimethanil 30:1 to 1:6 10:1 to 1:2 3:1 to 1:2 Phenfen 6:1 to 1:12 2 :1 to 1:4 2:1 to 1:4 Hundreds of fast 15:1 to 1:9 5:1 to 1:3 3:1 to 1:3 Nitrate 0-pyromycin 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 螨 fierce 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 快诺芬 4:1 to 1:18 1:1 To 1:6 1:1 to 1:6 Five-gas nitrobenzene 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 thiastrobin 7:1 to 1:18 2:1 To 1:6 2:1 to 1:4 Hydrazine 15:1 to 1:36 5:1 to 1:12 1:1 to 1:5 Spiral amine 22:1 to 1:4 7:1 to 1: 2 5:1 to 1:2 151284. Doc -194- 201117722 Component (b) Normal weight ratio more typical weight ratio Most typical weight ratio streptomycin 15:1 to 1:9 5:1 to 1:3 3:1 to 1:3 Sulfur 300:1 to 3:1 100:1 to 9:1 75:1 to 9:1 De Klee 7:1 to 1:18 2:1 to 1:6 1:1 to 1:5 Teflon 100:1 to 1:100 10:1 to 1:10 3:1 to 1:3 grams of rot 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 four gas nitro stupid 150:1 to 1:36 50:1 to 1:12 15··1 to 2_1 Tebinafin 150:1 to 1:36 50:1 to 1:12 15··1 to 2:1 Sikhli 15:1 to 1:36 5: 1 to 1:12 1:1 to 1:5 Thiamidazole 45:1 to 1:4 15:1 to 1:2 11:1 to 2:1 cyprofen 15:1 to 1:9 5:1 to 1:3 3:1 to 1:3 more than 45:1 to 1:3 15:1 to 2:1 11:1 to 2:1 Methyl multi-purity 45:1 to 1:3 15:1 to 2:1 11:1 to 2:1 付恩地150:1 to 1:2 50:1 to 2:1 37:1 to 5:1 Thiacin 12:1 to 1:9 4:1 to 1: 3 2:1 to 1:3 methyl phosgene 150:1 to 1:2 50:1 to 2:1 37:1 to 5:1 toluene sulfonamide 150:1 to 1:36 50:1 to 1: 12 15:1 to 2:1 triterpene ketone 15:1 to 1:36 5:1 to 1:12 1:1 to 1:5 triazolol 15:1 1:36 5:1 to 1:12 1:1 to 1:5 three zero sitting oxide 150:1 to 1:36 50:1 to 1:12 15:1 to 2:1 racazole 15:1 to 1:9 5:1 to 1:3 3:1 to 1:3 Thirteen scare · 30:1 to 1:3 10:1 to 1:1 7:1 to 1:1 Trifluoromin 6:1 to 1··18 2:1 to 1:6 2:1 to 1:4 赛福座15:1 to 1:9 5:1 to 1:3 3:1 to 1:3 Safranine 15:1 to 1 :9 5:1 to 1:3 3:1 to 1:3 Tridecylamine 45:1 to 1:9 15:1 to 1:3 7:1 to 1:2 Sterilization 嗤15:1 to 1:36 5:1 to 1:12 1:1 to 1:5 151284. Doc •195- 201117722 Component (b) Normal weight ratio More typical weight ratio Most typical weight ratio Difficulty ° Sit 15:1 to 1:36 5:1 to 1:12 1:1 to 1:5 Vesinomycin 150:1 to 1:36 50:1 to 1:12 3:1 to 1:3 and valifenalate (valiphenal) 6:1 to 1:18 2:1 to 1:6 2:1 to 1 :4 克宁宁120:1 to 1:2 40:1 to 2:1 15:1 to 2:1 Zinc Napo 150:1 to 1:2 50:1 to 2:1 37:1 to 5:1 Famine Zinc 150:1 to 1:2 50:1 to 2:1 37:1 to 5:1 Cedose 6:1 to 1:18 2:1 to 1:6 2:1 to 1:4 5-gas -6-(2,4,6-Triphenyl)-7-(4-methylhexahydropyridin-1-yl)[1,2,4]tri. Sit [l,5-a]°^ bite 15:1 to 1:36 5:1 to 1:12 1:1 to 1:6 N-[2-[4-[[3-(4-Phenylphenyl) )-2-propyn-1-yl]oxy]-3-indolyloxyphenyl]ethyl]-3-indolyl-2-[(methylsulfonyl)amino]butanamine 6:1 to 1 :18 2:1 to 1:6 2:1 to 1:4 N-[2-[4-[[3-(4-Phenylphenyl)-2-propyn-1-yl]oxy]-3-曱Phenylphenyl]ethyl]-3-methyl-2-[(ethylthio)amino]butanamine 6:1 to 1:18 2:1 to 1:6 2:1 to 1:4 2 - Butoxy-6-indole-3 -propyl-4H-1 -benzophenanyl-4-one 3:1 to 1:36 1:1 to 1:12 1:1 to 1:12 3- [5-(4-Phenylphenyl)-2,3-dimercapto-3-iso-17 ° 坐 坐 坐] bite 15:1 to 1:9 5:1 to 1:3 3:1 to 1:3 4-fluorophenyl N-[l-[[l-(4-cyanophenyl)ethyl]sulfonyl]methyl]propyl]amine decanoate 6:1 to 1:18 2:1 to 1:6 2:1 to 1:4 N-[[(cyclopropyldecyloxy)amino][6-(difluorodecyloxy)-2,3-difluorophenyl] Benzoamine benzophenone 1:1 to 1:90 1:2 to 1:30 1:2 to 1:24 α-[methoxyimino]-N-methyl-2-[[[1-[ 3-(Trifluoromethyl)phenyl]ethoxy]imino]methyl]benzamide 9:1 to 1:18 3:1 to 1:6 3:1 to 1:3 151284. Doc •196· 201117722 Component (b) Normal weight ratio is more typical than the most typical weight ratio \Γ_Γ/ί ΓΑ Preparation - even talk, 纪备----- Ϊ重比二气Τ Lane) -2,5-dimethylphenyl]-1^-ethyl-:^- adiamidine 15:1 to 1:18 5:1 to 1:6 3:1 to 1:3 N-(4-gas- 2-Nitrolyl)-N-ethyl-4-methylbenzenesulfonamide 15:1 to 1:18 5:1 to 1:6 3:1 to 1:3 2-[[[3-(2 ,6-di-phenylphenyl)-1-indenyl-2-propen-1-ylidene]amino]oxy]methyl]-α-(methoxyimino)-N-methylphenylacetamide 9:1 to 1:18 3:1 to 1:6 3:1 to 1:3 N-[4-[[[[(l-methyl-1H-tetrazol-5-yl)phenyl)] Amyl]oxy]indolyl]-2-thiazolyl]amyl formate 9:1 to 1_18 --~--- 3··1 to 1:6 ------ 3:1 to 1: 3 Ν·[6-[[[[(1-methyl-1H-tetrazol-5-yl)phenylmethylene]amino]oxy]methyl]-2-pyridyl]amine f-amyl ester 9:1 to 1:18 3:1 to 1:6 3:1 to 1:3 As described above, the present invention includes embodiments in which the composition contains components (a) and (1), wherein component (1) contains at least A fungicide derived from each of two groups selected from (b!) to (b46). Tables C to C27 list specific mixtures (compound numbers refer to compounds in index table a) to illustrate examples in which component (b) includes at least one from each of two groups selected from (M) to (b46). Fungicide. In Table ci, each line under the headings "Component (a)" and "Component (b)" specifically discloses a mixture of component (a) which is a compound 181 'and has at least two components (b) a fungicide. The sequence of the items disclosed in the heading "Description Ratio" reveals three specific weight ratios of component (a) relative to each component (b) fungicide. For example, the first line reveals a mixture of compound 181 and cypr〇c〇naz〇le and azoxystrobin, and lists 1:1: Bu 2:1:1 151284. Doc •197- 201117722 or 3. The weight ratio of compound 181 of 1 · 1 to cyproconazole (azoxystrobin). Table C1 Component (a) Component (b) Description Example ratio (*) Compound 181 Cyclosin Atomin 1:1:1 2:1:1 3:1:1 Compound 181 克克克克收欣1 :1:1 2:1:1 3:1:1 Compound 181 Cyclohexyloxypide 1:1:1 2:1:1 3:1:1 Compound 181 Cyclosyl kebamine 1:1:1 2:1:1 3:1:1 Compound 181 Cycloconazole: 1:1:1 2:1:1 3:1:1 Compound 181 Cyclosporin 1:1:1 2:1 :1 3:1:1 Compound 181 Cyclosyl-Fluorine 1:1:1 2:1:1 3:1:1 Compound 181 Cyclosylphenyrene 1:1:2 2:1:2 3: 1:2 Compound 181 Cyclosylvania 1:1:2 2:1:2 3:1:2 Compound 181 Cyclosyl-Secylamine 1:2:1 2:2:1 3:2:1 Compound 181 Cycloheximide flupirtine 1:1:2 2:1:2 3:1:2 Compound 181 Cyclosylvania sinensis 1:1:2 2:1:2 3:1:2 Compound 181 Cyclosporine Fennon 1:1:2 2:1:2 3:1:2 Compound 181 Cycloheximide 1:1:2 2:1:2 3:1:2 Compound 181 Ring gram Propoxyquine scare 1:1:1 2:1:1 3:1:1 Compound 181 Cyclosporin 1:1:2 2:1:2 3:1:2 Compound 181 Cyclosporus 1:1:1 2:1:1 3:1:1 compound 181 ring grams Syngenta 1:1:2 2:1:2 3:1:2 Compound 181 Cyclohexyloxypoxypropoxyl 1:1:1:1 2:1:1:1 3:1:1 :1 Compound 181 Cyclos-trifluoro-propoxyquinoline 1:1:1:1 2:1:1:1 3:1:1:1 Waiting for Klee 2:1:1 3:1:1 Compound 181 ( Difenconazole ) Atomicin 1:1:1 Compound 181 Waiting for Crickett Revenue 1:1:1 2:1:1 3:1:1 Compound 181 lysyloxylysate 1:1:1 2:1:1 3:1:1 Compound 181 to Klipbachmin 1:1:1 2:1:1 3:1:1 Compound 181 to cloxazolamide 1:1:1 2:1:1 3:1:1 compound 181 Waiting for Klee. Saccharomyces S: 1:1:1 2:1:1 3:1:1 151284. Doc -198- 201117722 Component (a) Component (b) Description Example ratio (" Compound 181 to Klein-Trifluoromide 1:1:1 2:1:1 3:1:1 Compound 181 to Cleopatra 1 :1:2 2:1:2 3:1:2 Compound 181 Waiting for Kleincliff 1:1:2 2:1:2 3:1:2 Compound 181 Waiting for Kristenamine 1:2:1 2: 2:1 3:2:1 Compound 181 Calcium fluoride 11 citrate 1:1:2 2:1:2 3:1:2 Compound 181 Waiting for Cleopatra 1:1:2 2:1: 2 3:1:2 Compound 181 to Clindefen 1:1:2 2:1:2 3:1:2 Compound 181 to Klee. Thiafenil 1:1:2 2:1:2 3:1 :2 Compound 181 Waiting for Cleopatra 1:1:1 2:1:1 3:1:1 Compound 181 Waiting for Klein Finnon 1:1:2 2:1:2 3:1:2 Compound 181 Waiting for Klee Fast Proven 1:1:1 2:1:1 3:1:1 Compound 181 Waiting for Krishna Synchronization 1:1:2 2:1:2 3:1:2 Compound 181 for clopidogrel propionate Lin 1:1:1:1 2:1:1:1 3:1:1:1 Compound 181 to Klein-Trifluoro-Methoxy 1#琳1:1:1:1 2:1:1:1 3: 1:1:1 Compound 181 Epto Atomic 1:1:1 2:1:1 3:1:1 Compound 181 Iptek Revenue 1:1:1 2:1:1 3:1: 1 Compound 181 Epsiridin Oxygen ester 1:1:1 2:1:1 3:1:1 Compound 181 Epson 100:1:1:1 2:1:1 3:1:1 Compound 181 Epoxazole 1 :1:1 2:1:1 3:1:1 Compound 181 Eptomycin 1:1:1 2:1:1 3:1:1 Compound 181 Eptotriene 1:1:1 2:1:1 3:1:1 Compound 181 Epson Benzene 1:1:2 2:1:2 3:1:2 Compound 181 Epson White 1:1:2 2:1: 2 3:1:2 Compound 181 Epsonide 1:2:1 2:2:1 3:2:1 Compound 181 Ectofluazone 1:1:2 2:1:2 3 :1:2 Compound 181 Ip seated to send mulberry 1:1:2 2:1:2 3:1:2 Compound 181 Ipodron fennon 1:1:2 2:1:2 3:1: 2 Compound 181 Epto ratio ° fenacetamide 1:1:2 2:1:2 3:1:2 Compound 181 Eptopropoxy 0i Lin 1:1:1 2:1:1 3:1: 1 Compound 181 Eppen Finnon 1:1:2 2:1:2 3:1:2 Compound 181 Eppen Fastin 1:1:1 2:1:1 3:1:1 Compound 181 The seat is up to 1:1:2 2:1:2 3:1:2 151284. Doc -199- 201117722 Component (a) Component (b) Description Example ratio (*) Compound 181 Eptomycin oxypropylene 011# 1:1:1:1 2:1:1:1 3: 1:1:1 Compound 181 Eptrifluoro-tripropionine 1:1:1:1 2:1:1:1 3:1:1:1 Compound 181 Chysozocilin Atomicin 1:1: 1 2:1:1 3:1:1 Compound 181 Cofazoxin 1:1:1 2:1:1 3:1:1 Compound 181 Leaf bacterium D-oxypicase 1:1:1 2 :1:1 3:1:1 Compound 181 Ghectin Baikemin 1:1:1 2:1:1 3:1:1 Compound 181 leaf fungus. Sodium pyraclostrobin 1:1:1 2:1:1 3:1:1 Compound 181 Chythaconazole alpha serotonin 1:1:1 2:1:1 3:1:1 Compound 181 Fluoride sensitivity 1:1:1 2:1:1 3:1:1 Compound 181 Ghectin Benzenol 1:1:2 2:1:2 3:1:2 Compound 181 Chythaconazole White Column 1: 1:2 2:1:2 3:1:2 Compound 181 Cofazosinide 1:2:1 2:2:1 3:2:1 Compound 181 Cistioconazole Fenoramide 1:1: 2 2:1:2 3:1:2 Compound 181 Leaf bacterium is different from sang 1:1:2 2:1:2 3:1:2 Compound 181 Leaf bacterium '• Sitting fennon 1:1:2 2:1:2 3:1:2 Compound 181 Xanthoxanthin 1:1:2 2:1:2 3:1:2 Compound 181 Ghectin propoxyquine 1:1:1 2: 1:1 3:1:1 Compound 181 Ghectabine Fennon 1:1:2 2:1:2 3:1:2 Compound 181 Ghectin Vonofol 1:1:1 2:1:1 3: 1:1 Compound 181 Chyrapidazole Syndrome 1:1:2 2:1:2 3:1:2 Compound 181 Leaf bacterium Lyticillin Propoxyquine 1:1:1:1 2:1 :1:1 3:1:1:1 Compound 181 Fencilazole Trifluoro-propoxyquine 1:1:1:1 2:1:1:1 3:1:1:1 Compound 181 McNeato Min 1:1:1 2:1:1 3:1:1 Compound 181 Mike Nick Revenue 1:1:1 2:1:1 3:1:1 Compound 181 McConnex-oxygenate 1:1:1 2:1:1 3:1:1 Compound 181 McAfee Nikkimin 1:1:1 2:1:1 3:1:1 Compound 181 McNezolamide Bacterial ester 1:1:1 2:1:1 3:1:1 Compound 181 McNeillide 1:1:1 2:1:1 3:1:1 Compound 181 McNeney Fluoride 1:1: 1 2:1:1 3:1:1 Compound 181 McNea Benzene 1:1:2 2:1:2 3:1:2 Compound 181 McNea White 1:1:2 2:1:2 3:1:2 Compound 181 麦尼尼塞芬amine 1:2:1 2:2:1 3:2:1 151284. Doc •200· 201117722 Component (a) Component (b) Description Example ratio (" Compound 181 McAfee Nitrocarbamide 1:1:2 2:1:2 3:1:2 Compound 181 McNea派桑桑1:1:2 2:1:2 3:1:2 Compound 181 McNea Fennon 1:1:2 2:1:2 3:1:2 Compound 181 dexamethasone 1: 1:2 2:1:2 3:1:2 Compound 181 麦尼丙氧啥1:1:1 2:1:1 3:1:1 Compound 181 McNea Finnon 1:1:2 2: 1:2 3:1:2 Compound 181 McNealy Fastin 1:1:1 2:1:1 3:1:1 Compound 181 McNeill Syngenta 1:1:2 2:1:2 3:1: 2 Compound 181 McNeill oxytocin propionate 1:1:1:1 2:1:1:1 3:1:1:1 Compound 181 McNein trifluoro-propoxy phenanthrene 1:1:1 :1 2:1:1:1 3:1:1:1 Compound 181 Propionibacterium. Sitting on Atomin 1:1:1 2:1:1 3:1:1 Compound 181 Propionibacterium. Xin 1:1:1 2:1:1 3:1:1 Compound 181 Propionibacterium oxycephala 1:1:1 2:1:1 3:1:1 Compound 181 Propionibacterium D sits 100 grams of sensitive 1:1:1 2:1:1 3:1:1 Compound 181 Propionibacterium. Sodium pyraclostrobin 1:1:1 2:1:1 3:1:1 Compound 181 Propionibacterium α Ester 1:1:1 2:1:1 3:1:1 Compound 181 Propionibacterium bismuth Fluoride 1:1:1 2:1:1 3:1:1 Compound 181 Propionisulfone salivation 1:1:2 2: 1:2 3:1:2 Compound 181 Propionibacterium sulphate 1:1:2 2:1:2 3:1:2 Compound 181 Propionibacterium. Selefenamide 1:2:1 2:2 :1 3:2:1 Compound 181 Propionate 嗤 ° ° 1:1:2 2:1:2 3:1:2 Compound 181 Propionisulfone sputum sent sang 1:1:2 2 :1:2 3:1:2 Compound 181 Propionibacterium '•Shenfenfen 1:1:2 2:1:2 3:1:2 Compound 181 Propionibacterium. Niecitabine 1:1: 2 2:1:2 3:1:2 Compound 181 Propionibacterium acetophenoxyquine 1:1:1 2:1:1 3:1:1 Compound 181 Propionibacterium. Sitting on Finnon 1:1: 2 2:1:2 3:1:2 Compound 181 Propionibacter quinone quinolone 1:1:1 2:1:1 3:1:1 Compound 181 Propionithiophene β sit-up 1:1:2 2 :1:2 3:1:2 Compound 181 Propionibacterium. Sodium oxypide propoxyphene 1:1:1:1 2:1:1:1 3:1:1:1 Compound 181 Propionibacterium α sitting on trifluoro-propion oxyfluoride 1:1:1: 1 2:1:1:1 3:1:1:1 Compound 181 Deklia Tomin 1:1:1 2:1:1 3:1:1 Compound 181 Klick Revenue 1:1:1 2 :1:1 3:1:1 151284. Doc •201 - 201117722 Component (a) Component (b) Description Example Proportion (*) Compound 181 Cleboxystrobin 1:1:1 2:1:1 3:1:1 Compound 181 Kleine 1:1:1 2:1:1 3:1:1 Compound 181: citazinamide 1:1:1 2:1:1 3:1:1 Compound 181: Cleazocin 1:1:1 2:1:1 3:1:1 Compound 181 Declixine 1:1 2:1:1 3:1:1 Compound 181 Dessert 1:1:2 2:1:2 3 :1:2 Compound 181 Declehcliff 1:1:2 2:1:2 3:1:2 Compound 181 Derived Cleceptin 1:2:1 2:2:1 3:2:1 Compound 181得克克利氟&quot;比菌胺1:1:2 2:1:2 3:1:2 Compound 181 Klein sent sang 1:1:2 2:1:2 3:1:2 Compound 181 Kleinfinon 1:1:2 2:1:2 3:1:2 Compound 181 Dessert 0 1:1:2 2:1:2 3:1:2 Compound 181咐1:1:1 2:1:1 3:1:1 Compound 181 Kleine Finnon 1:1:2 2:1:2 3:1:2 Compound 181 Klee Knofen 1:1:1 2 :1:1 3:1:1 Compound 181 Dekley Syngenta 1:1:2 2:1:2 3:1:2 Compound 181 acetoxypyroxypropoxyphene 1:1 :1:1 2:1:1:1 3:1:1:1 Compound 181 Klein trifluoro-propoxyquine 1:1:1:1 2:1:1:1 3:1:1:1 (*) The weight ratio of component (a) to component (b) in sequence. Tables C2 to C27 are structured in the same manner as Table C1 above except that the items under the heading "Component (a)" are replaced by the column names of the following components (a). Thus, for example, in Table C2, the items under the heading "Component (a)" are listed as r compounds 292", and the first line under the heading of column C2 specifically discloses a compound 292 and cyproconazole. And a mixture of azoXyStr〇bin, and compound 292. 环克座: The typical weight ratio of Atomin is m, 2. 1. 1 and 3. 1. 1. The tables C3 to C27 are similar in structure. 151284. Doc -202- 201117722 Table Code Component (a) Shelf Name Table Code Component (a) Field Name C2 Compound 292 C15 Compound 524 C3 Compound 469 C16 Compound 525 C4 Compound 513 C17 Compound 526 C5 Compound 514 C18 Compound 527 C6 Compound 515 C19 Compound 528 C7 Compound 516 C20 Compound 529 C8 Compound 517 C21 Compound 530 C9 Compound 518 C22 Compound 531 C10 Compound 519 C23 Compound 532 C11 Compound 520 C24 Compound 533 C12 Compound 521 C25 Compound 534 C13 Compound 522 C26 Compound 535 C14 Compound 523 C27 Compound 536 Notable is a composition of the invention comprising a compound of Formula 1 (or an N-oxide or a salt thereof), and at least one other killing having a different interaction with the compound of Formula 1 Fungal compounds. In this example, a composition of at least one fungicidal compound having the same control range but different sites of action would have particular benefits for drug resistance management. Accordingly, a composition of the present invention may advantageously comprise at least one fungicidally active compound selected from the group consisting of (bl) to (b46) as described above, which have the same control range but different sites of action. The composition of component (a) and component (b) may be further mixed with one or more other biologically active compounds or agents, including insecticides, nematicides, bactericides, snails, herbicides, herbicide safety Agents, growth regulators such as insect molting inhibitors and rooting stimulators, chemical sterilants, information chemicals, snorkels, attractants, information hormones, foraging stimulants, phytonutrients, other biologically active compounds or insect pathogens 151284 . Doc - 203 - 201117722 Bacteria, viruses or fungi to form a multi-component pesticide that provides a broader range of agricultural protection. The invention therefore also relates to a composition comprising a fungicidal effective amount of a mixture of component (a) and component (b) and a biologically effective amount of at least one additional biologically active compound or agent, and may further comprise at least A surfactant, a solid diluent or a liquid diluent. Other biologically active compounds or agents may also be formulated in a composition comprising at least one surfactant, a solid or a liquid diluent, respectively. With regard to the compositions of the present invention, one or more other biologically active compounds or agents may be formulated with one or both of components (a) and (b) to form a premix, or one or more other The biologically active compound or agent can be formulated from components (a) and (b), respectively, and the formulation is combined prior to application (eg, in a spray tank) or, when used, in combination, both Choose one. Examples of such biologically active compounds or agents, the sub-compositions of component (a) and component (b) may be formulated as follows: insecticides such as abametine, ethamamine, acetamiprid, Sub-killing, acetoprole, carbon disk, amidoflumet, amitrazide, avermectin, azadirachtin, sulphur-filled, bifenthene, biphenyl Ester ester, bistrifluron, bistrifluron. Sesone, carbofuran, chlorpyrifos, chlorpyrifos, chlorfenapyr, chlorfluazuron, chlorhexidine, chlorpyrifos, chlorpyrifos, ethyl sterol, ringworm, cotinine, Cyanide (3-bromo small (3-chloro-2-«pyridyl)-N-[4-cyano-2-indolyl-6-[(methylamino) thiol]phenyl]-1Η- °Bia-5-treacoamine), flubenzuron s s, gas-nitrogen nitrogen lijs, south-effect fluoride j gas chaos, green naphtha, cyano-cyhalothrin, high-efficiency chlorofluorocyanide Pyrethroid, cyclohexyl tin, cypermethrin, 151284. Doc -204· 201117722 Cyclopropyltriamine, deltamethrin, dibutyl ether urea, diazinon, kailesan, diltiazem, chlorpyrifos, diflubenzuron, tetrafluoroeththrin, dimethoate , dinotefuran, benzophenone, emamectin, endosulfan, high-grade fenvalerate, acetaminophen, acetamidine, gram-free phosphorus, quinacridone, phenbutyltin oxide, phenylthiosulfuron Ke, Fenoke, fenpropathrin, oxazolidine, fenfenyl, fentanyl, flunisamide, flufenamide, chlorin, fluvalinate, flufenerim, Flufenprol, fonufos (f〇n〇ph〇s), worms, hexaflurane, acetaminophen, amesone, imiCyaf〇s, edetamine, indek ,isophosphorus,lufenlong,malathion,methineine, fluorinated synthon, metaldehyde, methamidophos, chlorpyrifos, nadine, methine, oxime, fentanyl , trimethoprim, monocrotophos, nitenpyram, nisson, novalon, nomifomarin (n〇vi£|urnur〇n), cockroach, parathion, sulfur Phosphorus-fluorenyl, fenvalerate, arsenic, gibisson, chlorpyrifos, phosphonamine, antibiotic Converse, profenofos, fipronil, ketone, acesulfame, ruthenium, pr〇trjfenbute, genus, cockroach, chlorpyrifos, pyrethrum, Pythaben, Pyridoxine, pyrifluquinazon, pyridine fluoromethan, balippren, rotenone, nitinin, rattle, spinosad, spiridicl〇fen, snail A snail, snail ethyl ester, sulfoxaflor, thiopropionate, fenfenol, pyridoxamine, flubenzuron, tefluthrin, terbutazone, insecticide, tetrafluoroether Pyrethroid, Saiqi Pei, Sai Su An, Thiobacco, Insecticidal, Defenfen, Taifening, Zircon, Weibai, Sanfulong; nematicides such as aldicarb, neonicotin Class (hnicyaf〇s), cockroach killing and stupid line phosphorus; fungicides such as streptomycin; acaricides such as Sanya 螨, 螨 螨, ethyl ester sterol, acaricide (Cyen0pyrafen), tricyclotin, Kaile San, Zhilingling, etoxazole, quinacridone, chlorpyrifos, fenpropathrin, oxazolidine, thiazolone, I51284. Doc -205 · 201117722 gram, Pythaben and pyridoxamine; and biological agents including entomopathogens bacteria such as Suribacter aizavvai, Bacillus thuringiensis subsp.  Kurstaki) and encapsulated S. faecalis δ-endotoxin (eg, Cellcap, MPV, MPVII); entomopathogenic molds such as Metarhizium, and entomopathogenic viruses, including baculovirus, nuclear polyhedrosis virus (NPV), such as Helicoverpa armigera nuclear polyhedrosis virus (HzNPV), Anagaro nuclear polyhedrosis virus (AfNPV); and granulosis virus (GV) such as leaf roller moth granulosis virus (CpGV). A general reference to agricultural protective agents (ie, insecticides, fungicides, nematicides, acaricides, herbicides, and biologics) includes The Pesticide Manual, 13th Edition, C.  D.  S.  Tomlin, Ed. , British Crop Protection Council, Farnham, Surrey, U. K. , 2003 and The

BioPesticide Manual，2nd Edition, L. G· Copping，Ed” 英 國作物保護會，Farnham，Surrey，英國，2001年。 實施例中，其一或多個該些多種混合成分經使用， 這些多種不同的混合成分對於組分（a)與組分（b)的 重量比一般來說介於約1:3000以及約3000:1。值得注 意的是重量比介於約1:100及約3000:1，或介於約1:30 及約300:1 (例如，比例介於約ι:1以及約3〇:1)。很顯 然的，包括這些附加的組分較組分（a)與組分（b)的 混合物具有擴展疾病防治的效果。 組分（a)化合物及/或及其組成具有組分（b)化 合物及/或一或更多其他生物活性化合物或藥劑可以經 應用在僅改造植物來對非脊椎動物害蟲表現毒性蛋白 (如蘇力菌δ-内毒素）。外在單獨或合併應用本組分（a) 與組分（b)可與表現的毒素蛋白協同作用。 151284.doc •206- 201117722 值得注意的是如在發明摘要中描述的包括組分（a) 及（b)的組成物進一步包含至少一種非脊椎動物害蟲 防治化合物或藥劑（例如，殺蟲劑、殺蟎劑）。值得特 別注意的組合物’其包含組分（a)及至少一種（即— 種或多種）非脊椎動物害蟲防治化合物或藥劑，其可隨 後與組勿（b)結合以提供一個包含組分（a )及（b) 以及一種或多種的非脊椎動物害蟲防治化合物或藥劑 的組成物。另外，在未先與成分（b)混合的情況下， 可將包含成分（a)與至少 之組合物，以生物有效量施用於植物或植物種子（直接 或透過植物或植物種子之環境），以保護植物或植物種 子避免由AS制造成之疾病及由無脊軸物害蟲造 成之損害。 有關使用-種或以上之無脊椎動物害蟲防治化合 物之實施例，這魏合物（總計）對成分U)化合物 之典型重量比係介於約1:3_至約屬:1之間。 注f的是係介於約1:_至約之間之重量比（例 如介於約1:30至約3〇:丨之間之比例）。精於此技藝人士 可經由簡單實驗，輕易決定 伩衣人士 範圍必要之生物有效量Λ成774成所需生物活性BioPesticide Manual, 2nd Edition, L. G. Copping, Ed" British Crop Protection Society, Farnham, Surrey, UK, 2001. In the examples, one or more of these various mixed ingredients are used, these various different mixtures The weight ratio of the ingredients to component (a) to component (b) is generally between about 1:3000 and about 3000:1. It is worth noting that the weight ratio is between about 1:100 and about 3000:1, or Between about 1:30 and about 300:1 (for example, a ratio between about ι:1 and about 3〇:1). Obviously, including these additional components compared to components (a) and components (b) The mixture of the component (a) and/or its composition having the component (b) and/or one or more other biologically active compounds or agents may be applied to the transformation of the plant only It is a toxic protein (such as S. faecalis δ-endotoxin) for invertebrate pests. It can be used alone or in combination with this component (a) and component (b) to synergize with the expressed toxin protein. 151284.doc • 206-201117722 It is worth noting that the components (a) and (b) are included as described in the abstract of the invention. The composition further comprises at least one invertebrate pest control compound or agent (eg, insecticide, acaricide). Compositions that deserve special attention include 'components (a) and at least one (ie, one or more A non-vertebrate pest control compound or agent which can then be combined with the group (b) to provide a composition comprising components (a) and (b) and one or more of the non-vertebrate pest control compounds or agents. In addition, the component (a) and at least the composition may be applied to the plant or plant seed (directly or through the environment of the plant or plant seed) in a biologically effective amount without first mixing with the component (b). To protect plants or plant seeds from diseases caused by AS and damage caused by pests without spine. For examples of invertebrate pest control compounds using one or more species, this mixture (total) versus component U The typical weight ratio of the compound is between about 1:3 and about genus: 1. Note f is a weight ratio between about 1: _ to about (for example between about 1:30 and about 3〇: The ratio between). Thereto fine art through simple experimentation for persons, who readily determined Xin Yi biologically effective amount necessary range Λ 774 into a desired biological activity

值得注意的是本發明的組成物H ⑷化合物’其單獨或是結合組分（b)，及至：二 非脊椎動物害蟲防治化合物 夕 份組成的群組：阿巴汀、其選自於由以下成 ^ r 乙酰甲胺磷、亞滅培、阿攜同Of note is the composition of the present invention H (4) compound 'either alone or in combination with component (b), and to: a group of two non-vertebrate pest control compounds: abatatin, which is selected from the following ^ r 甲 甲 甲 甲 甲 甲 甲 甲 甲

普羅（acetoprole)、涕诘点 h , β、_ J ^ J :亞蹣、mu冬威、阿咪夕褐滿（amid()flumet)、 151284.doc 一亞瞒阿佛i素、印楝素、保棉备甲基、畢芬寧、 -207· 201117722 聯本肼g日、必撕傳福輪（bistr^uron)、布芬淨、咳喃丹、 培丹、滅蟎猛、克凡派、氟啶脲、剋安勃、陶斯松、陶 ，松-甲基、殺蟎酯、環蟲醯肼、可尼丁、氰特破、赛 :蟎、赛扶寧、p_赛扶寧、賽洛寧、γ_赛洛寧、λ_賽洛 甲、三環錫、赛滅寧、赛滅淨、第滅寧、丁醚脲、二嗪 農、開樂散、狄氏劑、除蟎靈、除蟲脲、四氟曱醚菊酯、 樂果、呋蟲胺、苯蟲醚、依馬菌素、硫丹、高氰戊菊酯、 乙蟲清、乙蟎唑、苯線磷、喹蟎醚、苯丁錫、笨硫威、 苯氧威、曱氰菊酯、唑蟎酯、氰戊菊酯、氟蟲腈、氟啶 蟲醯胺、氟蟲醯胺、護賽寧、頭、氟胺氰菊酯、福盧翻 泥輪（flufenerim)、氟芬隆、福農風（fonophos)、氯蟲 醯肼、氟鈐脲、噻蟎酮、氟蟻腙、新煙鹼類、吡蟲啉、 茚蟲威、異柳磷、氯芬奴隆、馬拉硫磷、每紕蜉新 (meperfluthrin)、氰氟蟲腙、四聚乙醛、甲胺嶙、殺撲 磷、滅多威、烯蟲酯、甲氧氯、甲氧、曱氧卞氟菊酯: 久效碟、稀。定蟲胺、泥赛新（nithiazine)、氟酿脲、糖 米扶木輪（noviflumuron)、殺線威、對硫磷、曱基對硫 磷、氣菊酯、甲拌磷、裕必松、亞胺硫磷、磷胺、抗辑 威、丙漠填、波幅輪（profluthrin )、克蜗特、剝翠凡不 特（protrifenbute)、吡蚜酮、吡嗪氟蟲腈、除蟲菊醋、 噠、啶蟲丙醚、皮楠福率那增（pyrifluquinazon)、η比咬 氟美腈、吡丙醚、魚藤酮、蘭尼、賜托拉、多殺菌素、 斯別立地佝恩（spiridiclofen)、螺曱蟎酯、螺蟲乙g旨、 桑發福耳（sulfoxaflor)、硫滅克磷、蟲酰肼、吡蜗胺、 伏蟲隆、汰福寧、托福松、殺蟲威、四甲基福聽 (tetramethylfluthin)、嘆轰琳、喧愚嗪、疏雙威、殺蟲 151284.doc •208- 201117722 雙、脫芬瑞、泰滅寧、β坐財威、敵百蟲、殺鈐脲、蘇力 菌（Bacillus thuringiensis subsp. aizawai )、蘇力菌 (Bacillus thuringiensis subsp. kurstaki)、核多角體病毒 (nucleopolyhedro viruses)、囊封的蘇力菌 δ-内毒素、 桿狀病毒、昆蟲病原體細菌、昆蟲病原體病毒以及昆蟲 病原體真菌。值得注意的是前述表列排除美福普勤 (meperflutrin)、殺福砩（sulfoxaflor)及四氟醚菊酯。 在如此的例子中，組分（a)化合物單獨或與組分 (b)、與其他生物活性化合物或藥劑的混合結合（特別 是非脊椎動物害蟲防治）（即活性成份）可導致一加— 大於二的效果（即協同作用）。因此可以降低活性成分 的環境排放量’同時確保有效之害蟲防治效果。當無脊 椎害蟲防治活性成分於施用比例展現農藝上足夠程度 之無脊椎動物害蟲防治協同作用，該組合可有益於減少 作物生產成本及降低環境負擔。 表D1列出無脊椎動物害蟲防治與化合物181 (如 索引表A中所示）作為成分（a)化合物之特定組合， 說明依據本發明包含的這些活性成分之混合物及組合 物和其使用方法。表D1第二襴列出該特定無脊椎動物 害蟲防治劑（例如：第一行中的「阿巴&gt;、丁（ abamectin )」）。 表D1第三欄列出該無脊椎動物害蟲防治劑作用模式 (若為已知）或化學種類。表D1的第四欄列出重量比 範圍的實施例’其比率為典型應用的非脊椎動物害蟲防 治藥劑相對於化合物181單獨或是結合組分（b)(例 如，「50:1到1:50」之阿巴汀在重量上相對於一化合物 181)。因此，例如表D1第一行具體揭露化合物181與 151284.doc •209· 201117722 阿巴、;丁（abamectin)的組合係通常以介於50:1至1:50 之間的重量比施用。表D1其餘行的架構類似。 表D1 成分（a) 無脊椎動物害蟲防治 劑 作用方式或化學 分類 通常 重量比 化合物181 阿巴汀 巨内酯環類 50:1 至 1:50 化合物181 亞滅培 新菸鹼類 150:1 至 1:200 化合物181 雙曱脒 縴胺受體配體類 200:1 至 1:100 化合物181 阿維菌素 巨内酯環類 50:1 至 1:50 化合物181 印棟素 脫皮激素促效劑 100:1 至 1:120 化合物181 貝塔-赛扶寧 鈉通道調控劑 150:1 至 1:200 化合物181 畢芬寧 鈉通道調控劑 100:1 至 1:10 化合物181 布芬淨 幾丁質合成抑制 劑 500:1 至 1:50 化合物181 培丹 沙蠶毒素類似物 100:1 至 1:200 化合物181 剋安勃 魚尼丁受體配體 100:1 至 1:120 化合物181 克凡派 線粒體電子傳遞 抑制劑 300:1 至 1:200 化合物181 陶斯松 膽鹼酯酶抑制劑 500:1 至 1:200 化合物181 可尼丁 新菸鹼類 100:1 至 1:400 化合物181 氰特破 (cyantraniliprole ) 魚尼丁受體配體 100:1 至 1:120 化合物181 赛扶寧 鈉通道調控劑 150:1 至 1:200 化合物181 赛洛寧 鈉通道調控劑 150:1 至 1:200 化合物181 赛滅寧 鈉通道調控劑 150:1 至 1:200 化合物181 赛滅淨 幾丁質合成抑制 劑 400:1 至 1:50 化合物181 第滅寧 鈉通道調控劑 50:1 至 1:400 151284.doc -210- 201117722 成分（a ) 無脊椎動物害蟲防治 劑 作用方式或化學 分類 通常 重量比 化合物181 地特靈 環雙烯殺蟲劑類 200:1 至 1:100 化合物181 達特南 新菸鹼類 150:1 至 1:200 化合物181 本蟲謎 脫皮抑制劑 150:1 至 1:200 化合物181 絕蟲靈 巨内酯環類 50:1 至 1:10 化合物181 安殺番 — 環雙烯殺蟲劑類 200:1 至 1:100 化合物181 益化利 鈉通道調控劑 100:1 至 1:400 化合物181 乙蟲清 GABA調節氣離子 通道阻斷劑 200:1 至 1:100 化合物181 芬硫克 150:1 至 1:200 化合物181 芬諾克 青春激素類似物 500:1 至 1:100 化合物181 芬化利 鈉通道調控劑 150:1 至 1:200 化合物181 芬普尼 GABA調節氣離子 通道阻斷劑 150:1 至 1:100 化合物181 氟尼胺 200:1 至 1:100 化合物181 氟蟲酿胺 魚尼丁受體配體 100:1 至 1:120 化合物181 氟芬隆 幾丁質合成抑制 劑 200:1 至 1:100 化合物181 六伏隆 幾丁質合成抑制 劑 300:1 至 1:50 化合物181 愛美松 線粒體電子傳遞 抑制劑 150:1 至 1:250 化合物181 益達胺 新終驗類 1000:1 至 1:1000 化合物181 因得克 鈉通道調控劑 200:1 至 1:50 化合物181 拉姆違·賽洛寧 鈉通道調控劑 50:1 至 1:250 化合物181 祿芬隆 幾丁質合成抑制 劑 500:1 至 1:250 化合物181 美派寧（meperfluthrin) 納通道調控劑 100:1 至 1:400 化合物181 美氟綜 200:1 至 1:200 151284.doc -211 · 201117722 成分（a) 無脊椎動物害蟲防治 劑 作用方式或化學 分類 通常 重量比 化合物181 納乃得 膽鹼酯酶抑制劑 500:1 至 1:100 化合物181 美賜平 青春激素類似物 500:1 至 1:100 化合物181 滅芬謹 脫皮激素促效劑 50:1 至 1:50 化合物181 烯啶蟲胺 新菸鹼類 150:1 至 1:200 化合物181 硝乙脲噻唑 新菸鹼類 150:1 至 1:200 化合物181 諾伐隆 幾丁質合成抑制 劑 500:1 至 1:150 化合物181 毆殺滅 膽鹼酯酶抑制劑 200:1 至 1:200 化合物181 派滅淨 200:1 至 1:100 化合物181 除蟲菊精 鈉通道調控劑 100:1 至 1:10 化合物181 畢達本 線粒體電子傳遞 抑制劑 200:1 至 1:100 化合物181 蟲丙 200:1 至 1:100 化合物181 百利普芬 青春激素類似物 500:1 至 1:100 化合物181 魚尼丁 魚尼丁受體配體 100:1 至 1:120 化合物181 賜諾特 巨内酯環類 150:1 至 1:100 化合物181 賜諾殺 巨内酯環類 500:1 至 1:10 化合物181 賜派芬 脂質生物合成抑 制劑 200:1 至 1:200 化合物181 曱蟎酯 脂質生物合成抑 制劑 200:1 至 1:200 化合物181 得芬諾 脫皮激素促效劑 500:1 至 1:250 化合物181 四氟醚菊酯 (Tetramethylfluthrin ) 鈉通道調控劑 100:1 至 1:40 化合物181 赛果培 新菸鹼類 100:1 至 1:200 化合物181 赛速安 新菸鹼類 1250:1 至 1:1000 化合物181 硫敵克 膽鹼酯酶抑制劑 500:1 至 1:400 化合物181 殺蟲雙 150:1 至 1:100 151284.doc -212- 201117722 成分（a ) 無脊椎動物害蟲防治 劑 作用方式或化學 分類 通常 重量比 化合物181 四溴菊酯 鈉通道調控劑 150:1 至 1:200 化合物181 唑財威 膽鹼酯酶抑制劑 250:1 至 1:100 化合物181 三福隆 幾丁質合成抑制 劑 200:1 至 1:100 化合物181 蘇力菌 生物劑 50:1 至 1:10 化合物181 蘇雲金芽孢桿菌δ内 毒素 生物劑 50:1 至 1:10 化合物181 核型多角體病毒（如， Gemstar ) 生物劑 50:1 至 1:10 表D2至D27除了「成分（a)」攔標題下項目分別 依下列成分（a)攔位名稱代替之外，其餘各以同上述 表D1之方式架構。因此，例如在表D2中，在「成分 (a)」攔標題下項目均列示為「化合物292」，在表D2 中欄標題下第一行具體揭露一種化合物292與阿巴汀 (abamectin)之混合物。表D3至D27架構類似。 表格代號 成分（a)欄位名稱 表格代號 成分（a)欄位名稱 D2 化合物292 D15 化合物524 D3 化合物469 D16 化合物525 D4 化合物513 D17 化合物526 D5 化合物514 D18 化合物527 D6 化合物515 D19 化合物528 D7 化合物516 D20 化合物529 D8 化合物517 D21 化合物530 D9 化合物518 D22 化合物531 D10 化合物519 D23 化合物532 D11 化合物520 D24 化合物533 151284.doc -213- 201117722 D12 化合物521 D25 化合物534 D13 化合物522 D26 化合物535 D14 化合物523 D27 化合物536 一非脊椎動物害蟲防治劑（例如：殺蟲劑及殺蟎劑） 欲與組分（a)之化合物混合之實施例，該組分（a)之 化合物包含納通道調控劑，如畢芬寧（bifenthrin)、赛 滅寧（cypermethrin)、赛洛寧（cyhalothrin)、X-賽洛寧 (lambda-cyhalothrin)、赛扶寧（cyfluthrin)、貝他-赛 扶寧（beta-cyfluthrin )、第滅寧（deltamethrin )、四氟 曱驗菊酉旨（dimefluthrin)、益化利（esfenvalerate)、芬 化利（fenvalerate )、因得克（indoxacarb )、美派寧 (meperfluthrin )、曱氧苄氟菊酯（metofluthrin )、丙氣 菊酯（profluthrin )、除蟲菊（pyrethrin )、四氟醚菊酯 (tetramethylfluthrin )及泰滅寧（tralomethrin );膽驗 酯酶抑制劑，如陶斯松（chlorpyrifos )、納乃得 (methomyl )、oxamyl、硫敵克（thiodicarb )及 triazamate ;新終驗類（neonicotinoids )，如亞滅培 (acetamiprid )、可尼丁（ clothianidin )、達特南 (dinotefuran )、益達胺（imidacloprid )、烯咬蟲胺 (nitenpyram)、尼殺赛（nithiazine)、赛果培（thiacloprid) 及赛速安（thiamethoxam );殺蟲的巨環内醋（macrocyclic lactones )’ 如賜托拉（spinetoram )、賜諾殺（spinosad)、 阿巴汀（abamectin )、阿佛菌素（avermectin )及因滅ί丁 (emamectin);受GABA (γ-氨基丁酸）調控之氯通道 阻斷劑’例如安殺番（end〇sulfan)、乙蟲清（ethiprole) 151284.doc •214- 201117722 及芬普尼（fipronil );幾丁質合成抑制劑，如布芬淨 (buprofezin)、賽滅淨（cyromazine)、氟芬隆、六伏隆 (hexaflumuron )、祿芬隆（iufenuron )、諾伐隆 (novaluron )、諾伏隆（noviflumuron )及三福隆 (triflumuron );青春激素類似物，如苯蟲趟 (diofenolan )、fenoxycarb，美賜平（methoprene )及百 利普芬（pyriproxyfen );章魚胺（oct〇pamine )接受器 配體接受器配體’例如，三亞瞒（amitraz );蜆皮激素 促效劑，如印楝素（azadirachtin )、滅芬諾 (methoxyfenozide)及得芬諾（tebufenozide);魚尼丁 (ryanodine)接受器配體，如魚尼丁（ryan〇dine)、鄰 胺苯曱二醯胺（anthranilic diamides )，如姓安勃 (chlorantraniliprole)、氰特破（cyantraniliprole)及氟 蟲醯胺（flubendiamide);沙蠶毒素類似物（nereistoxin analogs)，如培丹（cartap);粒線體電子傳遞抑制劑， 如克凡派（chlorfenapyr )、愛美松（hydramethylnon ) 及畢達本（pyridaben );脂質合成抑制劑，如賜派芬 (spirodiclofen)及螺甲蜗酉旨（spiromesifen);環雙烯殺 蟲劑，如地特靈（dieldrin);赛芬蜗（cyflumetofen); 芬硫克（fenothiocarb);氟尼胺（flonicamid);美氟综 (metaflumizone); °比°秦氣蟲腈（pyrafluprole);咬蟲丙 醚（pyridalyl );。比啶氟美腈（pyriprole );派滅淨 (pymetrozine );螺蟲乙酯（spirotetramat);及殺蟲單 (thiosultap-sodium)。一生物製劑欲與組分（a)之化 合物混合之實施例，該組分（a)之化合物包括核多角 體病毒如HzNPV及AfNPV;蘇力菌及蘇力菌之囊封δ- 151284.doc -215- 201117722 内毒素’如細胞冠、MPV及MPVII ;以及天然及基因 重組病毒殺蟲劑，包含桿狀病毒科的成員以及食蟲的真 菌。值得注意的是一種包括成分(a)及至少一種選自上面 表D1中所列無脊椎動物害蟲防治劑之其他生物活性化 合物或劑之組合物。 本發明之組合物可用作為植物病害防治劑。本發明 因此進一步包含一種防治真菌植物病原體所引起植物 病害之方法，其包含對植物或其欲保護部分或欲保護植 物種子或欲保護無性繁殖單元施用有效量之本發明之 組合物（例如一包含組分（a)及（b)之組合物）。也 可以將本發明的這個面向描述成—種用於保護植物或 植物種子免於由真菌病原體所引起病害的方法，包含向 該植物（或其-部分）或植物種子施予—殺真菌有效量 的本發明之組合物（直接錢過難物或植物種子 境（例如生長介質））。 义 植物病害防治-般係藉由於感染前或❹後，向該 植物之欲保護部分，如根、莖、葉子、果實、種子、塊 莖或鱗莖，或是向該欲賴植物所生長之介質（土 沙），施予-有效劑量的本發明之組合物（例如：包含 一組分⑴*⑴之混合物），其典型為—處方^ =:!種子施予該混合物以保護該種子，以及向： =::=該化合物。也一用水施 ^本發明之混合物及組合物_當比率（例如· 劑量、殺真菌有效劑量或殺昆 . 會受許多魏料㈣，雜實較时科定當施 I51284.doc -216. 201117722 用=活性成分比率從少於約1 g/ha到約5,000 g/ha時， 通裇可以保護葉子。當向種子施用的比率從約每公斤種 子〇.1到約10 g時，通常可以保護種子和幼苗；且當向 無眭繁殖單元（例如：插枝及塊莖）施用的比率從約每 △斤無性繁殖單元〇.1到約1〇 g時，通常可以保護無性 繁殖單元。須提供所欲範圍之植物保護及植物病害以及 視情況之其餘植物害蟲的防治之熟習該領域之技藝人 士可經由簡單實驗輕易決定包含本發明活性成分之特 疋組合的混合物及組合物的施用比率。 式1之化合物、其N-氧化物及其鹽類對防治真菌 致病原所引起的植物病害尤其有效。這些化合物與其它 殺真菌化合物的混合能防治由擔子菌綱、子囊菌綱、卵 菌綱及不完全菌綱中廣泛真菌植物病原體所引起的病 害。因此’此處所描述之混合物或組合物能防治廣泛的 植物病害’作物的葉片病原體包括：穀類作物，例如： 小麥（wheat)、大麥（wheat)、燕麥（wheat)、黑麥（rye)、 小黑麥（triticale)、稻米（dce)、玉米（maize)、高粱 (sorghum )及小米（);藤本作物，例如：食用 葡萄（table grapes )及酒葡萄（wine grapes );田間作 物’例如：油菜（oilseed rape )(芥花籽油（canola ))、 向曰葵（sunflower);甜菜（sugar beets )、甘蔗（ sugar cane )、黃豆（soybean )、花生（peanuts )(落花生 (groundnut))、菸草（t〇bacco )、紫花苜蓿（alfafa)、 苜蓿（clover)、胡枝子（iespedeza)、百脈根（trefoil) 及苕子（vetch);梨果，例如：蘋果（appie)、梨（pear)、 海棠果（crabapple)、枇杷（loquat)、mayhaw 及棍梓 -217- I51284.doc 201117722 (quince );核果，例如：桃子（peaches )、櫻桃（cherries )、 梅子（plums)、杏仁（apricots)、油桃（nectarines)及 杏仁（almonds);柑橘類水果，例如：檸檬（lemons)、 萊姆（limes)、甜撥（oranges)、葡萄柚（grapefruit)、 柑（mandarin )(紅橘（tangerines ))及金桔（kumquat); 根菜類以及田間作物（及其葉子），例如：朝鮮薊 (artichoke )、根甜菜（garden beet)及甜菜（sugar beet)、 胡蘿蔔（carrot)、樹薯（cassava)、薑（ginger )、人參 (ginseng )、山葵（horseradish )、防風（parsnip )、馬 鈴薯（potato )、蘿 g ( radish )、蒸青甘藍（rutabaga )、 番薯（sweet potato )、蒸菁（turnip )及山藥（yam ); 鱗莖類蔬菜，例如：大蒜（garlic )、韭菜（leek)、洋蔥 (onion)及青蔥（shallot);葉菜類，例如：芝麻菜（arugula (roquette ))、芹菜（celery )、水芹（cress )、苦苣（endive ) (菊苣（escarole))、小茴香（fennel)、結球萵苣（head lettuce )及葉萵苣（leaf lettuce )、洋完荽（parsley )、 紫萵苣（radicchio )(紅包生菜（red chicory ))、大黃 (rhubarb)、菠菜（spinach)及紅頭菜（Swiss chard); 十字花科（芸苔屬植物）葉菜類，例如：青花菜 (broccoli )、蕪青（broccoli raab )(硬花甘藍（rapini))、 球芽甘藍（Brussels sprouts )、甘藍菜（cabbage )、小白 菜（bok choy )、花椰菜（cauliflower )、羽衣甘藍 (collards )、芥藍（kale )、球莖甘藍（kohlrabi )、雪菜 (mustard greens);豆類蔬菜（肉汁植物或dried)，例 如：羽扇豆（lupin)、豆（菜豆屬（Phaseolus spp.))(包 括四季豆（field bean)、菜豆（kidney bean)、皇帝豆（lima 151284.doc •218· 201117722 bean )、敏豆（navy bean )、黑白斑豆（pinto bean )、红 花菜豆（runner bean )、菜豆（snap bean )、寬葉菜豆 (tepary bean )及蠛豆（wax bean ))、豆（紅豆屬）（包 括紅豆（adzuki bean )、裙帶豆（asparagus bean )、黑眼 豆（blackeyed pea)、紅豆（catjang )、中國長豆（Chinese longbean )、豇豆（cowpea )、克羅得婉豆（crowder pea )、 蝴蝶豆（moth bean )、綠豆（mung bean )、赤小豆（rice bean)、南豆（southern pea)、黑綠豆（urd bean)及菜 豆仔（yardlongbean))、蠶豆（broadbean (fava))、鷹 嘴豆（chickpea )(雞兒豆（garbanzo ))、膠豆（guar )、 大豆（jackbean)、白爲豆（lablab bean)、扁豆（lentil) 及婉豆（pea)(婉豆屬（Pisum spp.))(包括低矮型婉 豆（dwarf pea)、密糖豆（edible-podded pea)、甜婉豆 (English pea)、紅花豌豆（field pea)、豌豆（garden pea)、疏豆仁（green pea)、荷蘭豆（snowpea)、蜜豆 (sugar snap pea )、樹豆（pigeon pea )及黃豆 (soybean ));果菜類，例如：蘇子（eggpiant)、酸漿 (groundcherry )(酸漿屬（Physalis spp.))、香瓜茄 (pepino)及胡椒（包括甜椒（bell pepper)、辣椒（chili pepper )、料理用胡椒（co〇king pepper )、番椒 (pimento )、青栳ι ( sweet pepper );綠番茄（tomatillo ) 及番茄（tomato);瓜類蔬菜，例如：佛手瓜（Chayote) (果實）、冬瓜（Chinese waxgourd) ( Chinese preserving melon)、酶菜用西瓜（citron melon)、黃瓜（cucumber)、 胡瓜（gherkin)、可食用的葫蘆科植物（ediblegourd) (包括葫蘆（hyotan )、南瓜（cucuzza)、絲瓜（hechima) 151284.doc •219· 201117722 及十角絲瓜（Chinese okra ))、苦瓜屬（Momordica spp.) (包括苦瓜（balsam apple )、苦瓜（balsam pear )、苦瓜 (bittermelon )及小黃瓜（Chinese cucumber ))、綱紋甜 瓜（muskmelon )(包括洋香瓜（cantaloupe )及南瓜 (pumpkin))、南瓜（summer and winter squash)(包括 奶油瓜（butternut squash )、南瓜（calabaza )、筍瓜 (hubbard squash )、橡果形南瓜（acorn squash )、義大 利麵瓜（spaghetti squash ))以及西瓜（watermelon ); 聚果，例如：黑莓（blackberry )(包括賓格爾莓 (bingleberry )、波伊森每（boysenberry )、露珠每 (dewberry )、羅甘梅（l〇wberry )、紫藍每 (marionberry )、olallieberry 及小红每（youngberry ))、 藍每（blueberry )、蔓越苺（cranberry )、穗醋栗（currant)、 接骨木果實（elderberry)、醋栗（g00Seberry)、越橘果 (huckleberry )、羅甘梅（loganberry )、覆盆子（raspberry ) 以及草莓（strawberry);堅果，例如：杏仁（aim〇nd)、 山毛櫸堅果（beechnut)、巴西栗子（Brazil nut)、白胡 桃（butternut )、腰果（cashew )、栗實（chestnut )、毛 枝栗（chinquapin )、大榛子（filbert)(榛（hazelnut))、 山核桃（hickorynut)、澳洲胡桃（macadamianut)、胡 桃（pecan)及胡桃（wainut);熱帶果樹與其他作物， 例如：香蕉（bananas )、巴氏蕉（plantains )、芒果 (mangos )、椰子（coconuts )、木瓜（papaya )、番石榴 (guava)、路梨（avocad〇)、荔枝（lichee)、龍舌蘭 (agave)、咖啡（coffee)、可可（caca〇)、甘蔗 (sugar cane )、油棕櫊（〇il paim)、芝麻（sesame )、橡膠（mbber ) 151284.doc •220· 201117722 以及香料（spices);纖維作物，例如：棉花（cotton)、 亞麻（flax )以及麻（hemp );草坪植物（包括暖季性 (warm-season)及冷季性（cool-season)草坪），例如 小糖卓（bentgrass)、肯塔基藍草（Kentucky bluegrass)、 奥古斯丁卓（St. Augustine grass )、高牛毛草（tall fescue ) 以及狗牙根草（Bermuda grass)。 該等病原體包括：卵菌綱，包括疫病菌 (Phytophthora )疾病’例如：晚疫病菌（Phytophthora infestans)、大丑疫病菌（Phytophthora megasperma)、 煙草寄生疫菌（Phytophthora parasitica )、酷·梨疫病菌 (Phytophthora cinnamomi )以及茄科作物疫病菌 (Phytophthora capsici)、腐黴菌（Pythium)疾病，例 如：坪草腐黴枯萎病菌（Pythium aphanidermatum )，及 霜黴科（Peronosporaceae family ) 疾病，如：葡萄霜黴 病菌（Plasmopara viticola )、包葉菜類露菌（Peronospora spp.)(包括終草露菌病菌（Peronosporatabacina)以及 白菜露菌（Peronospora parasitica ))、瓜類露菌病菌 (Pseudoperonospora spp.)(包括胡瓜露菌 (Pseudoperonospora cubensis ))以及萵苣露菌（Bremia lactucae );子囊菌（Ascomycetes )，包括斑病菌 (Alternaria)疾病，例如：番祐早疫病菌（Alternaria solani)及甘藍黑斑病菌（Alternaria brassicae)，炫 f 菌 (Guignardia)疾病，例如：葡萄球痤菌（Guignardia bidwelli)，蘋果黑星病菌（Venturia)疾病，例如：蘋 果黑星病菌（Venturia inaequalis )，斑枯病（Septoria diseases)’ 例如：麥穎枯病菌（Septorianodorum)及小 151284.doc •221 · 201117722 麥葉斑病菌（Septoria tritici)，白粉菌（powdery mildew ) 疾病，包括：白粉菌屬（Blumeria spp.)(包括小麥白粉 病（Blumeria graminis))以及白粉菌屬（Erysiphe spp.) (包括亞麻白粉病菌（Erysiphe polygoni))、葡萄白粉 病菌（Uncinula necatur)、南瓜白粉病菌（Sphaerotheca fuligena ) 及梨果類白粉病菌（Podosphaera leucotricha )、小麥基腐病菌（Pseudocercosporella herpotrichoides) ’ 灰黴病菌（Botrytis)疾病，例如··灰 葡萄孢菌（Botrytis cinerea )、褐腐病菌（Monilinia fructicola)，菌核菌（Sclerotinia)疾病，例如：菌核病 菌（Sclerotiniasclerotiorum)、稻熱病菌（Magnaporthe grisea)、葡萄枝枯病（Phomopsis viticola)，麥類胡麻葉 炫f菌屬（Helminthosporium)疾病，例如：小麥德氏 黴菌（Helminthosporium tritici repentis )、大麥網斑病菌 (Pyrenophora teres)，炭疽病(anthracnose)疾病，例 如：小叢殼屬（Glomerella)或刺盤孢屬（Colletotrichum spp.)(包括炭疽病菌（Colletotrichum graminicola)及 瓜類炭疽病菌（Colletotrichum orbiculare))以及小麥全 名虫病菌（Gaeumannomyces graminis );擔子菌 (Basidiomycetes)，包括由銹病菌屬（Puccinia spp.)(例 如：麥類葉銹病菌（Puccinia recondita)、小麥條銹病菌 (Pucciniastriiformis)、大麥柄鎮菌（Pucciniahordei)、 小麥桿銹菌（Puccinia graminis )及落花生銹病（Puccinia arachidis))、咖啡錄病菌（Hemileiavastatrix)以及大豆 錄菌（Phakopsora pachyrhizi )所引起的錄病（rust diseases );其他病原體包含絲核菌屬（Rhizoctonia spp.) 151284.doc -222- 201117722 (例如：立枯絲核菌（Rhizoctoniasolani)及水稻絲核 菌（Rhizoctoniaoryzae));梭黴菌（Fusarium)疾病， 例如：康乃馨莖腐病菌（Fusarium roseum )、禾谷鐮刀 菌（Fusarium graminearum )以及唐菖蒲尖鐮孢菌 (Fusarium oxysporum);棉花黄萎病菌（Verticillium dahliae );白絹病菌（Sclerotium rolfsii);大麥雲紋病菌 (Rynchosporium secalis);球座尾孢菌（Cercosporidium personatum )、落花生褐斑病菌（Cercospora arachidicola) 以及甜菜褐斑病菌（Cercospora beticola) ; Rutstroemia floccosum (亦稱為 Sclerontina homoeocarpa);以及其 他和這些致病源緊密相關的屬和物種。某些殺真菌化合 物亦有殺細菌效果，因此除了它們的殺真菌活性，該組 合物或其結合體亦有對抗細菌之活性，例如：梨及蘋果 火傷病菌（Erwinia amylovora )、黃原桿菌（Xanthomonas campestris)、菜豆斑點病菌（Pseudomonas syringae)， 以及其他相關的種。 本發明的殺真菌組合物，組分（a)之該式1化合 物可與附加的組分（b)之殺真菌化合物協同作用以提 供上述的有益結果，其為擴大受防治的植物疾病之範 圍、延長預防性或治療性保護之持續時間、以及抑制抗 藥性真菌致病體的增生。在特定實施例中，按照本發明 所提供、包含部分之組分（a)及組分（b)之組合物， 對於防治特定真菌疾病特別有效（例如：馬鈴薯夏疫病 菌（Alternaria solani)、小麥白粉病菌（Blumeria graminis f. sp. tritici)、灰黴病菌（Botrytis cinerea)、小麥葉錄病 菌（Puccinia recondita f. sp. tritici )、立枯絲核菌 151284.doc -223- 201117722 (Rhizoctonia solani )、麥穎枯病菌（Septoria nodorum )、小麥葉斑病菌（sept〇ria tritici) ) 〇 殺真菌劑之混合物基於各組分之活性，亦可能提供 較預測明顯更佳之疾病防治。此種協作用經描述為「混 合物中兩種成分之合作行為，使總效較此兩種（或多種） 之效果各自發揮之總和更為顯著或持久」（見R M. L.Acetoprole, h point h, β, _ J ^ J : Aachen, mu Dongwei, Ami Xi Brown (amid()flumet), 151284.doc Aachen Afu, Azadirachtin , cotton-prepared methyl, Bifen-Ning, -207· 201117722 联本肼g日,必撕传福轮(bistr^uron), 布芬净, cough dan, Pei Dan, 螨 螨 、, 克凡派, 氟Pyridine, Keanbo, Taosson, pottery, pine-methyl, acaricidal ester, ringworm, cotinine, cyanide, race: 螨, Sai Fanning, p_赛扶宁,赛洛宁, γ_赛洛宁, λ_赛洛甲,三环锡,赛灭宁,赛灭净,第灭宁, dibutyl ether urea, diazinon, Kailesan, dieldrin, in addition to 螨灵, 除Insect urea, tetrafluthrin, dimethoate, dinotefuran, behenil, emamectin, endosulfan, fenvalerate, acetaminophen, acetazol, phenylphosphine, quinacridone , phenbutyltin, stupid thiophene, phenoxycarb, fenvalerate, oxazolidine, fenvalerate, fipronil, fluramide, flufenamide, chloramphenicol, head, fluoroamine Cypermethrin, flufenerim, flufenadol, fonophos, chlorfenapyr , fluoroquinone urea, thiazolone, fluoroantimony, neonicotinoids, imidacloprid, indoxacarb, isopphos, chlorfensulfuron, malathion, perperfluthrin, cyanofluorfen , tetraacetaldehyde, methotrexate, chlorpyrifos, methomyl, methoprene, methoxychlor, methoxy, oxime flumethrin: long-acting dish, thin. Insectamine, nithiazine, fluoroburea, noviflumuron, chlorpyrifos, parathion, sulfonium parathion, fenvalerate, phorate, ubiquinone, Isocarbophos, phosphonamine, anti-Ziwei, C-drug, profluthrin, gram, protrifenbute, pymetrozine, pyrazop sincerazine, pyrethrum vinegar,哒, pyridine propyl ether, piranbufenazon, η than biting fluramide, pyriproxyfen, rotenone, lanni, donola, spinosad, spiridiclofen, Spiroester, spirotetrazol, sulfoxaflor, thiocarbamate, tebufenozide, pyridoxamine, fumonis, rifampin, tofusone, insecticide, tetramethyl Listen (tetramethylfluthin), sing linlin, sputum, shuangwei, insecticide 151284.doc •208- 201117722 bis, defenfen, tai ning, β sitting weiwei, trichlorfon, chlorpyrifos, su Bacillus thuringiensis subsp. aizawai, Bacillus thuringiensis subsp. kurstaki, nucleopolyhedro viruses, Encapsulated S. faecalis δ-endotoxin, baculovirus, entomopathogenic bacterium, entomopathogenic virus, and insect pathogen fungi. It is worth noting that the above list excludes meperflutrin, sulfoxaflor and tetrafluthrin. In such an instance, the compound (a) alone or in combination with component (b), with other biologically active compounds or agents (especially invertebrate pest control) (ie active ingredient) may result in one plus - greater than The effect of two (ie synergy). Therefore, it is possible to reduce the environmental emissions of the active ingredient while ensuring effective pest control effects. When the non-ridged pest control active ingredient exhibits a synergistic effect on agronomically sufficient levels of invertebrate pest control, the combination can be beneficial in reducing crop production costs and reducing environmental burden. Table D1 lists invertebrate pest control and Compound 181 (as shown in Index Table A) as a specific combination of the components (a), illustrating mixtures and compositions of these active ingredients and methods of use thereof in accordance with the present invention. The specific invertebrate pest control agent is listed in the second column of Table D1 (for example: "Abba>, abamectin" in the first line). The third column of Table D1 lists the mode of action (if known) or chemical species of the invertebrate pest control agent. The fourth column of Table D1 lists examples of weight ratio ranges 'the ratio of typical applications of the non-vertebrate pest control agent relative to compound 181 alone or to component (b) (eg, "50:1 to 1: 50" of ababatin is relative in weight to a compound 181). Thus, for example, the first row of Table D1 specifically discloses that the combination of compound 181 and 151284.doc • 209· 201117722 aba, ab (abamectin) is usually applied in a weight ratio of between 50:1 and 1:50. The architecture of the remaining rows of Table D1 is similar. Table D1 Ingredients (a) Invertebrate pest control agent mode of action or chemical classification usually weight ratio compound 181 Abatatin giant lactone ring 50:1 to 1:50 Compound 181 Sub-exeter neonicotinoid 150:1 to 1:200 Compound 181 Biguanide Fibrin Receptor Ligand Class 200:1 to 1:100 Compound 181 Avermectin Macrolide Form 50:1 to 1:50 Compound 181 Indoline Ecdysone Agonist 100:1 to 1:120 Compound 181 Beta-Syrene Sodium Channel Regulator 150:1 to 1:200 Compound 181 Bifenin Sodium Channel Modulator 100:1 to 1:10 Compound 181 Buffing Net Chitin Synthetic Inhibitor 500:1 to 1:50 Compound 181 Pedanone Silkworm Toxin Analog 100:1 to 1:200 Compound 181 gram Anbendene Receptor Ligand 100:1 to 1:120 Compound 181 克凡派 mitochondrial electron transport Inhibitor 300:1 to 1:200 Compound 181 Tausson cholinesterase inhibitor 500:1 to 1:200 Compound 181 Cotinine neonicotinoid 100:1 to 1:400 Compound 181 Cyantraniliprole fish Nitin Receptor Ligand 100:1 to 1:120 Compound 181 Saifu Ning Channel Regulation Agent 150:1 to 1:200 Compound 181 Ceylonine Channel Regulator 150:1 to 1:200 Compound 181 Saline sodium channel modulator 150:1 to 1:200 Compound 181 Race-killing chitin synthesis inhibition Agent 400:1 to 1:50 Compound 181 Sodium sulfonate channel modulator 50:1 to 1:400 151284.doc -210- 201117722 Ingredient (a) Invertebrate pest control agent mode of action or chemical classification usually weight ratio compound 181 Diltia ring diene insecticides 200:1 to 1:100 Compound 181 Datnam neonicotinoids 150:1 to 1:200 Compound 181 This worm engraving inhibitor 150:1 to 1:200 compound 181 chlorfenapyr macrolactone ring 50:1 to 1:10 compound 181 amphibians - cyclodiene insecticides 200:1 to 1:100 compound 181 sulfonate channel modulator 100:1 to 1 :400 Compound 181 Ethionine GABA-regulated gas ion channel blocker 200:1 to 1:100 Compound 181 Fensulfide 150:1 to 1:200 Compound 181 Fenol youth hormone analogue 500:1 to 1:100 Compound 181 Fenicide Sodium Channel Regulator 150:1 to 1:200 Compound 181 Fenpney GABA Regulating gas ion channel blockers 150:1 to 1:100 Compound 181 Fluoramide 200:1 to 1:100 Compound 181 Flurazine enriched nicotine receptor ligand 100:1 to 1:120 Compound 181 Flufin Chitin synthesis inhibitor 200:1 to 1:100 Compound 181 Hexabolidine chitin synthesis inhibitor 300:1 to 1:50 Compound 181 Amesson mitochondrial electron transport inhibitor 150:1 to 1:250 Compound 181 IFA New Final Test Class 1000:1 to 1:1000 Compound 181 Indac Channel Channel Regulator 200:1 to 1:50 Compound 181 Ramine Ceylonine Channel Regulator 50:1 to 1:250 Compound 181 Lucendron Chitin Synthetic Inhibitor 500:1 to 1:250 Compound 181 meperfluthrin Nanochannel Modulator 100:1 to 1:400 Compound 181 US Fluoride 200:1 to 1:200 151284 .doc -211 · 201117722 Ingredients (a) Invertebrate pest control agent mode of action or chemical classification usually weight ratio compound 181 Na Na cholinesterase inhibitor 500:1 to 1:100 Compound 181 Meisping Youth hormone similar 500:1 to 1:100 Compound 181 Agonist 50:1 to 1:50 Compound 181 Nitenpyram Neonicotinoid 150:1 to 1:200 Compound 181 Nitroacetamide Thiazole Neonicotinoid 150:1 to 1:200 Compound 181 Norvaron Chitin synthesis inhibitor 500:1 to 1:150 Compound 181 殴Cholesteryl esterase inhibitor 200:1 to 1:200 Compound 181 Derived from 200:1 to 1:100 Compound 181 Pyrethrin sodium Channel Modulator 100:1 to 1:10 Compound 181 Pythaben mitochondrial electron transport inhibitor 200:1 to 1:100 Compound 181 Insect C: 200:1 to 1:100 Compound 181 Bollipfen Youth Hormone Analog 500: 1 to 1:100 Compound 181 Fish Nitinus Nitin Receptor Ligand 100:1 to 1:120 Compound 181 Schnottrolactone Ring 150:1 to 1:100 Compound 181 Schnauzer Co-Lactone Ring Class 500:1 to 1:10 Compound 181 Schiffin Lipid Biosynthesis Inhibitor 200:1 to 1:200 Compound 181 Oxime Ester Lipid Biosynthesis Inhibitor 200:1 to 1:200 Compound 181 Defenotropin Pharmacology 500:1 to 1:250 Compound 181 Tetramethylfluthrin Sodium channel modulator 100:1 1:40 Compound 181 Sai Pei Xin Nicotine 100:1 to 1:200 Compound 181 Sai Anxin Nicotine 1250:1 to 1:1000 Compound 181 Sulfuric Acid Cholinesterase Inhibitor 500:1 to 1:400 Compound 181 insecticidal double 150:1 to 1:100 151284.doc -212- 201117722 Ingredients (a) Invertebrate pest control agent mode of action or chemical classification usually weight ratio compound 181 tetramethrin sodium channel regulator 150:1 to 1:200 Compound 181 Oxalcone cholinesterase inhibitor 250:1 to 1:100 Compound 181 Sanfullon chitin synthesis inhibitor 200:1 to 1:100 Compound 181 Suramycin biologic agent 50:1 to 1:10 Compound 181 Bacillus thuringiensis δ Endotoxin Bioagent 50:1 to 1:10 Compound 181 Nuclear Polyhedrosis Virus (eg, Gemstar) Biological Agent 50:1 to 1:10 Tables D2 to D27 except The items under the heading (a) are replaced by the following components (a), and the rest are structured in the same manner as Table D1 above. Therefore, for example, in Table D2, the items under the heading "Component (a)" are listed as "Compound 292", and the first line under the column heading in Table D2 specifically discloses a compound 292 and abbatectin. a mixture. The tables D3 to D27 are similar in structure. Table Code Component (a) Field Name Table Code Component (a) Field Name D2 Compound 292 D15 Compound 524 D3 Compound 469 D16 Compound 525 D4 Compound 513 D17 Compound 526 D5 Compound 514 D18 Compound 527 D6 Compound 515 D19 Compound 528 D7 Compound 516 D20 Compound 529 D8 Compound 517 D21 Compound 530 D9 Compound 518 D22 Compound 531 D10 Compound 519 D23 Compound 532 D11 Compound 520 D24 Compound 533 151284.doc -213- 201117722 D12 Compound 521 D25 Compound 534 D13 Compound 522 D26 Compound 535 D14 Compound 523 D27 Compound 536 - a non-vertebrate pest control agent (for example, an insecticide and an acaricide). An example of a compound to be mixed with a compound of the component (a), the compound of the component (a) comprising a nanochannel modulator, such as Bifenthrin, cypermethrin, cyhalothrin, lambda-cyhalothrin, cyfluthrin, beta-cyfluthrin, Detamethrin, tetrahydroquinone, dimefluthrin, esfenva Lerate), fenvalerate, indoxacarb, meperfluthrin, metofluthrin, profluthrin, pyrethrin, four Tetramethylfluthrin and tralmethrin; cholesteryl esterase inhibitors such as chlorpyrifos, methomyl, oxamyl, thiodicarb and triazamate; new final test (neonicotinoids), such as acetamiprid, clothianidin, dinotefuran, imidacloprid, nitenpyram, nithiazine, fruit Thiacloprid and thiamethoxam; insecticidal macrocyclic lactones such as spinetoram, spinosad, abamectin, avermectin (avermectin) and emamectin; chloride channel blockers regulated by GABA (γ-aminobutyric acid), such as end〇sulfan, ethiprole 151284.doc •214 - 201117722 and Fipney (fipronil Chitin synthesis inhibitors, such as buprofezin, cyromazine, flufenadol, hexaflumuron, iufenuron, novaluron, novo Noviflumuron and triflumuron; youth hormone analogues such as diofenolan, fenoxycarb, metoprene and pyriproxyfen; octopamine (oct〇pamine) Receiver ligand acceptor ligands 'eg, amitraz; ecdysone agonists such as azadirachtin, methoxyfenozide, and tebufenozide; Ryanodine) receptor ligands such as ryan〇dine, anthranilic diamides, such as chlorantraniliprole, cyantraniliprole, and flubendiamide ); Nereistoxin analogs, such as cartap; mitochondrial electron transport inhibitors such as chlorfenapyr, hydramethylnon, and pyridaben; lipid synthesis Inhibitor (spirodiclofen) and spiromesifen; cyclodiene insecticides, such as dieldrin; cyflumetofen; fenothiocarb; flonicamid; Metaflumizone; ° ratio ° pyraprol (pyrafluprole); bitumin pyridalyl (pyridalyl); Pyriprole; pyrmetrozine; spirotetramat; and thiosultap-sodium. An embodiment in which a biological preparation is to be mixed with a compound of the component (a), and the compound of the component (a) includes a nuclear polyhedrosis virus such as HzNPV and AfNPV; and the encapsulation of S. cerevisiae and S. cerevisiae δ-151284.doc -215- 201117722 Endotoxins such as cell crowns, MPV and MPVII; and natural and genetic recombinant virus insecticides, including members of the baculoviridae and insectivorous fungi. Of note is a composition comprising ingredient (a) and at least one other biologically active compound or agent selected from the group consisting of the invertebrate pest control agents listed in Table D1 above. The composition of the present invention can be used as a plant disease controlling agent. The invention therefore further comprises a method of controlling a plant disease caused by a fungal plant pathogen comprising administering to the plant or a part thereof to be protected or to protect the plant seed or to protect the vegetative propagation unit an effective amount of the composition of the invention (for example one A composition comprising components (a) and (b)). It is also possible to describe this aspect of the invention as a method for protecting a plant or plant seed from a disease caused by a fungal pathogen, comprising administering to the plant (or a portion thereof) or plant seed a fungicidal effective amount The composition of the present invention (direct money or plant seed environment (e.g., growth medium)). Control of plant diseases - by means of pre- or post-infection, to the protected parts of the plant, such as roots, stems, leaves, fruits, seeds, tubers or bulbs, or to the medium in which the plants are grown ( Soil-sand), an effective dose of a composition of the invention (eg, comprising a mixture of components (1)*(1)), typically -prepared ^=:! seed is applied to the mixture to protect the seed, and : =::= This compound. Also, the mixture and the composition of the present invention are used as a ratio (for example, a dose, a fungicidal effective dose or a killing of Kun. It is subject to a lot of Wei (4), and it is used in the application of I51284.doc -216. 201117722 When the active ingredient ratio is from less than about 1 g/ha to about 5,000 g/ha, the leaves can be protected by overnight. When the ratio of application to the seed is from about 每1 to about 10 g per kg of seed, the seed can usually be protected. And seedlings; and when applied to innocent breeding units (eg, cuttings and tubers) from about △1 to about 1 〇g per gram of vegetative propagation unit, vegetative propagation units are usually protected. The plant protection and plant diseases as well as the control of the remaining plant pests as desired. Those skilled in the art can readily determine the application rates of the mixtures and compositions comprising the particular combination of active ingredients of the present invention by simple experimentation. The compound of 1, its N-oxide and its salts are particularly effective for controlling plant diseases caused by fungal pathogens. The mixing of these compounds with other fungicidal compounds can control the basidiomycetes and ascus. Diseases caused by a wide range of fungal plant pathogens in the fungi, oomycetes and incomplete genus. Therefore, the mixture or composition described herein is capable of controlling a wide range of plant diseases. The leaf pathogens of the crop include: cereal crops, for example: wheat (wheat), wheat, wheat, rye, triticale, rice (dce), corn (maize), sorghum (sorghum) and millet (); vine crops, for example : table grapes and wine grapes; field crops such as oilseed rape (canola), sunflower, sugar beets, sugar cane (sugar beets), sugar cane (sugar beets), sugar cane (sugar beets), sugar cane (sugar beets), sugar cane (sugar beets) Sugar cane ), soybean, peanuts (groundnut), tobacco (t〇bacco), alfalfa (alfafa), clover, iespedeza, trefoil And vetch; pear fruit, for example: apple (appie), pear (pear), crab apple (crabapple), loquat, mayhaw and stick-217- I51284.doc 201117722 (quince); For example: peach (pea Ches ), cherries, plums, apricots, nectarines and almonds; citrus fruits such as lemons, limes, oranges , grapefruit, mandarin (tangerines) and kumquat; root vegetables and field crops (and their leaves), for example: artichoke, garden beet And sugar beet, carrot, cassava, ginger, ginseng, horseradish, parsnip, potato, radish, steamed Brutabaga, sweet potato, turnip, and yam; bulbous vegetables such as garlic, leek, onion, and satlot; leafy vegetables For example: arugula (roquette), celery, cress, endive (escarole), fennel, head lettuce and leaf lettuce (leaf lettuce ) Parsley, radicchio (red chicory), rhubarb, spinach, and red wine (Swiss chard); cruciferous (Brassica) leafy vegetables, for example: Broccoli, broccoli raab (broccoli), Brussels sprouts, cabbage, bok choy, cauliflower, kale (cabbage) Collards ), kale, kohlrabi, mustard greens; legumes (succulent plants or dried), for example: lupin, beans (Phaseolus spp.) Including field bean, kidney bean, emperor bean (lima 151284.doc •218· 201117722 bean), navy bean, pinto bean, runner bean , bean bean, tepary bean and wax bean, bean (red bean) (including adzuki bean, asparagus bean, blackeyed pea) , red beans (catjang), medium Chinese longbean, cowpea, crowder pea, moth bean, mung bean, rice bean, southern pea, black mung bean (Chinese longbean) Urd bean) and yardlongbean), broadbean (fava), chickpea (garbanzo), guar, jackbean, white bean (lablab bean) ), lentil (lentil) and cowpea (pea) (Pisum spp.) (including dwarf pea, edible-podded pea, sweet pea (English pea) ), pea (field pea), pea (garden pea), green pea, snowpea, sugar pea, pigeon pea, and soybean (soybean); Classes, for example: eggpiant, groundcherry (Physalis spp.), pepino and pepper (including bell pepper, chili pepper, cooking pepper) Co〇king pepper ), pimento, sweet pepper, green tomato ) and tomatoes; melons such as Chayote (fruit), Chinese waxgourd (Chinese preserving melon), citron melon, cucumber, and gherkin ) edible cucurbits (ediblegourd) (including hyotan, cucuzza, hechima 151284.doc •219· 201117722 and Chinese okra), Momordica spp. (including balsam apple, balsam pear, bittermelon and Chinese cucumber), muskmelon (including cantaloupe and pumpkin), pumpkin ( Summer and winter squash) (including butternut squash, calabaza, hubbard squash, acorn squash, spaghetti squash) and watermelon (watermelon); Fruits, such as: blackberry (including bingleberry, boysenberry, dewberry, loman, l紫wberry, purple Every (marionberry), olallieberry and youngberry), blueberry, cranberry, currant, elderberry, gooseberry (g00Seberry), lingonberry Huckleberry, loganberry, raspberry, and strawberry; nuts, such as aim〇nd, beechnut, Brazil nut, butternut , cashew, chestnut, chinquapin, filbert (hazelnut), hickorynut, macadamianut, pecan, and walnut ( Wainut); tropical fruit trees and other crops such as bananas, plantains, mangos, coconuts, papaya, guava, avocado , lichee, agave, coffee, coca (caca), sugar cane, 油il paim, sesame, rubber (mbber) 151284. Doc •2 20· 201117722 and spices; fiber crops such as cotton, flax and hemp; lawn plants (including warm-season and cool-season) Lawn), such as bentgrass, Kentucky bluegrass, St. Augustine grass, tall fescue, and Bermuda grass. Such pathogens include: Oomycetes, including Phytophthora diseases such as: Phytophthora infestans, Phytophthora megasperma, Phytophthora parasitica, P. acuminata (Phytophthora cinnamomi) and Phytophthora capsici and Pythium diseases, such as Pythium aphanidermatum and Peronosporaceae family diseases, such as grape downy mildew Plasmopara viticola, Peronospora spp. (including Peronosporatabacina and Peronospora parasitica), Pseudoperonospora spp. (including Cucumber (Pseudoperonospora cubensis )) and Bremia lactucae; Ascomycetes, including Alternaria diseases, such as: Alternaria solani and Alternaria brassicae f (Guignardia) disease, for example: Staphylococcus aureus (G Uignardia bidwelli), Venturia disease, such as: Venturia inaequalis, Septoria diseases' For example: Septorianodorum and small 151284.doc • 221 · 201117722 Septoria tritici, powdery mildew disease, including: Blumeria spp. (including Blumeria graminis) and Erysiphe spp. (including flax white powder) Erysiphe polygoni), Uncinula necatur, Sphaerotheca fuligena and Podosphaera leucotricha, Pseudocercosporella herpotrichoides 'Botrytis' disease, For example, Botrytis cinerea, Monilinia fructicola, and Sclerotinia diseases, such as Sclerotinias cloridiorum, Magnaporthe grisea, and grape blight ( Phomopsis viticola), wheat flax leaf genus (Helmint Hosporium) diseases, such as: Helminthosporium tritici repentis, Pyrenophora teres, anthracnose diseases, for example, Glomerella or Colletotrichum spp. (including Colletotrichum graminicola and Colletotrichum orbiculare) and wheat genus Gaeumannomyces graminis; Basidiomycetes, including genus Puccinia spp. (eg wheat) Puccinia recondita, Puccinia striiformis, Puccinia hordei, Puccinia graminis and Puccinia arachidis, Hemileiavastatrix and soybean Russ diseases caused by Phachopsora pachyrhizi; other pathogens include Rhizoctonia spp. 151284.doc -222- 201117722 (eg Rhizoctonia solani and rice silk nucleus) Rhizoctoniaryzae); Fusarium disease, for example Carnation stalk rot fungus (Fusarium roseum), Fusarium graminearum and Fusarium oxysporum; Verticillium dahliae; Sclerotium rolfsii; Barley grisea (Rynchosporium secalis); Cercosporidium personatum, Cercospora arachidicola, and Cercospora beticola; Rutstroemia floccosum (also known as Sclerontina homoeocarpa); and other and these pathogens Closely related genus and species. Certain fungicidal compounds also have bactericidal effects, so that in addition to their fungicidal activity, the compositions or combinations thereof also have antibacterial activity, for example: pear and apple fire damage (Erwinia amylovora), Xanthomonas (Xanthomonas) Campestris), Pseudomonas syringae, and other related species. The fungicidal composition of the present invention, the compound of the formula (a) of the formula 1 may act synergistically with the additional fungicidal compound of component (b) to provide the above beneficial results, which is to expand the range of disease diseases to be controlled , prolong the duration of prophylactic or therapeutic protection, and inhibit the proliferation of drug-resistant fungal pathogens. In a particular embodiment, a composition comprising a portion of component (a) and component (b) provided in accordance with the present invention is particularly effective for controlling a particular fungal disease (eg, Alternaria solani, wheat) Blumeria graminis f. sp. tritici, Botrytis cinerea, Puccinia recondita f. sp. tritici, Rhizoctonia solani 151284.doc -223- 201117722 (Rhizoctonia solani ) The mixture of sputum fungicides, Septoria nodorum, and sept〇ria tritici, may also provide significantly better disease control than predicted based on the activity of the components. This collaboration is described as “the cooperative behavior of the two components in the mixture, making the overall effect more significant or longer than the sum of the effects of the two (or more)” (see R M. L.

Tames, Neth. J. piant path〇l〇gy 1964, 70, 73-80)。在提 供植物疾病防治的方法中，協同效果存在於施予該植物 或種子的活性成分組合（例如：殺真菌化合物），該活 性成分係以協同重量比以及協同（即，有協同地效果的） 劑量施用。熟習該領域之技藝人士可透過實驗輕易地鑑 別及優化該提供協同作用之殺真菌化合物的重量比及 施用率（即，量）。 下列測試包括效能證明之測試，顯示本發明之化合 物二用於殺真菌混合物，並用以防治特定病源體。下列 測試亦包括展林發明之混合物對於特定病源體之防 治^能的測試。然而，本發明之單獨化合物或其混合物 所提供之疾病料並不限於例示之致病真菌物種。 參見索彡丨表A之化合物描述。iHNMR實驗結果請 參見索引表B。下列縮寫用於後續之索引表中：i代^ iS〇、Me係甲基、&amp;係乙基、⑧係苯基、如係笨基、 MeO係甲氧基、邮係乙氧基、廳係甲硫基、a係 氰 1基以，NCS係氰硫基（㈣⑻。在索引表中，當 Q或Q —藉由CH2鏈結附著至式1剩餘部份之苯 基環的情形下（即苯曱基），該環之位標編號係和該環 與CH2鏈結之連接有關。縮寫「Cmpd」代表「化合物 151284.doc •224· 201117722 (Compound)」’及縮寫「Ex.」代表「實例（Example)」 且後方有一數字以指出該化合物係在哪一實例中經製 備。縮寫「m，p.」代表熔點。在索引表A令，攔位「Μ§ (M+1)」中所報導之數值係所觀察之分子離子的分子 量，該分子離子係藉由在具有最大同位素豐度（即M) 的分子申加入H+(分子量為〇 M)而形成。經報導之 M+1峰係藉由質譜測定術利用大氣壓力化學離化法 (atmospheric pressure chemical ionization，APCI)或電 喷灑離子化（electrospray ionization，ESI)觀察而得。 包含一或多個較低豐度之較高原子量同位素（例如： 37C1、81Br)之分子離子的存在未經報導。Tames, Neth. J. piant path〇l〇gy 1964, 70, 73-80). In a method of providing control of plant diseases, a synergistic effect is present in a combination of active ingredients (eg, fungicidal compounds) administered to the plant or seed, the active ingredients being synergistically weighted and synergistic (ie, synergistically effective) Dosage administration. Those skilled in the art can readily identify and optimize the weight ratio and application rate (i.e., amount) of the synergistic fungicidal compound by experiment. The following tests include tests for proof of efficacy, showing that the compound of the present invention is used in a fungicidal mixture and is used to control a particular pathogen. The following tests also included tests on the prevention and treatment of specific pathogens by mixtures of inventions. However, the disease materials provided by the individual compounds of the present invention or mixtures thereof are not limited to the exemplified pathogenic fungal species. See the compound description of Table A. See the index table B for the results of the iHNMR experiment. The following abbreviations are used in the subsequent index tables: i generation ^ iS〇, Me methyl, &amp; ethyl, 8 series phenyl, such as stupid, MeO methoxy, postal ethoxy, hall Methylthio group, a system cyanide group, NCS system cyanthio group ((4) (8). In the index table, when Q or Q - by the CH2 chain attached to the phenyl ring of the remainder of formula 1 ( That is, benzoquinone), the ring number of the ring is related to the connection of the ring to the CH2 chain. The abbreviation "Cmpd" stands for "compound 151284.doc •224· 201117722 (Compound)" and the abbreviation "Ex." "Example" and there is a number to indicate in which instance the compound was prepared. The abbreviation "m, p." stands for melting point. In the index table A, the block "Μ§ (M+1)" The values reported in the text are the molecular weights of the observed molecular ions formed by the addition of H+ (molecular weight 〇M) to the molecule with the largest isotopic abundance (ie, M). The peak system is subjected to mass pressure chemical ionization (APCI) or electrospray ionization by mass spectrometry. Of (electrospray ionization, ESI) were observed to give high atomic isotopes comprising one or a plurality of low abundance (e.g.: 37C1,81Br). Without the presence of the molecular ion reported.

索引表A R1Index Table A R1

化合物 Q1 Q2 R1 R2 m.p. (°C) MS (M+1 ) 1 (實例4) 2,6-二-F-Ph 4-Cl-Ph Cl Me 氺承本 * * * 2(實例3) 2,6-二-F-Ph 4-Cl-Ph Cl Cl ♦ * * 本丰* 3 (實例6) 4-F-Ph 4-Cl-Ph Cl Me *♦氺 4(實例2) 2,4,6-三-F-Ph 4-Cl-Ph Cl Cl * * * 5 4-Cl-Ph 2-C1, 4-F-Ph Cl Cl 129-131 6 2,6-二-F-Ph Ph Cl Br 371 7 2,4,6-三-F-Ph 4-Cl-Ph Cl Br 139-141 8 2,4,6-三-F-Ph 4-Cl-Ph Cl Me 148-150 9 2,6-二-F-Ph Ph Cl I 417 J 5 ] 284.doc -225 201117722 化合物 Q1 Q2 R1 R2 m.p. ΓΟ MS (M+l) 10 2,6-二-F-Ph Ph Cl Me 305 11 2,6-二-F-Ph 3-F-Ph Cl Cl 131-134 12 2,4,6-三-F-Ph 4-Cl-Ph Br Br 145-148 13 2,6-二-F-Ph 3-F-Ph Cl Br 120-122 14 2,4,6-三-F-Ph 4-C1, 3-F-Ph Cl Br 135-137 15 2,4,6-三-F-Ph 4-C1, 3-F-Ph Cl Cl 397 16 2,6-二-F-Ph 3-F-Ph Cl Me 323 17 2,4,6-三-F-Ph 4-C1, 3-F-Ph Cl Me 375 18 2,6-二-F， 4-MeO-Ph 4-C1, 3-F-Ph Cl Br 氺本 *本 19 2,6-二-F， 4-MeO-Ph 4-C1, 3-F-Ph Cl Me 387 20 2,6-二-F-Ph 4-Cl-Ph Cl Br 124-126 21 2,4,6-三-F-Ph 4-C1, 3-F-Ph Br Br 144-146 22 2,6-二-F， 4-MeO-Ph 4-Cl-Ph Cl Me 146-148 23 2,6-二-F， 4-MeO-Ph 4-Cl-Ph Cl Br 152-153 24 2,4,6-三-F-Ph 4-C1, 3-F-Ph Me Me 355 25 2,6,二-F， 4-MeO-Ph 4-Cl-Ph Br Br 166-168 26 2,6-二-F， 4-MeO-Ph 4-C1, 3-F-Ph Br Br 495 27 2,6-二-F， 4-MeO-Ph 4-C1, 3-F-Ph Me Me 367 28 2,4,6-三-F-Ph 4-Cl-Ph Me Me * ♦ 29 (實例 14) 2,6-二-F-Ph 3-F-Ph Cl CH=C 333 30 2,3,6-三-F-Ph 4-Cl-Ph Cl Me 357 31 2-C1, 4-F-Ph 4-Cl-Ph Cl Me 357 32 2,3,6-三-F-Ph 4-Cl-Ph Cl Br 124-127 33 2-C1, 4-F-Ph 4-Cl-Ph Cl Br 117-120 34 2-C1, 6-F-Ph 4-Cl-Ph Cl Br 174-177 35 2-C1, 6-F-Ph 4-Cl-Ph Cl Me 357 36 2,6-二-F-Ph 3,5-二-F-Ph Cl Br 407 37 2,6-二-F， 4-MeO-Ph 4-Cl-Ph Me Me 105-108 38 (實例 13) 2,3,6-三-F-Ph 4-Cl-Ph Cl CN 147-149 151284.doc -226- 201117722 化合物 Q1 Q2 Ri R2 m.p. rc) MS (M+l) 39 2,6-二-F-Ph 2-F-Ph Cl Br 113-115 40 2,6-二-F，4-MeO, 3-Me-Ph 4-Cl-Ph Br Me 143-147 41 2,6-二-F-Ph 2-F-Ph Cl Me 323 42 2,6-二-F-Ph 4-CF3〇-Ph Cl Br 355 43 2,6-二-F-Ph 4-Br-Ph Cl Br 143-145 44 2,6-二-F-Ph 4-F-Ph Cl Br 389 45 2,6-二-F-Ph 3,5-二-F-Ph Cl Me 341 46 2-C1，3,6-二 -F-Ph 4-Cl-Ph Cl Br 439 47 2-C1，3,6-二 -F-Ph 4-Cl-Ph Cl Me 373 48 2,6-二-F-Ph 4-CF3〇-Ph Cl Me 389 49 2,6-二-F-Ph 4-Me-Ph Cl Me 319 50 2,6-二-F-Ph 4-F-Ph Cl Me 323 51 2,6-二-F-Ph 4-CF3-Ph Cl Br 117-120 52 2,5-二-F-Ph 4-Cl-Ph Cl Br 114-117 53 2-CF3, 6-F-Ph 4-Cl-Ph Cl Br 455 54 2-C1, 6-F-Ph 4-Cl-Ph Cl cf3 409 55 3-Br? F-Ph 4-Cl-Ph Cl Me 419 56 2,6-二-F-Ph 4-CF3-Ph Cl Me 373 57 2,5-二-F-Ph 4-Cl-Ph Cl Me 339 58 2-CF3, 6-F-Ph 4-Cl-Ph Cl Me 389 59 2,6-二-F-Ph Bn Cl Br 85-87 60 2,6-二-F, 4-MeO-Ph 4-Cl-Ph Br MeO 141-144 61 3-C1，2, 6-二 -F-Ph 4-Cl-Ph Cl Br 439 62 2,6-二-F-Ph 3-Cl-Bn Cl Br 419 63 2,6-二-F-Ph 4-C1, 3-F-Bn Cl Br 437 64 2,6-二-F-Ph 4-Cl-Bn Cl Br 419 65 2,6-二-F, 3-Me-Ph 4-Cl-Ph Cl Br 419 66 2,6-二-F, 3-Me-Ph 4-Cl-Ph Cl Me 353 67 2,6-二-F-Ph 4-Cl-Ph Cl Et 125-126 68 3- Br, 2-F, 4- MeO-Ph 4-Cl-Ph Cl Br 498 151284.doc -227- 201117722 化合物 Q1 Q2 R1 R2 m.p. (t) Mb (M+l) 69 2-F, 4-MeO-Ph 4-Cl-Ph Cl Br 417 70 2-F, 4-MeO-Ph 4-Cl-Ph Cl Me 351 71 2-F, 4-MeO, 3-Me-Ph 4-Cl-Ph Cl Me 365 72 2,6dPh 4-Cl-Ph Cl i-Pr 106-108 73 2,6-二-F， 3-MeO-Ph 4-Cl-Ph Cl Br 435 74 2,6-二-F-Ph Bn Cl Me 319 75 2,6-二4， 4-HO-Ph 4-Cl-Ph Cl Me 355 76 2,6-二-F-Ph 4-Cl, 3-F-Bn Cl Me 371 77 2,6-二-F， 3-MeO-Ph 4-Cl-Ph Cl Me 369 78 2,6-二-F-Ph 3-Cl-Bn Cl Me 353 79 3-C1，2,6-二 -F-Ph 4-Cl-Ph Cl Me 375 80 2,6-二-F-Ph 4-Cl-Bn Cl Me 353 81 2,3,6-三-F-Ph 4-F-Ph Cl Cl 361 82 2,3,6-三-F-Ph 4-Me-Ph Cl Cl 357 83 4-Cl-Ph 2,4,6-三-F-Ph Cl Br 117-118 84 2,3,6-三-F-Ph 4-F-Ph Cl Br 407 85 2,3,6-三-F-Ph 4-Cl, 3-F-Ph Cl Cl 395 86 4-C1, 2-F, 6-MeO-Ph 4-Cl-Ph Cl Br 451 87 2,3,6-三-F-Ph 4-Me-Ph Cl Br 403 88 2,6-二-F， 4-MeO-Ph 4-F-Ph Cl Cl 373 89 2,3,6-三-F-Ph 4-Cl, 3-F-Ph Cl Br 441 90 2,6-二七 4-MeO-Ph 4-F-Ph Cl Br 419 91 2,3,6-三-F-Ph 4-F-Ph Cl Me 341 92 2,6-二-F， 4-MeO-Ph 4-Me-Ph Cl Cl 369 93 2,4,6·三-F-Ph 4-F-Ph Cl Cl 361 94 2,6-二-F， 4-MeO-Ph 4-Me-Ph Cl Br 415 95 4-Cl, 2-F, 6-MeO-Ph 4-Cl-Ph Cl Me 387 96 4-Cl-Ph 2,6-二-F-Ph Cl Cl 123-126 151284.doc -228- 201117722 化合物 Q' Q2 R1 R2 m.p. (°C ) MS (M+l) 97 2,6-:-F-Ph 4-Cl-Ph Me Me 146-148 98 2,4,6-S-F-Ph 4-F-Ph Cl Br 407 99 2,4,6-S-F-Ph 4-Me-Ph Cl Br 403 100 2,4,6-三-F-Ph 4-Me-Ph Cl Cl 357 101 2,3,6-S-F-Ph 4-Me-Ph Cl Me 337 102 4-EtO, 2,6-二 -F-Ph 4-Cl-Ph Cl Me 383 103 2,3,6-三-F_Ph 4-C1, 3-F-Ph Cl Me 375 104 2,6-二-F, 4-MeO-Ph 4-F-Ph Cl Me 353 105 2,6-二-F， 4-MeO-Ph 4-Me-Ph Cl Me 349 106 4-Cl-Ph 2,6-二-F-Ph Br Br 156-158 107 4-Cl-Ph 2,6-二-F-Ph Cl Br 148-150 108 2,4,6-三-F-Ph 4-F-Ph Cl Me 341 109 2,4,6-三-F-Ph 4-Me-Ph Cl Me 337 110 2,6-二-F-Ph 3,4-二-F-Ph Cl Br 407 111 2,6-二-F-Ph 3-F, 4-Me-Ph Cl Br 403 112 2-C1, 6-F, 4-MeO-Ph 4-Cl-Ph Cl Br 451 113 2-C1, 6-F, 4-MeO-Ph 4-Cl-Ph Cl Me 385 114 2,6-二-F-Ph 3,4-二-F-Ph Cl Me 341 115 2,6-二-F-Ph 3-F, 4-Me-Ph Cl Me 337 116 2-C1, 4-F-Ph 4-F-Ph Cl Br 111-112 117 2-C1, 4-F-Ph 4-F-Ph Cl Cl 359 118 2-C1, 4-F-Ph 4-Me-Ph Cl Br 127-128 119 2-C1, 6-F-Ph 4-F-Ph Cl Br 95-97 120 2-C1, 6-F-Ph 4-Me-Ph Cl Br 147-148 121 2-C1, 4-F-Ph 4-F-Ph Cl Me 101-106 122 2-C1, 4-F-Ph 4-Me-Ph Cl Me 148-149 123 2-C1, 6-F-Ph 4-F-Ph Cl Me 122-123 124 2-C1, 6-F-Ph 4-Me-Ph Cl Me 158-162 125 2-C1，3,6-二 -F-Ph 4-F-Ph Cl Br 423 126 2-C1，3,6-二 -F-Ph 4-F-Ph Cl Cl 378 151284.doc -229- 201117722 化合物 Q1 Q2 R1 R2 m.p. (°C) MS (M+l 127 2-Cl，3,6-二 -F-Ph 4-Me-Ph Cl Br 419 128 2-C1，3,6-二 -F-Ph 4-Me-Ph Cl Cl 374 129 2,6-二-F-Ph 3-啥琳基 Cl Me 158-160 130 4-CN，2,6-二 -F-Ph 4-Cl-Ph Cl Br 429 131 2-C1，4-F-Ph 4-C1, 3-F-Ph Cl Br 103-104 132 2-C1，6-F-Ph 4-C1, 3-F-Ph Cl Br 80-84 133 4-Cl-Ph 2,4,6-三-F-Ph Cl Cl 76-78 134 4-CN，2,6-二 -F-Ph 4-Cl-Ph Cl Me 429 135 2-C1，3,6-二 -F-Ph 4-F-Ph Cl Me 429 136 2-C1，3,6-二 -F-Ph 4-Me-Ph Cl Me 429 137 2,6-二-F-Ph 3-C1, 4-MeO-Bn Cl Cl 405 138 4-Cl-Ph 2,6-二-F， 4-MeO-Ph Br Cl 119-122 139 4-Cl-Ph 2,6-二-F-Ph Me Br 156-158 140 2,6-二-F-Ph 4-Cl-Ph h2c= CH Me 141-143 141 4-Cl-Ph 2,4,6-三-F-Ph Br Br 130-131 142 2-C1，3,6-二 -F-Ph 4-C1, 3-F-Ph Cl Br 457 143 2-C1，3,6-二 -F-Ph 4-C1, 3-F-Ph Cl Cl 413 144 2,6-二-F-Ph 3-Cl-Ph Cl Br 405 145 2,6-二-F-Ph 3-Cl-Ph Cl Cl 361 146 2,6-二-F-Ph 4-C1, 3-F-Ph Cl Br 423 147 2,3,6-三-F-Ph 3,4-二-Me-Ph Cl Br 417 148 2,6-二-F-Ph 4-C1, 3-F-Ph Cl Cl 379 149 2,3,6-三-F-Ph 3,4-二-Me-Ph Cl Cl 371 150 2-C1, 6-F-Ph 4-Me-Ph Cl Cl 142-143 151 2-C1, 6-F-Ph 4-F-Ph Cl Cl 102-103 152 2-C1, 4-F-Ph 4-C1, 3-F-Ph Cl Cl 116-117 153 2-C1, 6-F-Ph 4-C1, 3-F-Ph Cl Cl 66-67 151284.doc -230- 201117722 化合物 Q1 Q2 R1 R2 m.p. (°C) MS (M+l 154 2,6-二-F， 3-MeS-Ph 4-Cl-Ph Cl Br 451 155 4-Cl-Ph 2,4,6-三-F-Ph Br Cl 111-112 156 2,3,6-三-F-Ph 3,4-二-Cl-Ph Cl Cl 413 157 2,6-二-F， 3-MeS-Ph 4-Cl-Ph Cl Me 385 158 2,6-二-F-Ph 3-Cl-Ph Cl Me 339 159 2-C1，3,6-二 -F-Ph 4-C1，3-F-Ph Cl Me 393 160 2,3,6-S-F-Ph 3,4-二-Me-Ph Cl Me 351 161 2,6-二-F， 4-MeO-Ph 4-Cl-Ph Cl Cl 391 162 2,6-二-F， 4-MeO-Ph 4-C1, 3-F-Ph Cl Cl 407 163 2,6-二七 4-MeO-Ph 4-C1, 3-F-Ph Cl I 499 164 4-Cl-Ph 2,6-二-F， 4-MeO-Ph Br Br 137-139 165 2-C1, 4-F-Ph 4-C1, 3-F-Ph Cl Me 89-91 166 2-C1, 6-F-Ph 4-C1, 3-F-Ph Cl Me 140-142 167 2,6-二-F, 4-MeO-Ph 4-Cl-Ph Cl I 481 168 2,6-二-F-Ph 4-C1, 3-F-Ph Cl Me 358 169 4-Cl-Ph 2,6-二-F, 4-MeO-Ph Me Me 105-108 170 (實例 8) 2,6-二-F， 4-MeO-Ph 3-F-Ph Cl Br 418 171 2,6-二-F， 4-MeO-Ph 3-F-Ph Cl Cl 373 172 2,6-二-F-Bn 4-Cl-Ph Cl Me 353 173 2-F-Ph 4-C1, 3-F-Ph C1CH2 Cl 373 174 2-F-Ph 4-C1, 3-F-Ph Me Cl 339 175 2,6-二-F, 4-MeO-Ph 4-C1, 3-F-Ph Me Cl 387 176 3，5 -二-C1 - 4 - ntb 咬 基 4-C1, 3-F-Ph Me Cl 390 177 2,6-二-F, 4-MeO-Ph 6-C1-3-吡啶基 Me Cl 370 178 2-吡啶基 4-C1, 3-F-Ph Me Cl 322 -231 - 151284.doc 201117722 化合物 Q1 Q2 R1 R2 m.p. (°C) MS (M+l ) 179 2,6-二-F， 3-MeO-Ph 3-F-Ph Cl Br 419 180 2,6-二-F， 3-MeO-Ph 3-F-Ph Cl Cl 373 181 (實例 9) 2,6-二-F， 4-MeO-Ph 3-F-Ph Cl Me 354 182 2,6-二-F， 3-MeO-Ph 4-Me-Ph Cl Br 415 183 2-C1, 4-F-Ph 4-Me-Ph Cl Cl 72-73 184 2,6-二-F， 4-MeO-Ph 4-Cl-Bn Cl Br 139-140 185 2,6-二-F， 4-MeO-Ph 4-Cl-Bn Cl Cl 123-124 186 2,3,6-i-F-Ph 4-Cl-Bn Cl Cl 氺氺 187 2,3,6-三-F-Ph 4-Cl-Bn Cl Br 87-88 188 2,6-二-F， 4-MeO-Ph 4-Cl-Bn Cl Me 116-117 189 2,6-二-F， 3-MeO-Ph 4-Cl-Bn Cl Cl *氺 ** 190 2,6-二-F， 3-MeO-Ph 4-Cl-Bn Cl Br 449 191 4-Cl-Ph 3-Cl-Bn Cl Br 108-109 192 2,6-二-F， 4-MeO-Ph 4-Me-Bn Cl Cl 383 193 2,6-二-F， 4-MeO-Ph 4-Me-Bn Cl Br 104-105 194 2,3,6-三-F-Ph 4-Cl-Bn Cl Me 371 195 2,6-二-F， 3-MeO-Ph 4-Cl-Bn Cl Me 384 196 4-Cl-Ph 3-Cl-Bn Cl Me 113-114 197 2,6-二-F， 4-MeO-Ph 4-Me-Bn Cl Me 363 198 4-Cl-Ph 2,6-二-F， 4-MeO-Ph Cl Cl 117-118 199 (實例 15) 2,6-二-F， 4-MeO-Ph 4-F-Ph Cl HOCH2 氺氺 200 4-C1, 3-F-Ph 2-C1, 4-F-Ph Br Br 104-106 201 4-C1, 3-F-Ph 2-C1, 4-F-Ph Cl Cl 120-122 202 2,6-二-F-Ph 4-Cl-Ph Et Me 122-124 203 4-Cl-Ph 2-C1, 4-F-Ph Br Br 114-116 151284.doc •232· 201117722 化合物 Q1 Q2 R1 R2 m.p. (°C) MS (M+l) 204 4-Cl-Ph 2-Cl, 4-F-Ph Me Me 336 205 4-Cl-Ph 2,4,6-三-F-Ph Me Me 90-92 206 2,6-二-F， 3-MeO-Ph 4-Cl-Ph Cl Cl 391 207 2,6-二-F, 3-MeO-Ph 4-Me-Ph Cl Cl 369 208 2,6-二-F， 3-MeO-Ph 4-F-Ph Cl Br 419 209 2,6-二-F, 3-MeO-Ph 3-F-Ph Cl Me 353 210 2,6-二-F， 3-MeO-Ph 3-Me-Ph Cl Br 414 211 2,6-二-F， 3-MeO-Ph 4-C1，3-F-Ph Cl Br 453 212 2,6-二-F-Ph 5-C1-2-吡啶基 Me Cl * * 213 2-F-4-吡啶基 4-C1, 3-F-Ph C1CH2 Cl * * *氺 214 2-F-4-Dit 咬基 4-C1, 3-F-Ph Me Cl * % 215 4-Cl-Ph 2-Cl, 4-F-Ph Br Cl 106-109 216 4-C1, 3-F-Ph 2-Cl, 4-F-Ph Me Br 105-107 217 4-C1, 3-F-Ph 2-Cl, 4-F-Ph Br Cl 116-118 218 2,6-二-F-Ph 基 Cl Br 176-180 219 4-C1, 3-F-Ph 2-Cl, 4-F-Ph Cl Br 120-122 220 4-Cl-Ph 2-Cl, 4-F-Ph Cl Br 113-116 221 (實例 16) 2,6-二4， 4-MeO-Ph 4-F-Ph Cl fch2 水*本 氺氺氺 222 2,6-二-F, 3-MeO-Ph 4-Me-Ph Cl Me 349 223 2,6-二-F， 3-MeO-Ph 4-F-Ph Cl Me 353 224 2,6-二-F， 3-MeO-Ph 3-Me-Ph Cl Me 113-117 225 4-Cl-Ph 2-Cl, 4-F-Ph Br Me 127-131 226 4-Cl-Ph 2-Cl, 4-F-Ph Me Br 146-150 227 4-C1, 3-F-Ph 2-Cl, 4-F-Ph Br Me 125-127 228 2,3,6-三-F-Ph 4-C1, 3-F-Ph Br Cl * * 229 2,3,6-三-F-Ph 4-Cl-Ph Br Cl 幸氺 氺氺 230 2,3,6-三-F-Ph 4-F-Ph Br Cl 伞氺 幸本 231 2-Br-4-°tb 淀基 4-C1, 3-F-Ph C1CH2 Cl 434 232 2-Br-4-°比咬基 4-C1, 3-F-Ph Me Cl 400 151284.doc · 233 · 201117722 化合物 Q1 Q2 R1 R2 m.p. (°C) MS (M+1 ) 233 5-Br-3-B比咬基 4-Cl, 3-F-Ph C1CH2 Cl 434 234 5-Br-3-°比咬基 4-C1, 3-F-Ph Me Cl 400 235 5-Br-2-°比咬基 4-Cl, 3-F-Ph CICH2 Cl 水本 * * 236 5-ΒΓ-2·11比咬基 4-Cl, 3-F-Ph Me Cl 400 237 2-C1-3-吡啶基 4-Cl, 3-F-Ph CICH2 Cl 390 238 2-C1-3-吡啶基 4-Cl, 3-F-Ph Me Cl 356 239 4-Cl-Ph 3-Cl-Bn Cl Cl 107-109 240 2,4,6-三-F-Ph 3-F-Ph Cl Cl 78-81 241 2,3,6-三-F-Ph 3-F-Ph Cl Cl 143-145 242 2,4,6-三-F-Ph 3-F-Ph Cl Br 130-132 243 2,3,6-三-F-Ph 3-F-Ph Cl Br 137-138 244 2,3,6-三-F-Ph 3-F-Ph Cl Me 146-147 245 2,4,6-三-F-Ph 3-F-Ph Cl Me 150-152 4,5-二-Br， 246 1-Me-1H-咪唑 4-Cl-Ph Br Br 496 -2-基 4,5 ·Βγ， 247 1-Me-1H-咪唑 4-Cl-Ph Br Br 575 -2-基 248 4-Cl-Ph 2,6-二，F， 4-MeO-Ph Cl Br 118-125 249 2-C1，3,6-二 -F-Ph 4-Cl-Ph Br Br 氺φ 250 6 - M e - 2 - °比 基 4-Cl, 3-F-Ph Me Cl 本氺 *氺 251 6-Me-2-° 比 基 4-Cl, 3-F-Ph cich2 Cl 本氺 252 4-C1-5-噻唑基 4-Cl, 3-F-Ph Me Cl 氺* * * 253 2,4-二-Cl-5-噻唑 基 4-Cl, 3-F-Ph Me Cl 氺氺 254 2,3,6-三-F-Ph 4-Cl, 3-F-Ph Br Br 氺本 255 2,3,6-三-F-Ph 4-Cl-Ph Br Br 467 256 2,3,6-三-F-Ph 4-F-Ph Br Br 449 257 2-C1，3,6-二 -F-Ph 4-Cl-Ph Br Cl 439 258 2-C1, 3,6-二 -F-Ph 4-Cl-Ph Me Me 353 259 2,3,6-三-F-Ph 4-Cl, 3-F-Ph Me Cl 傘本 260 2,6-二 _F， 3-MeO-Ph 4-F-Ph Cl Cl 374 151284.doc •234 201117722 化合物 Q1 Q2 R1 R2 m.p. (°C ) MS (M+1 261 2,6-二-F， 3-MeO-Ph 3-Me-Ph Cl Cl 133-136 262 2,6-二-F, 3-MeO-Ph 4-C1, 3-F-Ph Cl Cl 84-86 263 2,6-二-F， 3-MeO-Ph 4-C1, 3-F-Ph Cl Me 387 264 4-Cl-Ph 2,6-二七 4-MeO-Ph Me Cl 104-106 265 4-Cl-Ph 2,6-二-F, 4-MeO-Ph C1CH2 Cl 127-129 266 2,6-二-F， 3-MeO-Ph 3-Et-Ph Cl Br 429 267 2,6-二-F, 3-MeO-Ph 4-C1, 3-Me-Ph Cl Cl 403 268 2,6-二-F, 3-MeO-Ph 3-F2CHO-Ph Cl Cl 100-102 269 2,6-二-F, 3-MeO-Ph 4-C1, 3-Me-Ph Cl Br 449 270 2,6-二-F, 3-MeO-Ph 3-F2CHO-Ph Cl Br 109-111 271 2,4-二-F-Bn 4-Cl-Ph Br Me 399 272 3-C1, 2,6-二-F， 4-MeO-Ph 4-Me-Ph Cl Cl 氺氺 本氺 273 2,6-二-F， 4-MeO-Ph 6-C1-3-吡啶基 Cl Cl 390 274 3-CN，2,6-二 -F-Ph 4-Cl-Ph Cl Cl 386 275 4-Br, 5-MeS-2- 噻吩基 4-Cl-Ph Br Br 545 276 2,3,6-S-F-Ph 4-Cl-Ph Me Cl 本本 277 2,3,6-S-F-Ph 4-F-Ph Me Cl 氺氺 * * 278 2-C1, 3,6-二 -F-Ph 4-Cl-Ph Me Cl 氺本 本* 279 2,3,6-2-F-Ph 4-C1, 3-F-Ph Me Me *氺 * * 280 2,3,6-三-F-Ph 4-Cl-Ph Me Me 氺* 281 2,3,6-三-F-Ph 4-F-Ph Me Me 氺氺 氺氺 282 2,6-二-F， 3-MeO-Ph 3-Et-Ph Cl Me 364 283 (實例 18) 3-CN, 2,6-二 -F-Ph 4-Cl-Ph Cl Br 430 151284.doc 235 · 201117722 化合物 Q1 Q2 R1 R2 m.p. (r) MS (M+l) 284 4-C1, 3-F-Ph 2-C1, 4-F-Ph Cl Me 108-110 285 4-Cl-Ph 2-C1, 4-F-Ph Cl Me 135-137 286 4-Cl-Ph 2,6-二-F， 4-MeO-Ph Cl Me 108-110 287 2,6-二-F， 3-MeO-Ph 4-C1, 3-Me-Ph Cl Me 383 288 2,6-二-F， 3-MeO-Ph 3-F2CHO-Ph Cl Me 401 289 2,6_ 二-F， 3-MeO-Ph 3-Et-Ph Cl Cl 93-95 290 3-Cl，2,6-二-F， 4-MeO-Ph Ph Cl Cl 391 291 3-Br，2,6-二-F， 4-MeO-Ph Ph Cl Br 479 292 (實例 19) 3-CN，2,6-二 -F-Ph 4-Cl-Ph Cl Me 364 293 6-Br-2-Dtb 基 4-C1, 3-F-Ph Cl Cl 420 294 6-MeO-3-a比咬基 4-C1, 3-F-Ph Cl Cl * * 295 3_F，5-MeO-4·0比 啶基 4-C1, 3-F-Ph Cl Cl 390 296 3-喹基 4-C1，3-F-Ph Cl Cl 392 297 2,6-二-Cl， 4-MeO-Ph 4-C1, 3-F-Ph Cl Cl 298 2,4-二-Cl， 6-MeO-Ph 4-C1, 3-F-Ph Cl Cl ** 299 2,6-二-F，4-MeO, 3-Me-Ph Ph Cl Me 349 300 2,3,6-三 _F-Ph 3,4-二-Cl-Ph Cl Br 457 301 2,6-二-F， 3-MeO-Ph 4-Et-Ph Cl Br 429 302 2,6-二-F， 3-MeO-Ph 4-Et-Ph Cl Cl 383 303 2,6_ 二-F， 3-MeO-Ph 4-I-Ph Cl Br 134-138 304 2,6-二-F， 3-MeO-Ph 4-I-Ph Cl Cl 481 305 4-Cl-Ph 2,4,6-三-F-Ph Me Br 123-125 306 4-Cl-Ph 2,4,6-三-F-Ph Me Cl 86-88 307 4-Cl-Ph 2,4,6-三-F-Ph Me H 110-112 151284.doc -236- 201117722 化合物 Q1 Q2 R1 R2 m.p. (°C) MS (M+1 308 2,6-二-F， 4-MeO-Ph 3-Cl-Ph Cl Cl 氺氺 * * 309 2,6-二-F， 4-MeO-Ph 3,4-二-F-Ph Cl Cl 391 310 3-F-4-°比咬基 4-Cl, 3-F-Ph Cl Cl 360 311 4-Cl, 2-MeO-5-D塞e坐基 4-Cl, 3-F-Ph Cl Cl 412 312 4-C1-5-噻唑基 4-Cl, 3-F-Ph Cl Cl 482 313 2-C1-3-吡啶基 4-Cl, 3-F-Ph Cl Cl 376 314 2-C1，3,6·二 -F-Ph 4-Cl, 3-F-Ph Br Br *氺 *本 315 2-C1，3,6-二 -F-Ph 4-Me-Ph Br Br *氺 氺本 316 2,3,6-三-F-Ph 4-Me-Ph Br Br 本丰 本本 317 2,4,6-三-F-Ph 4-F-Ph Br Br 氺本 318 2-C1, 3,6-二 -F-Ph 4-Cl, 3-F-Ph Br Cl 氺* 319 2-C1, 3,6-二 -F-Ph 4-Me-Ph Br Cl 氺氺 氺* 320 2,3,6-三-F-Ph 4-Me-Ph Br Cl *氺 *氺 321 4-Cl-Ph 2,6-二-F-Ph Me Cl 127-129 322 4-Cl-Ph 2,6-二-F-Ph MeO- ch2 Cl 95-97 323 2,6-二-F-Ph 6-quinolinyl Cl Me 210-215 324 2,6-二-F， 3-MeO-Ph 4-Cl-Ph Br Br 氺氺 * * 325 2,6-二-F， 3-MeO-Ph 4-F-Ph Br Cl 417 326 (實例 17) 2,6-二-F-Ph 4-Cl-Ph Br BrCH2 463 2-Br， 327 2,4-二-F-Bn 3,5-二 -MeO-Ph Br Me 582 328 2,6-二-F， 3-MeO-Ph 4-Et-Ph Cl Me 364 329 2,3,6-三-F-Ph 3,4_ 二 _C1-Ph Cl Me 391 330 2- C1, 6-F, 3- MeO-Ph 4-Cl-Ph Cl Cl 407 151284.doc -237 201117722 化合物 Q1 Q2 Ri R2 m.p. (°C) MS (M+1) 331 2,6-二-F， 4-MeO-Ph 3-Cl-Ph Cl Br 435 332 2,6-二-F， 4-MeO-Ph 3,4-二-F-Ph Cl Br 437 333 2-Br-4_e比咬基 4-C1, 3-F-Ph Cl Cl 420 334 5-Br-3-D比咬基 4-C1, 3-F-Ph Cl Cl 420 335 5-Br-2-Dtt 基 4-C1, 3-F-Ph Cl Cl 本丰 336 2,6-二-F， 4-MeO-Ph 6-CF3-3-°tt^ 基 Cl Cl 氺水 337 2-C1，3,6-二 -F-Ph 4-Cl, 3-F-Ph Me Me 氺氺 338 2,3,6-三-F-Ph 4-Me-Ph Me Me 氺氺 氺氺 339 2,4,6-三-F-Ph 4-F-Ph Me Me 氺* 340 2,4,6-三-F-Ph 4-F-Ph Me Cl 氺氺 參本 341 2-C1，3,6-二 -F-Ph 4-Me-Ph Me Me ㈣ 342 2-C1，3,6-二 -F-Ph 4-Cl, 3-F-Ph Me Cl Φ木 *氺 343 2-C1，3,6-二 -F-Ph 4-Me-Ph Me Cl 氺本 本氺 344 2,3,6-三-F-Ph 4-Me-Ph Me Cl 345 2,6-二-F， 4-MeO-Ph 3,4-二-F-Ph Cl Me 169-170 346 2,6-二-F， 4-MeO-Ph 3-Cl-Ph Cl Me 173-174 347 2- C1, 6-F, 3- MeO-Ph 4-Cl-Ph Cl Br 154-156 348 2,6-二-F， 4-MeO-Ph 3-C1, 4-Me-Ph Cl Cl 143-145 349 4-Cl-Ph 2-C1, 4-F-Ph Me Cl 123-127 350 (實例 10) 2,6-二-F， 3-MeO-Ph 4-F-Ph Br Br 134-136 351 2,6-二-F， 3-MeO-Ph 4-Cl-Ph Br Cl *本 ** 352 2,6-二-F， 3-MeO-Ph 4-Me-Ph Br Br 459 353 2-C1, 6-F, 5-MeO-Ph 4-Cl-Ph Cl Br 451 354 2,6-二-F， 4-MeO-Ph 2-C1-3-吡啶基 Cl Cl 390 151284.doc •238- 201117722 化合物 Q1 Q2 R1 R2 m.p. rc) MS (M+l) 355 2,6-二-F， 4-MeO-Ph 6-Cl, 2-MeO-3-° 比咬 基 Cl Cl 氺氺 氺氺 356 2,6-二-F， 4-MeO-Ph 2-C1, 6-MeO-3-° 比咬 基 Cl Cl 420 357 2,6-二-F， 4-MeO-Ph 6-MeO-3-° 比咬 基 Cl Cl 386 358 2,6_ 二-F， 3-MeO-Ph 4-Me-Ph Br Cl 415 359 2-C1, 6-F, 5-MeO-Ph 4-Cl-Ph Cl Cl 407 360 2- C1, 6-F, 3- MeO-Ph 4-Cl-Ph Cl Me 387 361 2,6d, 4-MeO-Ph 4-Me-Ph Me Me 本氺 本本 362 2,6-二-F， 4-MeO-Ph 4-F-Ph Me Me * * ** 363 2,6-二-F， 4-MeO-Ph 4-F-Ph Br Br 本氺 364 2,6-二-F， 4-MeO-Ph 4-Me-Ph Br Br 氺本 365 4-Me-Ph 2,6-二-F, 4-MeO-Ph Me Br 128-129 366 2,6-二-F, 3-MeO-Ph 4-Cl-Ph Me Cl 369 367 2,6-二-F-Ph 4-ClCH2S-Ph Cl Me 386 368 2,4,6-三-F-Bn 4-Cl-Ph H Me 338 369 2,4,6_ 三-F-Bn 4-Cl-Ph Cl Me 372 370 2,4,6-三-F-Bn 4-Cl-Ph Br Me 417 371 2,4,6-三-F-Bn 3,5-二 -MeO-Ph Cl Me 398 372 2,4,6-三-F-Bn 3,5-二 -MeO-Ph Br Me 442 373 2,4,6-三-F-Bn 2,6-二-Cl-Ph Cl Me 407 374 2,4,6·三-F-Bn 2,6-二-Cl-Ph Br Me 451 375 2,4,6-三-F-Bn 3,5-二-Cl-Ph Cl Me 407 376 2,4,6-三-F-Bn 3,5-二-Cl-Ph Br Me 451 151284.doc -239- 201117722 化合物 Q1 Q2 R1 R2 m.p. (°C) MS (M+l) 377 2,6-二-F， 4-MeO-Ph 3-C1，4-Me-Ph Cl Br 161-163 378 4-C1, 3-F-Ph 2-C1, 4-F-Ph Me Me 354 379 2,6-二-F， 4-MeO-Ph 3-F2CHO-Ph Cl Br 467 380 2,6-二-F， 4-MeO-Ph 4-F2CHO-Ph Cl Br 467 381 2,6-二-F, 4-MeO-Ph 3-CF30-Ph Cl Br 485 382 2,6-二-F, 4-MeO-Ph 4-CF30-Ph Cl Br 80-82 383 (實例 11) 2,6-二-F， 3-MeO-Ph 4-F-Ph Me Me 333 384 2-Cl，6-F， 5-MeO-Ph 4-Cl-Ph Cl Me 387 385 2,6-二-F， 3-MeO-Ph 3-F, 4-Me-Ph Cl Br 432 386 2,6-二-F， 3-MeO-Ph 4-CN-Ph Cl Cl 191-193 387 2,6-二-F， 4-MeO-Ph 基 Cl Cl 370 388 2,6-二-F， 4-MeO-Ph 6-Me-3-° 比咬 基 Br Br 458 389 2,6-二-F， 3-MeO-Ph 3-F, 4-Me-Ph Cl Cl 387 390 2,6-二-F， 3-MeO-Ph 4-Br-Ph Cl Cl 435 391 2,6-二-F， 3-MeO-Ph 4-Br-Ph Cl Br 479 392 4-Me-Ph 2,6-二-F, 4-MeO-Ph Me Cl 121-122 393 2,6-二-F， 4-MeO-Ph 3-F2CHO-Ph Cl Cl 68-70 394 2,6-二-F， 4-MeO-Ph 4-F2CHO-Ph Cl Cl 421 395 2,6-二-F， 4-MeO-Ph 3-CFsO-Ph Cl Cl 94-95 396 2,6-二-F， 4-MeO-Ph 4-CF30-Ph Cl Cl 90-91 151284.doc -240- 201117722 化合物 Q1 Q2 R1 R2 m.p. (°c ) MS (M+l ) 397 2,6-二-F， 4-MeO-Ph 4-F2CHO-Ph Cl Me 401 398 2,6-二七 4-MeO-Ph 3-CN, 4-Me-Ph Cl Cl 141-143 399 4-C1, 3-F-Ph 2-C1，4-F-Ph Me Cl 106-109 400 2,6-二-Cl， 4-MeO-Ph 4-C1，3-F-Ph Cl Br 3(E氺 %本 401 4-CN, 2-F, 6-MeO-Ph 4-C1, 3-F-Ph Cl Cl 氺孝 氺本 402 2,6-二-F， 4-MeO-Ph 2-Br-3 - Dtt* 咬基 Cl Cl 氺氺 ** 403 2,6-二-F-Ph 5-Me-2-n 比咬 基 Cl Cl * * 404 4-Me-Ph 2,6-二-F, 4-MeO-Ph C1CH2 Cl 伞本 *氺 405 2,6-二-F， 3-MeO-Ph 4-Br-Ph Cl Me 415 406 (實例 12) 2,6-二-F， 3-MeO-Ph 3-F2CHO-Ph Cl h2c=c H 413 407 2,6-二-F， 4-MeO-Ph 3-F2CHO-Ph Cl Me 401 408 2,6-二-F, 4-MeO-Ph 3-CF30-Ph Cl Me 419 409 2,6-二-F， 3-MeO-Ph 3-F, 4-Me-Ph Cl Me 367 410 2,6-二-F-Ph Ph Cl Cl 325 411 2,6dPh 6-C1-3-吡啶基 Cl Cl ** 氺* 412 3,5-二-?-4-°比咬 基 4-C1, 3-F-Ph Cl Cl 氺本 413 2,6-二-F, 3-MeO-Ph 4-CN-Ph Cl Br 426 414 2,4,6-三-F-Ph 3_F2CHO-Ph Cl Cl 82-83 415 2,4,6-三-F-Ph 4-F2CHO-Ph Cl Cl 91-92 416 2,4,6-三-F-Ph 3-CF30-Ph Cl Cl 76-77 417 2,4,6-三-F-Ph 4-CF30-Ph Cl Cl 75-76 418 2,6-二-F, 4-MeO-Ph 3-C1, 4-Me-Ph Cl Me 143-145 419 2,4,6-三-F-Ph 3-CF2HO-Ph Cl Br 89-90 420 2,4,6-三-F-Ph 4-F2CHO-Ph Cl Br 94-95 421 2,4,6-三-F-Ph 3-CF30-Ph Cl Br 80-81 151284.doc ·241· 201117722 化合物 Q1 Q2 R1 R2 m.p· (°C) MS (M+l) 422 2,4,6-三-F-Ph 4-CF30-Ph Cl Br 87-88 423 2,6-二-F， 4-MeO-Ph 3-CN, 4-Me-Ph Cl Br 145-147 424 2,4,6-三-F-Ph 3-FzCHO-Ph Cl Me 389 425 2,4,6-三-F-Ph 4-FzCHO Ph Cl Me 96-97 426 2,4,6-三-F-Ph 3-CF30-Ph Cl Me 93-94 427 2,4,6-三-F-Ph 4-CF30-Ph Cl Me 81-82 428 2,6-二-F， 4-MeO-Ph 3-CN, 4-Me-Ph Cl Me 123-125 429 2,6-二-F， 3-MeO-Ph 4-CN-Ph Cl Me 360 430 2,6-二-F-Ph 2-MeO-3-° 比咬 基 Cl Cl *本 氺* 431 2,6-二-F-Ph 2-C1-3-吡啶基 Cl Cl 360 432 2,6-二-F-Ph 2-C1-3-吡啶基 Br Br 448 6-C1, 433 2,6-二-F-Ph 2-MeO-3-D 比咬 Cl Cl 390 基 2-Cl, 434 2,6-二-F-Ph 6-MeO-3-° 比咬 Cl Cl 390 基 435 2,6-二-F-Ph 6-MeO-3-° 比咬 基 Cl Cl 356 436 2,6-二-F-Ph 6-Me〇-3-e 比咬 基 Br Br 444 437 (實例 20) 2,6-二-F， 4-HO-Ph 4-Me-Ph Cl Me 335 438 2,6_ 二-F， 4-F2CHO-Ph 4-Me-Ph Cl Me 385 439 2,6-二-F-Ph 4-CH3C (=0) NH，3-Cl-Ph Cl Cl 171-172 440 2,6-二-F-Ph 4-CH3C (=0) NH-Ph Cl Cl 191-195 441 2,6-二-F-Ph 4-CH3C (=0) NH-Ph Cl Br 224-225 442 2,6-二-F， 4-MeO-Ph 3-C1， 4-MeO-Ph Cl Br 126-128 443 2,6-二-F， 4-MeO-Ph 3-C1， 4-MeO-Ph Cl Cl 113-115 151284.doc -242- 201117722 化合物 Q1 Q2 R1 R2 m.p. (°C) MS (M+l ) 444 2,6-二-F， 4-MeO-Ph 3-1, 4-Me-Ph Cl Cl 105-107 445 2,6-二-F-Ph 4-MeOC 〇0) -Ph Cl Cl 173-174 446 3,5-二-MeO-Ph 2,6-二-F， 4-N02-Ph Br Me 456 447 2,6-二-F, 4-MeO-Ph 2-F, 4-Me-Ph Cl Cl 120-122 448 2,6-二-F, 4-MeO-Ph 2-F, 4-Me-Ph Cl Br 144-146 449 2,6-二-F， 4-MeO-Ph 3-1, 4-Me-Ph Cl Br 127-129 450 2,6-二-F， 4-MeO-Ph 3,5-二 -MeO-Ph Me Br 441 451 2,6-二-F, 4-MeO-Ph 2,6-二-Br, 3,5-二 -MeO-Ph Me Br 599 452 3-EtO，2,6-二 -F-Ph 4-Cl-Ph Cl Br 449 453 3-EtO,2,6-: -F-Ph 3-F-Ph Cl Br 433 454 3-EtO, 2,6-二 -F-Ph 4-Cl-Ph Cl Cl 403 455 3-EtO, 2,6-二 -F-Ph 3-F-Ph Cl Cl 487 456 2,6-二-F-Ph 6-C1-3-吡啶基 Cl Me 341 457 2,6-二-F， 6-CH3C (=0) Cl Cl 413 4-MeO-Ph NH-3-吡啶基 458 2,6·二-F， 4-MeO-Ph 2,6-二-Cl-3-吡啶基 Cl Cl 424 459 2,6-二-F, 4-MeO-Ph 2-Me-3-° 比咬 基 Cl Cl 370 460 2,6-二-F， 4-MeO-Ph 2-MeO-3-ntb°^ 基 Cl Cl 386 461 2,6-二-F， 4-MeO-Ph 2-Cl, 5-Me-3-°比啶基 Cl Cl 404 462 2,6-二-F， 4-MeO-Ph 5-Br-3-°比咬基 Cl Cl 434 463 3-CN，2,6-二 -F-Ph 4-F-Ph Cl Cl 368 151284.doc -243 - 201117722 化合物 Q1 Q2 R1 R2 m.p. (°c) MS (M+l) 464 3-CN，2,6-二 -F-Ph 4-Me-Ph Cl Cl 364 465 3-CN，2,6-二 -F-Ph 3-F-Ph Cl Cl 368 466 2,6-二-F-Ph 6 - C1 - 3 · °比咬基 Me Br 386 467 3-EtO，2,6-二 -F-Ph 4-Cl-Ph Cl Me 383 468 3-F-Ph 2,6-二-F, 4-MeO-Ph Me Cl φ承 469 3-F-Ph 2,6-二-F, 4-MeO-Ph Me Br 113-114 470 2,6-二-F-Ph 4-MeOC ( =0) -Ph Cl Br 186-187 471 3-CN，2,6-二 -F-Ph 6-C1-3-吡啶基 Cl Cl 387 472 2,6-二-F-Ph 6-C1-3-吡啶基 Me Cl 341 473 (實例 2,6-二-F， 3,5-二 Me Cl * * ♦ * * * 7) 4-MeO-Ph -MeO-Ph 474 2,6-二-F， 4-MeO-Ph 4-Me-Ph Cl MeS 381 475 (實例 24) 6-C1-3-吡啶基 2,6-二-F， 4-MeO-Ph Me Cl 94-95 476 3-CN，2,6-二 -F-Ph 6-C1-3-吡啶基 H Cl 351 477 4-MeO-Ph 2,4-二-Cl-Ph Cl Cl 389 478 3-CN，2,6-二 -F-Ph 6-C1-3-吡啶基 Cl Br 429 479 2,6-二-F， 4-MeO-Ph 6-MeO-3-°比咬 基 Cl Br 432 480 2,6-二-F， 4-MeO-Ph 6-CF3-3-atb 咬 基 Br Cl 470 481 (實例 22) 2,6-二-F, 4-MeO-Ph 6-CF3-3· ° 比咬 基 Cl Br 470 482 4-Cl-Ph 2,6-二-F， 4-N02-Ph Cl Me 384 483 2,6-二-F， 3-MeO-Ph 6 - C1 3 -D比咬基 Cl Cl 392 484 2,6-二-F， 4-MeO-Ph 6-MeO-3-° 比咬 基 Br Cl 432 151284.doc -244- 201117722 化合物 Q1 Q2 R1 R2 m.p. (°C ) MS (M+l ) 485 2,6-二-F-Ph 6-C1-3-吡啶基 C1 Br 406 486 3-F-Ph 2,6-二-F， 4-MeO-Ph C1CH2 Cl ** 氺氺 487 (實例 2,6-二-F， 6-CF3-3-0tt^ Cl Me 404 23) 4-MeO-Ph 基 488 2,6-二-F， 4-MeO-Ph 6-MeO-3-° 比咬 基 Cl Me 366 489 3-CN，2,6c -F-Ph 6-α-3-吡啶基 Me Br 409 490 3-CN，2,6-二 -F-Ph 6-C1-3-吡啶基 Me Cl 365 491 3-CN, 2,6-二 -F-Ph 6-C1-3-吡啶基 C1CH2 Cl 401 492 2,6-二-F-Ph 6-MeO-3-° 比咬 基 Me Cl 337 493 2,6-二-F-Ph 6·ΜεΟ-3·β 比咬 基 Me Br 381 494 3-EtO，2,6-二 -F-Ph 3-F-Ph Cl Me 367 495 2-Cl, 4-MeO-Ph 4-F-Ph Cl Br 115-118 497 2,6-二-F， 4-MeO-Ph 5-F-3-0比咬基 Cl Cl 374 498 2,6-二-F, 4-MeO-Ph 6-C1-3-吡啶基 Cl Br 434 499 2,6-二-F， 3-MeO-Ph 6 - C1 - 3 - °比咬基 Cl Br 436 500 2,6-二-F， 4-MeO-Ph 6-CF3-3-° 比咬 基 Me Br 450 501 2,6-二-F， 4-MeO-Ph 6-CF3-3-atba^. 基 Me Cl 404 502 2,6-二-F, 3-MeO-Ph 6-C1-3-。比咬基 Me Cl 370 503* 2,6-二-F，4- (實例 (MeNHCH2CH2 4-Me-Ph Cl Me 406 21) CH2) -Ph 504 2,6-二-F, 3-MeO-Ph 6-C1-3-吡啶基 Me Br 416 505 2,6-二-F， 4-MeO-Ph 6-MeO-3_° 比咬 基 Me Br 412 151284.doc •245 · 201117722 化合物 Q1 Q2 R1 R2 m.p. rc) MS (M+1) 506 2,6-二-F， 4-MeO-Ph 6-MeO-3-° 比咬 基 Me Cl 366 507 2,6-二-F， 3-MeO-Ph 6-C1-3-吡啶基 Cl Me 370 508 2,6-二4， 4-MeO-Ph 6-C1-3-吡啶基 Cl Me 370 509 (實例 5) 2,6-二-F-Ph 4-Cl-Ph Br Me 氺氺幸 * * * 510 (實例 25) 2,6-二-F， 4-MeO-Ph 4-NCS-Ph Cl Me 丰*氺 氺申氺 511 2,6-二-F， 4-HO-Ph 3-F-Ph Cl Me 339 512 (實例 2,6-二-F，4- 3-F-Ph Cl Me 26) (NCCH20) -Ph 513 4-CN，2,6-二 -F-Ph 6-C1-3-吡啶基 Me Cl 氺本 本氺 514 4-EtO,2,6-: -F-Ph 3-F-Ph Cl Br * * 515 4-EtO, 2,6-二 -F-Ph 4-Me-Ph Cl Me 150-156 516 4_EtO，2,6_二 -F-Ph 4-F-Ph Cl Me 167-171 517 4-EtO, 2,6-二 -F-Ph 3-F-Ph Cl Me 136-140 518 4-EtO, 2,6-二 -F-Ph 3-CF2HO-Ph Cl Br 109-119 519 4-EtO，2,6-二 -F-Ph 3-CF2HO-Ph Cl Cl 100-104 520 4-CN，2,6-二 -F-Ph 6-MeO-3-° 比咬 基 Me Cl 361 521 4-CN，2,6-二 -F-Ph 6-MeO-3-° 比咬 基 Me Br 405 522 4-CN，2,6-二 -F-Ph 4-Me-Ph Cl Br 409 523 4-EtO,2,6-: -F-Ph 3-CF2HO-Ph Cl Me 116-120 524 4-CN，2,6-二 -F-Ph 3-F-Ph Cl Br 413 525 4-CN，2,6-二 -F-Ph 3,4-二-F-Ph Cl Me 366 151284.doc -246- 201117722 化合物 Q1 Q2 R1 R2 m.p. (°C ) MS (M+l) 526 4-CN, 2,6-二 -F-Ph 3-F-Ph Cl Me 348 527 4-CN，2,6-二 -F-Ph 4-F-Ph Cl Br 413 528 2,6-二-F， 4-MeO-Ph 4-CF2HO-Ph Me Cl 401 529 4-CN，2,6-二 -F-Ph 4-CI-Ph Me Cl 365 530 4-CN，2,6-二 -F-Ph 3-F-Ph Me Cl 348 531 4-CN，2,6-二 -F-Ph 2,4-二-F-Ph Cl Me 366 532 4-CN，2,6-二 -F-Ph 3-CF2HO-Ph Me Cl 396 533 4-CN，2,6·二 -F-Ph 4-CF2HO-Ph Cl Cl 416 534 4-CN，2,6-二 -F-Ph 2-F, 4-Me-Ph Cl Me 362 535 4-CN，2,6c -F-Ph 2-F, 4-Me-Ph Br Me 407 536 4-CN, 2,6-二 -F-Ph 3-F-Ph Br Br 458 * HC1 鹽。 ** 1H核磁共振數據參見索引表B。 *** 1H核磁共振數據參見合成實例。Compound Q1 Q2 R1 R2 mp (°C) MS (M+1) 1 (Example 4) 2,6-di-F-Ph 4-Cl-Ph Cl Me 氺本* * * 2 (Example 3) 2, 6-di-F-Ph 4-Cl-Ph Cl Cl ♦ * * Benfeng* 3 (Example 6) 4-F-Ph 4-Cl-Ph Cl Me *♦氺4 (Example 2) 2,4,6 -Tri-F-Ph 4-Cl-Ph Cl Cl * * * 5 4-Cl-Ph 2-C1, 4-F-Ph Cl Cl 129-131 6 2,6-di-F-Ph Ph Cl Br 371 7 2,4,6-tri-F-Ph 4-Cl-Ph Cl Br 139-141 8 2,4,6-tri-F-Ph 4-Cl-Ph Cl Me 148-150 9 2,6-II -F-Ph Ph Cl I 417 J 5 ] 284.doc -225 201117722 Compound Q1 Q2 R1 R2 mp ΓΟ MS (M+l) 10 2,6-Di-F-Ph Ph Cl Me 305 11 2,6-II -F-Ph 3-F-Ph Cl Cl 131-134 12 2,4,6-tri-F-Ph 4-Cl-Ph Br Br 145-148 13 2,6-di-F-Ph 3-F- Ph Cl Br 120-122 14 2,4,6-Tri-F-Ph 4-C1, 3-F-Ph Cl Br 135-137 15 2,4,6-Tri-F-Ph 4-C1, 3- F-Ph Cl Cl 397 16 2,6-di-F-Ph 3-F-Ph Cl Me 323 17 2,4,6-tri-F-Ph 4-C1, 3-F-Ph Cl Me 375 18 2 ,6-di-F, 4-MeO-Ph 4-C1, 3-F-Ph Cl Br 氺本*本19 2,6-di-F, 4-MeO-Ph 4-C1, 3-F-Ph Cl Me 387 20 2,6-di-F-Ph 4-Cl-Ph Cl Br 124-126 21 2,4,6-tri-F-Ph 4-C1, 3-F-Ph Br Br 1 44-146 22 2,6-di-F, 4-MeO-Ph 4-Cl-Ph Cl Me 146-148 23 2,6-di-F, 4-MeO-Ph 4-Cl-Ph Cl Br 152- 153 24 2,4,6-Tri-F-Ph 4-C1, 3-F-Ph Me Me 355 25 2,6,2-F, 4-MeO-Ph 4-Cl-Ph Br Br 166-168 26 2,6-di-F, 4-MeO-Ph 4-C1, 3-F-Ph Br Br 495 27 2,6-di-F, 4-MeO-Ph 4-C1, 3-F-Ph Me Me 367 28 2,4,6-Tri-F-Ph 4-Cl-Ph Me Me * ♦ 29 (Example 14) 2,6-Di-F-Ph 3-F-Ph Cl CH=C 333 30 2,3 ,6-Tri-F-Ph 4-Cl-Ph Cl Me 357 31 2-C1, 4-F-Ph 4-Cl-Ph Cl Me 357 32 2,3,6-Tri-F-Ph 4-Cl- Ph Cl Br 124-127 33 2-C1, 4-F-Ph 4-Cl-Ph Cl Br 117-120 34 2-C1, 6-F-Ph 4-Cl-Ph Cl Br 174-177 35 2-C1 , 6-F-Ph 4-Cl-Ph Cl Me 357 36 2,6-di-F-Ph 3,5-di-F-Ph Cl Br 407 37 2,6-di-F, 4-MeO-Ph 4-Cl-Ph Me Me 105-108 38 (Example 13) 2,3,6-tri-F-Ph 4-Cl-Ph Cl CN 147-149 151284.doc -226- 201117722 Compound Q1 Q2 Ri R2 mp rc ) MS (M+l) 39 2,6-di-F-Ph 2-F-Ph Cl Br 113-115 40 2,6-di-F,4-MeO, 3-Me-Ph 4-Cl-Ph Br Me 143-147 41 2,6-di-F-Ph 2-F-Ph Cl Me 323 42 2,6-di-F-Ph 4-CF3〇-Ph Cl Br 355 43 2,6-di-F-Ph 4-Br-Ph Cl Br 143-145 44 2,6-di-F-Ph 4-F-Ph Cl Br 389 45 2,6-di-F-Ph 3,5 -B-Ph Cl Me 341 46 2-C1,3,6-di-F-Ph 4-Cl-Ph Cl Br 439 47 2-C1,3,6-di-F-Ph 4-Cl-Ph Cl Me 373 48 2,6-di-F-Ph 4-CF3〇-Ph Cl Me 389 49 2,6-di-F-Ph 4-Me-Ph Cl Me 319 50 2,6-di-F-Ph 4-F-Ph Cl Me 323 51 2,6-di-F-Ph 4-CF3-Ph Cl Br 117-120 52 2,5-di-F-Ph 4-Cl-Ph Cl Br 114-117 53 2 -CF3, 6-F-Ph 4-Cl-Ph Cl Br 455 54 2-C1, 6-F-Ph 4-Cl-Ph Cl cf3 409 55 3-Br? F-Ph 4-Cl-Ph Cl Me 419 56 2,6-di-F-Ph 4-CF3-Ph Cl Me 373 57 2,5-di-F-Ph 4-Cl-Ph Cl Me 339 58 2-CF3, 6-F-Ph 4-Cl- Ph Cl Me 389 59 2,6-di-F-Ph Bn Cl Br 85-87 60 2,6-di-F, 4-MeO-Ph 4-Cl-Ph Br MeO 141-144 61 3-C1,2 , 6-di-F-Ph 4-Cl-Ph Cl Br 439 62 2,6-di-F-Ph 3-Cl-Bn Cl Br 419 63 2,6-di-F-Ph 4-C1, 3- F-Bn Cl Br 437 64 2,6-di-F-Ph 4-Cl-Bn Cl Br 419 65 2,6-di-F, 3-Me-Ph 4-Cl-Ph Cl Br 419 66 2,6 -di-F, 3-Me-Ph 4-Cl-Ph Cl Me 353 67 2,6-di-F-Ph 4-Cl-Ph Cl Et 125-126 68 3- Br, 2-F, 4- MeO -Ph 4-Cl-Ph Cl Br 498 151284.doc -227- 201117722 Compound Q1 Q2 R1 R2 mp (t) Mb (M+l) 69 2-F, 4-MeO-Ph 4-Cl-Ph Cl Br 417 70 2 -F, 4-MeO-Ph 4-Cl-Ph Cl Me 351 71 2-F, 4-MeO, 3-Me-Ph 4-Cl-Ph Cl Me 365 72 2,6dPh 4-Cl-Ph Cl i- Pr 106-108 73 2,6-di-F, 3-MeO-Ph 4-Cl-Ph Cl Br 435 74 2,6-di-F-Ph Bn Cl Me 319 75 2,6-di 4, 4- HO-Ph 4-Cl-Ph Cl Me 355 76 2,6-di-F-Ph 4-Cl, 3-F-Bn Cl Me 371 77 2,6-di-F, 3-MeO-Ph 4-Cl -Ph Cl Me 369 78 2,6-di-F-Ph 3-Cl-Bn Cl Me 353 79 3-C1,2,6-di-F-Ph 4-Cl-Ph Cl Me 375 80 2,6- bis-F-Ph 4-Cl-Bn Cl Me 353 81 2,3,6-tri-F-Ph 4-F-Ph Cl Cl 361 82 2,3,6-tri-F-Ph 4-Me-Ph Cl Cl 357 83 4-Cl-Ph 2,4,6-tri-F-Ph Cl Br 117-118 84 2,3,6-tri-F-Ph 4-F-Ph Cl Br 407 85 2,3, 6-Tri-F-Ph 4-Cl, 3-F-Ph Cl Cl 395 86 4-C1, 2-F, 6-MeO-Ph 4-Cl-Ph Cl Br 451 87 2,3,6-Tri- F-Ph 4-Me-Ph Cl Br 403 88 2,6-di-F, 4-MeO-Ph 4-F-Ph Cl Cl 373 89 2,3,6-tri-F-Ph 4-Cl, 3 -F-Ph Cl Br 441 90 2,6-27-4-MeO-Ph 4-F-Ph Cl Br 419 91 2,3,6-Tri-F-Ph 4-F-Ph Cl Me 341 92 2,6-di-F, 4-MeO-Ph 4-Me-Ph Cl Cl 369 93 2,4,6·Tri-F-Ph 4-F-Ph Cl Cl 361 94 2,6-di- F, 4-MeO-Ph 4-Me-Ph Cl Br 415 95 4-Cl, 2-F, 6-MeO-Ph 4-Cl-Ph Cl Me 387 96 4-Cl-Ph 2,6-di-F -Ph Cl Cl 123-126 151284.doc -228- 201117722 Compound Q' Q2 R1 R2 mp (°C) MS (M+l) 97 2,6-:-F-Ph 4-Cl-Ph Me Me 146- 148 98 2,4,6-SF-Ph 4-F-Ph Cl Br 407 99 2,4,6-SF-Ph 4-Me-Ph Cl Br 403 100 2,4,6-Tri-F-Ph 4 -Me-Ph Cl Cl 357 101 2,3,6-SF-Ph 4-Me-Ph Cl Me 337 102 4-EtO, 2,6-di-F-Ph 4-Cl-Ph Cl Me 383 103 2, 3,6-tri-F_Ph 4-C1, 3-F-Ph Cl Me 375 104 2,6-di-F, 4-MeO-Ph 4-F-Ph Cl Me 353 105 2,6-di-F, 4-MeO-Ph 4-Me-Ph Cl Me 349 106 4-Cl-Ph 2,6-di-F-Ph Br Br 156-158 107 4-Cl-Ph 2,6-di-F-Ph Cl Br 148-150 108 2,4,6-tri-F-Ph 4-F-Ph Cl Me 341 109 2,4,6-tri-F-Ph 4-Me-Ph Cl Me 337 110 2,6-di- F-Ph 3,4-di-F-Ph Cl Br 407 111 2,6-di-F-Ph 3-F, 4-Me-Ph Cl Br 403 112 2-C1, 6-F, 4-MeO- Ph 4-Cl-Ph Cl Br 451 113 2-C1, 6-F, 4-MeO-Ph 4-Cl-Ph Cl Me 385 114 2,6-di-F-Ph 3,4- bis-F-Ph Cl Me 341 115 2,6-di-F-Ph 3-F, 4-Me-Ph Cl Me 337 116 2-C1, 4-F-Ph 4-F-Ph Cl Br 111-112 117 2-C1, 4-F-Ph 4-F-Ph Cl Cl 359 118 2-C1, 4-F-Ph 4-Me-Ph Cl Br 127-128 119 2-C1, 6-F-Ph 4- F-Ph Cl Br 95-97 120 2-C1, 6-F-Ph 4-Me-Ph Cl Br 147-148 121 2-C1, 4-F-Ph 4-F-Ph Cl Me 101-106 122 2 -C1, 4-F-Ph 4-Me-Ph Cl Me 148-149 123 2-C1, 6-F-Ph 4-F-Ph Cl Me 122-123 124 2-C1, 6-F-Ph 4- Me-Ph Cl Me 158-162 125 2-C1,3,6-di-F-Ph 4-F-Ph Cl Br 423 126 2-C1,3,6-di-F-Ph 4-F-Ph Cl Cl 378 151284.doc -229- 201117722 Compound Q1 Q2 R1 R2 mp (°C) MS (M+l 127 2-Cl,3,6-di-F-Ph 4-Me-Ph Cl Br 419 128 2-C1 ,3,6-di-F-Ph 4-Me-Ph Cl Cl 374 129 2,6-di-F-Ph 3-啥琳基 Cl Me 158-160 130 4-CN,2,6-di-F -Ph 4-Cl-Ph Cl Br 429 131 2-C1,4-F-Ph 4-C1, 3-F-Ph Cl Br 103-104 132 2-C1,6-F-Ph 4-C1, 3- F-Ph Cl Br 80-84 133 4-Cl-Ph 2,4,6-tri-F-Ph Cl Cl 76-78 134 4-CN,2,6-di-F-Ph 4-Cl-Ph Cl Me 429 135 2-C1,3,6-di-F-Ph 4-F-Ph Cl Me 429 136 2-C1,3,6-di-F -Ph 4-Me-Ph Cl Me 429 137 2,6-di-F-Ph 3-C1, 4-MeO-Bn Cl Cl 405 138 4-Cl-Ph 2,6-di-F, 4-MeO- Ph Br Cl 119-122 139 4-Cl-Ph 2,6-di-F-Ph Me Br 156-158 140 2,6-di-F-Ph 4-Cl-Ph h2c= CH Me 141-143 141 4 -Cl-Ph 2,4,6-tri-F-Ph Br Br 130-131 142 2-C1,3,6-di-F-Ph 4-C1, 3-F-Ph Cl Br 457 143 2-C1 ,3,6-di-F-Ph 4-C1, 3-F-Ph Cl Cl 413 144 2,6-di-F-Ph 3-Cl-Ph Cl Br 405 145 2,6-di-F-Ph 3-Cl-Ph Cl Cl 361 146 2,6-di-F-Ph 4-C1, 3-F-Ph Cl Br 423 147 2,3,6-tri-F-Ph 3,4-di-Me- Ph Cl Br 417 148 2,6-di-F-Ph 4-C1, 3-F-Ph Cl Cl 379 149 2,3,6-tri-F-Ph 3,4-di-Me-Ph Cl Cl 371 150 2-C1, 6-F-Ph 4-Me-Ph Cl Cl 142-143 151 2-C1, 6-F-Ph 4-F-Ph Cl Cl 102-103 152 2-C1, 4-F-Ph 4-C1, 3-F-Ph Cl Cl 116-117 153 2-C1, 6-F-Ph 4-C1, 3-F-Ph Cl Cl 66-67 151284.doc -230- 201117722 Compound Q1 Q2 R1 R2 Mp (°C) MS (M+l 154 2,6-di-F, 3-MeS-Ph 4-Cl-Ph Cl Br 451 155 4-Cl-Ph 2,4,6-tri-F-Ph Br Cl 111-112 156 2,3,6-tri-F-Ph 3,4-di-Cl-Ph Cl Cl 413 157 2,6-di-F, 3-MeS-Ph 4-Cl-P h Cl Me 385 158 2,6-di-F-Ph 3-Cl-Ph Cl Me 339 159 2-C1,3,6-di-F-Ph 4-C1,3-F-Ph Cl Me 393 160 2 ,3,6-SF-Ph 3,4-di-Me-Ph Cl Me 351 161 2,6-di-F, 4-MeO-Ph 4-Cl-Ph Cl Cl 391 162 2,6-di-F , 4-MeO-Ph 4-C1, 3-F-Ph Cl Cl 407 163 2,6-27-4-MeO-Ph 4-C1, 3-F-Ph Cl I 499 164 4-Cl-Ph 2, 6-di-F, 4-MeO-Ph Br Br 137-139 165 2-C1, 4-F-Ph 4-C1, 3-F-Ph Cl Me 89-91 166 2-C1, 6-F-Ph 4-C1, 3-F-Ph Cl Me 140-142 167 2,6-di-F, 4-MeO-Ph 4-Cl-Ph Cl I 481 168 2,6-di-F-Ph 4-C1, 3-F-Ph Cl Me 358 169 4-Cl-Ph 2,6-di-F, 4-MeO-Ph Me Me 105-108 170 (Example 8) 2,6-di-F, 4-MeO-Ph 3-F-Ph Cl Br 418 171 2,6-di-F, 4-MeO-Ph 3-F-Ph Cl Cl 373 172 2,6-di-F-Bn 4-Cl-Ph Cl Me 353 173 2 -F-Ph 4-C1, 3-F-Ph C1CH2 Cl 373 174 2-F-Ph 4-C1, 3-F-Ph Me Cl 339 175 2,6-di-F, 4-MeO-Ph 4- C1, 3-F-Ph Me Cl 387 176 3,5 -di-C1 - 4 - ntb bite 4-C1, 3-F-Ph Me Cl 390 177 2,6-di-F, 4-MeO-Ph 6-C1-3-pyridyl Me Cl 370 178 2-pyridyl 4-C1, 3-F-Ph Me Cl 322 -231 - 151284.doc 201 117722 Compound Q1 Q2 R1 R2 mp (°C) MS (M+l) 179 2,6-di-F, 3-MeO-Ph 3-F-Ph Cl Br 419 180 2,6-di-F, 3- MeO-Ph 3-F-Ph Cl Cl 373 181 (Example 9) 2,6-di-F, 4-MeO-Ph 3-F-Ph Cl Me 354 182 2,6-di-F, 3-MeO- Ph 4-Me-Ph Cl Br 415 183 2-C1, 4-F-Ph 4-Me-Ph Cl Cl 72-73 184 2,6-di-F, 4-MeO-Ph 4-Cl-Bn Cl Br 139-140 185 2,6-di-F, 4-MeO-Ph 4-Cl-Bn Cl Cl 123-124 186 2,3,6-iF-Ph 4-Cl-Bn Cl Cl 氺氺187 2,3 ,6-tri-F-Ph 4-Cl-Bn Cl Br 87-88 188 2,6-di-F, 4-MeO-Ph 4-Cl-Bn Cl Me 116-117 189 2,6-di-F , 3-MeO-Ph 4-Cl-Bn Cl Cl *氺** 190 2,6-di-F, 3-MeO-Ph 4-Cl-Bn Cl Br 449 191 4-Cl-Ph 3-Cl-Bn Cl Br 108-109 192 2,6-di-F, 4-MeO-Ph 4-Me-Bn Cl Cl 383 193 2,6-di-F, 4-MeO-Ph 4-Me-Bn Cl Br 104- 105 194 2,3,6-tri-F-Ph 4-Cl-Bn Cl Me 371 195 2,6-di-F, 3-MeO-Ph 4-Cl-Bn Cl Me 384 196 4-Cl-Ph 3 -Cl-Bn Cl Me 113-114 197 2,6-di-F, 4-MeO-Ph 4-Me-Bn Cl Me 363 198 4-Cl-Ph 2,6-di-F, 4-MeO-Ph Cl Cl 117-118 199 (Example 15) 2,6-di-F, 4-MeO-Ph 4-FP h Cl HOCH2 氺氺200 4-C1, 3-F-Ph 2-C1, 4-F-Ph Br Br 104-106 201 4-C1, 3-F-Ph 2-C1, 4-F-Ph Cl Cl 120-122 202 2,6-di-F-Ph 4-Cl-Ph Et Me 122-124 203 4-Cl-Ph 2-C1, 4-F-Ph Br Br 114-116 151284.doc •232· 201117722 Compound Q1 Q2 R1 R2 mp (°C) MS (M+l) 204 4-Cl-Ph 2-Cl, 4-F-Ph Me Me 336 205 4-Cl-Ph 2,4,6-Tri-F- Ph Me Me 90-92 206 2,6-di-F, 3-MeO-Ph 4-Cl-Ph Cl Cl 391 207 2,6-di-F, 3-MeO-Ph 4-Me-Ph Cl Cl 369 208 2,6-di-F, 3-MeO-Ph 4-F-Ph Cl Br 419 209 2,6-di-F, 3-MeO-Ph 3-F-Ph Cl Me 353 210 2,6-two -F, 3-MeO-Ph 3-Me-Ph Cl Br 414 211 2,6-di-F, 3-MeO-Ph 4-C1,3-F-Ph Cl Br 453 212 2,6-di-F -Ph 5-C1-2-pyridyl Me Cl * * 213 2-F-4-pyridyl 4-C1, 3-F-Ph C1CH2 Cl * * *氺214 2-F-4-Dit bite base 4- C1, 3-F-Ph Me Cl * % 215 4-Cl-Ph 2-Cl, 4-F-Ph Br Cl 106-109 216 4-C1, 3-F-Ph 2-Cl, 4-F-Ph Me Br 105-107 217 4-C1, 3-F-Ph 2-Cl, 4-F-Ph Br Cl 116-118 218 2,6-di-F-Ph-based Cl Br 176-180 219 4-C1, 3-F-Ph 2-Cl, 4-F-Ph Cl Br 120-122 220 4-Cl-Ph 2-Cl, 4-F -Ph Cl Br 113-116 221 (Example 16) 2,6-di 4, 4-MeO-Ph 4-F-Ph Cl fch2 Water* 本氺氺氺222 2,6-di-F, 3-MeO- Ph 4-Me-Ph Cl Me 349 223 2,6-di-F, 3-MeO-Ph 4-F-Ph Cl Me 353 224 2,6-di-F, 3-MeO-Ph 3-Me-Ph Cl Me 113-117 225 4-Cl-Ph 2-Cl, 4-F-Ph Br Me 127-131 226 4-Cl-Ph 2-Cl, 4-F-Ph Me Br 146-150 227 4-C1, 3-F-Ph 2-Cl, 4-F-Ph Br Me 125-127 228 2,3,6-tri-F-Ph 4-C1, 3-F-Ph Br Cl * * 229 2,3,6 -Tri-F-Ph 4-Cl-Ph Br Cl Lucky 230 2,3,6-Tri-F-Ph 4-F-Ph Br Cl Umbrella 231 2-Br-4-°tb 4-C1, 3-F-Ph C1CH2 Cl 434 232 2-Br-4-° ratio bite base 4-C1, 3-F-Ph Me Cl 400 151284.doc · 233 · 201117722 Compound Q1 Q2 R1 R2 mp ( °C) MS (M+1) 233 5-Br-3-B ratio bite base 4-Cl, 3-F-Ph C1CH2 Cl 434 234 5-Br-3-° ratio bite base 4-C1, 3-F -Ph Me Cl 400 235 5-Br-2-° ratio bite base 4-Cl, 3-F-Ph CICH2 Cl water present* * 236 5-ΒΓ-2·11 ratio bite base 4-Cl, 3-F- Ph Me Cl 400 237 2-C1-3-pyridyl 4-Cl, 3-F-Ph CICH2 Cl 390 238 2-C1-3-pyridyl 4-Cl, 3-F-Ph Me Cl 356 239 4-Cl -Ph 3-Cl-Bn Cl Cl 107 -109 240 2,4,6-tri-F-Ph 3-F-Ph Cl Cl 78-81 241 2,3,6-tri-F-Ph 3-F-Ph Cl Cl 143-145 242 2,4 ,6-tri-F-Ph 3-F-Ph Cl Br 130-132 243 2,3,6-tri-F-Ph 3-F-Ph Cl Br 137-138 244 2,3,6-tri-F -Ph 3-F-Ph Cl Me 146-147 245 2,4,6-tri-F-Ph 3-F-Ph Cl Me 150-152 4,5-di-Br, 246 1-Me-1H-imidazole 4-Cl-Ph Br Br 496 -2-yl 4,5 ·Βγ, 247 1-Me-1H-imidazole 4-Cl-Ph Br Br 575 -2-yl 248 4-Cl-Ph 2,6-di, F, 4-MeO-Ph Cl Br 118-125 249 2-C1,3,6-di-F-Ph 4-Cl-Ph Br Br 氺φ 250 6 - M e - 2 - ° ratio 4-Cl, 3-F-Ph Me Cl 氺*氺251 6-Me-2-° Ratio 4-Cl, 3-F-Ph cich2 Cl 氺252 4-C1-5-thiazolyl 4-Cl, 3-F -Ph Me Cl 氺* * * 253 2,4-di-Cl-5-thiazolyl 4-Cl, 3-F-Ph Me Cl 氺氺254 2,3,6-tri-F-Ph 4-Cl, 3-F-Ph Br Br 255 255 2,3,6-tri-F-Ph 4-Cl-Ph Br Br 467 256 2,3,6-tri-F-Ph 4-F-Ph Br Br 449 257 2-C1,3,6-di-F-Ph 4-Cl-Ph Br Cl 439 258 2-C1, 3,6-di-F-Ph 4-Cl-Ph Me Me 353 259 2,3,6- Tri-F-Ph 4-Cl, 3-F-Ph Me Cl Umbrella 260 2,6-di_F, 3-MeO-Ph 4-F-Ph Cl Cl 374 151284.doc •234 201117722 Compound Q1 Q2 R1 R2 mp (°C ) MS (M+1 261 2,6-di-F, 3-MeO-Ph 3- Me-Ph Cl Cl 133-136 262 2,6-di-F, 3-MeO-Ph 4-C1, 3-F-Ph Cl Cl 84-86 263 2,6-di-F, 3-MeO-Ph 4-C1, 3-F-Ph Cl Me 387 264 4-Cl-Ph 2,6-27-4-MeO-Ph Me Cl 104-106 265 4-Cl-Ph 2,6-di-F, 4- MeO-Ph C1CH2 Cl 127-129 266 2,6-di-F, 3-MeO-Ph 3-Et-Ph Cl Br 429 267 2,6-di-F, 3-MeO-Ph 4-C1, 3- Me-Ph Cl Cl 403 268 2,6-di-F, 3-MeO-Ph 3-F2CHO-Ph Cl Cl 100-102 269 2,6-di-F, 3-MeO-Ph 4-C1, 3- Me-Ph Cl Br 449 270 2,6-di-F, 3-MeO-Ph 3-F2CHO-Ph Cl Br 109-111 271 2,4-di-F-Bn 4-Cl-Ph Br Me 399 272 3 -C1, 2,6-di-F, 4-MeO-Ph 4-Me-Ph Cl Cl 氺 氺 273 2,6-di-F, 4-MeO-Ph 6-C1-3-pyridyl Cl Cl 390 274 3-CN,2,6-di-F-Ph 4-Cl-Ph Cl Cl 386 275 4-Br, 5-MeS-2-thienyl 4-Cl-Ph Br Br 545 276 2,3, 6-SF-Ph 4-Cl-Ph Me Cl 277 2,3,6-SF-Ph 4-F-Ph Me Cl 氺氺* * 278 2-C1, 3,6-di-F-Ph 4- Cl-Ph Me Cl 氺本本* 279 2,3,6-2-F-Ph 4-C1, 3-F-Ph Me Me *氺* * 280 2,3,6-Tri-F-Ph 4-Cl-Ph Me Me 氺* 281 2,3,6-Tri-F-Ph 4-F-Ph Me Me 氺氺氺氺282 2,6-di-F, 3-MeO-Ph 3-Et-Ph Cl Me 364 283 (Example 18) 3-CN, 2,6-di-F-Ph 4-Cl-Ph Cl Br 430 151284.doc 235 · 201117722 Compound Q1 Q2 R1 R2 mp (r) MS (M+l) 284 4-C1, 3-F-Ph 2-C1, 4-F-Ph Cl Me 108-110 285 4 -Cl-Ph 2-C1, 4-F-Ph Cl Me 135-137 286 4-Cl-Ph 2,6-di-F, 4-MeO-Ph Cl Me 108-110 287 2,6-di-F , 3-MeO-Ph 4-C1, 3-Me-Ph Cl Me 383 288 2,6-di-F, 3-MeO-Ph 3-F2CHO-Ph Cl Me 401 289 2,6_ Di-F, 3- MeO-Ph 3-Et-Ph Cl Cl 93-95 290 3-Cl,2,6-di-F, 4-MeO-Ph Ph Cl Cl 391 291 3-Br,2,6-di-F, 4- MeO-Ph Ph Cl Br 479 292 (Example 19) 3-CN,2,6-di-F-Ph 4-Cl-Ph Cl Me 364 293 6-Br-2-Dtb Group 4-C1, 3-F- Ph Cl Cl 420 294 6-MeO-3-a ratio bite base 4-C1, 3-F-Ph Cl Cl * * 295 3_F, 5-MeO-4·0-pyridyl 4-C1, 3-F-Ph Cl Cl 390 296 3-Quinyl 4-C1,3-F-Ph Cl Cl 392 297 2,6-Di-Cl, 4-MeO-Ph 4-C1, 3-F-Ph Cl Cl 298 2,4- Di-Cl, 6-MeO-Ph 4-C1, 3-F-Ph Cl Cl ** 299 2,6-di-F,4-MeO, 3-Me-Ph Ph Cl Me 349 300 2,3,6-tri-F-Ph 3,4-di-Cl-Ph Cl Br 457 301 2,6-di-F, 3-MeO-Ph 4-Et-Ph Cl Br 429 302 2,6-di-F, 3-MeO-Ph 4-Et-Ph Cl Cl 383 303 2,6_ di-F , 3-MeO-Ph 4-I-Ph Cl Br 134-138 304 2,6-di-F, 3-MeO-Ph 4-I-Ph Cl Cl 481 305 4-Cl-Ph 2,4,6- Tri-F-Ph Me Br 123-125 306 4-Cl-Ph 2,4,6-Tri-F-Ph Me Cl 86-88 307 4-Cl-Ph 2,4,6-Tri-F-Ph Me H 110-112 151284.doc -236- 201117722 Compound Q1 Q2 R1 R2 mp (°C) MS (M+1 308 2,6-di-F, 4-MeO-Ph 3-Cl-Ph Cl Cl 氺氺* * 309 2,6-di-F, 4-MeO-Ph 3,4-di-F-Ph Cl Cl 391 310 3-F-4-° ratio bite 4-Cl, 3-F-Ph Cl Cl 360 311 4-Cl, 2-MeO-5-D plug-in 4-yl, 3-F-Ph Cl Cl 412 312 4-C1-5-thiazolyl 4-Cl, 3-F-Ph Cl Cl 482 313 2-C1-3-pyridyl 4-Cl, 3-F-Ph Cl Cl 376 314 2-C1,3,6·di-F-Ph 4-Cl, 3-F-Ph Br Br *氺*本315 2-C1,3,6-di-F-Ph 4-Me-Ph Br Br *氺氺本316 2,3,6-Tri-F-Ph 4-Me-Ph Br Br 本丰本本317 2,4 ,6-Tri-F-Ph 4-F-Ph Br Br 318 318 2-C1, 3,6-B-F-Ph 4- Cl, 3-F-Ph Br Cl 氺* 319 2-C1, 3,6-di-F-Ph 4-Me-Ph Br Cl 氺氺氺* 320 2,3,6-Tri-F-Ph 4- Me-Ph Br Cl *氺*氺321 4-Cl-Ph 2,6-di-F-Ph Me Cl 127-129 322 4-Cl-Ph 2,6-di-F-Ph MeO- ch2 Cl 95- 97 323 2,6-di-F-Ph 6-quinolinyl Cl Me 210-215 324 2,6-di-F, 3-MeO-Ph 4-Cl-Ph Br Br 氺氺* * 325 2,6-two -F, 3-MeO-Ph 4-F-Ph Br Cl 417 326 (Example 17) 2,6-di-F-Ph 4-Cl-Ph Br BrCH2 463 2-Br, 327 2,4-di-F -Bn 3,5-di-MeO-Ph Br Me 582 328 2,6-di-F, 3-MeO-Ph 4-Et-Ph Cl Me 364 329 2,3,6-tri-F-Ph 3, 4_二_C1-Ph Cl Me 391 330 2- C1, 6-F, 3- MeO-Ph 4-Cl-Ph Cl Cl 407 151284.doc -237 201117722 Compound Q1 Q2 Ri R2 mp (°C) MS (M +1) 331 2,6-di-F, 4-MeO-Ph 3-Cl-Ph Cl Br 435 332 2,6-di-F, 4-MeO-Ph 3,4-di-F-Ph Cl Br 437 333 2-Br-4_e ratio bite base 4-C1, 3-F-Ph Cl Cl 420 334 5-Br-3-D ratio bite base 4-C1, 3-F-Ph Cl Cl 420 335 5-Br- 2-Dtt base 4-C1, 3-F-Ph Cl Cl 本丰336 2,6-di-F, 4-MeO-Ph 6-CF3-3-°tt^ base Cl Cl 337水337 2-C1, 3,6-di-F-Ph 4-Cl, 3-FP h Me Me 氺氺338 2,3,6-Tri-F-Ph 4-Me-Ph Me Me 氺氺氺氺339 2,4,6-Tri-F-Ph 4-F-Ph Me Me 氺* 340 2,4,6-tri-F-Ph 4-F-Ph Me Cl 氺氺 本 341 2-C1,3,6-di-F-Ph 4-Me-Ph Me Me (4) 342 2-C1,3 ,6-di-F-Ph 4-Cl, 3-F-Ph Me Cl Φ木*氺343 2-C1,3,6-di-F-Ph 4-Me-Ph Me Cl 氺本氺 344 2, 3,6-tri-F-Ph 4-Me-Ph Me Cl 345 2,6-di-F, 4-MeO-Ph 3,4-di-F-Ph Cl Me 169-170 346 2,6-two -F, 4-MeO-Ph 3-Cl-Ph Cl Me 173-174 347 2- C1, 6-F, 3-MeO-Ph 4-Cl-Ph Cl Br 154-156 348 2,6-di-F , 4-MeO-Ph 3-C1, 4-Me-Ph Cl Cl 143-145 349 4-Cl-Ph 2-C1, 4-F-Ph Me Cl 123-127 350 (Example 10) 2,6-II -F, 3-MeO-Ph 4-F-Ph Br Br 134-136 351 2,6-di-F, 3-MeO-Ph 4-Cl-Ph Br Cl *本** 352 2,6-di- F, 3-MeO-Ph 4-Me-Ph Br Br 459 353 2-C1, 6-F, 5-MeO-Ph 4-Cl-Ph Cl Br 451 354 2,6-di-F, 4-MeO- Ph 2-C1-3-pyridyl Cl Cl 390 151284.doc •238- 201117722 Compound Q1 Q2 R1 R2 mp rc) MS (M+l) 355 2,6-di-F, 4-MeO-Ph 6-Cl , 2-MeO-3-° than bite Cl Cl 氺氺氺氺 356 2,6 -di-F, 4-MeO-Ph 2-C1, 6-MeO-3-° ratio bite base Cl Cl 420 357 2,6-di-F, 4-MeO-Ph 6-MeO-3-° ratio bite Cl Cl 386 358 2,6_ di-F, 3-MeO-Ph 4-Me-Ph Br Cl 415 359 2-C1, 6-F, 5-MeO-Ph 4-Cl-Ph Cl Cl 407 360 2- C1, 6-F, 3-MeO-Ph 4-Cl-Ph Cl Me 387 361 2,6d, 4-MeO-Ph 4-Me-Ph Me Me 氺本本362 2,6-二-F, 4- MeO-Ph 4-F-Ph Me Me * * ** 363 2,6-di-F, 4-MeO-Ph 4-F-Ph Br Br 氺364 2,6-di-F, 4-MeO- Ph 4-Me-Ph Br Br 365 365 4-Me-Ph 2,6-di-F, 4-MeO-Ph Me Br 128-129 366 2,6-di-F, 3-MeO-Ph 4- Cl-Ph Me Cl 369 367 2,6-di-F-Ph 4-ClCH2S-Ph Cl Me 386 368 2,4,6-tri-F-Bn 4-Cl-Ph H Me 338 369 2,4,6_ Tri-F-Bn 4-Cl-Ph Cl Me 372 370 2,4,6-Tri-F-Bn 4-Cl-Ph Br Me 417 371 2,4,6-Tri-F-Bn 3,5-II -MeO-Ph Cl Me 398 372 2,4,6-tri-F-Bn 3,5-di-MeO-Ph Br Me 442 373 2,4,6-tri-F-Bn 2,6-di-Cl -Ph Cl Me 407 374 2,4,6·Tri-F-Bn 2,6-di-Cl-Ph Br Me 451 375 2,4,6-tri-F-Bn 3,5-di-Cl-Ph Cl Me 407 376 2,4,6-tri-F-Bn 3,5-di-Cl-Ph Br Me 451 151284.doc -239- 201117722 Compound Q1 Q2 R1 R2 mp (°C) MS (M+l) 377 2,6-di-F, 4-MeO-Ph 3-C1,4-Me-Ph Cl Br 161-163 378 4-C1, 3 -F-Ph 2-C1, 4-F-Ph Me Me 354 379 2,6-di-F, 4-MeO-Ph 3-F2CHO-Ph Cl Br 467 380 2,6-di-F, 4-MeO -Ph 4-F2CHO-Ph Cl Br 467 381 2,6-di-F, 4-MeO-Ph 3-CF30-Ph Cl Br 485 382 2,6-di-F, 4-MeO-Ph 4-CF30- Ph Cl Br 80-82 383 (Example 11) 2,6-di-F, 3-MeO-Ph 4-F-Ph Me Me 333 384 2-Cl,6-F, 5-MeO-Ph 4-Cl- Ph Cl Me 387 385 2,6-di-F, 3-MeO-Ph 3-F, 4-Me-Ph Cl Br 432 386 2,6-di-F, 3-MeO-Ph 4-CN-Ph Cl Cl 191-193 387 2,6-di-F, 4-MeO-Ph group Cl Cl 370 388 2,6-di-F, 4-MeO-Ph 6-Me-3-° ratio bite Br Br 458 389 2,6-di-F, 3-MeO-Ph 3-F, 4-Me-Ph Cl Cl 387 390 2,6-di-F, 3-MeO-Ph 4-Br-Ph Cl Cl 435 391 2, 6-di-F, 3-MeO-Ph 4-Br-Ph Cl Br 479 392 4-Me-Ph 2,6-di-F, 4-MeO-Ph Me Cl 121-122 393 2,6-di- F, 4-MeO-Ph 3-F2CHO-Ph Cl Cl 68-70 394 2,6-di-F, 4-MeO-Ph 4-F2CHO-Ph Cl Cl 421 395 2,6-di-F, 4- MeO-Ph 3-CFsO-Ph Cl Cl 94-95 396 2,6-di-F, 4 -MeO-Ph 4-CF30-Ph Cl Cl 90-91 151284.doc -240- 201117722 Compound Q1 Q2 R1 R2 mp (°c ) MS (M+l ) 397 2,6-di-F, 4-MeO- Ph 4-F2CHO-Ph Cl Me 401 398 2,6-27-Me-Ph 3-CN, 4-Me-Ph Cl Cl 141-143 399 4-C1, 3-F-Ph 2-C1,4 -F-Ph Me Cl 106-109 400 2,6-di-Cl, 4-MeO-Ph 4-C1,3-F-Ph Cl Br 3 (E氺% 401 4-CN, 2-F, 6 -MeO-Ph 4-C1, 3-F-Ph Cl Cl 氺孝氺本402 2,6-di-F, 4-MeO-Ph 2-Br-3 - Dtt* 咬基 Cl Cl 氺氺** 403 2,6-di-F-Ph 5-Me-2-n ratio bite group Cl Cl * * 404 4-Me-Ph 2,6-di-F, 4-MeO-Ph C1CH2 Cl umbrella *氺405 2 ,6-di-F, 3-MeO-Ph 4-Br-Ph Cl Me 415 406 (Example 12) 2,6-di-F, 3-MeO-Ph 3-F2CHO-Ph Cl h2c=c H 413 407 2,6-di-F, 4-MeO-Ph 3-F2CHO-Ph Cl Me 401 408 2,6-di-F, 4-MeO-Ph 3-CF30-Ph Cl Me 419 409 2,6-di- F, 3-MeO-Ph 3-F, 4-Me-Ph Cl Me 367 410 2,6-di-F-Ph Ph Cl Cl 325 411 2,6dPh 6-C1-3-pyridyl Cl Cl ** 氺* 412 3,5-di-?-4-° ratio bite base 4-C1, 3-F-Ph Cl Cl 氺 413 2,6-di-F, 3-MeO-Ph 4-CN-Ph Cl Br 426 414 2,4,6-three-F-Ph 3_F2CHO-Ph Cl Cl 82-83 415 2,4,6-tri-F-Ph 4-F2CHO-Ph Cl Cl 91-92 416 2,4,6-tri-F-Ph 3-CF30-Ph Cl Cl 76-77 417 2,4,6-tri-F-Ph 4-CF30-Ph Cl Cl 75-76 418 2,6-di-F, 4-MeO-Ph 3-C1, 4-Me-Ph Cl Me 143-145 419 2,4,6-tri-F-Ph 3-CF2HO-Ph Cl Br 89-90 420 2,4,6-tri-F-Ph 4-F2CHO-Ph Cl Br 94-95 421 2,4,6- Tri-F-Ph 3-CF30-Ph Cl Br 80-81 151284.doc ·241· 201117722 Compound Q1 Q2 R1 R2 mp· (°C) MS (M+l) 422 2,4,6-Tri-F- Ph 4-CF30-Ph Cl Br 87-88 423 2,6-di-F, 4-MeO-Ph 3-CN, 4-Me-Ph Cl Br 145-147 424 2,4,6-tri-F- Ph 3-FzCHO-Ph Cl Me 389 425 2,4,6-Tri-F-Ph 4-FzCHO Ph Cl Me 96-97 426 2,4,6-Tri-F-Ph 3-CF30-Ph Cl Me 93 -94 427 2,4,6-Tri-F-Ph 4-CF30-Ph Cl Me 81-82 428 2,6-di-F, 4-MeO-Ph 3-CN, 4-Me-Ph Cl Me 123 -125 429 2,6-di-F, 3-MeO-Ph 4-CN-Ph Cl Me 360 430 2,6-di-F-Ph 2-MeO-3-° than bite Cl Cl *Ben* 431 2,6-di-F-Ph 2-C1-3-pyridyl Cl Cl 360 432 2,6-di-F-Ph 2-C1-3-pyridyl Br Br 448 6-C1, 433 2,6 -di-F-Ph 2-MeO-3-D is more than a bit of Cl Cl 390 base 2-Cl, 434 2,6-di-F-Ph 6-MeO-3-° than bite Cl Cl 390 base 435 2,6-di-F-Ph 6-MeO-3-° ratio bite Cl Cl 356 436 2,6 - bis-F-Ph 6-Me〇-3-e ratio bitr Br Br 444 437 (Example 20) 2,6-di-F, 4-HO-Ph 4-Me-Ph Cl Me 335 438 2,6_ 2-F, 4-F2CHO-Ph 4-Me-Ph Cl Me 385 439 2,6-di-F-Ph 4-CH3C (=0) NH,3-Cl-Ph Cl Cl 171-172 440 2,6 -di-F-Ph 4-CH3C (=0) NH-Ph Cl Cl 191-195 441 2,6-di-F-Ph 4-CH3C (=0) NH-Ph Cl Br 224-225 442 2,6 -2-F, 4-MeO-Ph 3-C1, 4-MeO-Ph Cl Br 126-128 443 2,6-di-F, 4-MeO-Ph 3-C1, 4-MeO-Ph Cl Cl 113 -115 151284.doc -242- 201117722 Compound Q1 Q2 R1 R2 mp (°C) MS (M+l) 444 2,6-di-F, 4-MeO-Ph 3-1, 4-Me-Ph Cl Cl 105-107 445 2,6-di-F-Ph 4-MeOC 〇0) -Ph Cl Cl 173-174 446 3,5-di-MeO-Ph 2,6-di-F, 4-N02-Ph Br Me 456 447 2,6-di-F, 4-MeO-Ph 2-F, 4-Me-Ph Cl Cl 120-122 448 2,6-di-F, 4-MeO-Ph 2-F, 4- Me-Ph Cl Br 144-146 449 2,6-di-F, 4-MeO-Ph 3-1, 4-Me-Ph Cl Br 127-129 450 2,6-di-F, 4-MeO-Ph 3,5-di-MeO-Ph Me Br 441 451 2,6- 2-F, 4-MeO-Ph 2,6-di-Br, 3,5-di-MeO-Ph Me Br 599 452 3-EtO,2,6-di-F-Ph 4-Cl-Ph Cl Br 449 453 3-EtO,2,6-: -F-Ph 3-F-Ph Cl Br 433 454 3-EtO, 2,6-di-F-Ph 4-Cl-Ph Cl Cl 403 455 3-EtO, 2,6-di-F-Ph 3-F-Ph Cl Cl 487 456 2,6-di-F-Ph 6-C1-3-pyridyl Cl Me 341 457 2,6-di-F, 6-CH3C (=0) Cl Cl 413 4-MeO-Ph NH-3-pyridyl 458 2,6·di-F, 4-MeO-Ph 2,6-di-Cl-3-pyridyl Cl Cl 424 459 2, 6-di-F, 4-MeO-Ph 2-Me-3-° ratio bite group Cl Cl 370 460 2,6-di-F, 4-MeO-Ph 2-MeO-3-ntb°^ group Cl Cl 386 461 2,6-di-F, 4-MeO-Ph 2-Cl, 5-Me-3-°pyridyl-based Cl Cl 404 462 2,6-di-F, 4-MeO-Ph 5-Br- 3-° ratio bite Cl Cl 434 463 3-CN,2,6-di-F-Ph 4-F-Ph Cl Cl 368 151284.doc -243 - 201117722 Compound Q1 Q2 R1 R2 mp (°c) MS ( M+l) 464 3-CN,2,6-di-F-Ph 4-Me-Ph Cl Cl 364 465 3-CN,2,6-di-F-Ph 3-F-Ph Cl Cl 368 466 2 ,6-di-F-Ph 6 - C1 - 3 · ° ratio bite Me Br 386 467 3-EtO, 2,6-di-F-Ph 4-Cl-Ph Cl Me 383 468 3-F-Ph 2 ,6-di-F, 4-MeO-Ph Me Cl φ承469 3-F-Ph 2,6-di-F, 4-MeO-Ph Me Br 113-114 470 2,6-di-F-Ph 4-MeOC ( =0) -Ph Cl Br 186-187 471 3-CN,2,6 -di-F-Ph 6-C1-3-pyridyl Cl Cl 387 472 2,6-di-F-Ph 6-C1-3-pyridyl Me Cl 341 473 (Example 2,6-di-F, 3 ,5-diMe Cl * * ♦ * * * 7) 4-MeO-Ph -MeO-Ph 474 2,6-di-F, 4-MeO-Ph 4-Me-Ph Cl MeS 381 475 (Example 24) 6-C1-3-pyridyl 2,6-di-F, 4-MeO-Ph Me Cl 94-95 476 3-CN,2,6-di-F-Ph 6-C1-3-pyridyl H Cl 351 477 4-MeO-Ph 2,4-di-Cl-Ph Cl Cl 389 478 3-CN,2,6-di-F-Ph 6-C1-3-pyridyl Cl Br 429 479 2,6- -F, 4-MeO-Ph 6-MeO-3-° ratio bite base Cl Br 432 480 2,6-di-F, 4-MeO-Ph 6-CF3-3-atb bite group Br Cl 470 481 (example 22) 2,6-di-F, 4-MeO-Ph 6-CF3-3· ° ratio bite Cl Br 470 482 4-Cl-Ph 2,6-di-F, 4-N02-Ph Cl Me 384 483 2,6-di-F, 3-MeO-Ph 6 - C1 3 -D ratio bite group Cl Cl 392 484 2,6-di-F, 4-MeO-Ph 6-MeO-3-° ratio bite base Br Cl 432 151284.doc -244- 201117722 Compound Q1 Q2 R1 R2 mp (°C) MS (M+l) 485 2,6-di-F-Ph 6-C1-3-pyridyl C1 Br 406 48 6 3-F-Ph 2,6-di-F, 4-MeO-Ph C1CH2 Cl ** 氺氺 487 (Example 2,6-di-F, 6-CF3-3-0tt^ Cl Me 404 23) 4 -MeO-Ph group 488 2,6-di-F, 4-MeO-Ph 6-MeO-3-° ratio bite group Cl Me 366 489 3-CN,2,6c -F-Ph 6-α-3- Pyridyl Me Br 409 490 3-CN, 2,6-di-F-Ph 6-C1-3-pyridyl Me Cl 365 491 3-CN, 2,6-di-F-Ph 6-C1-3- Pyridyl C1CH2 Cl 401 492 2,6-di-F-Ph 6-MeO-3-° than bite Me Cl 337 493 2,6-di-F-Ph 6·ΜεΟ-3·β ratio bite Me Br 381 494 3-EtO,2,6-di-F-Ph 3-F-Ph Cl Me 367 495 2-Cl, 4-MeO-Ph 4-F-Ph Cl Br 115-118 497 2,6-di- F, 4-MeO-Ph 5-F-3-0 ratio bite Cl Cl 374 498 2,6-di-F, 4-MeO-Ph 6-C1-3-pyridyl Cl Br 434 499 2,6- 2-F, 3-MeO-Ph 6 - C1 - 3 - ° ratio bite base Cl Br 436 500 2,6-di-F, 4-MeO-Ph 6-CF3-3-° ratio bite base Me Br 450 501 2,6-di-F, 4-MeO-Ph 6-CF3-3-atba^. Group Me Cl 404 502 2,6-di-F, 3-MeO-Ph 6-C1-3-. Specific bite Me Cl 370 503* 2,6-di-F,4- (example (MeNHCH2CH2 4-Me-Ph Cl Me 406 21) CH2) -Ph 504 2,6-di-F, 3-MeO-Ph 6-C1-3-pyridyl Me Br 416 505 2,6-di-F, 4-MeO-Ph 6-MeO-3_° ratio bite Me Br 412 151284.doc •245 · 201117722 Compound Q1 Q2 R1 R2 mp Rc) MS (M+1) 506 2,6-di-F, 4-MeO-Ph 6-MeO-3-° ratio bite Me Cl 366 507 2,6-di-F, 3-MeO-Ph 6 -C1-3-pyridyl Cl Me 370 508 2,6-di 4, 4-MeO-Ph 6-C1-3-pyridyl Cl Me 370 509 (Example 5) 2,6-di-F-Ph 4- Cl-Ph Br Me lucky* * * 510 (Example 25) 2,6-di-F, 4-MeO-Ph 4-NCS-Ph Cl Me 丰*氺氺申氺511 2,6-di-F , 4-HO-Ph 3-F-Ph Cl Me 339 512 (Example 2,6-di-F,4- 3-F-Ph Cl Me 26) (NCCH20) -Ph 513 4-CN,2,6- bis-F-Ph 6-C1-3-pyridyl Me Cl 氺 氺 514 4-EtO,2,6-: -F-Ph 3-F-Ph Cl Br * * 515 4-EtO, 2,6- 2-F-Ph 4-Me-Ph Cl Me 150-156 516 4_EtO,2,6_di-F-Ph 4-F-Ph Cl Me 167-171 517 4-EtO, 2,6-di-F- Ph 3-F-Ph Cl Me 136-140 518 4-EtO, 2,6-di-F-Ph 3-CF2HO-Ph Cl Br 109-119 519 4-EtO,2,6-di-F-Ph 3-CF2HO-Ph Cl Cl 100-104 520 4-CN,2,6-di-F-Ph 6-MeO-3-° than bite Me Cl 361 521 4-CN,2,6-di-F-Ph 6-MeO-3-° ratio bite Me Br 405 522 4-CN,2,6-di-F-Ph 4-Me-Ph Cl Br 409 523 4-EtO,2,6-: -F-Ph 3-CF2HO-Ph Cl Me 116-120 524 4-CN,2,6-di-F-Ph 3-F-Ph Cl Br 413 525 4-CN ,2,6-di-F-Ph 3,4-di-F-Ph Cl Me 366 151284.doc -246- 201117722 Compound Q1 Q2 R1 R2 mp (°C) MS (M+l) 526 4-CN, 2,6-di-F-Ph 3-F-Ph Cl Me 348 527 4-CN,2,6-di-F-Ph 4-F-Ph Cl Br 413 528 2,6-di-F, 4- MeO-Ph 4-CF2HO-Ph Me Cl 401 529 4-CN,2,6-di-F-Ph 4-CI-Ph Me Cl 365 530 4-CN,2,6-di-F-Ph 3-F -Ph Me Cl 348 531 4-CN,2,6-di-F-Ph 2,4-di-F-Ph Cl Me 366 532 4-CN,2,6-di-F-Ph 3-CF2HO-Ph Me Cl 396 533 4-CN,2,6·di-F-Ph 4-CF2HO-Ph Cl Cl 416 534 4-CN,2,6-di-F-Ph 2-F, 4-Me-Ph Cl Me 362 535 4-CN,2,6c -F-Ph 2-F, 4-Me-Ph Br Me 407 536 4-CN, 2,6-di-F-Ph 3-F-Ph Br Br 458 * HC1 salt . ** 1H NMR data can be found in Index Table B. *** 1H NMR data can be found in the synthesis example.

索引表B 化合物 核磁共振資料（除非另外說明，否則均沪 六Index Table B Compound NMR data (unless otherwise stated, otherwise

18 δ 7.43 (t &gt; 1Η) ^ 7.03 ( dd . 1H) ^ 6.9^ 1H) ；4T 2H)、3.78 (s，3H)。 28 δ 7.36-7.30 (m ’ 2H)、7.08-7.01 (m ’ 2H)、6.66-6.57 (m， 2H)、2.30 (s，3H)、2·14 (s，3H)。 186 δ 7.34-7.20 ( m ’ 3H)、6.96-6.88 ( m ’ 1H)、6.80 ( m，2H)、 5.00 (s，2H)。 189 δ 7.20 (d，2H)、6.99-7.08 (m，1H)、6.93-6.80 (m，3H)、 4.99 (s，2H) 、3.88 (s，3H)。 151284.doc -247- 201117722 化合物 核磁共振資料（除非另外說明，否則均指CDC13溶液）a 212 δ 34 (m，1H)、7.74 (d，1H)、7.29 (m，2H)、6.84 (t， 2H)、2.17 (s，3H)。 213 δ8·50 (d ’ 1H)、8.45 (s，1H)、7.44 (t ’ 1H)、7.30 (t ’ 1H)、7.04 (dd，lH)、4.50 (s，2H) » 214 δ 8.45 (s，1H)、8.38 (d，1H)、7.42 (t ’ 1H)、7.02 (m， 2H)、6.88 (d，1H)、2.23 (s，3H)、 228 δ 7.46-7.42 (t，J = 8.0 Hz，1H)、7.24 (m，1H)、7.06-7.03 (dd，J = 8.0，4.0 Hz，1H)、6.96-6.94 ( d，J = 8.0 Hz，1H)、 6.85 (m，1H)。 229 δ 7.38 ( d，J = 8.0 Hz，2H)、7.23-7.15 (m ’ 1H)、7.13 ( d， J = 8.0 Hz，2H ) ' 6.86-6.81 ( m，1H )。 230 δ 7.20-7.10 (m，3H)、7.11-7.07 (t，J = 8·0 Hz，2H)、6.85-6.80 (m，1H)。 235 δ 8.54 (d ’ 1H)、7.82 (dd，1H)、7.46 (t，1H)、7·21 (d， 1H) ' 7.10 (dd，1H)、6.97 (m，1H)、4.70 (s，2H)。 249 δ 7.36 ( d，J = 8.0 Hz，2H)、7.17-7.13 ( m，3H)、6.97-6.93 (m，1H)。 250 δ 7.51 (t，1H)、7.40 (t ’ 1H)、7.08 (dd，1H)、6.96 (m， 3H)、2_39 ( s，3H)、2.33 (s，3H)。 251 δ 7.57 (t，1H)、7.44 (t，1H)、7.11 (m，2H)、7·05 (d， 1H)、7.00 (m，1H)、4.73 ( s，2H)、2.37 (s，3H)。 252 δ 8.75 ( s，1H)、7.45 (t，1H)、7·03 ( dd，1H)、6.93 ( m， 1H) ' 2.22 (s，3H)。 253 δ 7.50 (t，lH)、7.05 ( dd，1H)、6.95 ( m，1H)、2.24 ( s， 3H)。 254 δ 7.46-7.42 (t，J = 8.0 Hz，1H) ' 7.22 (m，lH)、7.06-7.03 (dd，J = 8.0，4.0 Hz，1H)、6.97-6.94 ( dd，J = 8.0，4.0 Hz， 1H)、6.88-6.85 (m，1H)。 259 δ 7.22-7.18 (m，3H)、7·09·7·07 (t，J = 8·0 Hz，2H)、6.84-6.79 (m，1H)。 272 δ 7.19 (d，2H)、7.06 (d，2H)、7.04 (m，1H)、3.87 (s， 3H)、2.35 (s，3H)。 276 δ 7.34 (d，J = 8.0 Hz，2H)、7.18-7.13 ( m，1H)、7.11 ( d， J = 8.0 Hz » 2H)、6.82-6.77 (m，lH)、2.81 (s，3H)。 277 δ 7.17-7.03 (m，5H)、6.82-6.77 (m，1H)、2.18 (s，3 H)。 278 δ 7.32 (d，J = 8·0 Hz，2H)、7.17-7.12 ( m，1H)、7.10 ( d， J = 8.0Hz，2H) ' 6.94-6.89 (m，lH)、2.13 (s，3H)。 -248- 151284.doc 核磁共振資料（除非另外說明，否則均指cDCb溶液）a δ 7.42-7.40 (t’J = 8.0 Hz，1H)、7.14-7.12 (m，1H)、6.97-6.95 (d’J = 8.0Hz’lH)、6.89-6.87 ( d &gt; J = 8 〇 Hz » 1H) ' 6.80 (m’lH)、2.33 (s’ 3H)、2.16 (s，3H)。 δ7.19 (d’J = 8.0 Hz’ 2H)、7.02-6.97 (m，1H)、6.91 (d， J = 8.0 Hz，2H) ' 6.67-6.63 ( m，1 H) '1.97 ( s，3H)、 1.88 (s，3H) δ 7.11-7.03 ( m，5H)、6.79-6.76 (m，lH)、2.32 (s，3H)、 2.17 (s，3H)。 δ8.00 (d，lH)、7.48 (t’lH)、7.34 (dd，lH)、7.03 (dd， 1H)、6.95 (m，lH)、6.70 (d，lH)、3.92 (s，3H)。 δ7.47 (t，lH)、7.10 (dd’lH)、7.01 (m，iH)、6.87 (s， 2H) ' 3.80 ( s，3H)。 δ7.39 (t，lH)、7.06 (d，lH)、7.02 (dd，lH)、6.92 (m， 1H) ' 6.74 (d，1H)、3.70 (s，3H)。 δ 7.43-7.20 (m，3H)、7.09 (d，lH)、6.42 (d，2H)、3.78 (s，3H)。 δ 7.44-7.40 (t，J = 8.0Hz，1H) 、7.25-7.16 (m，lH) 、7.05 (d &gt; J = 8.0 Hz &gt; 1H)、6.97-6.95 (m &gt; 2H)。 δ 7.16 (d，J = 8.0 Hz，2H)、7.15-7.12 (m，lH)、7.06 (d， J = 8.0Hz，2H)、6.93-6.92 (m，lH) ' 2.34 (s，3H)。 δ 7.17 (d，J = 8.0 Hz，2H)、7.15-7.10 (m，lH)、7.05 (d， J = 8.0 Hz * 2H)、6.82-6.78 (m，lH) '2.36 (s，3H)。 57.19-7.16 (m，2H)、7.11-7.07 (t’J = 8.0Hz’2H)、6.67-6.63 (t，J = 8.0 Hz，2H )。 6 7.45-7.40 (t，J = 8.0 Hz，1H)、7.21-7.06 (m，lH) ' 7.05 (d，J = 8.0 Hz，1H) ' 6.96-6.94 (m，2H)。 δ7·16 (d，J = 8.0 Hz，2 Η,)、7.15-7.10 (m，lH)、7.06 (d， J = 8.0 Hz &gt; 2H)、6.95-6.92 (m，lH)、2.34 (s，3H)。 δ7·18 (d，J = 8.0Hz’2H)、7.15-7.10 (m，lH)、7.05 (d， J = 8.0 Hz - 2H)、6.81-6.78 ( m，1H)、2.36 ( s ’ 3H) » δ7.35 (d，2H)、7.14 (d，2H)、6.95 (m，lH)、6.79 (m， 1 H) ' 3.83 (s，3 H)。 δ8.40 (m，lH)、7.85 (dd’lH)、7.61 (d，lH)、7.45 (t， 1H)、7.08 (dd，lH)、6.97 (m，lH)。 δ8.57 (brs，lH)、7.77 (m’2H)、6.44 (d’2H)、3.79 (s’ 3H)。 -249- 201117722 化合物 1H核磁共振資料（除非另外說明，否則均指CDC13溶液）a ~~337 δ 7.39-7.35 (t’ J = 8.0 Hz，1H)、7.12-7.08 (m，2H)、6.95-6-91 (m，1H)、6.86-6.79 ( d，J = 8.0 Hz，1H)、2.33 (s，3H)、 2.11 (s，3H)。 338 δ 7.14-7.12 (d，J = 8.0 Hz，2H)、7.11-7.02 (m，1H)、6.99-6.97 (d，J = 8.0Hz’2H)、6.77-6.72 (m，2H)、2.34 (s，3H)、 2_16 ( s，3H)。 339 δ 7.11-7.02 (m，4 H)、6.62-6.50 (t，J = 8.0 Hz，2H)、2.28 (s，3H)、2_13 (s，3H)。 340 5 7.15-7.13 ( m » 2H ) ' 7.05-7.03 ( t &gt; J = 8.0 Hz &gt; 2H ) ' 6.61-6.64 (t，J = 8.0 Hz，2H)、2.15 (s，3H)。 341 δ 7.11-7.09 (d，J = 8.0 Hz，2H)、7.14-7.01 (m，1H)、6.99-6.97 (d，J = 8_0Hz，2H)、6.88-6.83 (m，lH)、2.32 (s，3H)、 2.12 (s，3H) 〇 342 δ 7.40-7.36 ( t，J = 8.0 Hz，1H)、7.19 (m，2H)、7.01 (d， J = 8.0 Hz &gt; 1H)、6.98-6.90 (m，2H)、2.13 (s，3H)。 343 δ7_12 (d，J = 8.0Hz，2H)、7.10-7.05 (m，lH)、7.03 (d， J = 8.0 Hz &gt; 2H)、6.91-6.87 (m，lH)、2.33 (s，3H)、 2.13 (s，3H)。 344 δ 7.15 (d，J = 8.0 Hz，2H)、7.13-7.05 (m，lH)、7.03 (d， J = 8.0Hz，2H)、6.80-6.75 (m，lH) ' 2.35 (s，3H)、 2.17 ( s，3H)。 351 δ 7.35 (d，2H)、7.14 (d，2H)、6.95 (m，lH)、6.80 (m， 1 H) ' 3.84 ( s，3 H)。 355 δ 7.46 (d，1H)、6.96 (d，1H)、6.41 (m，2H)、3.85 (s， 3H)、3.78 (s，3H)。 361 δ 7.12 ( d，J = 8.0 Hz，2H )、6.98 ( d ’ J = 8.0 Hz ’ 2H )、6.36 (d，J = 8.0 Hz，2H)、3.74 ( s，3H)、2.27 ( s，3H)、 2.13 (s，3H)。 362 δ 7.11-7.00 (m，4H)、6.37 ( d，J = 8.0 Hz，2H)、3.75 (s’ 3H)、2.28 (s，3H)、2.13 (s，3H)。 363 δ 7.19-7.17 (m，2H)，7.05-7.09 (t，J = 8.0 Hz，2H)，6.40 (d，J = 8.0 Hz，2H) ' 3.71 (s，3H)。 364 δ 7.16 ( d，J = 8.0 Hz，2H，）、7.05 ( d，J = 8.0 Hz ’ 2H)、 6.39 (d，J = 8.0Hz，2H)、3.76 (s，3H)、2.36 (s，3H)。 400 δ 7.41 (t，1H)、7.11 (dd，1H)、7.01 (m，1H)、6.86 (s， 2H)、3.80 (s，3H)。 4〇l δ 7.42 ( t，1H)、7.01 ( m，2H)、6·90 ( m，2H)、3.75 ( s ’ 3H)。 -250- 151284.doc 201117722 化合物 1H核磁共振資料（除非另外說明，否則均指CDC13溶液）a 402 δ 8.46 (m，1H)、7.73 ( m，1H)、7.39 ( m，1H) ' 6.48 ( m &gt; 1H)、6.34 (m，1H)、3.77 (s，3H)。 403 δ 8.25 (s，1H)、7.59 (d，1H)、7.32 (m，1H)、7.19 (d ’ 1H)、6.86 (t，2H)、2.36 (s，3H)。 404 δ 7.15-7.10 (m，4H)、6.53-6.47 (m，2H)、4.54 ( s，2H)、 3.80 (s，3H)、2.33 (s，3H) » 411 δ 8.24 (s，1H)、7.54 (d，1H)、7.39 (m，2H)、6.91 (t ’ 2H) 412 δ 8.39 (s，2H)、7.46 (t ’ 1H)、7.07 (dd，1H)、6.94 (d ’ 1H)。 430 δ 8.20 (dd，1H)、7.54 (m ’ 1H)、7.31 (m，1H)、6.93 ( m， 2H)、6.81 (t，lH)、3.81 (s，3H)。 468 δ 7.35-7.29 (m ’ 1H)、7.08-6.92 (m，3H)、6.56-6.50 ( m， 2H)、4.54 (s’ 2H)、3.82 (s，3H)。 486 δ 7.36-7.28 (m，1H)、7.08-7.02 (m，2H)、6.98-6.92 (m， 1H)、6.53 (d，2H)、4.54 (s，2H)、3.82 (s，3H)。 513 δ 8.18 ( m，1H)、7.54-7.52 ( m，1H)、7.41-7.39 ( m，1H)、 7.23-7.21 (m’2H)、2.19 (s，3H)。 514 δ 7.4 (m ’ 1H)、7.1 (m，1H)、6.9 (m，2H)、6.4 (d， 2H)、4.0 (q，2H)、1.4 (t，3H)。 a H核磁共振資料係為偏離自四曱基碎烧的低場ppm。偶合係以（s)_單 峰、⑷-二重峰、⑴·三重峰、（m)_多重峰、（dd)雙二重峰、扣s)寬單 峰標明。 本發明生物實例 製備試驗A-J之檢測懸浮液之一般規範：測試化合 物首先以相當於最終體積3%的量溶解於丙酮，然後在 (m ppm)目標濃度之丙酮及純化水（5〇/5〇混合）中 懸浮，其含有250 ppm的界面活性劑Trem® 014 (多元 醇酉a )。產生的測試懸浮液其後經用於試驗a_j。每個測 试為二重複測試，而結果為平均值。噴灑200 ppm的測 試懸浮液到能夠從受測植物上留下來的程度，其相當於 151284.doc -251 - 201117722 800 g/ha的速率。（在速率值旁邊的星號「*」表示4〇ppm 測試懸浮液。）18 δ 7.43 (t &gt; 1Η) ^ 7.03 ( dd . 1H) ^ 6.9^ 1H) ; 4T 2H), 3.78 (s, 3H). 28 δ 7.36-7.30 (m ' 2H), 7.08-7.01 (m ' 2H), 6.66-6.57 (m, 2H), 2.30 (s, 3H), 2·14 (s, 3H). 186 δ 7.34-7.20 (m ' 3H), 6.96-6.88 (m ' 1H), 6.80 (m, 2H), 5.00 (s, 2H). 189 δ 7.20 (d, 2H), 6.99-7.08 (m, 1H), 6.93-6.80 (m, 3H), 4.99 (s, 2H), 3.88 (s, 3H). 151284.doc -247- 201117722 Compound NMR data (both CDC13 solution unless otherwise stated) a 212 δ 34 (m, 1H), 7.74 (d, 1H), 7.29 (m, 2H), 6.84 (t, 2H), 2.17 (s, 3H). 213 δ8·50 (d ' 1H), 8.45 (s, 1H), 7.44 (t ' 1H), 7.30 (t ' 1H), 7.04 (dd, lH), 4.50 (s, 2H) » 214 δ 8.45 (s , 1H), 8.38 (d, 1H), 7.42 (t ' 1H), 7.02 (m, 2H), 6.88 (d, 1H), 2.23 (s, 3H), 228 δ 7.46-7.42 (t, J = 8.0 Hz, 1H), 7.24 (m, 1H), 7.06-7.03 (dd, J = 8.0, 4.0 Hz, 1H), 6.96-6.94 (d, J = 8.0 Hz, 1H), 6.85 (m, 1H). 229 δ 7.38 ( d, J = 8.0 Hz, 2H), 7.23 - 7.15 (m ' 1H), 7.13 ( d, J = 8.0 Hz, 2H ) ' 6.86-6.81 ( m, 1H ). 230 δ 7.20-7.10 (m, 3H), 7.11-7.07 (t, J = 8·0 Hz, 2H), 6.85-6.80 (m, 1H). 235 δ 8.54 (d ' 1H), 7.82 (dd, 1H), 7.46 (t, 1H), 7·21 (d, 1H) ' 7.10 (dd, 1H), 6.97 (m, 1H), 4.70 (s, 2H). 249 δ 7.36 ( d, J = 8.0 Hz, 2H), 7.17-7.13 (m, 3H), 6.97-6.93 (m, 1H). 250 δ 7.51 (t, 1H), 7.40 (t ' 1H), 7.08 (dd, 1H), 6.96 (m, 3H), 2_39 (s, 3H), 2.33 (s, 3H). 251 δ 7.57 (t,1H), 7.44 (t,1H), 7.11 (m,2H), 7·05 (d, 1H), 7.00 (m,1H), 4.73 (s,2H), 2.37 (s, 3H). 252 δ 8.75 ( s, 1H), 7.45 (t, 1H), 7·03 ( dd, 1H), 6.93 ( m, 1H) ' 2.22 (s, 3H). 253 δ 7.50 (t, lH), 7.05 (dd, 1H), 6.95 (m, 1H), 2.24 (s, 3H). 254 δ 7.46-7.42 (t, J = 8.0 Hz, 1H) ' 7.22 (m, lH), 7.06-7.03 (dd, J = 8.0, 4.0 Hz, 1H), 6.97-6.94 ( dd, J = 8.0, 4.0 Hz, 1H), 6.88-6.85 (m, 1H). 259 δ 7.22-7.18 (m, 3H), 7·09·7·07 (t, J = 8·0 Hz, 2H), 6.84-6.79 (m, 1H). 272 δ 7.19 (d, 2H), 7.06 (d, 2H), 7.04 (m, 1H), 3.87 (s, 3H), 2.35 (s, 3H). 276 δ 7.34 (d, J = 8.0 Hz, 2H), 7.18-7.13 (m, 1H), 7.11 (d, J = 8.0 Hz » 2H), 6.82-6.77 (m, lH), 2.81 (s, 3H) . 277 δ 7.17-7.03 (m, 5H), 6.82-6.77 (m, 1H), 2.18 (s, 3 H). 278 δ 7.32 (d, J = 8·0 Hz, 2H), 7.17-7.12 (m, 1H), 7.10 (d, J = 8.0Hz, 2H) ' 6.94-6.89 (m, lH), 2.13 (s, 3H). -248- 151284.doc NMR data ( unless otherwise stated, refer to cDCb solution) a δ 7.42-7.40 (t'J = 8.0 Hz, 1H), 7.14-7.12 (m, 1H), 6.97-6.95 (d 'J = 8.0Hz'lH), 6.89-6.87 ( d &gt; J = 8 〇Hz » 1H) ' 6.80 (m'lH), 2.33 (s' 3H), 2.16 (s, 3H). Δ7.19 (d'J = 8.0 Hz' 2H), 7.02-6.97 (m, 1H), 6.91 (d, J = 8.0 Hz, 2H) ' 6.67-6.63 ( m,1 H) '1.97 ( s,3H ), 1.88 (s, 3H) δ 7.11-7.03 (m, 5H), 6.79-6.76 (m, lH), 2.32 (s, 3H), 2.17 (s, 3H). Δ8.00 (d,lH), 7.48 (t'lH), 7.34 (dd,lH), 7.03 (dd, 1H), 6.95 (m,lH), 6.70 (d,lH), 3.92 (s,3H) . δ 7.47 (t, lH), 7.10 (dd'lH), 7.01 (m, iH), 6.87 (s, 2H) ' 3.80 (s, 3H). δ 7.39 (t, lH), 7.06 (d, lH), 7.02 (dd, lH), 6.92 (m, 1H) ' 6.74 (d, 1H), 3.70 (s, 3H). δ 7.43-7.20 (m, 3H), 7.09 (d, lH), 6.42 (d, 2H), 3.78 (s, 3H). δ 7.44-7.40 (t, J = 8.0 Hz, 1H), 7.25-7.16 (m, lH), 7.05 (d &gt; J = 8.0 Hz &gt; 1H), 6.97-6.95 (m &gt; 2H). δ 7.16 (d, J = 8.0 Hz, 2H), 7.15-7.12 (m, lH), 7.06 (d, J = 8.0 Hz, 2H), 6.93-6.92 (m, lH) ' 2.34 (s, 3H). δ 7.17 (d, J = 8.0 Hz, 2H), 7.15-7.10 (m, lH), 7.05 (d, J = 8.0 Hz * 2H), 6.82-6.78 (m, lH) '2.36 (s, 3H). 57.19-7.16 (m, 2H), 7.11-7.07 (t'J = 8.0 Hz'2H), 6.67-6.63 (t, J = 8.0 Hz, 2H). 6 7.45-7.40 (t, J = 8.0 Hz, 1H), 7.21-7.06 (m, lH) ' 7.05 (d, J = 8.0 Hz, 1H) ' 6.96-6.94 (m, 2H). Δ7·16 (d, J = 8.0 Hz, 2 Η,), 7.15-7.10 (m, lH), 7.06 (d, J = 8.0 Hz &gt; 2H), 6.95-6.92 (m, lH), 2.34 (s , 3H). Δ7·18 (d, J = 8.0Hz '2H), 7.15-7.10 (m, lH), 7.05 (d, J = 8.0 Hz - 2H), 6.81-6.78 (m, 1H), 2.36 (s ' 3H) » δ7.35 (d, 2H), 7.14 (d, 2H), 6.95 (m, lH), 6.79 (m, 1 H) ' 3.83 (s, 3 H). δ 8.40 (m, lH), 7.85 (dd'lH), 7.61 (d, lH), 7.45 (t, 1H), 7.08 (dd, lH), 6.97 (m, lH). δ 8.57 (brs, lH), 7.77 (m'2H), 6.44 (d'2H), 3.79 (s' 3H). -249- 201117722 Compound 1H NMR data (unless otherwise stated, refer to CDC13 solution) a ~~337 δ 7.39-7.35 (t' J = 8.0 Hz, 1H), 7.12-7.08 (m, 2H), 6.95- 6-91 (m, 1H), 6.86-6.79 (d, J = 8.0 Hz, 1H), 2.33 (s, 3H), 2.11 (s, 3H). 338 δ 7.14-7.12 (d, J = 8.0 Hz, 2H), 7.11-7.02 (m, 1H), 6.99-6.97 (d, J = 8.0Hz '2H), 6.77-6.72 (m, 2H), 2.34 ( s, 3H), 2_16 ( s, 3H). 339 δ 7.11-7.02 (m, 4 H), 6.62-6.50 (t, J = 8.0 Hz, 2H), 2.28 (s, 3H), 2_13 (s, 3H). 340 5 7.15-7.13 ( m » 2H ) ' 7.05-7.03 ( t &gt; J = 8.0 Hz &gt; 2H ) ' 6.61-6.64 (t, J = 8.0 Hz, 2H), 2.15 (s, 3H). 341 δ 7.11-7.09 (d, J = 8.0 Hz, 2H), 7.14-7.01 (m, 1H), 6.99-6.97 (d, J = 8_0Hz, 2H), 6.88-6.83 (m, lH), 2.32 (s , 3H), 2.12 (s, 3H) 〇 342 δ 7.40-7.36 ( t, J = 8.0 Hz, 1H), 7.19 (m, 2H), 7.01 (d, J = 8.0 Hz &gt; 1H), 6.98-6.90 (m, 2H), 2.13 (s, 3H). 343 δ7_12 (d, J = 8.0Hz, 2H), 7.10-7.05 (m, lH), 7.03 (d, J = 8.0 Hz &gt; 2H), 6.91-6.87 (m, lH), 2.33 (s, 3H) , 2.13 (s, 3H). 344 δ 7.15 (d, J = 8.0 Hz, 2H), 7.13-7.05 (m, lH), 7.03 (d, J = 8.0Hz, 2H), 6.80-6.75 (m, lH) ' 2.35 (s, 3H) , 2.17 ( s, 3H). 351 δ 7.35 (d, 2H), 7.14 (d, 2H), 6.95 (m, lH), 6.80 (m, 1 H) ' 3.84 ( s, 3 H). 355 δ 7.46 (d, 1H), 6.96 (d, 1H), 6.41 (m, 2H), 3.85 (s, 3H), 3.78 (s, 3H). 361 δ 7.12 ( d, J = 8.0 Hz, 2H ), 6.98 ( d ' J = 8.0 Hz ' 2H ), 6.36 (d, J = 8.0 Hz, 2H), 3.74 ( s, 3H), 2.27 ( s, 3H ), 2.13 (s, 3H). 362 δ 7.11-7.00 (m, 4H), 6.37 (d, J = 8.0 Hz, 2H), 3.75 (s' 3H), 2.28 (s, 3H), 2.13 (s, 3H). 363 δ 7.19-7.17 (m, 2H), 7.05-7.09 (t, J = 8.0 Hz, 2H), 6.40 (d, J = 8.0 Hz, 2H) ' 3.71 (s, 3H). 364 δ 7.16 ( d, J = 8.0 Hz, 2H,), 7.05 ( d, J = 8.0 Hz ' 2H), 6.39 (d, J = 8.0 Hz, 2H), 3.76 (s, 3H), 2.36 (s, 3H). 400 δ 7.41 (t, 1H), 7.11 (dd, 1H), 7.01 (m, 1H), 6.86 (s, 2H), 3.80 (s, 3H). 4〇l δ 7.42 ( t,1H), 7.01 ( m,2H), 6.90 ( m,2H), 3.75 ( s ' 3H). -250- 151284.doc 201117722 Compound 1H NMR data (both CDC13 solution unless otherwise stated) a 402 δ 8.46 (m,1H), 7.73 (m,1H), 7.39 ( m,1H) ' 6.48 ( m &gt; 1H), 6.34 (m, 1H), 3.77 (s, 3H). 403 δ 8.25 (s, 1H), 7.59 (d, 1H), 7.32 (m, 1H), 7.19 (d '1H), 6.86 (t, 2H), 2.36 (s, 3H). 404 δ 7.15-7.10 (m, 4H), 6.53-6.47 (m, 2H), 4.54 (s, 2H), 3.80 (s, 3H), 2.33 (s, 3H) » 411 δ 8.24 (s, 1H), 7.54 (d, 1H), 7.39 (m, 2H), 6.91 (t ' 2H) 412 δ 8.39 (s, 2H), 7.46 (t ' 1H), 7.07 (dd, 1H), 6.94 (d ' 1H). 430 δ 8.20 (dd, 1H), 7.54 (m ′ 1H), 7.31 (m, 1H), 6.93 (m, 2H), 6.81 (t, lH), 3.81 (s, 3H). 468 δ 7.35-7.29 (m ' 1H), 7.08-6.92 (m, 3H), 6.56-6.50 (m, 2H), 4.54 (s' 2H), 3.82 (s, 3H). 486 δ 7.36-7.28 (m, 1H), 7.08-7.02 (m, 2H), 6.98-6.92 (m, 1H), 6.53 (d, 2H), 4.54 (s, 2H), 3.82 (s, 3H). 513 δ 8.18 (m, 1H), 7.54-7.52 (m, 1H), 7.41-7.39 (m, 1H), 7.23-7.21 (m'2H), 2.19 (s, 3H). 514 δ 7.4 (m ' 1H), 7.1 (m, 1H), 6.9 (m, 2H), 6.4 (d, 2H), 4.0 (q, 2H), 1.4 (t, 3H). The a H NMR data is a low field ppm deviating from the tetradecyl calcination. The coupling system is indicated by a broad single peak of (s)_single peak, (4)-doublet, (1)·triplet, (m)_multiplet, (dd) doublet, and s). General Example for the Preparation of Test Suspension of Test AJ of the Invention Example: The test compound is first dissolved in acetone in an amount equivalent to 3% of the final volume, and then acetone and purified water at a target concentration of (m ppm) (5〇/5〇) Suspended in suspension) containing 250 ppm of the surfactant Trem® 014 (Polyol 酉a). The resulting test suspension was then used for the test a_j. Each test was a duplicate test and the results were average. Spray 200 ppm of the test suspension to the extent that it can be left on the plant to be tested, which corresponds to a rate of 151284.doc -251 - 201117722 800 g/ha. (The asterisk "*" next to the rate value indicates 4 〇ppm test suspension.)

試驗A 葡萄苗幼接種葡萄露病菌孢子懸浮液（葡萄霉病致 病因„子?並於飽和大氣中以耽培養24小時。短暫的 乾燥之後’ S萄幼苗經噴l錢浮液至誠的程度， 到耽的生長箱5天，其後葡萄幼苗移回 L 口大氣壓24小時。在移除時，進行外觀疾病評 口八艰Jt5 γ液經賴錢小糠草幼苗上溢 菌的糠以及菌絲二1天將該幼苗接種立枯絲核 於士 ’二，卓坪褐斑病的病原菌）以及培養 ^天=:Γ小時，然後移到坑生長箱放 在此時間後，進行外觀疾病評級。 試驗c 將該浮液噴灑於番祐苗至溢流為止。於第二天 菌的病原菌的孢子懸浮液（番莊灰黴病 然後移到24ΐ生長觀置2Gt飽和大紐下邮小時， 觀疾病評級。 3天，在此時間後，進行外Test A Grape seedlings were inoculated with a suspension of grape rot fungus spores (the cause of grape mold was sputum? and cultured in a saturated atmosphere for 24 hours with sputum. After a short drying period, 'S seedlings were sprayed with l money to the extent of honesty. After 5 days of growth in the growth chamber, the grape seedlings were moved back to the mouth pressure of L for 24 hours. When the removal was carried out, the appearance of the disease was judged by the Jt5 γ liquid, and the bacteria and bacteria of the larvae of the larvae On the second day of the silk, the seedlings were inoculated with the nucleus of the nucleus in the genus of the genus, and the culture was carried out for 2 days, and then moved to the pit growth box. Test c spray the floating liquid on the seedlings until the overflow. On the second day, the spore suspension of the pathogen of the fungus (Pan Cong gray mold and then moved to the 24 ΐ growth view 2Gt saturated big New Zealand under the hour, view Disease rating. 3 days, after this time, outside

試驗D 151284.doc •252- 201117722 將測試懸浮液喷灑於番茄苗至溢流為止。於第二天 將番祐早疫病菌（Alternaria solani)(番茄早疫病的病 原菌）孢子懸浮液接種於植苗，於27°C飽和大氣壓下 培養48小時，接著移至20°C生長箱中放置5天，在此 時間後，進行外觀疾病評級。Test D 151284.doc • 252- 201117722 Spray the test suspension on tomato seedlings until overflow. On the next day, the spore suspension of Alternaria solani (pathogen of tomato early blight) was inoculated into the seedlings, cultured at 27 ° C under saturated atmospheric pressure for 48 hours, and then transferred to a growth chamber at 20 ° C for 5 hours. Days, after this time, the appearance of disease rating.

試驗E 將測試懸浮液喷灑於番茄苗至溢流為止。於第二天 將番莊疫病菌（Phytophthora infestans )(番茄疫病的病 原菌）孢子懸浮液接種於植苗，於20°C飽和大氣壓下 培養24小時，接著移至20°C生長箱中放置5天，在此 時間後，進行外觀疾病評級。Test E The test suspension was sprayed on tomato seedlings until overflow. On the next day, the spore suspension of Phytophthora infestans (pathogen of tomato blight) was inoculated into the seedlings, cultured at 20 ° C for 24 hours under saturated atmosphere, and then transferred to a growth chamber at 20 ° C for 5 days. After this time, the appearance disease rating is performed.

試驗F 將測試懸浮液喷灑於小麥苗至溢流為止。於第二天 將該幼苗接種於麥穎枯病菌的孢子懸浮液（小麥glume blotch的病原菌）以及培養於24°C飽和大氣壓下48小 時，然後移到20°C生長箱放置6天，在此時間後，進 行外觀疾病評級。Test F The test suspension was sprayed onto the wheat seedlings until it overflowed. On the next day, the seedlings were inoculated into a spore suspension of wheat blast fungus (pathogen of wheat glume blotch) and cultured at 24 ° C under saturated atmospheric pressure for 48 hours, and then moved to a growth chamber at 20 ° C for 6 days. After the time, the appearance of the disease rating.

試驗G 將測試懸浮液喷灑於小麥苗至溢流為止。於第二天 將該幼苗接種於小麥葉斑病菌的孢子懸浮液（小麥葉枯 病的病原菌）以及培養於24°C飽和大氣壓下48小時， 然後移到20°C生長箱放置19天，在此時間後，進行外 觀疾病評級。 151284.doc -253 - 201117722 5式驗Η 小麥幼苗紅接種麥類葉錄病菌（讎以他f =子懸浮液（小麥葉錄病的病原菌）以及 培養於20C飽和大氣壓下24小時然後移到贼生長 箱放置2天，在此時間德 ％ I、„ ]便，進仃外觀疾病評級。最後測 試懸淨液喷》麗於小麥苗$、、兴、&amp;达 w ^ 至溢&amp;為止，然後該幼苗移到 20 C生長相放置6天，在从卩主叫μTest G The test suspension was sprayed onto the wheat seedlings until it overflowed. On the next day, the seedlings were inoculated into a spore suspension of wheat leaf spot pathogen (pathogen of wheat leaf blight) and cultured at 24 ° C under saturated atmospheric pressure for 48 hours, and then moved to a growth chamber at 20 ° C for 19 days. After this time, the appearance of the disease rating. 151284.doc -253 - 201117722 5 type test 小麦 Wheat seedlings red inoculated with wheat leaf pathogens (雠 with his f = sub-suspension (the pathogen of wheat leaf disease) and cultured at 20C saturated atmosphere for 24 hours and then moved to the thief The growth box is placed for 2 days, at this time, the % I, „] will enter the 仃 appearance disease rating. Finally, the test suspension liquid spray “Let the wheat seedlings $, 兴, &amp; reach w ^ to overflow &amp; Then the seedlings are moved to the 20 C growth phase for 6 days, in the slave 卩

廿此時間後，進行外觀疾病評級。 試驗I 將測試懸浮液錢於小麥苗至溢流為止。於第二天 將該幼苗接種於小麥__®的孢子液（小麥葉 錄病的病)以及料於聊鮮大氣壓下24小 時，然後移到贼生長箱放置 行外觀疾病評級。After this time, the appearance of the disease rating. Test I will test the suspension for the wheat seedlings until it overflows. On the next day, the seedlings were inoculated into the spore solution of wheat __® (the disease of wheat leaf disease) and expected to be under the atmospheric pressure for 24 hours, and then moved to the thief growth box to place the appearance disease rating.

試驗J 將測試懸浮时灑於小麥苗至溢流為止。於第二天 將該幼苗鍾則、麥自㈣（BlumeHa g_inis f $ tritici)的孢子懸浮液（亦稱為 Erysiphe graminis f. sp. tritici，小麥白粉菌病原菌）然後移到生長箱放置 8天，在此時間後，進行外觀疾病評級。 測試A-J的結果在表A中呈現。表中，等級1〇〇 表示100%疾病防治，而等級0表示無疾病防治效果（相 對於對照組）。破折號（-)表示無檢測結果。所有結果 151284.doc -254- 201117722 皆對於200 ppm，除了其後出現星號「*」者，其表示 40 ppm ° 化合物 試驗 A 試驗 B 試驗 C 試驗 D 表A 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 1 0 65 99 100 0 100 100 0* 100 100 2 0 99 99 100 0 99 100 - 99 100 3 0 38 98 99 0 0 100 - 88 99 4 0 99 99 100 0 95 100 - 100 100 5 0 81 100 100 0 0 99 • 98 99 6 - - 99* 99* - 0* 94* - 97* 100* 7 6 99 100 100 0 99 99 - 100 100 8 20 99 87* 100* 0 94* 96* - 99* 100* 9 - - 0 - 0 97 - 99 90 10 - 98* 100* - 0* 84* - 97* 95* 11 - _ 99 99 - 0 88 - 100 95 12 13 100 99 100 0 100 100 - 99 100 13 - - 93 100 - 0 91 - 100 100 14 - - 99 100 - - 88 - 100 99 15 - - 97 100 - 51 95 - 100 100 16 - - 99 100 - 74 91 - 100 100 17 琴 - 99* 100* - 0* 94* - 100* 100* 18 - - 99 100 - 100 95 - 100 100 19 - - 99* 100* - 99* 90* 91* 100* 100* 20 20 100 100 100 0 100 100 - 100 100 21 - - 99 100 - 99 92 - 100 100 22 - 99* 100* - 100* 92* - 100* 100* 23 - - 99* 100* - 99* 95* 98* 100* 24 - - 99 100 - 64 94 - 99 98 25 - - 99* 100* - 99* 93* - 91* 100* 26 - - 98* 100* - 97* 96* - 97* 99* 27 151284.doc 99* 100* -255 - 40* 92* 99* 98* 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 28 - - 100 98 _ 100 100 99 100 100 29 - - 94 42 - 0 77 - 54 93 30 - - 99 100 - 100 94 - 100 100 31 - - 98 100 - 100 94 - 99 99 32 - - 98 100 - 100 92 100 100 33 - - 94 100 - 100 94 - 97 99 34 - - 84 100 - 0 97 - 99 100 35 _ - 89 100 - 0 95 - 100 99 36 - - 92 24 - 0 87 - 99 91 37 - - 94* 100* - 98* 93* - 99* 100* 38 - - 84 99 - 0 87 - 96 100 39 - - 98 100 - 51 79 - 99 100 40 - - 93* 100* - 82* 97* - 86* 97* 41 - - 99 100 - 95 95 - 100 96 42 - - 0 100 - 0 95 - 41 95 43 - - 99 100 - 99 94 - 99 99 44 - - 96 100 - 92 97 - 99 100 45 - - 100 100 - 60 87 - 100 100 46 - - 37 99 - 60 97 - 99 100 47 - 90 100 - 100 98 - 100 100 48 - - 81 100 - 69 93 - 98 100 49 - - 90 100 - 100 91 - 99 100 50 - - 97 100 - 99 98 - 100 100 51 - _ 0 99 - 0 88 - 91 99 52 - - 73 100 - 11 98 - 96 100 53 - - 0 0 - 0 93 - 27 99 54 - - 0 0 - 0 0 - 54 0 55 - - 98 100 - 100 99 - 96 100 56 - - 76 100 - 0 98 - 89 100 57 - - 97 100 100 99 - 98 100 58 - - 56 53 - 0 95 - 99. 100 59 • - 96 97 - 95 95 • 100 100 151284.doc •256· 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 60 - - 98* 100* - 97* 97* - 97* 99* 61 - 97 93 - 99 97 - 98 99 62 - - 88 0 - 0 97 - 100 99 63 - - 98 0 - 55 97 - 99 99 64 - - 79 92 - 90 98 - 100 99 65 - - 98 99 - 94 94 - 99 100 66 - - 96 100 - 100 96 - 100 100 67 - - 100* 100* - 0* 74* - 98* 99* 68 - - 94 57 - 0 94 - 68 63 69 - - 94 99 - 100 95 - 97 96 70 - - 98 99 - 97 95 - 97 97 71 - - 93 0 - 0 95 - 41 72 72 _ - 0* 0* - 0* 0* - 0* 0* 73 - - 96 100 - 99 97 - 99 100 74 - - 99 100 - 60 94 - 99 100 75 - - 96 80 - 40 91 - 80 0 76 - - 98 0 - 0 96 - 90 92 77 - - 98 100 - 100 96 - 100 100 78 - - 97 99 - 69 96 - 99 99 79 - 99 100 - 98 95 - 100 100 80 - - 97 96 - 96 93 - 97 100 81 - - 99 100 - 0 89 - 74 95 82 - - 98 100 - 0 85 99 96 83 - - 90* 99* - 0* 85* - 0* 48* 84 - - 97 100 - 99 93 - 99 100 85 - - 99 100 - 0 93 - 100 100 86 - 0 0 - 0 93 - 55 39 87 - - 99 100 - 0 91 - 99 100 88 - - 99 100 - 97 94 - 100 100 89 - - 99 100 - 100 100 - 100 100 90 - - 100 100 - 100 100 - 100 100 91 - - 99 100 _ 100 100 • 100 100 151284.doc •257· 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 92 - - 99 100 _ 100 100 - 100 100 93 - 91 100 - 82 100 100 99 94 - - 99 100 - 99 100 - 100 100 95 - - 53 0 - 98 96 - 95 95 96 - - 99 100 - 60 98 - 97 100 97 - - 97* 100* - 69* 99* 89* 96* 98 - - 99 99 - 69 96 - 89 99 99 - - 98 100 - 69 96 - 99 100 100 - - 99 100 - 0 93 - 86 99 101 - - 99 100 - 87 95 - 99 100 102 攀 - 98* 100* - 99* 97* - 97* 99* 103 - - 97 99 - 98 97 - 100 100 104 - - 99 100 - 96 97 - 100 100 105 - 99 100 - 99 97 - 100 100 106 - - 88* 97* - 0* 93* - 23* 94* 107 - - 91* 88* - 0* 96* - 19* 94* 108 - 99* 100* - 0* 95* - 0* 98* 109 - - 97 99 _ 84 98 - 100 100 110 - - 99 100 - 40 96 - 88 99 111 - - 97 98 - 0 95 - 99 99 112 - - 99 100 - 100 98 - 98 99 113 - - 99 99 - 100 98 - 99 99 114 - - 98 99 - 82 98 - 100 100 115 - - 97 97 - 82 98 - 100 99 116 - - 99 100 - 73 96 - 97 99 117 - - 99* 91* - 0* 85* - 66* 48* 118 - - 99 100 - 0 97 - 100 100 119 - - 99 100 - 78 94 - 100 99 120 - - 98 88 0 97 - 100 100 121 - - 99 100 94 97 - 100 100 122 - - 98 100 0 97 100 99 123 98 100 51 97 _ 100 99 151284.doc •258· 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 124 - - 97 100 - 0 93 - 100 100 125 - - 99 100 - 64 94 - 100 94 126 - - 99 100 - 0 92 - 100 97 127 - - 99 99 - 0 93 - 100 100 128 - - 98 99 - 0 90 - 100 95 129 - - 92 100 - 100 96 - 98 95 130 - - 99 100 - 100 98 - 96 100 131 - - 91 61 - 98 97 - 98 100 132 - - 87 98 - 87 97 - 100 99 133 - - 90* 91* - 0* 90* - 18* 26* 134 - - 99 100 - 100 98 - 100 100 135 - - 95 99 0 98 - 100 99 136 - - 93 99 - 80 98 - 100 99 137 - - 63 0 - 0 96 - 100 42 138 - - 100* 99* - 97* 94* - 97* 98* 139 - 99* 100* - 0* 96* - 93* 94* 140 - - 33* 57* - 0* 13* - 0* 0* 141 - - 99* 99* - 0* 91* - 80* 73* 142 33 99 98 97 0 51 96 - 99 99 143 82 99 98 99 0 0 97 - 99 100 144 - - 99 99 - 0 95 - 97 98 145 - - 99 99 - 0 99 - 97 98 146 - - 99 100 - 60 98 - 99 100 147 - - 93 51 - 0 90 - 80 98 148 - - 96 100 墨 0 98 - 99 100 149 - 76 67 - 0 88 0 95 150 - - 98 96 - 0 94 - 99 99 151 - - 96 99 - 0 98 - 94 99 152 - - 98 99 - 0 98 - 89 91 153 - - 99 97 - 0 99 - 94 99 154 - - 87 61 100 99 - 96 98 155 - - 96* 88* • 0* 95* 41* 94* 151284.doc •259- 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 156 - - 95 99 - 0 98 - 55 98 157 - - 99 99 - 92 99 - 97 99 158 _ - 100 100 99 96 - 100 100 159 - 100 100 - 100 98 100 100 160 - - 99 99 - 0 93 - 96 100 161 - - 100 100 - 100 96 99 100 162 - - 100 100 - 100 97 - 100 100 163 - 100 100 - 100 96 - 96 93 164 - - 99* 95* - 51* 95* - 89* 92* 165 - - 99 100 - 98 99 - 100 98 166 - - 100 100 - 99 96 - 99 100 167 - - 100 99 - 100 97 - 95 99 168 - - 100 100 - 100 97 - 100 100 169 - - 100* 99* - 73* 93* - 74* 81* 170 - - 100 100 - 100 97 100 100 99 171 - - 100 100 - 99 95 _ 100 100 172 - - 99 0 - 42 87 - 97 78 173 - - 99 16 - 0 63 - 82 93 174 - - 100 95 - 0 92 - 94 99 175 - - 99 100 - 100 95 _ 100 100 176 - - 99 99 - 69 96 - 100 100 177 - - 99 100 - 100 95 - 100 100 178 - - 99 88 - 0 95 98 99 179 - - 99 100 - 100 95 - 100 100 180 - - 100 100 - 100 93 - 100 100 181 - - 100 100 - 100 95 - 100 100 182 - - 100 100 - 97 96 - 100 100 183 - - 99 99 - 0 93 65 99 100 184 - 100 98 - 0 93 0 93 99 185 - 100 99 - 92 95 6 99 100 186 - - 99 85 - 83 94 98 100 100 187 _ _ 99 96 - 79 95 64 99 100 151284.doc • 260· 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 188 - - 100 100 - 99 95 17 100 99 189 - 100 91 - 73 94 32 96 99 190 - - 100 96 - 0 94 11 94 97 191 - - 95 0 - 0 85 11 19 0 192 - - 99 80 - 0 94 6 98 94 193 - - 99 98 - 69 93 11 99 99 194 - - 99 91 - 0 95 6 99 100 195 - - 99 100 - 98 96 11 98 97 196 - - 99 0 - 0 94 0 80 0 197 - - 100 96 - 86 96 17 99 97 198 - - 99* 100* - 99* 94* - 99* 100* 199 - - 100 100 - 0 96 0 98 0 200 - - 100 94 - 0 95 6 91 96 201 - - 100 100 - 0 94 17 98 100 202 - 63* 0* - 0* 23* 11* 0* 0* 203 - - 99 96 - 0 94 6 91 99 204 - - 100 99 - 0 97 11 97 99 205 - - 99* 100* - 0* 88* 11* 41* 0* 206 - - 100 100 - 100 97 11 100 100 207 - - 99 100 - 99 96 61 100 100 208 - - 99 100 - 100 93 32 100 100 209 - - 99 100 - 100 95 86 100 100 210 - - 99 99 - 95 93 6 99 100 211 - - 100 100 - 100 95 17 99 100 212 - - 100 100 - 100 100 83 100 100 213 - - 62* 0* - 0* 0* 63* 28* 0* 214 - - 100 99 - 0 100 70 100 99 215 - - 99 99 - 82 93 9 97 99 216 - - 94 91 - 51 96 0 97 99 217 - - 100 100 - 51 96 67 98 100 218 - - 99* 98* - 0* 94* 0* 86* 0* 219 _ _ 100 98 _ 0 95 9 94 98 151284.doc -261 - 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 220 - _ 99 99 - 0 94 0 90 99 221 - 100 100 - 99 95 85 100 100 222 - - 100* 100* - 99* 91* 0* 100* 100* 223 - - 100* 100* - 90* 93* 0* 100* 100* 224 - - 100* 100* - 82* 91* 0* 99* 99* 225 - 100 100 - 80 93 0 99 99 226 - _ 100 99 - 78 95 0 96 96 227 - - 99 98 - 0 92 0 94 95 228 - - 99 100 - 82 91 0 99 100 229 - - 100 100 - 99 93 54 100 100 230 - - 100 100 - 87 92 18 97 77 231 - - 0 0 - 0 8 0 41 0 232 - - 100 99 - 0 93 0 98 97 233 - - 0 0 - 0 3 0 28 0 234 - 攀 98 57 - 0 72 17 0 0 235 - - 63 0 - 100 50 0 55 0 236 - - 99 0 - 0 90 0 41 0 237 - - 98 0 - 0 35 0 80 0 238 - - 100 99 - 0 95 9 99 98 239 - - 99 0 - 0 93 9 74 80 240 - - 100 100 - 40 91 54 99 96 241 - - 100 100 - 64 91 41 99 97 242 - - 99 100 - 89 90 9 98 97 243 - - 99 100 畢 0 92 0 99 96 244 - - 99 100 - 98 92 74 99 99 245 - - 99 100 - 87 89 100 100 100 246 - - 31* 0* - 0* 48* 0* 0* 0* 247 - - 99 0 禪 0 91 0 74 0 248 - - 99* 98* - 60* 92* 0* 95* 99* 249 - - 99 99 - 0 94 0 90 98 250 - - 100 0 0 93 0 74 75 251 • _ 99 0 0 86 0 27 0 151284.doc · 262 - 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 252 - - 100 91 - 0 91 0 99 99 253 - - 94 0 - 0 78 0 0 0 254 - - 100* 99* - 0* 96* 0* 95* 97* 255 - - 100* 99* - 35* 96* 0* 91* 98* 256 - - 100* 99* - 0* 95* 0* 67* 95* 257 墨 - 99* 99* - 0* 95* 0* 95* 99* 258 - - 99 100 - 60 99 - 100 100 259 - - 98 100 - 0 91 - 99 98 260 - - 100 100 - 99 95 18 100 100 261 - - 100 99 一 0 94 0 99 100 262 - - 100 100 - 100 97 60 99 100 263 - 99 100 - 99 95 79 99 100 264 - - 100* 100* - 99* 93* 0* 100* 99* 265 - - 100* 98* - 0* 94* 0* 88* 13* 266 - - 100 80 - 79 96 0 79 100 267 - - 100 99 - 82 96 0 82 100 268 - - 100 100 - 99 94 0 99 100 269 - - 99 100 - 0 96 0 73 100 270 - - 100 100 - 99 96 0 94 99 271 - - 100 0 - 0 99 0 97 98 272 - - 99 98 - 0 100 0 98 99 273 - - 100 100 - 100 93 100 100 100 274 - - 100 0 - 92 96 0 97 98 275 - - 0* 0* - 0* 3* 0* 〇* 0* 276 - - 100* 100* - 0* 99* 0* 74* 99* 277 - - 100* 99* - 0* 14* 9* 0* 0* 278 - - 99* 99* - 0* 96* 0* 93* 100* 279 - - 100* 100* - 0* 99* 0* 94* 98* 280 - - 100* 100* - 0* 97* 0* 26* 99* 281 - - 100* 99* - 0* 89* 9* 9* 94* 282 - - 100 100 - 99 100 0 97 100 283 • • 100 100 _ 100 100 0 97 99 151284.doc -263 - 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 284 - 100 98 0 100 0 100 100 285 - - 100 100 - 60 100 0 99 100 286 - 100* 0* 69* 94* 0* 91* 99* 287 - - 100 100 100 100 0 96 100 288 - - 100 100 - 100 100 27 100 100 289 - - 100 100 - 99 100 0 93 100 290 - 100 100 - 0 99 0 100 100 291 - - 99 77 - 0 99 0 98 98 292 - - 100 100 - 100 100 0 100 100 293 - - 50 0 - 0 92 0 0 0 294 - - 96 9 - 0 99 0 68 76 295 - - 99 24 - 0 99 0 68 0 296 學 87 98 - 0 81 0 0 0 297 - - 99 80 - 60 100 0 98 98 298 - - 0 0 - 0 86 0 0 0 299 - - 97 100 - 95 94 - 100 100 300 - 99 100 - 98 95 - 98 99 301 - - 97 99 0 97 97 99 302 - - 99 99 - 0 95 - 99 100 303 - - 99 99 - 99 97 - 89 100 304 - - 99 100 _ 100 98 95 99 305 - 97* 100* - 92* 95 - 97* 98* 306 - - 96* 100* - 〇* 95* - 68* 91* 307 - 94 80 - 0 30 - 0 81 308 - - 99 100 - 90* 93 - 100 100 309 - - 77 100 - 33 93 - 100 100 310 - 99 95 - 0 95 - 99 68 311 - - 0 0 - 0 88 - 0 43 312 - - 85 0 - 0 91 - 97 97 313 _ - 96 16 0 92 - 95 89 314 _ _ 99* 63* - 0* 95* 9* 98* 98* 315 • _ 99* 85* _ 0* 97* 0* 93* 96* 151284.doc -264- 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 316 - - 99* 99* - 0* 94* 0* 97* 98* 317 - - 100* 100* - 0* 96* 0* 78* 99* 318 - - 99* 99* 0* 95* 0* 100* 99* 319 - - 99* 89* - 0* 72* 0* 99* 100* 320 - - 100* 99* - 0* 88* 0* 99* 99* 321 - - 99* 100* - 0* 82* 0* 93* 100* 322 - - 94* 0* - 0* 32* 0* 71* 96* 323 - - 99* 99* - 0* 96* 0* 91* 58* 324 - - 100 100 - 100 97 0 98 100 325 - - 100 100 - 100 96 80 100 100 326 _ - 98 26 - 0 92 0 87 42 327 - - 9 0 - 0 0 0 75 0 328 - - 100 100 - 95 94 0 99 100 329 - - 100 100 - 95 96 0 99 100 330 - - 100 100 - 99 95 0 97 100 331 - 100 99 - 0 94 32 98 100 332 - - 100 100 - 89 95 28 100 100 333 - - 96 88 - 0 95 0 98 98 334 - - 66 0 - 0 0 0 14 0 335 - - 96 0 - 0 88 0 78 0 336 - - 99 100 - 100 93 41 100 100 337 - - 96* 98* - 0* 93* 0* 100* 100* 338 - - 97* 99* - 0* 87* 0* 76* 100* 339 - - 92* 99* - 0* 91* 0* 0* 0* 340 - - 94* 100* - 0* 82* 0* 0* 0* 341 - - 96* 99* - 0* 93* 0* 97* 99* 342 - - 89* 99* - 0* 89* 0* 99* 99* 343 - - 97* 99* - 0* 31* 0* 99* 100* 344 - - 93* 99* - 0* 6* 0* 0* 97* 345 - - 99 100 - 100 93 100 100 100 346 - - 98 100 - 100 94 98 100 100 347 一 _ 98 99 _ 98 95 0 67 99 151284.doc -265 · 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 348 - - 90* 92* _ 60* 93* 0* 98* 100* 349 - - 99 99 - 99 96 0 100 100 350 - - 99 100 100 97 0 99 100 351 _ _ 99 100 - 100 99 9 98 100 352 - - 99 99 _ 99 99 0 99 100 353 - - 97 98 - 0 98 40 79 99 354 - - 99 100 - 100 100 100 100 100 355 - - 99 99 - 73 100 0 93 99 356 - - 97 99 - 0 100 100 100 100 357 - - 97 100 - 100 100 100 100 100 358 - - 100 100 - 96 98 0 99 100 359 - - 100 99 - 99 98 0 98 100 360 - - 100 100 - 100 97 0 100 100 361 - - 99* 99* - 0* 98* 0* 98* 90* 362 - - 100* 100* - 0* 98* 0* 99* 96* 363 - - 100* 100* - 0* 98* 0* 99* 97* 364 - - 99* 100* - 60* 98* 85* 99* 97 365 - - 100* 100* - 80* 98* 68* 100* 98* 366 - 100 100 - 100 99 0 100 100 367 - - 0 0 - 0 82 9 48 0 368 - - 0 0 - 0 58 0 88 71 369 - - 100 0 - 0 99 41 99 95 370 - - 97 0 - 0 99 0 99 91 371 - - 38 0 - 0 2 0 0 0 372 - - 0 0 - 0 2 0 0 0 373 - - 99 76 - 60 97 9 100 99 374 - - 99 0 - 0 99 27 100 100 375 - - 15 0 - 0 3 0 0 21 376 - - 0 0 - 0 0 0 0 0 377 - - 99* 96* - 0* 97* 0* 98* 89* 378 - - 99* 60* - 0* 97* 0* 95* 0* 379 _ 100 100 - 98 99 27 100 99 151284.doc .266- 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 380 - - 100 100 - 99 98 0 100 100 381 - - 99 88 - 60 97 0 99 100 382 - - 98 100 - 94 96 0 99 100 383 - - 100 100 - 99 98 0 100 100 384 - - 100 100 - 100 97 0 99 100 385 - - 100 100 - 96 98 0 100 100 386 - - 99 100 - 0 96 0 46 98 387 - - 100 100 - 100 99 100 100 100 388 - - 100 100 - 100 99 100 100 100 389 - - 99 100 - 97 100 9 100 100 390 - - 100 100 - 99 100 0 99 100 391 - - 100 100 - 100 100 0 94 100 392 - - 99* 100* - 64* 99* 66* 100* 100* 393 - - 100 100 - 100 96 97 100 100 394 - - 100 100 - 100 97 97 100 100 395 - - 99 67 - 0 94 7 99 100 396 - - 99 100 - 98 94 72 100 100 397 - - 100 100 - 100 97 84 100 99 398 - - 100* 99* - 92* 95* 0* 99* 71* 399 - - 100 100 - 0 96 22 100 99 400 - - 100 0 - 60 100 0 98 97 401 - - 96 0 - 0 73 0 76 72 402 - 100 99 - 100 100 100 100 99 403 - - 100 100 - 87 100 97 100 100 404 - - 99* 33* - 0* 96* 84* 98* 21* 405 - - 100 100 - 99 97 15 99 100 406 - 99 97 - 0 94 0 85 83 407 - - 100 100 - 100 97 100 100 100 408 - - 100 99 - 98 98 97 100 100 409 - - 100* 100* - 94* 96* 7* 100* 100* 410 - - 100 100 _ 0 97 96 98 98 411 - - 100 100 • 100 96 100 100 100 151284.doc -267- 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 412 - - 100 100 - 99 96 99 100 100 413 - - 94 73 _ 0 98 0 74 97 414 - - 100 100 - 97 98 99 - 100 415 - - 100 100 - 100 99 99 100 100 416 - - 26 0 - 0 9 0 0 0 417 - 86 100 0 94 7 0 99 418 - 99* 98* - 87* 99* 7* 97* 97* 419 - - 99 100 - 99 99 98 100 100 420 - - 99 100 - 100 99 97 100 100 421 - - 19 0 - 0 73 0 0 94 422 - 99 100 - 0 99 0 28 100 423 - 100* 96* - 31* 99* 7* 86* 82* 424 _ - 99 100 - 100 99 100 100 100 425 - - 99 100 - 99 99 100 100 100 426 - 91 66 - 0 81 0 16 57 427 - - 99 100 - 60 96 0 8 100 428 - - 99* 100* - 64* 99* 15* 97* 21* 429 - - 100 100 0 100 0 99 100 430 - - 100 0 - 0 99 0 98 99 431 - - 99 99 - 0 100 100 100 99 432 - - 98 85 - 0 98 99 99 97 433 - 99 53 - 0 96 51 98 99 434 - - 100 99 - 90 98 100 100 99 435 - - 100 100 - 99 98 100 100 100 436 _ - 100 100 - 99 99 100 100 100 437 - - 99 64 - 0 94 0 99 90 438 - - 99 99 - 0 100 40 99 100 439 - - 90* 24* - 0* 95* 0* 52* 0* 440 - - 97* 0* - 0* 92* 0* 65* 0* 441 - - 〇* 0* - 0* 87* 0* 52* 0* 442 - - 99* 17* - 0* 95* 〇* 83* 35* 443 93* 47* • 0* 97* 0* 92* 35* 151284.doc -268- 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 444 - - 0* 0* - 0* 95 0* 0* 69* 445 - - 0* 0* - 0* 97* 0* 61* 0* 446 - - 97 0 - 60 97 0 95 79 447 - - 99* 99* - 78* 100* 99* 100* 99* 448 - - 100* 99* - 91* 98* 100* 99* 100* 449 - - 8* 0* - 0* 97* 49* 9* 0* 450 - - 99* 99* - 99* 99* 100* 100* 96* 451 - - 0 0 - 0 55 0 61 61 452 - - 100 99 - 100 99 0 98 100 453 - - 100 99 - 99 99 54 99 100 454 - - 100 99 - 96 99 46 97 100 455 - - 100 99 - 99 99 54 99 100 456 - - 100 100 - 99 99 100 100 100 457 - - 99 100 - 99 99 9 100 90 458 - - 99 93 - 98 99 98 100 94 459 - - 100 100 - 99 98 100 100 100 460 - - 100 99 - 99 99 99 100 98 461 - - 100 100 - 100 99 100 100 100 462 - - 100 100 - 100 99 100 100 100 463 - - 100 100 - 99 99 18 100 100 464 - - 99 100 - 98 100 0 100 100 465 - - 99 100 - 98 99 0 99 100 466 - 100 100 - 99 100 97 100 100 467 - - 100 100 - 100 99 53 99 100 468 - - 100* 100* - 82* 98* 98* 99* 98* 469 - - 100* 100* - 99* 98* 100* 100* 100* 470 - - 78 0 0 98 0 74 81 471 - - 99* 99* - 51* 95* 39* 82* 64* 472 - - 100 100 - 99 99 100 100 100 473 - - 100* 100* - 99* 98* 0* 99* 98* 474 - - 100 99 - 97 99 97 99 96 475 - - 100* 100* _ 100* 99* 99* 99* 100* 151284.doc -269- 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 476 - - 100 91 0 98 8 19 93 477 - - 99 0 - 0 99 0 83 56 478 - - 100 100 - 91 99 7 100 95 479 - - 99 100 - 99 99 100 100 100 480 - - 57 100 - 0 99 25 86 100 481 - - 100 100 - 100 99 67 100 100 482 - - 100 0 - 82 99 7 80 89 483 - - 100 100 - 100 99 100 100 100 484 - - 100 100 - 100 98 99 100 98 485 - - 100 100 - 99 99 98 99 99 486 - 100* 57* - 〇* 95 Ί* 86* 61* 487 - - 100 100 - 100 100 78 100 100 488 - - 100 100 - 100 99 100 100 100 489 - - 100 100 - 78 99 0 99 73 490 - - 100 100 - 95 100 - 99 99 491 - - 100 100 - 0 99 0 96 79 492 - 100 100 - 97 100 99 100 100 493 - - 99 100 - 98 99 99 100 100 494 - - 100 100 - 97 98 0 100 99 495 - - 100 99 73 99 15 91 98 497 - - 100 100 - 100 99 100 100 100 498 - - 100 100 - 99 99 - 100 100 499 - - 100 100 - 99 100 9 99 100 500 - - 99 100 - 99 100 0 99 100 501 - - 100 100 - 100 99 0 99 100 502 - - 100 100 - 100 100 41 100 100 503 - 100 99 - 99 99 41 100 95 504 - 100 100 - 99 100 9 100 100 505 - - 99 100 - 97 100 99 100 100 506 - - 100 100 - 100 100 100 100 100 507 - - 100 100 - 100 100 96 100 100 508 _ 100 100 _ 100 100 100 100 100 151284.doc -270- 201117722 化合物 試驗 A 試驗 B 試驗 C 試驗 D 試驗 E 試驗 F 試驗 G 試驗 Η 試驗 I 試驗 J 509 37 99 100 100 0 100 100 - 100 100 510 - - 100 99 - 92 98 0 99 72 511 - - 100 99 - 0 97 0 98 72 512 - - 100 100 - 100 99 41 100 100 513 - - 100 100 - 100 100 41 99 99 514 - - 99 99 - 100 99 89 97 100 515 - - 99 99 - 100 98 95 99 99 516 - - 100 100 - 99 100 98 99 100 517 - - 100 100 - 100 100 100 100 100 518 - - 100 97 - 90 100 90 98 99 519 - - 100 100 - 99 99 96 99 99 520 - - 99 99 - 100 100 98 100 100 521 - - 100 100 - 87 100 32 100 100 522 - - 100 100 - 98 99 0 99 99 523 - - 100 100 琴 100 100 100 10 99 524 - - 100 100 - 99 99 0 98 100 525 - - 99 99 - 99 100 0 99 100 526 - - 100 100 - 99 99 97 100 100 527 - - 99 99 - 100 100 18 100 100 528 - - 98 97 - 97 99 0 100 100 529 - - 100 100 - 100 98 0 99 100 530 - - 100 100 - 100 100 99 100 100 531 - - 100 99 - 100 100 100 100 100 532 - 99 99 - 90 100 0 98 97 533 - - 100* 100* - 99* 100* 0* 92* 100* 534 - - 99* 100* - 90* 100* 8* 100* 100* 535 - - 99* 100 - 95* 100* 0* 100* 100* 536 - _ 99 100 - 98 100 0 99 100 製備試驗K、L以及Μ的檢測組合物的一般規範如 下。化合物181，百殺芬、5-氣-6-(2,4,6-三氟苯基)-7-(4- t51284.doc •271 - 201117722 甲基六氫0比咬-1-基）[1，2,4]三β坐[l，5-a]°f 咬（BAS600)、 環克座、異派來桑、吡噻菌胺、撲殺熱、快諾芬及葚孢 菌素取得為未經配製、工業級原料。亞托敏、白克列、 百菌清、氫氧化銅、霜脲氰、待克利、達滅芬、依普座、 丁苯嗎啉、扶吉胺、咯菌酯、滅菌丹、異菌脲、丙森鋅、 辞錳乃浦、右滅達樂（亦稱滅達樂、邁克尼、啶氧 菌酯、丙氧喹琳、丙硫菌唑、百克敏、四克利及三環唑 (tricyclozole)取得為未經配製、工業級原料，其以商Test J Sprinkle the test on the wheat seedling until it overflows. On the next day, the spore suspension of the seedling clock, BlumeHa g_inis f $ tritici (also known as Erysiphe graminis f. sp. tritici, wheat powdery mildew pathogen) was then transferred to the growth chamber for 8 days. After this time, the appearance disease rating is performed. The results of testing A-J are presented in Table A. In the table, grade 1 〇〇 indicates 100% disease prevention, and grade 0 indicates no disease control effect (relative to the control group). A dash (-) indicates no test result. All results 151284.doc -254- 201117722 for 200 ppm, except for the presence of the asterisk "*", which means 40 ppm ° Compound Test A Test B Test C Test D Table A Test E Test F Test G Test Η Test I Test J 1 0 65 99 100 0 100 100 0* 100 100 2 0 99 99 100 0 99 100 - 99 100 3 0 38 98 99 0 0 100 - 88 99 4 0 99 99 100 0 95 100 - 100 100 5 0 81 100 100 0 0 99 • 98 99 6 - - 99* 99* - 0* 94* - 97* 100* 7 6 99 100 100 0 99 99 - 100 100 8 20 99 87* 100* 0 94* 96* - 99 * 100* 9 - - 0 - 0 97 - 99 90 10 - 98* 100* - 0* 84* - 97* 95* 11 - _ 99 99 - 0 88 - 100 95 12 13 100 99 100 0 100 100 - 99 100 13 - - 93 100 - 0 91 - 100 100 14 - - 99 100 - - 88 - 100 99 15 - - 97 100 - 51 95 - 100 100 16 - - 99 100 - 74 91 - 100 100 17 Piano - 99* 100* - 0* 94* - 100* 100* 18 - - 99 100 - 100 95 - 100 100 19 - - 99* 100* - 99* 90* 91* 100* 100* 20 20 100 100 100 0 100 100 - 100 100 21 - - 99 100 - 99 92 - 100 100 22 - 99* 100* - 100* 92* - 100* 100* 23 - - 99* 100* - 99* 95* 98* 100* 24 - - 99 100 - 64 94 - 99 98 25 - - 99* 100* - 99* 93* - 91* 100* 26 - - 98* 100* - 97* 96* - 97* 99 * 27 151284.doc 99* 100* -255 - 40* 92* 99* 98* 201117722 Compound Test A Test B Test C Test D Test E Test F Test G Test Η Test I Test J 28 - - 100 98 _ 100 100 99 100 100 29 - - 94 42 - 0 77 - 54 93 30 - - 99 100 - 100 94 - 100 100 31 - - 98 100 - 100 94 - 99 99 32 - - 98 100 - 100 92 100 100 33 - - 94 100 - 100 94 - 97 99 34 - - 84 100 - 0 97 - 99 100 35 _ - 89 100 - 0 95 - 100 99 36 - - 92 24 - 0 87 - 99 91 37 - - 94* 100* - 98* 93* - 99* 100* 38 - - 84 99 - 0 87 - 96 100 39 - - 98 100 - 51 79 - 99 100 40 - - 93* 100* - 82* 97* - 86* 97* 41 - - 99 100 - 95 95 - 100 96 42 - - 0 100 - 0 95 - 41 95 43 - - 99 100 - 99 94 - 99 99 44 - - 96 100 - 92 97 - 99 100 45 - - 100 100 - 60 87 - 100 100 46 - - 37 99 - 60 97 - 99 100 47 - 90 100 - 100 98 - 100 100 48 - - 81 100 - 69 93 - 98 100 49 - - 90 100 - 100 91 - 99 100 50 - - 97 100 - 99 98 - 100 100 51 - _ 0 99 - 0 88 - 91 99 52 - - 73 100 - 11 98 - 96 100 53 - - 0 0 - 0 93 - 27 99 54 - - 0 0 - 0 0 - 54 0 55 - - 98 100 - 100 99 - 96 100 56 - - 76 100 - 0 98 - 89 100 57 - - 97 100 100 99 - 98 100 58 - - 56 53 - 0 95 - 99. 100 59 • - 96 97 - 95 95 • 100 100 151284.doc •256· 201117722 Compound Test A Test B Test C Test D Test E Test F Test G Test Η Test I Test J 60 - - 98* 100* - 97* 97* - 97* 99* 61 - 97 93 - 99 97 - 98 99 62 - - 88 0 - 0 97 - 100 99 63 - - 98 0 - 55 97 - 99 99 64 - - 79 92 - 90 98 - 100 99 65 - - 98 99 - 94 94 - 99 100 66 - - 96 100 - 100 96 - 100 100 67 - - 100* 100* - 0* 74* - 98* 99* 68 - - 94 57 - 0 94 - 68 63 69 - - 94 99 - 100 95 - 97 96 70 - - 98 99 - 97 95 - 97 97 71 - - 93 0 - 0 95 - 41 72 72 _ - 0* 0* - 0* 0* - 0* 0* 73 - - 96 100 - 99 97 - 99 100 74 - - 99 100 - 60 94 - 99 100 75 - - 96 80 - 40 91 - 80 0 76 - - 98 0 - 0 96 - 90 92 77 - - 98 100 - 100 96 - 100 100 78 - - 97 99 - 69 96 - 99 99 79 - 99 100 - 98 95 - 100 100 80 - - 97 96 - 96 93 - 97 100 81 - - 99 100 - 0 89 - 74 95 82 - - 98 100 - 0 85 99 96 83 - - 90* 99* - 0* 85* - 0* 48* 84 - - 97 100 - 99 93 - 99 100 85 - - 99 100 - 0 93 - 100 100 86 - 0 0 - 0 93 - 55 39 87 - - 99 100 - 0 91 - 99 100 88 - - 99 100 - 97 94 - 100 100 89 - - 99 100 - 100 100 - 100 100 90 - - 100 100 - 100 100 - 100 100 91 - - 99 100 _ 100 100 • 100 100 151284.doc • 257· 201117722 Compound Test A Test B Test C Test D Test E Test F Test G Test Η Test I Test J 92 - - 99 100 _ 100 100 - 100 100 93 - 91 100 - 82 100 100 99 94 - - 99 100 - 99 100 - 100 100 95 - - 53 0 - 98 96 - 95 95 96 - - 99 100 - 60 98 - 97 100 97 - - 97* 100* - 69* 99* 89* 96 * 98 - - 99 99 - 69 96 - 89 99 99 - - 98 100 - 69 96 - 99 100 100 - - 99 100 - 0 93 - 86 99 101 - - 99 100 - 87 95 - 99 100 102 Climbing - 98* 100* - 99* 97* - 97* 99* 103 - - 97 99 - 98 97 - 100 100 104 - - 99 100 - 96 97 - 100 100 105 - 99 100 - 99 97 - 100 100 106 - - 88* 97* - 0* 93* - 23* 94* 107 - - 91* 88* - 0* 96* - 19* 94* 108 - 99* 100* - 0* 95* - 0* 98* 109 - - 97 99 _ 84 98 - 100 100 110 - - 99 100 - 40 96 - 88 99 111 - - 97 98 - 0 95 - 99 99 112 - - 99 100 - 100 98 - 98 99 113 - - 99 99 - 100 98 - 99 99 114 - - 98 99 - 82 98 - 100 100 115 - - 97 97 - 82 98 - 100 99 116 - - 99 100 - 73 96 - 97 99 117 - - 99* 91* - 0* 85* - 66* 48* 118 - - 99 100 - 0 97 - 100 100 119 - - 99 100 - 78 94 - 100 99 120 - - 98 88 0 97 - 100 100 121 - - 99 100 94 97 - 100 100 122 - - 98 100 0 97 100 99 123 98 100 51 97 _ 100 99 151284.doc • 258· 201117722 Compound test A test B test C test D test E test F test G test Η test I Test J 124 - - 97 100 - 0 93 - 100 100 125 - - 99 100 - 64 94 - 100 94 126 - - 99 100 - 0 92 - 100 97 127 - - 99 99 - 0 93 - 100 100 128 - - 98 99 - 0 90 - 100 95 129 - - 92 100 - 100 96 - 98 95 130 - - 99 100 - 100 98 - 96 100 131 - - 91 61 - 98 97 - 98 100 132 - - 87 98 - 87 97 - 100 99 133 - - 90* 91* - 0* 90* - 18* 26* 134 - - 99 100 - 100 98 - 100 100 135 - - 95 99 0 98 - 100 99 136 - - 93 99 - 80 98 - 100 99 137 - - 63 0 - 0 96 - 100 42 138 - - 100* 99* - 97* 94* - 97* 98* 139 - 99* 100* - 0* 96* - 93* 94* 140 - - 33* 57* - 0* 13* - 0* 0* 141 - - 99* 99* - 0* 91* - 80* 73* 142 33 99 98 97 0 51 96 - 99 99 143 82 99 98 99 0 0 97 - 99 100 144 - - 99 99 - 0 95 - 97 98 145 - - 99 99 - 0 99 - 97 98 146 - - 99 100 - 60 98 - 99 100 147 - - 93 51 - 0 90 - 80 98 148 - - 96 100 Ink 0 98 - 99 100 149 - 76 67 - 0 88 0 95 150 - - 98 96 - 0 94 - 99 99 151 - - 96 99 - 0 98 - 94 99 152 - - 98 99 - 0 98 - 89 91 153 - - 99 97 - 0 99 - 94 99 154 - - 87 61 100 99 - 96 98 155 - - 96* 88* • 0* 95* 41* 94* 151284 .doc •259- 201117722 Compound Test A Test B Test C Test D Test E Test F Test G Test Η Test I Test J 156 - - 95 99 - 0 98 - 55 98 157 - - 99 99 - 92 99 - 97 99 158 _ - 100 100 99 96 - 100 100 159 - 100 100 - 100 98 100 100 160 - - 99 99 - 0 93 - 96 100 161 - - 100 100 - 100 96 99 100 162 - - 100 100 - 100 97 - 100 100 163 - 100 100 - 100 96 - 96 93 164 - - 99* 95* - 51* 95* - 89* 92* 165 - - 99 100 - 98 99 - 100 98 166 - - 100 100 - 99 96 - 99 100 167 - - 100 99 - 100 97 - 95 99 168 - - 100 100 - 100 97 - 100 100 169 - - 100* 99* - 73* 93* - 74* 81* 170 - - 100 100 - 100 97 100 100 99 171 - - 100 100 - 99 95 _ 100 100 172 - - 99 0 - 42 87 - 97 78 173 - - 99 16 - 0 63 - 82 93 174 - - 100 95 - 0 92 - 94 99 175 - - 99 100 - 100 95 _ 100 100 176 - - 99 99 - 69 96 - 100 100 177 - - 99 100 - 100 95 - 100 100 178 - - 99 88 - 0 95 98 99 179 - - 99 100 - 100 95 - 100 100 180 - - 100 100 - 100 93 - 100 100 181 - - 100 100 - 100 95 - 100 100 182 - - 100 100 - 97 96 - 100 100 183 - - 99 99 - 0 93 65 99 100 184 - 100 98 - 0 93 0 93 99 185 - 100 99 - 92 95 6 99 100 186 - - 99 85 - 83 94 98 100 100 187 _ _ 99 96 - 79 95 64 99 100 151284 .doc • 260· 201117722 Compound Test A Test B Test C Test D Test E Test F Test G Test Η Test I Test J 188 - - 100 100 - 99 95 17 100 99 189 - 100 91 - 73 94 32 96 99 190 - - 100 96 - 0 94 11 94 97 191 - - 95 0 - 0 85 11 19 0 192 - - 99 80 - 0 94 6 98 94 193 - - 99 98 - 69 93 11 99 99 194 - - 99 91 - 0 95 6 99 100 195 - - 99 100 - 98 96 11 98 97 196 - - 99 0 - 0 94 0 80 0 197 - - 100 96 - 86 96 17 99 97 198 - - 99* 100* - 99* 94* - 99 * 100* 199 - - 100 100 - 0 96 0 98 0 200 - - 100 94 - 0 95 6 91 96 201 - - 100 100 - 0 94 17 98 100 202 - 63* 0* - 0* 23* 11* 0 * 0* 203 - - 99 96 - 0 94 6 91 99 204 - - 100 99 - 0 97 11 97 99 205 - - 99* 100* - 0* 88* 11* 41* 0* 206 - - 100 100 - 100 97 11 100 100 207 - - 99 100 - 99 96 61 100 100 208 - - 99 100 - 100 93 32 100 100 209 - - 99 100 - 100 95 86 100 100 210 - - 99 99 - 95 93 6 99 100 211 - - 100 100 - 100 95 17 99 100 212 - - 100 100 - 100 100 83 100 100 213 - - 62* 0* - 0* 0* 63* 28* 0* 214 - - 100 99 - 0 100 70 100 99 215 - - 99 99 - 82 93 9 97 99 216 - - 94 91 - 51 96 0 97 99 217 - - 100 100 - 51 96 67 98 100 218 - - 99* 98* - 0* 94* 0* 86* 0* 219 _ _ 100 98 _ 0 95 9 94 98 151284.doc -261 - 201117722 Compound test A test B test C test D test E test F test G test Η test I test J 220 - _ 99 99 - 0 94 0 90 99 221 - 100 100 - 99 95 85 100 100 222 - - 100* 100* - 99* 91* 0* 100* 100* 223 - - 100* 100* - 90* 93 * 0* 100* 100* 224 - - 100* 100* - 82* 91* 0* 99* 99* 225 - 100 100 - 80 93 0 99 99 226 - _ 100 99 - 78 95 0 96 96 227 - - 99 98 - 0 92 0 94 95 228 - - 99 100 - 82 91 0 99 100 229 - - 100 100 - 99 93 54 100 100 230 - - 100 100 - 87 92 18 97 77 231 - - 0 0 - 0 8 0 41 0 232 - - 100 99 - 0 93 0 98 97 233 - - 0 0 - 0 3 0 28 0 234 - Climbing 98 57 - 0 72 17 0 0 235 - - 63 0 - 100 50 0 55 0 236 - - 99 0 - 0 90 0 41 0 237 - - 98 0 - 0 35 0 80 0 238 - - 100 99 - 0 95 9 99 98 239 - - 99 0 - 0 93 9 74 80 240 - - 100 100 - 40 91 54 99 9 6 241 - - 100 100 - 64 91 41 99 97 242 - - 99 100 - 89 90 9 98 97 243 - - 99 100 Completion 0 92 0 99 96 244 - - 99 100 - 98 92 74 99 99 245 - - 99 100 - 87 89 100 100 100 246 - - 31* 0* - 0* 48* 0* 0* 0* 247 - - 99 0 Zen 0 91 0 74 0 248 - - 99* 98* - 60* 92* 0* 95 * 99* 249 - 99 99 - 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 Test E Test F Test G Test Η Test I Test J 252 - - 100 91 - 0 91 0 99 99 253 - - 94 0 - 0 78 0 0 0 254 - - 100* 99* - 0* 96* 0* 95* 97* 255 - - 100* 99* - 35* 96* 0* 91* 98* 256 - - 100* 99* - 0* 95* 0* 67* 95* 257 Ink - 99* 99* - 0* 95* 0* 95* 99* 258 - - 99 100 - 60 99 - 100 100 259 - - 98 100 - 0 91 - 99 98 260 - - 100 100 - 99 95 18 100 100 261 - - 100 99 1 0 94 0 99 100 262 - - 100 100 - 100 97 60 99 100 263 - 99 100 - 99 95 79 99 100 264 - - 100* 100* - 99* 93* 0* 100* 99* 265 - - 100* 98* - 0* 94 * 0* 88* 13* 266 - - 100 8 0 - 79 96 0 79 100 267 - - 100 99 - 82 96 0 82 100 268 - - 100 100 - 99 94 0 99 100 269 - - 99 100 - 0 96 0 73 100 270 - - 100 100 - 99 96 0 94 99 271 - - 100 0 - 0 99 0 97 98 272 - - 99 98 - 0 100 0 98 99 273 - - 100 100 - 100 93 100 100 100 274 - - 100 0 - 92 96 0 97 98 275 - - 0* 0* - 0* 3* 0* 〇* 0* 276 - - 100* 100* - 0* 99* 0* 74* 99* 277 - - 100* 99* - 0* 14* 9* 0* 0* 278 - - 99* 99* - 0* 96* 0* 93* 100* 279 - - 100* 100* - 0* 99* 0* 94* 98* 280 - - 100* 100* - 0* 97* 0* 26 * 99* 281 - - 100* 99* - 0* 89* 9* 9* 94* 282 - - 100 100 - 99 100 0 97 100 283 • • 100 100 _ 100 100 0 97 99 151284.doc -263 - 201117722 Compound Test A Test B Test C Test D Test E Test F Test G Test Η Test I Test J 284 - 100 98 0 100 0 100 100 285 - - 100 100 - 60 100 0 99 100 286 - 100* 0* 69* 94 * 0* 91* 99* 287 - - 100 100 100 100 0 96 100 288 - - 100 100 - 100 100 27 100 100 289 - - 100 100 - 99 100 0 93 100 290 - 100 100 - 0 99 0 100 100 291 - - 9 9 77 - 0 99 0 98 98 292 - - 100 100 - 100 100 0 100 100 293 - - 50 0 - 0 92 0 0 0 294 - - 96 9 - 0 99 0 68 76 295 - - 99 24 - 0 99 0 68 0 296 87700 - 0 81 0 0 297 - - 99 80 - 60 100 0 98 98 298 - - 0 0 - 0 86 0 0 0 299 - - 97 100 - 95 94 - 100 100 300 - 99 100 - 98 95 - 98 99 301 - - 97 99 0 97 97 99 302 - - 99 99 - 0 95 - 99 100 303 - - 99 99 - 99 97 - 89 100 304 - - 99 100 _ 100 98 95 99 305 - 97* 100* - 92* 95 - 97* 98* 306 - - 96* 100* - 〇* 95* - 68* 91* 307 - 94 80 - 0 30 - 0 81 308 - - 99 100 - 90* 93 - 100 100 309 - - 77 100 - 33 93 - 100 100 310 - 99 95 - 0 95 - 99 68 311 - - 0 0 - 0 88 - 0 43 312 - - 85 0 - 0 91 - 97 97 313 _ - 96 16 0 92 - 95 89 314 _ _ 99* 63* - 0* 95* 9* 98* 98* 315 • _ 99* 85* _ 0* 97* 0* 93* 96* 151284.doc -264- 201117722 Compound Test A Test B Test C Test D Test E Test F Test G Test Η Test I Test J 316 - - 99* 99* - 0* 94* 0* 97* 98* 317 - - 100* 100* - 0* 96* 0* 78 * 99* 318 - - 99* 99* 0* 95* 0* 100* 99* 319 - - 99* 89* - 0* 72* 0* 99* 100* 320 - - 100* 99* - 0* 88* 0* 99* 99* 321 - - 99 * 100* - 0* 82* 0* 93* 100* 322 - - 94* 0* - 0* 32* 0* 71* 96* 323 - - 99* 99* - 0* 96* 0* 91* 58* 324 - - 100 100 - 100 97 0 98 100 325 - - 100 100 - 100 96 80 100 100 326 _ - 98 26 - 0 92 0 87 42 327 - - 9 0 - 0 0 0 75 0 328 - - 100 100 - 95 94 0 99 100 329 - - 100 100 - 95 96 0 99 100 330 - - 100 100 - 99 95 0 97 100 331 - 100 99 - 0 94 32 98 100 332 - - 100 100 - 89 95 28 100 100 333 - - 96 88 - 0 95 0 98 98 334 - - 66 0 - 0 0 0 14 0 335 - - 96 0 - 0 88 0 78 0 336 - - 99 100 - 100 93 41 100 100 337 - - 96* 98* - 0* 93* 0* 100* 100* 338 - - 97* 99* - 0* 87* 0* 76* 100* 339 - - 92* 99* - 0* 91* 0* 0* 0* 340 - - 94 * 100* - 0* 82* 0* 0* 0* 341 - - 96* 99* - 0* 93* 0* 97* 99* 342 - - 89* 99* - 0* 89* 0* 99* 99* 343 - - 97* 99* - 0* 31* 0* 99* 100* 344 - - 93* 99* - 0* 6* 0* 0* 97* 345 - - 99 100 - 100 93 100 100 100 346 - - 98 100 - 100 94 98 100 100 347 _ 98 99 _ 98 95 0 67 99 151284.doc -265 · 201117722 Compound test A test B test C test D test E test F test G test Η test I test J 348 - - 90* 92* _ 60* 93* 0* 98* 100* 349 - - 99 99 - 99 96 0 100 100 350 - - 99 100 100 97 0 99 100 351 _ _ 99 100 - 100 99 9 98 100 352 - - 99 99 _ 99 99 0 99 100 353 - - 97 98 - 0 98 40 79 99 354 - - 99 100 - 100 100 100 100 100 355 - - 99 99 - 73 100 0 93 99 356 - - 97 99 - 0 100 100 100 100 357 - - 97 100 - 100 100 100 100 100 358 - - 100 100 - 96 98 0 99 100 359 - - 100 99 - 99 98 0 98 100 360 - - 100 100 - 100 97 0 100 100 361 - - 99* 99* - 0* 98* 0 * 98* 90* 362 - - 100* 100* - 0* 98* 0* 99* 96* 363 - - 100* 100* - 0* 98* 0* 99* 97* 364 - - 99* 100* - 60 * 98* 85* 99* 97 365 - - 100* 100* - 80* 98* 68* 100* 98* 366 - 100 100 - 100 99 0 100 100 367 - - 0 0 - 0 82 9 48 0 368 - - 0 0 - 0 58 0 88 71 369 - - 100 0 - 0 99 41 99 95 370 - - 97 0 - 0 99 0 99 91 371 - - 38 0 - 0 2 0 0 0 372 - - 0 0 - 0 2 0 0 0 373 - - 99 76 - 60 97 9 100 99 374 - - 99 0 - 0 99 27 100 100 375 - - 15 0 - 0 3 0 0 21 376 - - 0 0 - 0 0 0 0 0 377 - - 99* 96* - 0* 97* 0* 98* 89* 378 - - 99* 60* - 0* 97* 0* 95* 0* 379 _ 100 100 - 98 99 27 100 99 151284.doc .266- 201117722 Compound test A test B test C test D test E test F test G test Η test I test J 380 - - 100 100 - 99 98 0 100 100 381 - - 99 88 - 60 97 0 99 100 382 - - 98 100 - 94 96 0 99 100 383 - - 100 100 - 99 98 0 100 100 384 - - 100 100 - 100 97 0 99 100 385 - - 100 100 - 96 98 0 100 100 386 - - 99 100 - 0 96 0 46 98 387 - - 100 100 - 100 99 100 100 100 388 - - 100 100 - 100 99 100 100 100 389 - - 99 100 - 97 100 9 100 100 390 - - 100 100 - 99 100 0 99 100 391 - - 100 100 - 100 100 0 94 100 392 - - 99* 100* - 64* 99* 66* 100* 100* 393 - - 100 100 - 100 96 97 100 100 394 - - 100 100 - 100 97 97 100 100 395 - - 99 67 - 0 94 7 99 100 396 - - 99 100 - 98 94 72 100 100 397 - - 100 100 - 100 97 84 100 99 398 - - 1 00* 99* - 92* 95* 0* 99* 71* 399 - - 100 100 - 0 96 22 100 99 400 - - 100 0 - 60 100 0 98 97 401 - - 96 0 - 0 73 0 76 72 402 - 100 99 - 100 100 100 100 99 403 - - 100 100 - 87 100 97 100 100 404 - - 99* 33* - 0* 96* 84* 98* 21* 405 - - 100 100 - 99 97 15 99 100 406 - 99 97 - 0 94 0 85 83 407 - - 100 100 - 100 97 100 100 100 408 - - 100 99 - 98 98 97 100 100 409 - - 100* 100* - 94* 96* 7* 100* 100* 410 - - 100 100 _ 0 97 96 98 98 411 - - 100 100 • 100 96 100 100 100 151284.doc -267- 201117722 Compound test A test B test C test D test E test F test G test Η test I test J 412 - - 100 100 - 99 96 99 100 100 413 - - 94 73 _ 0 98 0 74 97 414 - - 100 100 - 97 98 99 - 100 415 - - 100 100 - 100 99 99 100 100 416 - - 26 0 - 0 9 0 0 0 417 - 86 100 0 94 7 0 99 418 - 99* 98* - 87* 99* 7* 97* 97* 419 - - 99 100 - 99 99 98 100 100 420 - - 99 100 - 100 99 97 100 100 421 - - 19 0 - 0 73 0 0 94 422 - 99 100 - 0 99 0 28 100 423 - 100* 96* - 31* 99* 7* 86* 82* 424 _ - 99 100 - 100 99 100 100 100 425 - - 99 100 - 99 99 100 100 100 426 - 91 66 - 0 81 0 16 57 427 - - 99 100 - 60 96 0 8 100 428 - - 99* 100* - 64* 99* 15* 97* 21* 429 - - 100 100 0 100 0 99 100 430 - - 100 0 - 0 99 0 98 99 431 - - 99 99 - 0 100 100 100 99 432 - - 98 85 - 0 98 99 99 97 433 - 99 53 - 0 96 51 98 99 434 - - 100 99 - 90 98 100 100 99 435 - - 100 100 - 99 98 100 100 100 436 _ - 100 100 - 99 99 100 100 100 437 - - 99 64 - 0 94 0 99 90 438 - - 99 99 - 0 100 40 99 100 439 - - 90* 24* - 0* 95* 0* 52* 0* 440 - - 97* 0* - 0* 92* 0* 65* 0* 441 - - 〇* 0* - 0* 87* 0* 52* 0* 442 - - 99* 17* - 0* 95* 〇* 83* 35* 443 93* 47* • 0* 97* 0* 92* 35* 151284.doc -268- 201117722 Compound Test A Test B Test C Test D Test E Test F Test G Test Η Test I Test J 444 - - 0* 0* - 0 * 95 0* 0* 69* 445 - - 0* 0* - 0* 97* 0* 61* 0* 446 - - 97 0 - 60 97 0 95 79 447 - - 99* 99* - 78* 100* 99 * 100* 99* 448 - - 100* 99* - 91* 98* 100* 99* 100* 449 - - 8* 0* - 0* 97* 49* 9* 0* 450 - - 99* 99* - 99* 99* 100* 100* 96* 451 - - 0 0 - 0 55 0 61 61 452 - - 100 99 - 100 99 0 98 100 453 - - 100 99 - 99 99 54 99 100 454 - - 100 99 - 96 99 46 97 100 455 - - 100 99 - 99 99 54 99 100 456 - - 100 100 - 99 99 100 100 100 457 - - 99 100 - 99 99 9 100 90 458 - - 99 93 - 98 99 98 100 94 459 - - 100 100 - 99 98 100 100 100 460 - - 100 99 - 99 99 99 100 98 461 - - 100 100 - 100 99 100 100 100 462 - - 100 100 - 100 99 100 100 100 463 - - 100 100 - 99 99 18 100 100 464 - - 99 100 - 98 100 0 100 100 465 - - 99 100 - 98 99 0 99 100 466 - 100 100 - 99 100 97 100 100 467 - - 100 100 - 100 99 53 99 100 468 - - 100* 100* - 82* 98* 98* 99* 98* 469 - - 100* 100* - 99* 98* 100* 100* 100* 470 - - 78 0 0 98 0 74 81 471 - - 99* 99* - 51* 95* 39* 82* 64* 472 - - 100 100 - 99 99 100 100 100 473 - - 100* 100* - 99* 98* 0* 99* 98* 474 - - 100 99 - 97 99 97 99 96 475 - - 100* 100* _ 100* 99* 99* 99* 100* 151284.doc - 269- 2011177 22 Compound test A Test B Test C Test D Test E Test F Test G Test Η Test I Test J 476 - - 100 91 0 98 8 19 93 477 - - 99 0 - 0 99 0 83 56 478 - - 100 100 - 91 99 7 100 95 479 - - 99 100 - 99 99 100 100 100 480 - - 57 100 - 0 99 25 86 100 481 - - 100 100 - 100 99 67 100 100 482 - - 100 0 - 82 99 7 80 89 483 - - 100 100 - 100 99 100 100 100 484 - - 100 100 - 100 98 99 100 98 485 - - 100 100 - 99 99 98 99 99 486 - 100* 57* - 〇* 95 Ί* 86* 61* 487 - - 100 100 - 100 100 78 100 100 488 - - 100 100 - 100 99 100 100 100 489 - - 100 100 - 78 99 0 99 73 490 - - 100 100 - 95 100 - 99 99 491 - - 100 100 - 0 99 0 96 79 492 - 100 100 - 97 100 99 100 100 493 - - 99 100 - 98 99 99 100 100 494 - - 100 100 - 97 98 0 100 99 495 - - 100 99 73 99 15 91 98 497 - - 100 100 - 100 99 100 100 100 498 - - 100 100 - 99 99 - 100 100 499 - - 100 100 - 99 100 9 99 100 500 - - 99 100 - 99 100 0 99 100 501 - - 100 100 - 100 99 0 99 100 502 - - 100 100 - 100 100 41 100 100 503 - 100 99 - 99 99 41 100 95 504 - 100 100 - 99 100 9 100 100 505 - - 99 100 - 97 100 99 100 100 506 - - 100 100 - 100 100 100 100 100 507 - - 100 100 - 100 100 96 100 100 508 _ 100 100 _ 100 100 100 100 100 151284.doc -270- 201117722 Compound test A test B test C test D test E test F test G test Η test I test J 509 37 99 100 100 0 100 100 - 100 100 510 - - 100 99 - 92 98 0 99 72 511 - - 100 99 - 0 97 0 98 72 512 - - 100 100 - 100 99 41 100 100 513 - - 100 100 - 100 100 41 99 99 514 - - 99 99 - 100 99 89 97 100 515 - - 99 99 - 100 98 95 99 99 516 - - 100 100 - 99 100 98 99 100 517 - - 100 100 - 100 100 100 100 100 518 - - 100 97 - 90 100 90 98 99 519 - - 100 100 - 99 99 96 99 99 520 - - 99 99 - 100 100 98 100 100 521 - - 100 100 - 87 100 32 100 100 522 - - 100 100 - 98 99 0 99 99 523 - - 100 100 piano 100 100 100 10 99 524 - - 100 100 - 99 99 0 98 100 525 - - 99 99 - 99 100 0 99 100 526 - - 100 100 - 99 99 97 100 100 527 - - 99 99 - 100 100 18 100 100 528 - - 98 97 - 97 99 0 100 100 529 - - 100 100 - 100 98 0 99 100 530 - - 100 100 - 100 100 99 100 100 531 - - 100 99 - 100 100 100 100 100 532 - 99 99 - 90 100 0 98 97 533 - - 100* 100* - 99* 100* 0* 92* 100* 534 - - 99* 100* - 90* 100* 8* 100* 100* 535 - - 99* 100 - 95* 100* 0* 100* 100* 536 - _ 99 100 - 98 100 0 99 100 The general specifications for the preparation of test compositions for tests K, L and hydrazine are as follows. Compound 181, chlorfenapyr, 5-gas-6-(2,4,6-trifluorophenyl)-7-(4-t51284.doc •271 - 201117722 methylhexahydrogen 0 to bit-1-yl) [1,2,4]Three β sitting [l,5-a]°f bite (BAS600), cyclazone, sinensis, pirfenium, chlorpyrifos, velocin and fusarium were obtained as Unformulated, industrial grade raw materials. Atomin, leucoside, chlorothalonil, copper hydroxide, cymoxanil, chlorhexidine, daxen, ezine, butyl morpholine, chlorpromazine, oxystrobin, sterilized dan, iprodione , Bensen Zinc, Citroganum, dextromethord (also known as madura, McAfee, oxypide, propoxyquinol, prothioconazole, baikemin, quaternary and tricyclozole) Obtained as an unformulated, industrial grade raw material

標 AMISTAR，ENDURA，BRAVO, KOCIDE，CURZATE， SCORE, ACROBAT, OPUS, CORBEL, OMEGA, MAXIM, PHALTAN, ROVRAL, MELODY, MANZATE, RIDOMIL GOLD, nova, acanto, talius, proline, HEADLINE, DOMARK以及BEAM分別進行商業販 售。未經配製的原料首先溶解在丙酮中，然後在（以 ppm)丙酮及純化水中懸浮至目標濃度（ 50/50體積混 合），其含有250 ppm的界面活性劑Trem® 014 (多元 醇酯）。已配製之原料經分散在不足的水中以產生目標 濃度，以及不論有機溶劑或界面活性劑皆不加入於懸浮 液中。產生的檢測混合物於其後用於檢測K、L以及M。 喷灑一 200 ppm的檢測懸浮液於檢測植物上直到溢流 程度，其相當於800 g/ha的速率。試驗重複三次並將三 次所得結果平均。 藉由Colby等式建立兩種活性成分間之協同作用關 係（見 Colby，S. R.「Calculating Synergistic and Antagonistic Responses of Herbicide Combinations」， Weeds, ( 1967) , 15, 20-22)： 151284.doc • 272· 201117722AMISTAR, ENDURA, BRAVO, KOCIDE, CURZATE, SCORE, ACROBAT, OPUS, CORBEL, OMEGA, MAXIM, PHALTAN, ROVRAL, MELODY, MANZATE, RIDOMIL GOLD, nova, acanto, talius, proline, HEADLINE, DOMARK and BEAM Sold. The unformulated material was first dissolved in acetone and then suspended in (in ppm) acetone and purified water to the target concentration (50/50 volume mixture) containing 250 ppm of the surfactant Trem® 014 (polyol ester). The formulated material is dispersed in insufficient water to produce the target concentration, and neither the organic solvent nor the surfactant is added to the suspension. The resulting detection mixture is then used to detect K, L, and M. A 200 ppm test suspension was sprayed onto the plants until the level of overflow, which corresponds to a rate of 800 g/ha. The experiment was repeated three times and the results obtained were averaged three times. The synergy between the two active ingredients is established by the Colby equation (see Colby, SR "Calculating Synergistic and Antagonistic Responses of Herbicide Combinations", Weeds, (1967), 15, 20-22): 151284.doc • 272· 201117722

AxB 100 p = A + B _ 利用Colby之方法，兩種活性成分間之協同交互影 響關係之建立方式首先係基於兩種成分單獨使用之活 性計算混合物之預測活性p。若p低於實驗確定效果， 則兩者間具有協同作用。上述計算中，A為殺真菌活性 百分比相對於一成分單獨使用比率X。B為殺真菌活性 百分比相對於第二成分使用率y。計算預估值p，A於X 比率且B於y比率混合物之預期殺真菌活性，其效果直 接相加且無交互作用。 試驗 K (即試驗 ΚΙ、K2、K4、K5、K6、K7、K8) 將測試懸浮液喷灑於小麥苗至溢流為止。接下來的 第二日該幼苗經接種小麥白粉病之孢子粉劑。（亦稱 Erisyphe graminis f. sp. tritici,小麥白粉菌的致病菌）， 然後培養於20°C生長箱7天，在此時間後，進行外觀 疾病評級。 試驗 L (即試驗 U、L2、L3、L4、L6、L7) 將測試懸浮液喷灑於小麥苗至溢流為止。接下來的 第二日該幼苗經接種麥類葉銹病菌之孢子粉劑。（小麥 葉銹病的致病菌）以及培養於20°C飽和大氣壓下24小 151284.doc •273 - 201117722 時’然後移到2〇t生長箱放置6天，在此時間後，進 行外觀疾病評級。 試驗 M (即試驗 Ml、M2、M3、M4、M5、M7) 將測試懸浮液噴灑於小麥苗至溢流為止。接下來的 第二日該幼苗經接種小麥葉斑病菌之孢子粉劑。（小麥 葉枯病的致病菌）以及培養於24〇C飽和大氣壓下48小 時。然後該幼苗移到2(TC生長箱放置19天，在此時間 後，進行外觀疾病評級。 檢測K-M的結果經呈現於接下來的表b到卜ι〇0 的評分表示1〇〇%疾病防治以及G的評絲示無疾病防 it目對於控制組）。破折號（~)代表無測試結果。欄 位;^為f測值⑺bsd)」者表示三次實驗結果平均 值。標示「期望值（Εχρ)」的攔位表示對於每個利用 Colby方知式計算的使用混合物之期望效果。AxB 100 p = A + B _ Using the Colby method, the synergistic interaction relationship between the two active ingredients is first established based on the activity of the two components alone to calculate the predicted activity p of the mixture. If p is lower than the experimentally determined effect, there is a synergy between the two. In the above calculation, A is the percentage of fungicidal activity used alone relative to a component. B is the percentage of fungicidal activity relative to the second component usage y. The predicted fungal activity of the predicted values p, A at the X ratio and B at the y ratio mixture was calculated, the effects of which were directly additive and had no interaction. Test K (ie test ΚΙ, K2, K4, K5, K6, K7, K8) The test suspension was sprayed onto the wheat seedlings until overflow. On the second day following, the seedlings were inoculated with spore powder of wheat powdery mildew. (also known as Erisyphe graminis f. sp. tritici, the pathogen of wheat powdery mildew), and then cultured in a growth chamber at 20 ° C for 7 days, after which time the appearance disease rating was performed. Test L (ie test U, L2, L3, L4, L6, L7) The test suspension was sprayed onto the wheat seedlings until overflow. On the second day, the seedlings were inoculated with spore powder of wheat leaf rust. (pathogenic bacteria of wheat leaf rust) and cultured at 20 ° C saturated atmospheric pressure 24 small 151284.doc • 273 - 201117722 'then moved to 2 〇 t growth box for 6 days, after which time, the appearance of disease rating . Test M (ie test Ml, M2, M3, M4, M5, M7) The test suspension was sprayed onto the wheat seedlings until overflow. On the second day following, the seedlings were inoculated with spore powder of wheat leaf spot pathogen. (pathogenic bacteria of wheat leaf blight) and cultured at 24 ° C for 24 hours under saturated atmospheric pressure. The seedlings were then moved to 2 (the TC growth chamber was placed for 19 days, after which time the appearance disease rating was performed. The results of the detection of KM are presented in the next table b to the rating of ι〇0 indicating 1% disease prevention And G's evaluation shows that there is no disease prevention for the control group). A dash (~) indicates no test results. The field; ^ is the f measurement (7) bsd)" means the average of the three experimental results. The block indicating the "expected value (Εχρ)" indicates the desired effect for each use mixture calculated using the Colby formula.

表B 化合物181單獨或與撲殺熱、鋅欽乃浦、依普同、白克列、 氫氧化銅L讀異笨腈混合對於㈣持自粉菌、葉 --竺葉1古病的▼測值及期望值。Table B Compound 181 alone or in combination with chlorpyrifos, zinc chinepazine, yuppe, leucoside, copper hydroxide L read isoform nitrile for (four) from the fungus, leaf - eucalyptus 1 paleopathic Value and expected value.

化合物181 之施用率 (ppm) 0 組分（b) 組分（b) 之施用 率（ppm) 0 檢測 實測~ 值 0 K1 「 —--- 檢淠 L1 檢谀 Ml 期望 值— 實測 一值 〇 期望 值 實測 值 π 期望 值 0.01 無 0 0 0 U 0 0.1 i 10 無 0 21 18 22 無 0 91 82 94 無 0 100 100 QR 151284.doc -274- 201117722 化合物181 組分（b ) 檢測K1 檢淠 L1 檢測Ml 之施用率 之施用 實測 期望 實測 期望 實測 期望 (ppm) 組分（b ) 率（ppm) 值 值 值 值 值 值 0 撲殺熱 10 0 0 0 0 撲殺熱 40 0 27 0 0 撲殺熱 200 76 41 10 0.1 撲殺熱 10 0 21 9 18 0 22 0.1 撲殺熱 40 21 21 18 41 0 22 0.1 撲殺熱 200 21 81 69 52 20 30 1 撲殺熱 10 91 91 74 82 96 94 1 撲殺熱 40 98 91 88 87 94 94 1 撲殺熱 200 97 98 95 90 96 95 0 鋅錳乃浦 10 0 55 0 0 鋅錳乃浦 40 0 96 0 0 鋅錳乃浦 200 0 99 84 0.1 鋅錳乃浦 !0 0 21 68 63 0 22 0.1 鋅錳乃浦 40 0 21 96 97 61 22 0.1 鋅錳乃浦 200 21 21 99 99 77 88 1 鋅錳乃浦 10 50 91 91 92 80 94 1 鋅錳乃浦 40 71 91 98 99 83 94 1 鋅錳乃浦 200 96 91 100 100 96 99 0 依普同 10 0 0 0 0 依普同 40 0 0 0 0 依普同 200 0 18 8 0.1 依普同 10 0 21 0 18 0 22 0.1 依普同 40 0 21 9 18 0 22 0.1 依普同 200 0 21 27 33 0 28 1 依普同 10 64 91 68 82 77 94 1 依普同 40 76 91 74 82 90 94 1 依普同 200 96 91 85 86 91 95 0 白克列 10 0 9 70 0 白克列 40 0 91 90 0 白克列 200 74 100 97 -275 - 15I284.doc 201117722 化合物181 之施用率 (ppm) 組分（b ) 組分（b) 之施用 率（ppm) 檢測K1 檢測L1 檢淠 Ml 實測 值 期望 值 實測 值 期望 值 實測 值 期望 值 0.1 白克列 10 64 21 55 26 66 77 0.1 白克列 40 0 21 97 93 99 92 0.1 白克列 200 0 79 99 100 99 97 1 白克列 10 97 91 80 84 97 98 1 白克列 40 91 91 99 98 100 99 1 白克列 200 98 98 99 100 99 100 0 氫氧化銅 10 0 — 0 0 氫氧化銅 40 0 一 0 0 氫氧化銅 200 0 0 82 0.1 氫氧化銅 10 0 21 一 0 22 0.1 氫氧化銅 40 0 21 0 0 22 0.1 氫氧化銅 200 0 21 0 18 77 86 1 氮氧化銅 10 71 91 27 88 94 1 氛氧化銅 40 0 91 41 87 94 1 氫氧化銅 200 0 91 55 82 98 99 0 克絕 10 0 0 0 0 克絕 40 0 0 0 0 克絕 200 0 9 0 0.1 克絕 10 0 21 0 18 0 22 0.1 克絕 40 0 21 0 18 0 22 0.1 克絕 200 0 21 0 26 0 22 1 克絕 10 95 91 55 82 65 94 1 克絕 40 81 91 68 82 70 94 1 克絕 200 84 91 80 84 78 94 0 克羅赛尼 (chlorothalanil) 10 0 27 0 0 克羅赛尼 (chlorothalanil) 40 0 74 68 0 克羅赛尼 (chlorothalanil) 200 0 98 96 •276- 151284.doc 201117722 化合物181 組分（b) 檢須· K1 檢淠 L1 檢測 Ml 之施用率 之施用 實測 期望 實測 期望 實測 期望 (ppm) 組分（b) 率（ppm) 值 值 值 值 值 值 克羅赛尼 , -赏 - 0.1 (chlorothalanil) 10 0 21 27 41 0 22 克羅賽尼 0.1 (chlorothalanil) 40 0 21 74 79 55 75 克羅赛尼 0.1 (chlorothalanil) 200 72 21 93 98 99 97 克羅赛尼 1 (chlorothalanil) 10 76 91 27 87 70 94 克羅赛尼 1 (chlorothalanil) 40 96 91 74 95 81 98 克羅賽尼 — __!__ (chlorothalanil) — 91 97 100 100 100 表cApplication rate of compound 181 (ppm) 0 Component (b) Application rate of component (b) (ppm) 0 Test measured ~ Value 0 K1 "---- Check L1 Check 谀 Ml Expected value - Measured value 〇 Expected value Measured value π Expected value 0.01 No 0 0 0 U 0 0.1 i 10 No 0 21 18 22 No 0 91 82 94 No 0 100 100 QR 151284.doc -274- 201117722 Compound 181 Component (b) Detection K1 Inspection L1 Detection Ml The application rate of the application rate is expected to be measured. The expected actual measurement expectation (ppm) The component (b) rate (ppm) Value value value value value 0 culling heat 10 0 0 0 0 culling heat 40 0 27 0 0 culling heat 200 76 41 10 0.1 杀杀热10 0 21 9 18 0 22 0.1 culling heat 40 21 21 18 41 0 22 0.1 culling heat 200 21 81 69 52 20 30 1 culling heat 10 91 91 74 82 96 94 1 culling heat 40 98 91 88 87 94 94 1 杀杀热200 97 98 95 90 96 95 0 Zinc Manganese 10 0 55 0 0 Zinc Manganese 40 0 96 0 0 Zinc Manganus 200 0 99 84 0.1 Zinc Manganese! 0 0 21 68 63 0 22 0.1 Zinc Manganese 40 0 21 96 97 61 22 0.1 Zinc Manganese 200 21 21 99 99 77 88 1 Zinc Naipu 10 50 91 91 92 80 94 1 Zinc Manganese 40 71 91 98 99 83 94 1 Zinc Manganese 200 96 91 100 100 96 99 0 Yi Putong 10 0 0 0 0 Yi Putong 40 0 0 0 0 Yiputong 200 0 18 8 0.1 Yiputong 10 0 21 0 18 0 22 0.1 Yiputong 40 0 21 9 18 0 22 0.1 Yiputong 200 0 21 27 33 0 28 1 Yipu Tong 10 64 91 68 82 77 94 1 依普同40 76 91 74 82 90 94 1 依普同200 96 91 85 86 91 95 0 白克列10 0 9 70 0 白克列40 0 91 90 0 白克列200 74 100 97 -275 - 15I284.doc 201117722 Application rate of compound 181 (ppm) Component (b) Application rate of component (b) (ppm) Detection K1 Detection L1 Inspection 淠 Ml Measured value Expected value Measured value Expected value Measured value Expected value 0.1 White column 10 64 21 55 26 66 77 0.1 White Column 40 0 21 97 93 99 92 0.1 White Column 200 0 79 99 100 99 97 1 White Column 10 97 91 80 84 97 98 1 White Column 40 91 91 99 98 100 99 1白克列200 98 98 99 100 99 100 0 Copper hydroxide 10 0 — 0 0 Copper hydroxide 40 0 — 0 0 Copper hydroxide 200 0 0 82 0.1 Copper hydroxide 10 0 21 A 0 22 0.1 copper hydroxide 40 0 21 0 0 22 0.1 copper hydroxide 200 0 21 0 18 77 86 1 copper oxynitride 10 71 91 27 88 94 1 copper oxide 40 0 91 41 87 94 1 copper hydroxide 200 0 91 55 82 98 99 0 克绝10 0 0 0 0 克绝40 0 0 0 0 克绝200 0 9 0 0.1 克绝10 0 21 0 18 0 22 0.1 克绝40 0 21 0 18 0 22 0.1 克绝200 0 21 0 26 0 22 1 克绝10 95 91 55 82 65 94 1 克绝40 81 91 68 82 70 94 1 克绝200 84 91 80 84 78 94 0 克罗特尼 (chlorothalanil) 10 0 27 0 0 克Chlorothalanil 40 0 74 68 0 chlorothalanil 200 0 98 96 •276- 151284.doc 201117722 Compound 181 Component (b) Detector · K1 淠 L1 Detecting the application rate of M1 Measured expected expected measured expected expected (ppm) component (b) rate (ppm) value value value value value Crosini, - reward - 0.1 (chlorothalanil) 10 0 21 27 41 0 22 Crosini 0.1 (chlorothalanil 40 0 21 74 79 55 75 Crothoni 0.1 (chlorothalanil) 200 72 21 93 98 99 97 Croseni 1 (chlorothalanil) 10 76 91 27 87 70 94 Crothani 1 (chlorothalanil) 40 96 91 74 95 81 98 Croseni — __!__ (chlorothalanil) — 91 97 100 100 100 Table c

I51284.doc •277· 201117722 化合物181 組分（b )之 試驗K2 試驗L2 試驗M2 之施用率 施用率 實測 期望 實測 期望 實測 期望 (ppm) 組分（b ) (ppm) 值 值 值 值 值 值- 0.1 三赛唑 200 0 89 27 46 0 67 1 三赛唑 10 95 98 27 95 84 99 1 三赛唑 40 98 99 68 95 95 99 1 三赛唑 200 99 99 74 95 71 99 0 扶吉胺 10 0 27 0 0 扶吉胺 40 96 68 87 0 扶吉胺 200 100 88 99 0.1 扶吉胺 10 0 76 27 57 74 67 0.1 扶吉胺 40 65 99 68 81 89 96 0.1 扶吉胺 200 96 100 88 93 100 100 1 扶吉胺 10 92 98 54 96 99 99 1 扶吉胺 40 99 100 80 98 97 100 1 扶吉胺 200 99 100 88 99 100 100 0 達滅芬 10 0 0 0 0 達滅芬 40 0 0 0 0 達滅芬 200 0 0 0 0.1 達滅芬 10 0 76 0 41 0 67 0.1 達滅芬 40 42 76 0 41 0 67 0.1 »jb- »Λ&gt; 違滅分 200 0 76 9 41 32 67 1 達滅芬 10 84 98 54 95 95 99 1 達滅芬 40 95 98 91 95 94 99 1 達滅芬 200 95 98 88 95 94 99 0 異丙菌胺 10 0 0 0 0 異丙菌胺 40 0 0 0 0 異丙菌胺 200 0 0 0 0.1 異丙菌胺 10 0 76 0 41 0 67 0.1 異丙菌胺 40 0 76 9 41 38 67 0.1 異丙菌胺 200 0 76 9 41 27 67 1 異丙菌胺 10 93 98 41 95 93 99 1 異丙菌胺 40 96 98 27 95 94 99 -278- 151284.doc 201117722 化合物181 組分（b )之 試驗K2 試驗L2 試驗M2 之施用率 施用率 實測 期望 實測 期望 實測 期望 (ppm) 組分（b) (ppm) 值 值 值 值 值 值 1 異丙菌胺 200 98 98 74 95 95 99 0 咯菌酯 10 84 0 — 0 咯菌酯 40 63 0 — 0 咯菌酯 200 34 54 — 0.1 咯菌酯 10 13 96 0 41 — 0.1 咯菌酯 40 68 91 27 41 — 0.1 咯菌酯 200 81 84 54 73 — 1 咯菌酯 10 94 100 68 95 — 1 咯菌酯 40 100 99 95 95 — 1 咯菌酯 200 98 99 98 98 — 0 右滅達樂 10 0 0 0 0 右滅達樂 40 0 0 0 0 右滅達樂 200 64 0 0 0.1 右滅達樂 10 0 76 0 41 38 67 0.1 右滅達樂 40 0 76 0 41 0 67 0.1 右滅達樂 200 0 91 0 41 32 67 1 右滅達樂 10 89 98 18 95 77 99 1 右滅達樂 40 95 98 41 95 90 99 1 右滅達樂 200 98 99 80 95 86 99 0 福爾培 10 0 0 0 0 福爾培 40 0 9 83 0 福爾培 200 0 54 98 0.1 福爾培 10 0 76 27 41 21 67 0.1 福爾培 40 0 76 47 46 90 94 0.1 福爾培 200 48 76 85 73 95 99 1 福爾培 10 95 98 68 95 90 99 1 福爾培 40 96 98 74 95 99 100 1 福爾培 200 98 98 88 98 98 100 0 邁克尼 10 — — 0 0 邁克尼 40 — — 25 • 279- 151284.doc 201117722 組分（b) 邁克尼 邁克尼 邁克尼 邁克尼 邁克尼 邁克尼 邁克尼I51284.doc •277· 201117722 Compound 181 Component (b) Test K2 Test L2 Test M2 Application rate Application rate Actual measurement Expected actual measurement Expected measured expected (ppm) Component (b) (ppm) Value value value value value - 0.1 Trioxazole 200 0 89 27 46 0 67 1 Trioxazole 10 95 98 27 95 84 99 1 Trioxazole 40 98 99 68 95 95 99 1 Trioxazole 200 99 99 74 95 71 99 0 Cougiamine 10 0 27 0 0 助吉胺40 96 68 87 0 助吉胺200 100 88 99 0.1 焦吉胺10 0 76 27 57 74 67 0.1 助吉胺40 65 99 68 81 89 96 0.1 焦吉胺200 96 100 88 93 100 100 1 gibberellin 10 92 98 54 96 99 99 1 gibberellin 40 99 100 80 98 97 100 1 chlordiachlor 200 99 100 88 99 100 100 0 damfinten 10 0 0 0 0 da fenfen 40 0 0 0 0 Dafenfen 200 0 0 0 0.1 Dafenfen 10 0 76 0 41 0 67 0.1 Dafenfen 40 42 76 0 41 0 67 0.1 »jb- »Λ&gt; Violation 200 0 76 9 41 32 67 1 Fen 10 84 98 54 95 95 99 1 Dafenfen 40 95 98 91 95 94 99 1 Dafenfen 200 95 98 88 95 94 99 0 Isoprofen 10 0 0 0 0 Isoprofen 40 0 0 0 0 Isoprofen 200 0 0 0 0.1 Isoprofen 10 0 76 0 41 0 67 0.1 Isoprofen 40 0 76 9 41 38 67 0.1 Isoprofen 200 0 76 9 41 27 67 1 Isoprofen 10 93 98 41 95 93 99 1 Isoprofen 40 96 98 27 95 94 99 -278- 151284.doc 201117722 Compound 181 Test of component (b) K2 test L2 test rate of M2 application rate measured actual expected expected actual expected (ppm) Component (b) (ppm) Value Value Value Value 1 Isoprofen 200 98 98 74 95 95 99 0 Coxample 10 84 0 — 0 Froxyl ester 40 63 0 — 0 Pyruvate 200 34 54 — 0.1 Froxyl ester 10 13 96 0 41 — 0.1 Froxyl ester 40 68 91 27 41 — 0.1 Froxyl ester 200 81 84 54 73 — 1 Froxil ester 10 94 100 68 95 — 1 Froxil 40 100 99 95 95 — 1 serotonin 200 98 99 98 98 — 0 右灭乐乐 10 0 0 0 0 右灭达乐40 0 0 0 0 右灭达乐200 64 0 0 0.1 右灭达乐10 0 76 0 41 38 67 0.1 右灭乐乐 40 0 76 0 41 0 67 0.1 右灭乐乐200 0 91 0 41 32 67 1 右灭达 10 89 98 18 95 77 99 1 右灭达 40 19 9 8 41 95 90 99 1 右灭达200 98 99 80 95 86 99 0 Forpe 10 0 0 0 0 Forepe 40 0 9 83 0 Forte 200 0 54 98 0.1 Foreppe 10 0 76 27 41 21 67 0.1 Forte's 40 0 76 47 46 90 94 0.1 Forte 200 48 76 85 73 95 99 1 Forte 10 95 98 68 95 90 99 1 Forte 40 96 98 74 95 99 100 1 Forte 200 98 98 88 98 98 100 0 麦尼尼 10 — — 0 0 麦尼尼40 — — 25 • 279- 151284.doc 201117722 Component (b) Mikeny McKinney Mikeny Mikeny Mikeny Mikeny McKinney

化合物181 之施用率 (ppm) 0 0.1 0.1 0.1 化合物181早獨或是與快嗓兄士 .'、厌：分、百克敏、亞托敏、啶氧菌g丨 四 孢菌素、芬普福或丙氧啥琳的混合物對於防治 I笹姓.rfTH让t丨丄..丄 . 化合物181 之施用率 (ppm) 組分（b) 組分（b) 之施用率 (ppm) 試驗L3 試驗M3 實測值 期望值 實測值 期望信 0 無 0 0 〇 0.01 無 0 0 〇 0.1 無 0 9 〇 1 無 0 68 74 —. 10 Ml 0 98 98 0 快諾芬 10 41 〇 0 快諾芬 40 18 〇 0 快諾芬 200 18 0 0.1 快諾芬 10 9 46 58 〇 0.1 快諸芬 40 9 26 38 〇 0.1 快諾芬 200 18 26 〇 〇 1 快諾芬 10 55 81 45 74 1 快諾芬 40 55 74 88 74 1 快諾芬 200 74 74 82 74 151284.doc •280· 201117722 化合物181 之施用率 (ppm) 組分（b) 組分（b) 之施用率 (PPm) 試驗L3 試驗M3 實測值 期望值 實測值 期望值 0 百克敏 10 — 0 0 百克敏 40 — 42 0 百克敏 200 — 92 0.1 百克敏 10 — 0 0 0.1 百克敏 40 — 0 42 0.1 百克敏 200 — 84 92 1 百克敏 10 — 65 74 1 百克敏 40 — 88 85 1 百克敏 200 — 95 98 0 亞托敏 10 - 0 0 亞托敏 40 — 0 0 亞托敏 200 — 27 0.1 亞托敏 10 - 0 0 0.1 亞托敏 40 — 12 0 0.1 亞托敏 200 — 79 27 1 亞托敏 10 — 91 74 1 亞托敏 40 — 92 74 1 亞托敏 200 — 92 81 0 啶氧菌酯 10 — 0 0 啶氧菌酯 40 — 0 0 啶氧菌酯 200 — 0 0.1 咬氧菌酯 10 — 0 0 0.1 啶氧菌酯 40 — 0 0 0.1 咬氧菌酯 200 — 17 0 1 啶氧菌酯 10 — 70 74 1 啶氧菌酯 40 — 93 74 1 啶氧菌酯 200 一 91 74 0 四克利 10 — 0 0 四克利 40 — 0 0 四克利 200 — 94 151284.doc -281 · 201117722 化合物181 之施用率 (ppm) 組分（b) 組分（b ) 之施用率 (ppm) 試驗L3 試驗M3 實測值 期望值 實測值 期望值 0.1 四克利 10 — 30 0 0.1 四克利 40 — 63 0 0.1 四克利 200 — 98 94 1 四克利 10 — 89 74 1 四克利 40 — 97 74 1 四克利 200 — 99 99 0 螺旋胺 10 - 0 0 螺旋胺 40 — 0 0 螺旋胺 200 - 0 0.1 螺旋胺 10 — 20 0 0.1 螺旋胺 40 — 17 0 0.1 螺旋胺 200 — 37 0 1 螺旋胺 10 — 92 74 1 螺旋胺 40 — 94 74 1 螺旋胺 200 — 95 74 0 芬普福 10 0 0 0 芬普福 40 0 0 0 芬普福 200 87 0 0.1 芬普福 10 0 9 30 0 0.1 芬普福 40 1 0 9 0 0 0.1 芬普福 200 41 88 17 0 1 芬普福 10 41 68 94 74 1 芬普福 40 68 68 93 74 1 芬普福 200 80 96 94 74 0 丙氧喹啉 10 0 0 0 丙氧啥啭 40 0 0 0 丙氧喹咐 200 1 0 13 0.1 丙氧喹啦 10 0 9 0 0 0.1 丙氧喹咐 40 9 9 0 0 0.1 丙氧啥啦 200 9 9 20 13 151284.doc •282- 201117722 化合物181 組分（b) 1 試驗L3 試驗M3 之施用率 (ppm) 組分（b)_ 之施用率1 _(ppm) 實測值 期望值 實測值 期望值 1 丙氧01淋 27 68 28 74 1 丙氧0f# 40 1 68 68 0 74 1 丙氧01淋 200 68 68 85 78Application rate of compound 181 (ppm) 0 0.1 0.1 0.1 Compound 181 as early as or with 嗓 嗓 .. ', 厌: points, 100 grams of sensitization, atorenosin, oxysporin g sporin, Fenfen Or a mixture of propoxygenin for controlling I. surname.rfTH let t丨丄..丄. application rate of compound 181 (ppm) component (b) application rate of component (b) (ppm) test L3 test M3 Measured value expected value measured value expectation letter 0 no 0 0 〇0.01 no 0 0 〇0.1 no 0 9 〇1 no 0 68 74 —. 10 Ml 0 98 98 0 快诺芬 10 41 〇0 快诺芬40 18 〇0 快诺芬200 18 0 0.1 Vaughan 10 9 46 58 〇 0.1 Quicken 40 19 26 38 〇 0.1 Vaughan 200 18 26 〇〇 1 Vaughan 10 55 81 45 74 1 Vaughan 40 55 74 88 74 1 Vaughan 200 74 74 82 74 151284.doc •280· 201117722 Application rate of compound 181 (ppm) Component (b) Application rate of component (b) (PPm) Test L3 Test M3 Actual value expected value Actual value expected 0 克克敏10 — 0 0 Kemin 40 — 42 0 Bai Kemin 200 — 92 0.1 Bai Kemin 10 — 0 0 0.1 Bai Kemin 40 — 0 42 0.1 百克敏200 — 84 92 1 克克敏10 — 65 74 1 百克敏40 — 88 85 1 百克敏200 — 95 98 0 Atomic 10 - 0 0 Atomin 40 — 0 0 Atomin 200 — 27 0.1 Atomin 10 - 0 0 0.1 Atomin 40 — 12 0 0.1 Atomin 200 — 79 27 1 Atomin 10 — 91 74 1 Atomin 40 — 92 74 1 Atomin 200 — 92 81 0 oxypoxystrobin 10 - 0 0 oxypoxystrobin 40 - 0 0 oxypoxylate 200 - 0 0.1 oxycides 10 - 0 0 0.1 oxypoxystrobin 40 - 0 0 0.1 oxygerpene 200 - 17 0 1 picoxystrobin 10 — 70 74 1 picoxystrobin 40 — 93 74 1 picoxystrobin 200 a 91 74 0 four klitres 10 — 0 0 four klitres 40 — 0 0 four knicks 200 — 94 151284.doc - 281 · 201117722 Application rate of compound 181 (ppm) Component (b) Application rate of component (b) (ppm) Test L3 Test M3 Measured value Expected value Actual value expected 0.1 Minkley 10 — 30 0 0.1 Sikhli 40 — 63 0 0.1 Four Klee 200 — 98 94 1 Four Klee 10 — 89 74 1 Four Klee 40 — 97 74 1 Sikhli 200 — 99 99 0 Heliconia 10 - 0 0 Heliconia 40 — 0 0 Helixamine 200 - 0 0.1 Helixamine 10 — 20 0 0.1 Heliconia 40 — 17 0 0.1 Heliconia 200 — 37 0 1 Spiramine 10 — 92 74 1 Heliconia 40 — 94 74 1 Heliconia 200 — 95 74 0 Fenford 10 0 0 Fenford 40 0 0 Fofford 200 87 0 0.1 Fenfou 10 0 9 30 0 0.1 Fenpu福40 1 0 9 0 0 0.1 Fenford 200 41 88 17 0 1 Fenfen 10 41 68 94 74 1 Fenford 40 68 68 93 74 1 Fenford 200 80 96 94 74 0 Propoxyquinoline 10 0 0 0 propoxyfluoride 40 0 0 0 propoxyquinoxaline 200 1 0 13 0.1 propoxyquine 10 0 9 0 0 0.1 propoxyquinoxaline 40 9 9 0 0 0.1 propoxydol 200 9 9 20 13 151284. Doc •282- 201117722 Compound 181 Component (b) 1 Test L3 Test M3 application rate (ppm) Component (b) _ application rate 1 _ (ppm) measured value expected value measured value expected value 1 propoxy 01 shower 27 68 28 74 1 Propoxy 0f# 40 1 68 68 0 74 1 Propoxy 01 dripping 200 68 68 85 78

表ETable E

I51284.doc 化合物181單獨或是與環克座、依普座、丙硫菌唾、待克利、 邁克尼或斯必羅胺（Spiroamine)的混合物對於防治小麥白 粉产、葉錢病以及p枯病的實測果 -283 - 201117722 化合物181 (b)之 試驗K4 試驗L4 試驗M4 之施用率 施用率 實測 期望 實測 期望 實測 期望 (ppm) 組分（b) (ppm) 值 值 值 值 值 值 0 依普座 2 — — 0 0 依普座 10 — — 86 0 依普座 40 — — 97 0.1 依普座 0.4 — — 0 47 0.1 依普座 2 — — 17 47 0.1 依普座 10 — — 91 93 0.1 依普座 40 — — 98 99 1 依普座 0.4 — — 95 93 1 依普座 2 — — 96 93 1 依普座 10 — — 99 99 1 依普座 40 — — 99 100 0 丙硫菌°坐 0.4 — — 0 0 丙硫菌嗤 2 — — 0 0 丙硫菌°坐 10 一 — 58 0 丙硫菌β坐 40 — — 98 0.1 丙硫菌吐 0.4 — — 0 47 0.1 丙硫菌。坐 2 — — 64 47 0.1 丙硫菌-坐 10 — — 71 78 0.1 丙硫菌α坐 40 — — 96 99 1 丙硫菌。坐 0.4 — — 89 93 1 丙硫菌β坐 2 — — 94 93 1 丙硫菌。坐 10 — — 95 97 1 丙硫菌-坐 40 — — 99 100 0 待克利 0.4 — — 0 0 待克利 2 — — 25 0 待克利 10 — — 75 0 待克利 40 — — 96 0.1 待克利 0.4 — — 0 47 0.1 待克利 2 — — 47 60 0.1 待克利 10 — — 82 87 151284.doc -284- 201117722 化合物181 (b)之 試驗K4 試驗L4 試驗M4 之施用率 施用率 實測 期望 實測 期望 實測 期望 (ppm) 組分（b) (ppm) 值 值 值 值 值 值 0.1 待克利 40 — — 99 98 1 ·' 待克利 0.4 — — 93 93 1 待克利 2 — — 96 95 1 待克利 10 — — 96 98 1 待克利 40 — — 99 100 0 邁克尼 0.4 21 0 — 0 邁克尼 2 81 0 — 0 邁克尼 10 98 60 — 0 邁克尼 40 100 100 — 0.1 邁克尼 0.4 42 21 9 9 — 0.1 邁克尼 2 84 81 9 9 — 0.1 邁克尼 10 99 98 92 64 — 0.1 邁克尼 40 100 100 100 100 — 1 邁克尼 0.4 98 99 55 80 — 1 邁克尼 2 99 100 55 80 — 1 邁克尼 10 100 100 98 92 — 1 邁克尼 40 100 100 100 100 — 0 螺旋胺 0.4 — 9 — 0 螺旋胺 2 — 0 — 0 螺旋胺 10 — 0 — 0 螺旋胺 40 — 0 — 0.1 螺旋胺 0.4 — 0 17 — 0.1 螺旋胺 2 — 0 9 — 0.1 螺旋胺 10 — 0 9 — 0.1 螺旋胺 40 — 9 9 — 1 螺旋胺 0.4 — 68 82 — 1 螺旋胺 2 — 68 80 — 1 螺旋胺 10 — 74 80 — 1 螺旋胺 40 — 80 80 — 151284.doc -285 - 201117722 表F 化合，⑻單獨或是與百殺芬、ntb賴胺、異派來桑、，嘻菌 醋、分普褐、待克利、亞托敏或葚抱菌素的混合物對於防治 -的實測及期望效果 組公广ν*、1 mrm * 化合物181 之施用率 (ppm) 組分（b) 組分（b) 之施用率 (ppm)I51284.doc Compound 181 alone or in combination with cyclosporine, Epto, thiophene saliva, sylvain, mcgne or spiroamine for the control of wheat white flour, leaf blight and p-blight Measured fruit -283 - 201117722 Compound 181 (b) Test K4 Test L4 Test M4 Application rate Application rate Actual measurement Expected actual measurement Expected measured expected (ppm) Component (b) (ppm) Value value Value value 0 依普Block 2 — — 0 0 Ip Block 10 — — 86 0 Ip Block 40 — — 97 0.1 Ip Block 0.4 — — 0 47 0.1 Ip Block 2 — — 17 47 0.1 Ip Block 10 — — 91 93 0.1普座40 — — 98 99 1 Ip seat 0.4 — 95 93 1 Ip seat 2 — — 96 93 1 Ip seat 10 — — 99 99 1 Ip seat 40 — — 99 100 0 Propionate ° ° 0.4 — — 0 0 Propionibacterium 嗤 2 — — 0 0 Propionisulfone ° sitting 10 — 58 0 Propionibacterium β sitting 40 — — 98 0.1 Propionisulfone spit 0.4 — — 0 47 0.1 Propionibacterium. Sit 2 – 64 47 0.1 Propionibacterium - Sit 10 – 71 78 0.1 Propionibacterium a sitting 40 – 96 99 1 Prothiotoxin. Sit 0.4 – 89 93 1 Prothiotoxin β sitting 2 – 94 93 1 Prothiotoxin. Sit 10 – 95 97 1 Propionibacterium - sit 40 – 99 100 0 Wait Klee 0.4 – 0 0 Wait Klee 2 – 25 0 Wait Klee 10 – 75 0 Wait Klee 40 – 96 0.1 to Klee 0.4 — — 0 47 0.1 待克利 2 — — 47 60 0.1 待克利 10 — — 82 87 151284.doc -284- 201117722 Compound 181 (b) Test K4 Test L4 Test M4 Application rate Application rate Actual measurement Expected actual expected expected measurement ( Ppm) Component (b) (ppm) Value Value Value Value 0.1 Waiting for Kelly 40 – 99 98 1 · 'Kelly 0.4 — 93 93 1 Waiting for Klee 2 — 96 95 1 Waiting for Kerry 10 — — 96 98 1 Waiting for Kelly 40 – 99 100 0 Mikeny 0.4 21 0 — 0 Mikeny 2 81 0 — 0 Mikeny 10 98 60 — 0 Mikeny 40 100 100 — 0.1 McNea 0.4 42 21 9 9 — 0.1 Mikeny 2 84 81 9 9 — 0.1 McAfee 10 99 98 92 64 — 0.1 McAfee 40 100 100 100 100 — 1 McAfee 0.4 98 99 55 80 — 1 McAfee 2 99 100 55 80 — 1 McAfee 10 100 100 98 92 — 1Kenny 40 100 100 100 100 — 0 Spiramide 0.4 — 9 — 0 Helixamine 2 — 0 — 0 Helixamine 10 — 0 — 0 Helixamine 40 — 0 — 0.1 Helixamine 0.4 — 0 17 — 0.1 Helixamine 2 — 0 9 — 0.1 Heliconia 10 — 0 9 — 0.1 Helixamine 40 — 9 9 — 1 Spirylamine 0.4 — 68 82 — 1 Spirylamine 2 — 68 80 — 1 Spirylamine 10 — 74 80 — 1 Spiramide 40 — 80 80 — 151284.doc -285 - 201117722 Table F compound, (8) alone or with chlorfenapyr, ntb lysine, sinensis, sorghum vinegar, sulphate, sylvestre, atornamine or sputum The measured and expected effect of the mixture for the control - the application rate (ppm) of the compound 181, the application rate (ppm) of the component (b)

151284.doc •286- 201117722 化合物181 之施用率 (ppm) 組分（b ) 組分（b ) 之施用率 (ppm) 試驗K5 試驗M5 實測值 期望值 實測值 期望值 1 吡噻菌胺 0.08 95 91 93 93 1 吡噻菌胺 0.4 87 91 92 93 1 吡噻菌胺 2 84 97 97 99 1 吡噻菌胺 10 100 100 96 100 0 異派來桑 0.08 0 0 0 異派來桑 0.4 21 73 0 異派來桑 2 82 93 0 異派來桑 10 99 99 0.1 異派來桑 0.08 0 0 68 82 0.1 異派來桑 0.4 0 21 67 95 0.1 異派來桑 2 95 82 97 99 0.1 異派來桑 10 100 99 99 100 1 異派來桑 0.08 83 91 93 93 1 異派來桑 0.4 91 93 98 98 1 異派來桑 2 98 98 99 100 1 異派來桑 10 100 100 100 100 0 咯菌酯 0.08 — 0 0 咯菌酯 0.4 — 68 0 咯菌酯 2 — 96 0 咯菌酯 10 — 97 0.1 咯菌酯 0.08 — 43 82 0.1 咯菌酯 0.4 — 84 94 0.1 咯菌酯 2 — 93 99 0.1 咯菌酯 10 — 99 99 1 咯菌酯 0.08 — 88 93 1 咯菌酯 0.4 — 96 98 1 咯菌酯 2 — 100 100 1 咯菌酯 10 — 100 100 0 芬普福 0.08 0 一 0 芬普福 0.4 0 — 151284.doc -287- 201117722 化合物181 之施用率 (ppm) 組分（b) 組分（b) 之施用率 (ppm) 試驗K5 試驗M5 實測值 期望值 實測值 期望值 0 芬普福 2 0 — 0 芬普福 10 64 — 0.1 芬普福 0.08 0 0 — 0.1 芬普福 0.4 0 0 — 0.1 芬普福 2 0 0 — 0.1 芬普福 10 63 64 — 1 芬普福 0.08 98 91 — 1 芬普福 0.4 100 91 — 1 芬普福 2 100 91 — 1 芬普福 10 100 97 — 0 待克利 0.08 0 — 0 待克利 0.4 0 — 0 待克利 2 63 — 0 待克利 10 100 — 0.1 待克利 0.08 0 0 — 0.1 待克利 0.4 0 0 — 0.1 待克利 2 65 63 — 0.1 待克利 10 99 100 — 1 待克利 0.08 99 91 — 1 待克利 0.4 98 91 — 1 待克利 2 I 100 97 — 1 待克利 10 1 100 100 — 0 亞托敏 0.08 1 0 — 0 亞托敏 0.4 0 — 0 亞托敏 2 0 — 0 亞托敏 10 50 — 0.1 亞托敏 0.08 0 0 — 0.1 亞托敏 0.4 0 0 — 0.1 亞托敏 2 0 0 一 0.1 亞托敏 10 71 50 — 151284.doc -288 - 201117722 化合物181 之施用率 (ppm) ———1 組分（b) 試驗K5 試驗M5 組分 之施用率 (ppm) 實測值 期望值 實測值 期望值 1 亞托__ 0.08 96 91 — 1 亞托敏 0.4 99 91 - 1 亞托敏 2 98 91 - 1 亞托敏 10 100 96 — 0 螺旋胺 0.08 0 一 0 螺旋胺 0.4 0 一 0 螺旋胺 2 0 - 0 螺旋胺 10 0 - 0.1 螺旋胺 0.08 0 0 — 0.1 螺旋胺 0.4 0 0 一 0.1 螺旋胺 2 0 0 — 0.1 螺旋胺 10 29 0 一 1 螺旋胺 0.08 98 91 - 1 螺旋胺 0.4 93 91 — 1 螺旋胺 2 97 91 — 1 螺旋胺 10 100 91 —151284.doc •286- 201117722 Application rate of compound 181 (ppm) Component (b) Application rate of component (b) (ppm) Test K5 Test M5 Measured value Expected value Actual value 1 Expected value 1 Tipirizil 0.08 95 91 93 93 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0来桑2 82 93 0 异派来桑 10 99 99 0.1 异派来桑 0.08 0 0 68 82 0.1 异派来桑 0.4 0 21 67 95 0.1 异派来桑 2 95 82 97 99 0.1 异派来桑10 100 99 99 100 1 异派来桑 0.08 83 91 93 93 1 异派来桑 0.4 91 93 98 98 1 异派来桑 2 98 98 99 100 1 异派来桑 10 100 100 100 100 0 菌菌酯0.08 — 0 0 oxystrobin 0.4 — 68 0 oxystrobin 2 — 96 0 oxystrobin 10 — 97 0.1 oxystrobin 0.08 — 43 82 0.1 oxystrobin 0.4 — 84 94 0.1 oxystrobin 2 — 93 99 0.1 oxystrobin 10 — 99 99 1 oxystrobin 0.08 — 88 93 1 oxystrobin 0.4 — 96 98 1 oxystrobin 2 — 100 100 1 oxystrobin 10 — 100 100 0 Fenfeef 0.08 0 - 0 Fenford 0.4 0 — 151284.doc -287- 201117722 Application rate of compound 181 (ppm) Component (b) Application rate of component (b) (ppm) Test K5 Test M5 Measured Value Expected Value Expected Value 0 Fenfen 2 0 — 0 Fenfen 10 64 — 0.1 Fenfu 0.08 0 0 — 0.1 Fenfu 0.4 0 0 — 0.1 Fenfu 2 0 0 — 0.1 Fenfu 10 63 64 — 1 Fenfeef 0.08 98 91 — 1 Fenford 0.4 100 91 — 1 Fenfford 2 100 91 — 1 Fenfford 10 100 97 — 0 Waiting for Kerry 0.08 0 — 0 Waiting for Kelly 0.4 0 — 0 Waiting for Klee 2 63 — 0 待克利 10 100 — 0.1 待克利 0.08 0 0 — 0.1 待克利 0.4 0 0 — 0.1 待克利 2 65 63 — 0.1 待克利 10 99 100 — 1 待克利 0.08 99 91 — 1 待克利 0.4 98 91 — 1 Waiting for Klee 2 I 100 97 — 1 Waiting for Klee 10 1 100 100 — 0 Atomin 0.08 1 0 — 0 Atomic 0.4 0 — 0 Atomin 2 0 — 0 Atomin 10 50 — 0.1 Atomin 0.08 0 0 — 0.1 Atomomin 0.4 0 0 — 0.1 Atomomin 2 0 0 0.1 Atomomin 10 71 50 — 151284.doc -288 - 201117722 Application rate of compound 181 (ppm) ———1 Component (b) Test K5 Test M5 component application rate (ppm) measured value expected value measured value expected value 1 Yato __ 0.08 96 91 — 1 Atoximin 0.4 99 91 - 1 Atomiens 2 98 91 - 1 Atoximin 10 100 96 — 0 Spirulina 0.08 0 0 Ospiramide 0.4 0 0 Ospiramide 2 0 - 0 Heliconia 10 0 - 0.1 Helixamine 0.08 0 0 — 0.1 Helixamine 0.4 0 0 A 0.1 Helixamine 2 0 0 — 0.1 Helixamine 10 29 0 A 1 Helixamine 0.08 98 91 - 1 Spiramide 0.4 93 91 — 1 Spiramine 2 97 91 — 1 Spiramine 10 100 91 —

表G 化合物181單獨或是與BAS6〇〇、百殺芬、環克座、依普座、 丙硫菌唑、百克敏、四克利或啶氧菌酯的混合物對於防么Table G Compound 181 alone or in combination with BAS6 oxime, chlorfenapyr, cyclazone, ezine, prothioconazole, baikemin, tetrakis or picoxystrobin

15l284.doc -289- 201117722 化合物181 之施用率 (ppm) 組分（b ) 組分（b) 之施用率 (ppm) 試驗K6 試驗L6 實測值 期望值 實測值 期望值 0 BAS600 0.08 73 — 0 BAS600 0.4 93 — 0 BAS600 2 98 — 0 BAS600 10 100 — 0.1 BAS600 0.08 76 97 — 0.1 BAS600 0.4 76 99 — 0.1 BAS600 2 98 100 — 0.1 BAS600 10 100 100 — 1 BAS600 0.08 98 99 — 1 BAS600 0.4 99 100 — 1 BAS600 2 99 100 — 1 BAS600 10 100 100 — 0 百殺芬 0.08 — 0 0 百殺芬 0.4 | - 76 0 百殺芬 2 — 100 0 百殺芬 10 — 100 0.1 百殺芬 0.08 — 0 0 0.1 百殺芬 0.4 83 76 0.1 百殺芬 2 100 100 0.1 百殺芬 10 100 100 1 百殺芬 0.08 — 91 76 1 百殺芬 0.4 一 93 94 1 百殺芬 2 — 100 100 1 百殺芬 10 — 100 100 0 環克座 0.08 68 71 0 環克座 0.4 97 99 0 環克座 2 99 100 0 環克座 10 100 100 0.1 環克座 0.08 20 96 97 71 0.1 環克座 0.4 98 100 99 99 151284.doc -290· 201117722 化合物181 之施用率 (ppm) 組分（b) 組分（b) 之施用率 (ppm) 試驗K6 試驗L6 實測值 期望值 實測值 期望值 0.1 環克座 2 100 100 100 100 0.1 環克座 10 100 100 100 100 1 環克座 0.08 92 99 100 93 1 環克座 0.4 100 100 100 100 1 環克座 2 100 100 100 100 1 環克座 10 100 100 100 100 0 依普座 0.08 0 10 0 依普座 0.4 97 100 0 依普座 2 100 100 0 依普座 10 100 100 0.1 依普座 0.08 83 89 99 10 0.1 依普座 0.4 99 100 100 100 0.1 依普座 2 100 100 100 100 0.1 依普座 10 100 100 100 100 1 依普座 0.08 100 98 100 79 1 依普座 0.4 100 100 100 100 1 依普座 2 100 100 100 100 1 依普座 10 100 100 100 100 0 丙硫菌α坐 0.08 59 31 0 丙硫菌'•坐 0.4 65 5 0 丙硫菌D坐 2 68 10 0 丙硫菌。坐 10 100 89 0.1 丙硫菌β坐 0.08 59 96 5 31 0.1 丙硫菌α坐 0.4 96 96 10 .5 0.1 丙硫菌嗤 2 98 96 5 10 0.1 丙硫菌α坐 10 100 100 70 89 1 丙硫菌α坐 0.08 100 99 63 84 1 丙硫菌。坐 0.4 100 99 83 78 1 丙硫菌吐 2 100 99 76 79 1 丙硫菌。坐 10 100 100 94 98 151284.doc -291 - 201117722 化合物181 之施用率 (ppm) 組分（b) 組分（b) 之施用率 (ppm) 試驗K6 試驗L6 實測值 期望值 實測值 期望值 0 百克敏 0.08 11 31 0 百克敏 0.4 89 86 0 百克敏 _2_1 97 100 0 百克敏 10 100 100 0.1 百克敏 0.08 65 90 10 31 0.1 百克敏 0.4 39 99 95 86 0.1 百克敏 2 99 100 100 100 0.1 百克敏 10 100 100 100 100 1 百克敏 0.08 98 98 84 84 1 百克敏 0.4 98 100 97 97 1 百克敏 2 100 100 100 100 1 百克敏 10 100 100 100 100 0 四克利 0.08 59 5 0 四克利 0.4 65 0 0 四克利 2 99 70 0 四克利 10 100 100 0.1 四克利 0.08 59 96 0 5 0.1 四克利 0.4 84 96 0 0 0.1 四克利 2 98 100 86 70 0.1 四克利 10 100 100 100 100 1 四克利 0.08 99 99 76 78 1 四克利 0.4 100 99 89 76 1 四克利 2 100 100 100 93 1 四克利 10 100 100 100 100 0 啶氧菌酯 0.08 70 0 0 啶氧菌酯 0.4 95 0 0 啶氧菌酯 2 100 97 0 咬氧菌酯 10 100 100 0.1 啶氧菌酯 0.08 71 97 0 0 0.1 咬氧菌酯 0.4 93 99 10 0 151284.doc -292- 201117722 化合物181 之施用率 (ppm) 組分（b) 組分（b) 之施用率 (ppm) 試驗K6 試驗L6 實測值 期望值 實測值 期望值 0.1 啶氧菌酯 2 100 100 91 97 0.1 咬氧菌酯 10 100 100 100 100 1 咬氧菌酯 0.08 100 99 83 76 1 啶氧菌酯 0.4 100 100 76 76 1 咬氧菌酯 2 100 100 93 99 1 啶氧菌酯 10 100 100 100 100 表Η 化合物181單獨或是與快諾芬、BAS600、吡噻菌胺、異派 來桑、待克利或亞托敏的混合物對於防治小麥白粉菌、葉銹 病及葉枯病的實測及期望效果 化合物181 組分（b) 試驗K7 試驗L7 試驗M7 之施用率 之施用 實測 期望 實測 期望 實測 期望 (ppm) 組分（b) 率（ppm) 值 值 值 值 值 值 0 無 0 71 0 0 0.01 無 0 64 0 0 0.1 無 0 63 37 32 1 無 0 96 94 94 10 無 0 100 100 99 0 快諾芬 0.016 0 — — 0 快諾芬 0.08 21 — — 0 快諾芬 0.4 81 — — 0 快諾芬 2 96 — — 0.1 快諾芬 0.016 56 63 — — 0.1 快諾芬 0.08 21 71 — — 0.1 快諾芬 0.4 64 93 — — 0.1 快諾芬 2 95 99 — — 1 快諾芬 0.016 98 96 — 一 1 快諾芬 0.08 99 97 — — 151284.doc -293 · 201117722 化合物181 組分（b ) 試驗K7 試驗L7 試驗M7 之施用率 之施用 實測 期望 實測 期望 實測 期望 (ppm) 組分（b) 率（ppm ) 值 值 值 值 值 值 1 快諾芬 0.4 99 99 — — 1 快諾芬 2 99 100 — — 0 BAS600 0.016 — 30 0 0 BAS600 0.08 — 37 91 0 BAS600 0.4 — 85 98 0 BAS600 2 — 100 100 0.1 BAS600 0.016 — 8 56 8 32 0.1 BAS600 0.08 — 43 61 66 94 0.1 BAS600 0.4 — 78 90 99 99 0.1 BAS600 2 — 100 100 99 100 1 BAS600 0.016 — 87 96 97 94 1 BAS600 0.08 — 92 97 93 99 1 BAS600 0.4 — 96 99 98 100 1 BAS600 2 — 100 100 100 100 0 &quot;比°塞菌胺 0.016 — 8 — 0 吡噻菌胺 0.08 — 23 — 0 吡噻菌胺 0.4 — 72 — 0 吡噻菌胺 2 — 100 — 0.1 吡噻菌胺 0.016 — 0 42 — 0.1 吡噻菌胺 0.08 — 23 52 — 0.1 吡噻菌胺 0.4 — 72 83 — 0.1 吡噻菌胺 2 — 100 100 — 1 吡噻菌胺 0.016 — 64 95 — 1 吡噻菌胺 0.08 — 87 96 — 1 吡噻菌胺 0.4 — 92 98 — 1 0比嘆菌胺 2 — 100 100 — 0 異派來桑 0.016 — 81 — 0 異派來桑 0.08 — 99 — 0 異派來桑 0.4 — 100 — 0 異派來桑 2 - 100 一 151284.doc -294- 201117722 化合物181 組分（b) 試驗K7 試驗L7 試驗M7 之施用率 之施用 實測 期望 實測 期望 實測 期望 (ppm) 組分（b ) 率（ppm) 值 值 值 值 值 值 0.1 異派來桑 0.016 — 89 88 — 0.1 異派來桑 0.08 — 98 99 一 0.1 異派來桑 0.4 — 100 100 — 0.1 異派來桑 2 — 100 100 — 1 異派來桑 0.016 一 98 99 — 1 異派來桑 0.08 — 99 100 — 1 異派來桑 0.4 — 100 100 — 1 異派來桑 2 — 100 100 — 0 待克利 0.016 — 0 — 0 待克利 0.08 — 37 — 0 待克利 0.4 — 100 一 0 待克利 2 — 100 — 0.1 待克利 0.016 — 8 37 — 0.1 待克利 0.08 — 92 61 — 0.1 待克利 0.4 — 100 100 — 0.1 待克利 2 — 100 100 — 1 待克利 0.016 — 87 94 — 1 待克利 0.08 — 99 97 — 1 待克利 0.4 — 100 100 — 1 待克利 2 — 100 100 — 0 亞托敏 0.016 — 8 一 0 亞托敏 0.08 — 98 一 0 亞托敏 0.4 — 100 — 0 亞托敏 2 — 100 — 0.1 亞托敏 0.016 — 22 42 — 0.1 亞托敏 0.08 — 99 98 — 0.1 亞托敏 0.4 — 100 100 — 0.1 亞托敏 2 — 100 100 — 1 亞托敏 0.016 — 81 95 — 1 亞托敏 0.08 - 100 100 — 151284.doc -295 - 201117722 表i 化合物181單獨或是與丙氧喹啉的混合物對於防治小麥白粉 _ 菌的實測及期望效果 化合物181之施 組分（b)之施用 試驗K8~ — 用率（ppm) 組分（b) 率（ppm) 實測值 0 無 0 0 0.01 無 0 0 ------ 0.1 無 0 0 ---- 1 無 0 97 — 10 無 0 100 ---- 0 丙氧啥琳 0.016 0 ------ 0 丙氧啥琳 0.08 21 ---— 0 丙氧喹琳 0.4 93 ------ 0 丙氧啥琳 2 99 — — 0.1 丙氧啥·#· 0.016 0 --- 0 0.1 丙氧喹啦 0.08 13 21 0.1 丙氧喹啉 0.4 68 93 0.1 丙氧喧咐 2 98 ------ 00 1 丙氧啥·# 0.016 97 ] —------------ 97 1 丙氧啥琳 0.08 91 98 1 丙氧喹淋 0.4 96 ---— ion 1 1 丙氧喹啉 2 100 ---- 100 化合物181 之施用率 (ppm) 組分（b) 組分（b) 之施用 率（ppm) 試驗K7 試驗L7 一 咸驗M7 實測 值 期望 值 實測 值 期望 值 實測 值 期望 值 1 亞托敏 0.4 一 100 100 ======¾¾¾ 1 亞托敏 2 - 100 100 — 表B到I顯示本發明的組合物，其包含代表性的式 1化合物與種種組分（b)化合物的混合物，其展現了， I5l284.doc -296· 201117722 在某些例子中，協同抑制小麥白粉菌、葉銹病、以及特 別是葉枯病。由於抑制不能達到100%、增加活性大於 期望的殺真菌活性無法總是在混合物中觀測到，但更可 能當個別的活性成份組分施用率其提供相當顯著少於 100%抑制時經觀測到。在施用率低且個別活性成分單 獨具有低活性時，協同效果並不明顯。然而，在某些例 子中，對於組合物其單獨的活性成份應用率具有很小或 是無活性時，更好的活性可經觀測到。根據以上所展示 的，本發明提供了一個抑制白粉菌（小麥白粉病 Blumeria graminis f. sp. tritici)、葉錄病（麥類葉錄病菌 f. sp. tritici)、以及小麥葉枯病（小麥葉斑病菌）的方法。 151284.doc •297 ·15l284.doc -289- 201117722 Application rate of compound 181 (ppm) Component (b) Application rate of component (b) (ppm) Test K6 Test L6 Actual value Expected value Actual value expected 0 BAS600 0.08 73 — 0 BAS600 0.4 93 — 0 BAS600 2 98 — 0 BAS600 10 100 — 0.1 BAS600 0.08 76 97 — 0.1 BAS600 0.4 76 99 — 0.1 BAS600 2 98 100 — 0.1 BAS600 10 100 100 — 1 BAS600 0.08 98 99 — 1 BAS600 0.4 99 100 — 1 BAS600 2 99 100 — 1 BAS600 10 100 100 — 0 Baishenfen 0.08 — 0 0 Baishenfen 0.4 | - 76 0 Baifenfen 2 — 100 0 Baifenfen 10 — 100 0.1 Baifenfen 0.08 — 0 0 0.1 Baifenfen 0.4 83 76 0.1 baifenfen 2 100 100 0.1 baifenfen 10 100 100 1 baifenfen 0.08 — 91 76 1 baifenfen 0.4 a 93 94 1 baifenfen 2 — 100 100 1 baifenfen 10 — 100 100 0环克座 0.08 68 71 0 环克座 0.4 97 99 0 环克座 2 99 100 0 环克座10 100 100 0.1 环克座 0.08 20 96 97 71 0.1 环克座 0.4 98 100 99 99 151284.doc -290 · 201117722 Compound 181 Application rate (ppm) Component (b) Application rate of component (b) (ppm) Test K6 Test L6 Actual value Expected value Actual value Expected value 0.1 Ring holder 2 100 100 100 100 0.1 Ring holder 10 100 100 100 100 1环克座 0.08 92 99 100 93 1 环克座 0.4 100 100 100 100 1 环克座 2 100 100 100 100 1 环克座10 100 100 100 100 0 依普座 0.08 0 10 0 依普座 0.4 97 100 0 Ip seat 2 100 100 0 Ip seat 10 100 100 0.1 Ip seat 0.08 83 89 99 10 0.1 Ip seat 0.4 99 100 100 100 0.1 Ip seat 2 100 100 100 100 0.1 Ip seat 10 100 100 100 100 1依普座 0.08 100 98 100 79 1 Ip seat 0.4 100 100 100 100 1 Ip seat 2 100 100 100 100 1 Ip seat 10 100 100 100 100 0 Propionate α sitting 0.08 59 31 0 Propionate '• Sit 0.4 65 5 0 Propionibacterium D sit 2 68 10 0 Prothiotoxin. Sit 10 100 89 0.1 Propionibacterium β sitting 0.08 59 96 5 31 0.1 Propionate α sitting 0.4 96 96 10 .5 0.1 Propionate 2 98 96 5 10 0.1 Propionate α sitting 10 100 100 70 89 1 C Thiobacillus alpha sits 0.08 100 99 63 84 1 prothiotoxin. Sit 0.4 100 99 83 78 1 Prothiotoxin spit 2 100 99 76 79 1 Prothiotoxin. Sit 10 100 100 94 98 151284.doc -291 - 201117722 Application rate of compound 181 (ppm) Component (b) Application rate of component (b) (ppm) Test K6 Test L6 Measured value Expected value Actual value expected 0 克克敏0.08 11 31 0 Bai Kemin 0.4 89 86 0 Bai Kemin_2_1 97 100 0 Bai Kemin 10 100 100 0.1 Bai Kemin 0.08 65 90 10 31 0.1 Bai Kemin 0.4 39 99 95 86 0.1 Bai Kemin 2 99 100 100 100 0.1 Bai Kemin 10 100 100 100 100 1 100 grams of sensitive 0.08 98 98 84 84 1 100 grams of sensitive 0.4 98 100 97 97 1 100 grams of sensitive 2 100 100 100 100 1 100 grams of 100 100 100 100 100 0 four grams 0.08 59 5 0 four miles 0.4 65 0 0 four Klee 2 99 70 0 Four Klee 10 100 100 0.1 Four Kerry 0.08 59 96 0 5 0.1 Four Klee 0.4 84 96 0 0 0.1 Four Klee 2 98 100 86 70 0.1 Four Klee 10 100 100 100 100 1 Four Kerry 0.08 99 99 76 78 1 Four Klima 0.4 100 99 89 76 1 Four Klee 2 100 100 100 93 1 Four Klee 10 100 100 100 100 0 Pyloxil 0.08 70 0 0 Pyloxyl ester 0.4 95 0 0 Pyloxil 2 100 97 0 Bite Oxygen ester 10 100 100 0.1 Oxygen ester 0.08 71 97 0 0 0.1 Oxygen ester 0.4 93 99 10 0 151284.doc -292- 201117722 Application rate of compound 181 (ppm) Component (b) Application rate of component (b) (ppm) Test K6 test L6 measured value expected value expected value 0.1 picoxystrobin 2 100 100 91 97 0.1 oxydans 10 100 100 100 100 1 oxydans 0.08 100 99 83 76 1 picoxystrobin 0.4 100 100 76 76 1 Oxygen ester 2 100 100 93 99 1 oxypoxystrobin 10 100 100 100 100 Table 化合物 Compound 181 alone or in combination with venofen, BAS600, pirimicarb, acesulfame, chlorhexidine or atoreno For the control of wheat powdery mildew, leaf rust and leaf blight, the measured and expected effect of compound 181 component (b) test K7 test L7 test M7 application rate of the actual measurement expected actual expected expected measurement (ppm) component (b) rate (ppm) Value Value Value Value 0 No 0 71 0 0 0.01 No 0 64 0 0 0.1 No 0 63 37 32 1 No 0 96 94 94 10 No 0 100 100 99 0 Fast Provin 0.0116 0 — — 0 Fast Provin 0.08 21 — — 0 Fast Noven 0.4 81 — — 0 Fast Provin 2 96 – 0.1 Fast Provin 0.0116 56 63 – 0.1 Fast Provin 0.08 21 71 – 0.1 Fast Provin 0.4 64 93 – 0.1 Fast Provin 2 95 99 – 1 Fast Provin 0.0116 98 96 — One 1 Fast Nofi 0.08 99 97 — — 151284.doc -293 · 201117722 Compound 181 Component (b) Test K7 Test L7 Test Application rate of M7 Application Measurement Expected Actual Measurement Expected Actual Measurement Expectation (ppm) Component (b) Rate (ppm) Value Value value value 1 Fastovin 0.4 99 99 — 1 Fastovin 2 99 100 — — 0 BAS600 0.016 — 30 0 0 BAS600 0.08 — 37 91 0 BAS600 0.4 — 85 98 0 BAS600 2 — 100 100 0.1 BAS600 0.016 — 8 56 8 32 0.1 BAS600 0.08 — 43 61 66 94 0.1 BAS600 0.4 — 78 90 99 99 0.1 BAS600 2 — 100 100 99 100 1 BAS600 0.016 — 87 96 97 94 1 BAS600 0.08 — 92 97 93 99 1 BAS600 0.4 — 96 99 98 100 1 BAS600 2 — 100 100 100 100 0 &quot;比°塞菌胺 0.016 — 8 — 0 phenothiamine 0.08 — 23 — 0 pirimifen 0.4 — 72 — 0 pyridine Bitheloline 2 — 100 — 0.1 pirfenamide 0.016 — 0 42 — 0.1 pirfenamide 0.08 — 23 52 — 0.1 pirfenamide 0.4 — 72 83 — 0.1 pirimipenem 2 — 100 100 — 1 Amine 0.016 — 64 95 — 1 Nipenthamide 0.08 — 87 96 — 1 Nipenthenamide 0.4 — 92 98 — 1 0 sinamide 2 — 100 100 — 0 派派来桑 0.016 — 81 — 0桑0.08 — 99 — 0 派派来桑 0.4 — 100 — 0 派派来桑 2 - 100 151284.doc -294- 201117722 Compound 181 Component (b) Test K7 Test L7 Test M7 application rate application measurement expectation Measured expected expected measurement (ppm) Component (b) Rate (ppm) Value value Value value 0.1 派派来桑 0.016 — 89 88 — 0.1 派派来桑 0.08 — 98 99 一 0.1 异派来桑 0.4 — 100 100 — 0.1 派派来桑 2 — 100 100 — 1 派派来桑 0.016 一 98 99 — 1 异派来桑 0.08 — 99 100 — 1 异派来桑 0.4 — 100 100 — 1 异派来桑 2 — 100 100 — 0 Waiting for Kelly 0.016 — 0 — 0 待克利克0.08 — 37 — 0 Waiting for Klein 0.4 — 100 — 0 Waiting for Klee 2 — 100 — 0.1 Waiting for Kelly 0.016 — 8 37 — 0.1 Waiting for Kerry 0.08 — 92 61 — 0.1 Waiting for Kerry 0.4 — 100 100 — 0.1 Waiting for Klee 2 — 100 100 — 1 Waiting for Kelly 0.016 — 87 94 — 1 Waiting for Kerry 0.08 — 99 97 — 1 Waiting for Klee 0.4 — 100 100 — 1 Waiting for Kli 2 — 100 100 — 0 Atomin 0.016 — 8 A 0 Atomin 0.08 — 98-0 Atomin 0.4 — 100 — 0 Atomin 2 — 100 — 0.1 Atomin 0.016 — 22 42 — 0.1 Atomin 0.08 — 99 98 — 0.1 Atomin 0.4 — 100 100 — 0.1 Atomin 2 — 100 100 — 1 亚托敏 0.016 — 81 95 — 1 亚托敏 0.08 - 100 100 — 151284.doc -295 - 201117722 Table i Compound 181 alone or in combination with propoxyquinoline for the control of wheat white powder _ bacteria Measured and expected effect Compound 181 Application (b) Application test K8~ — Usage rate (ppm) Component (b) Rate (ppm) Measured value 0 No 0 0 0.01 No 0 0 ------ 0.1None 0 0 ---- 1 No 0 97 — 10 No 0 100 ---- 0 Propoxyline 0.016 0 ------ 0 Propoxyline 0.08 21 --- 0 Propoxyquine 0.4 93 ------ 0 propoxyline 2 99 — — 0.1 propoxy 啥·#· 0.016 0 --- 0 0.1 propoxyquine 0.08 13 21 0.1 propoxyquinoline 0.4 68 93 0.1 propoxy oxime 2 98 ------ 00 1 propoxy 啥 · # 0.016 97 ] —------------ 97 1 propoxyline 0.08 91 98 1 propoxyquind 0.4 96 --- — ion 1 1 propoxyquinoline 2 100 ---- 100 Compound 181 application rate (ppm) component (b) component (b) application rate (ppm) test K7 test L7 a salt test M7 measured value expected value Measured value expected value measured value expected 1 atorine 0.4 - 100 100 ======3⁄43⁄43⁄4 1 Atomiens 2 - 100 100 - Tables B to I show compositions of the invention comprising representative compounds of formula 1 and Mixtures of various component (b) compounds which exhibit, I5l284.doc -296· 201117722 In some instances, synergistic inhibition of wheat powdery mildew, leaf rust, and in particular leaf blight. Since inhibition of 100%, increased activity greater than the desired fungicidal activity cannot always be observed in the mixture, it is more likely to be observed when the individual active ingredient component application rates provide considerably less than 100% inhibition. The synergistic effect is not significant when the application rate is low and the individual active ingredients have a low activity alone. However, in some instances, better activity can be observed for compositions where the rate of application of the individual active ingredients is small or inactive. In accordance with the above, the present invention provides an inhibition of powdery mildew (Blumeria graminis f. sp. tritici), leaf recorded disease (f. sp. tritici), and wheat leaf blight (wheat) Method of leaf spot pathogen). 151284.doc •297 ·

Claims (1)

201117722 七、申請專利範圍： 1. 一種殺真菌組合物，包含： (a)至少一選自式1之化合物、其氧化物及其鹽類：201117722 VII. Patent Application Range: 1. A fungicidal composition comprising: (a) at least one compound selected from formula 1, an oxide thereof and a salt thereof: I Q2 其中 Q1係苯基、噻吩基、噻唑基、吡唑基、咪唑基、吡 啶基、嗒畊基、嘧啶基、喹啉基或节基，各視情 況以多達4個獨立選自R3的取代基在碳原子環 員上取代，及選自R4的取代基在氮原子環員^ 取代； Q2係苯基、噻吩基、噻唑基、吡唑基、咪唑基、吡 啶基、嗒畊基、嘧啶基'喹啉基或苄基，各視情 況以多達4個獨立選自R5的取代基在碳原子環 員上取代，及選自R6的取代基在氮原子環^ 取代； R及R2係獨立為鹵素、氰基、硝基、crc3烷基、 C2-C3烯基、c2-c3炔基、環丙基、crc3 _烧美、 c2-c3 _烯基、（^(^烷氧基、CrC3鹵烷氧 CrC3烷硫基、CrC：3鹵烷硫基或Ci_C7羥烷基； 15I284.doc 201117722 各R3及R5係獨立為鹵素、氰基、羥基、硝基、CrC7 炫基、C2-C7稀基、C2-C7快基、C2-C7乱烧基、 C1-C7鹵烧基、C2-C7鹵烯基、C3-C7 •院基、 函環烧基、C4-C1Q炫環炫基、C4-C1Q環烧院基、 c6-c14環烷環烷基、c3-c7環烷氧基、c3-c7鹵環 烷氧基、crc7烷氧基、c2-c7氰烷氧基、crc7 南院氧基、C1-C6烧硫基、C1-C7鹵烧硫基、C1-C7 烧亞續醯基、C1-C7炫續醯基、C1-C7鹵烧亞續醯 基、C1-C7鹵烧續酿基、C1-C7炫·胺基、C2-C7二 烷胺基、c2-c7烷羰基、c2-c7烷氧羰基、胺羰基、 C2-C7烧胺幾基、C3-C7二烧胺裁基、C2-C7烧幾 胺基、C3-C1()三烷矽基、-SCN、C(=S)NH2 或 -X-U-Z ; 各R4及R6係獨立為氰基、CVC6烷基、C3-C6烯基、 C3-C6炔基、CVC6鹵烷基、c3-c6環烷基、crc6 烷氧基、c2-c6烷氧烷基、c2-c6烷羰基、c2-c6 烧氧毅基、C2-C6院胺烧基或C3-C6二烧胺烧基； 各X係獨立為Ο、S(=0)n、NR7或一直接鍵結； 各U係獨立為crc6伸烷基、c2-c6伸烯基、c3-c6 伸炔基、c3-c6環伸烷基或c3-c6環伸烯基，其中 多達3個碳原子係獨立選自C(=0)，各視情況以 多達5個獨立選自鹵素、氰基、硝基、羥基、CrC6 烧基、C1-C6 _烧基、C1-C6烧氧基及C1-C6鹵烧 氧基的取代基所取代； 各 Z 係獨立為 NR8aR8b、OR9 或 S(=0)nR1G ; 151284.doc 201117722 各R7係獨立為Η、crc6烷基、crc6鹵烷基、C2-C6 烷羰基、c2-c6烷氧羰基、c2-c6(烷硫基)羰基、 C2**C6烧氧基(硫幾基）、c4-C8環烧基幾基、C4-C8 環烧氧羰基、C4-C8(環烷硫基)羰基或C4-C8環烷 氧基(硫羰基）； 各R8a及R8b係獨立為H、Crc6烷基、CrC6鹵烷基、 c2-c6烯基、c3-C6炔基、c3-c6環烷基、c3-c6鹵 環烧基、c2-c6烷羰基、c2-c6烷氧羰基、c2-c6(炫 硫基)羰基、c2-c6烷氧基(硫羰基）、c4-c8環烷基 幾基、C4-C8環烷氧羰基、C4-C8(環烷硫基)幾基 或匸4&lt;8環烷氧基(硫羰基）； 各R9及R10係獨立為H、CrC6烷基、Ci_C6鹵烷基、 c2-c6烯基、c3_c6炔基、c3_Cpf 烷基、c3_c6 鹵 環燒基、cvc6烧幾基、C2_C6烷氧羰基、C2-C6(烧 硫基)羰基、Cz-C6烷氧基(硫羰基）、c4-C8環烷基 羰基、Q-C8環烷氧羰基、C4_C8(環烷硫基)羰基 或Q-C8環烷氧基(硫羰基）； 各η係獨立為〇、1或2 ;及 至&gt;、一附加的殺真菌化合物。 2.如凊求項第1項所述之組合物，其中組分⑷包含1 化合物或其鹽類，其中式丨中， Q係苯基、嗟吩基、麵基ϋ基、咪絲、吼咬基、 ^3基、錢基或¥基，各視情況以多達3個獨立選 的取代基切料環貞上取代，謂自Μ的取 代基在氮原子環員上取代； 151284.doc 201117722 Q2係苯基、嚷吩基、嗟11坐基、°比π坐基、0米°坐基、D比咬基、 嗒畊基、嘧啶基或苄基，各視情況以多達3個獨立選 自R5的取代基在碳原子環員上取代，及選自R6的取 代基在氮原子環員上取代；以及 R1及R2係獨立為鹵素、氰基、乙烯基、乙炔基、曱氧基 或曱硫基；或曱基視情況以選自於鹵素、-OH及曱基 的取代基所取代。 3. 如請求項第2項所述之組合物，其中式1中， Q1係苯基、吡啶基或苄基，各視情況以多達3個獨立選自 R3的取代基在碳原子環員上取代； Q2係苯基、吡啶基或苄基，各視情況以多達3個獨立選自 R5的取代基在碳原子環員上取代；以及 各R3及R5係獨立為函素、氰基、CrC3烷基、C2-C3烯基、 C2-C3炔基、（VC3鹵烧基、環丙基、CVC3烧氧基、 CVQ鹵烷氧基、CrC3烷硫基、CrC3烷胺基、C2-C4 二烷胺基、C2-C4烷羰基、C2-C4烷氧羰基或C2-C4烷 羰胺基。 4. 如請求項第3項所述之組合物，其中式1中， Q1係苯基或3-吡啶環，視情況以多達3個獨立選自R3的 取代基在碳原子環員上取代；以及 Q2係一苯基或3-吡啶環，視情況以多達3個獨立選自R5 的取代基在碳原子環員上取代。 5. 如請求項第4項所述之組合物，其中式1中， R1及R2係獨立為鹵素、氰基或曱氧基；或曱基，視情況 以一選自於F、C1或曱基的取代基取代；以及 151284.doc -4 - 201117722 C1-C3烧基、C2-C3稀基 各R3及R5係獨立為鹵素、氰基、 c】-c3 i烧基、Cl_c3^氧基、Ci_C3函烧氧基、Ci_C3 烷硫基或（^-(:3烷胺基。 6 .如請求項第5項所述之組合物，其中式丨中， R1及R2係獨立為α、Βγ、ί或Crc2烷基； 各R3及R5係獨立為F、C卜Br、氰基、Ci_c2烧基、Cl-C2 1函f基crc2烧氧基或匸】々鹵炫氧基；以及 Q及Q之任一環係以2或3個取代基取代，且Ql及Q2 另一環係以1或2個取代基取代。 .如1請求項第6所述之組合物，其中式丨中， R1及R2係獨立為α、价或曱基； Q1及Q2任一環係笨基或3_吡啶環，在間位或對位以一選 自於F、C1、甲基、甲氧基及氟甲氧基的取代基所取 1代j且於所剩位置視情況經一 F所取代的；以及 Q及Q2另一者的環係苯環，在兩個鄰位皆經F取代，且 間位或對位經選自於氰基及CrC2烷氧基的取代基所 取代。 8.如吻求項第1項所述之組合物，其中組分（a)包含-選 自由下列所組成群組的化合物： 4氣5-(2,6-二氟+曱氧苯基H_(3-氟笨基)-2-曱基-1H-咪 [4氣1-(4_氯苯基)_2曱基_1H咪唑_5基]_2,4_二氟苯甲 腈、 溴-β^(2,6-二氟_4·曱氧苯基)-5-(3-氟苯基)-4-甲基-1H-咪 151284.doc 201117722 4-[2-氣-1-(6-氣-3-吡啶基)-4-曱基-1H-咪唑-5-基]-3,5-二氟 苯曱腈、 2-溴-4-氯-5-(4-乙氧基-2,6-二氟苯基)-1-(3-氟苯基)-1Η-咪 口坐、 4-氯-5-(4_乙氧基-2,6-二說苯基）-2-曱基-1-(4-曱基苯 基)-1Η-咪唑、 4-氯-5-(4-乙氧基-2,6-二氟苯基)-1-(4-氟苯基)-2曱基_1H- σ米唾、 4-氣-5-(4-乙氧基-2,6-二氟苯基)-1-(3-氟苯基)-2-曱基-1Η- 口米0坐、 2-&gt;臭基-4-氯-1-[3-(二氣曱氧基）苯基]-5-(4-乙氧基-2,6-二 氟苯基)-1Η-咪唑、 2,4-二氯-1-[3-(二氟曱氧基）苯基]-5-(4-乙氧基-2,6-二氣苯 基)-1Η-咪唑、 4-[2-氯-1-(6-曱氧基-3-吡啶基)-4-曱基-1H-咪唑-5-基]-3,5-二氟苯曱腈、 4-[2-溴-1-(6-曱氧基-3-吡啶基)-4-曱基-1H-咪唑-5-基]-3,5-二氟苯曱腈、 4-[2-溴-4-氯-1-(4-曱基苯基)-1Η-咪唑-5-基]-3,5-二氟苯曱 腈、 4-氯小[3-(二氟曱氧基）苯基]-5-(4-乙氧基-2,6-二氟苯 基)-2-曱基-1H-咪唑、 4-[2-溴-4-氯-1-(3-氟苯基)-1Η-咪唑-5-基]-3,5-二氟苯曱 腈、 4-[4-氯-l-(3,4-二氟苯基)-2-曱基-1H-咪唑-5-基]-3,5-二氟 苯曱腈、 151284.doc -6- 201117722 4_[4_氣小(3·氟苯基)-2-曱基-1H-咪唑-5·基]-3,5-二氟苯曱 猜、 4-[2_漠-4-氣小(4-氟笨基;)_1Η-咪唑_5_基；|_3,5-二氟苯甲 猜、 2-氣小[4·(二氟甲氧基）苯基]_5·(2 6_二氟_4-甲氧笨基) 甲基-1Η-ρ米β坐、 4-[2_氯小(4-氯笨基Μ-甲基-1Η-咪唑-5·基]-3,5-二氟笨甲 猜、 4_[2-氯-1·(3-氟苯基)_4_甲基·m_咪唑-5_基]_3,5_二氟笨甲 猜、 4-[4-氯-1_(2,4_二氟苯基)_2_ 甲基_1Η_咪唑基]_3,5-二氟 苯甲腈、 4_[2_氯-1_[3-(二氟甲氧基）苯基]-4-甲基-1Η-咪唑-5-基]-3,5-二氟苯甲腈、 4_[2’4-二氯二氟甲氧基）苯基]-1Η-咪唑-5-基;h3,5-二 氟笨甲腈、 4 [4-氣小(2_氟·4_曱基笨基)_2_曱基_ih咪唑_5_基]_3,5_二 氟笨甲腈、 4 [4 /臭-1-(2-氟_4_曱基苯基)_2_曱基_1H咪唑士基]_3,5二 氣笨甲腈，及 4_[^4-二溴-1-(3-氟苯基)-111-咪唑-5-基]-3,5-二氟苯曱腈。 9_^求項第1項至第8項中任-項所述之組合物，其中 I真括至少—殺真8劑，選自^下酬組成群組的 (bl)甲基笨并咪唑胺甲酸鹽類殺真菌劑 (b2)二羧醯胺類殺真菌劑； 15l284.doc 201117722 (b3)脫甲基作用抑制麵殺真菌劑； (b4)苯胺類殺真菌劑； (b5)版/嗎福林類殺真菌劑； (b6)碟脂質生合成抑制劑類殺真菌劑； (b7)幾g篮胺類殺真菌劑； (b8)羥基(2-胺基_)嘧啶類殺真菌劑； (b9)苯胺嘧啶類殺真菌劑； (blO) N-苯基胺甲酸鹽類殺真菌劑； (bll)醌外抑制劑類殺真菌劑； (M2)苯基吼咯類殺真菌劑； (bl3)喹啉類殺真菌劑； (bl4)脂質過氧化抑制劑類殺真菌劑； (bl5)黑色素生合成抑制劑_還原酶類殺真菌劑； (bl6)黑色素生合成抑制劑_脫水酶殺真菌劑； (bl7)羥基苯胺類殺真菌劑； (M8)鯊烯-環氧酶抑制劑類殺真菌劑； (bl9)多氧菌素（p〇iyoxin)類殺真菌劑； (b20)苯脲類殺真菌劑； (b21)醌内抑制劑類殺真菌劑； (b22)苯曱醯胺類殺真菌劑； (b23) «比喃醣醛酸抗生素類殺真菌劑； (b24)己吼喃基（hexopyranosyl)抗生素類殺真菌劑； (b25) 0比喃葡萄糖苦（glUC〇pyran〇Syl)抗生素：蛋白 質合成類殺真菌劑； (b26)吡喃葡萄糖苷類抗生素：繭蜜糖酶及肌醇生人 成類殺真菌劑； σ 151284.doc 201117722 (b27)氰肟乙醯胺類殺真菌劑； (b28)胺曱酸鹽類殺真菌劑； (b29)氧化磷酸化解偶合類殺真菌劑； (b30)有機錫類殺真菌劑； (b31)羧酸類殺真菌劑； (b32)芳香雜環類殺真菌劑； (b33)膦酸鹽類殺真菌劑； (b34)鄰胺甲醯苯曱酸類殺真菌劑； (b35)苯並三p井（benzotriazine)類殺真菌劑； (b36)苯-磺化醯胺殺真菌劑； (b37)嗒畊酮類殺真菌劑； (b38)噻吩-羧醯胺類殺真菌劑； (b39) 定酿胺（pyrimidinamide)類殺真菌劑； (b40)羧酸醯胺類殺真菌劑； (b41)四環素類抗生素類殺真菌劑； (b42)硫代胺基曱酸鹽類殺真菌劑； (b43)苯曱醯胺類殺真菌劑； (b44)誘發寄主植物防禦類殺真菌劑； (b45)多重作用類殺真菌劑； (b46)其餘非組分（a)及組分（bl)至（b45)的殺 真菌劑；及化合物（bl)至（b46)的鹽類。 10. 如請求項第9項所述之組合物，其中組分（b)包含至少 一殺真菌劑且該殺真菌劑來自選自（bl)到（b46)中的 二不同群組的各一種殺真菌劑。 11. 如請求項第1項所述之組合物，其中組分（b)包括至少 一化合物，選自阿拉酸式苯-S-曱基 151284.doc 201117722 (acibenzolar-S-methyl)、巴丹（aldimoirph)、辛嗤0密菌 胺（ametoctradin )、吲唑磺菌胺（amisulbrom )、敵菌靈 (anilazine )、阿札康 坐（azaconazole )、亞托敏 (azoxystrobin )、右本達樂（benalaxyl)、右本達樂-M (benalaxyl-M)、麥鏽靈（benodanil)、免賴得（benomyl)、 0塞菌胺（benthiavalicarb )、苯嗟菌胺-異丙基 (benthiavalicarb-isopropyl)、貝殺新（bethoxazin)、百 蜗克（binapacryl )、聯苯（biphenyl )、比多農（bitertanol)、 百殺芬（bixafen )、保米黴素（blasticidin-S )、白克列 (boscalid )、漠克座（bromuconazole )、布瑞莫 (bupirimate )、嘉保信（carboxin )、加普胺 (carpropamid)、四氣丹（captafol)、蓋普丹（captan)、 貝芬替（carbendazim)、地茂散（chloroneb)、四氣異苯 腈（chlorothalonil )、克氣得（chlozolinate )、克霉0坐 (clotrimazole )、銅鹽（copper salts )、賽座滅 (cyazofamid )、環敗菌胺（cyflufenamid )、克絕 (cymoxanil )、環克座（cyproconazole )、賽普洛 (cyprodinil )、益發靈（dichlofluanid )、雙氯氰菌胺 (diclocymet )、達滅淨（diclomezine )、大克爛 (dicloran )、乙霉威（diethofencarb )、待克利 (difenoconazole )、二氟林（diflumetorim )、二曱嘧酚 (dimethirimol )、達滅芬（dimethomorph )、醚菌胺 (dimoxystrobin )、達克利（diniconazole )、達克利-M (diniconazole-M )、，敵蜗普（dinocap )、腈硫西昆 (dithianon )、十二環嗎啉（dodemorph )、多寧（dodine )、 護粒松（edifenphos )、烯肟菌酯（enestroburin )、依普座 151284.doc .10- 201117722 (epoxiconazole )、噻唑菌胺（ethaboxam )、依瑞莫 (ethirimol )、依得利（etridiazole )、凡殺克絕 (famoxadone )、咪唑菌酮（fenamid〇ne )、芬瑞莫 (fenarimol )、芬克座（fenbuconazole )、甲0夫醯胺 (fenfuram )、環醯菌胺（fenhexamid )、氰菌胺 (fenoxanil )、拌種 p各（fenpiclonil )、苯鐵咬 (fenpropidin )、芬普福（fenpropimorph )、 fenpyrazamine、三苯醋錫（fentin acetate)、三苯氯化錫 (fentin chloride)、三苯經錫（fentin hydroxide)、富爾 邦（ferbam )、富米綜（ferimzone )、扶吉胺（fluazinam )、 護汰寧（fludioxonil)、氟醯菌胺（flumetover)、氟嗎琳 (flumorph )、氟比來（fluopicolide )、氟。比菌醯胺 (fluopyram )、唑呋草（fluoroimide )、氟嘧菌醋 (fluoxastrobin )、氟喧嗤（fluquinconazole )、護石夕得 (flusilazole)、氟硫滅（flusulfamide)、福提泥（flutianil)、 福多寧（flutolanil )、護汰芬（flutriafol )、福批殺 (fluxapyroxad )、福爾培（folpet )、福赛得 (fosetyl-aluminum )、麥穗寧（fuberidazole )、咬霜靈 (furalaxy )、福拉比（furametpyr )、菲克利 (hexaconazole )、殺紋寧（hymexazol )、克熱淨 (guazatine )、依滅列（imazalil )、易胺座 (imibenconazole )、克熱淨（iminoctadine )、峨菌威 (iodocarb )、種菌嗤（ipconazole )、丙基喜樂松 (iprobenfos )、依普同（iprodione )、丙森鋅 (iprovalicarb )、亞賜圃（isoprothiolane )、異派來桑 (isopyrazam )、異噻菌胺（isotianil )、嘉賜黴素 151284.doc 201117722 (kasugamycin)、克收欣（kresoxim-methyl)、鋅錳乃浦 (mancozeb )、雙炔醯菌胺（mandipropamid )、錳乃浦 (maneb )、滅普寧（mepronil)、敵瞒普（meptyldinocap )、 滅達樂（metalaxyl)、滅達樂-M (metalaxyl-M)、滅特座 (metconazole )、滅速克（methasulfocarb )、免得爛 (metiram )、苯氧菌胺（metominostrobin )、滅派林 (mepanipyrim )、滅芬農（metrafenone )、邁克尼 (myclobutanil)、奈桂胺（naftifme )、新阿蘇仁（neo-asozin (ferric methanearsonate ))、尼瑞莫（nuarimol)、辛噻酮 (octhilinone )、呋醯胺（ofurace )、肟醚菌胺 (orysastrobin)、歐殺斯（oxadixyl)、歐索林酸（oxolinic acid)、惡味11坐（oxpoconazole)、嘉保信（oxycarboxin)、 氧四環素（oxytetracycline)、平克座（penconazole)、賓 克隆（pencycuron )、派福芬（penflufen )、0比β塞菌胺 (penthiopyrad)、披扶座（pefurazoate)、亞鱗酸及其鹽 類（phosphorous acid and salts )、熱必斯（phthalide )、咬 氧菌酯（picoxystrobin)、粉病靈（piperalin)、多氧菌素 (polyoxin )、撲殺熱（probenazole )、撲克拉 (prochloraz )、撲滅寧（procymidone )、普拔克 (propamocarb ) 拔克 鹽酸鹽 (propamocarb-hydrochloride)、普克利（propiconazole)、 甲基鋅乃浦（propineb)、丙氧啥琳（proquinazid)、硫菌 威（prothiocarb)、丙硫菌0坐（prothioconazole)、百克敏 (pyraclostrobin)、嗤胺菌醋（pyrametostrobin)、〇坐菌醋 (pyraoxystrobin )、白粉松(pyrazophos ) ' 防霉丹 (pyribencarb )、稗草畏（pyributicarb )、比芬諾 151284.doc -12· 201117722 (pyrifenox )、派美尼（pyrimethanil)、pyriofenone、百 快隆（pyroquilon )、吡咯尼群（pyrr〇lnitrin )滅蟎猛 (quinomethionate)、快諾芬（quinoxyfen)、五氯硝基笨 (quintozene )、赛得先（sedaxane )、矽噻菌胺 (silthiofam )、石夕氟。坐（simeconazole ) ' 葚孢菌素 (spiroxamine)、鍵徽素（streptomycin)、硫（sulfur)、 得克利（tebuconazole)、泰伏勤（tebufloquin)、克枯爛 (tecloftalam )、四氯硝基苯（tecnazene )、特比萘芬 (terbinafine )、四克利（tetraconazole )、腐絕 (thiabendazole )、賽氟滅（thifluzamide )、多保淨 (thiophanate )、曱基多保淨（thiophanate-methyl)、得恩 地（thiram )、噻醯菌胺（tiadinil )、甲基立枯磷 (tolclofos-methyl)、曱基益發靈（t〇iyifluanid)、三泰芬 (triadimefon )、三泰隆（triadimenol )、咪唑口秦 (triazoxide )、三賽唾（tricyclazole )、三得芬 (tridemorph )、賽福座（triflumizole )、三賽唑 (tricyclazole )、三氣敏（trifloxystrobin )、赛福寧 (triforine )、垂嗎酸胺（trimorphamide )、滅菌嗤 (triticonazole )、烯效唑（uniconazole )、維利黴素 (validamycin )、及瓦芬耐（vaiifenaiate )、免克寧 (vinclozolin )、鋅乃浦（Zineb )、福美鋅（Ziram )、座赛 胺（zoxamide)、N'-[4-[4-氯-3-(三氟曱基）苯氧基]_2,5-二 曱基苯基]-N-乙基-N-曱基甲亞胺基胺、5-氣-6-(2,4,6-三 氟苯基）-7-(4-甲基哌啶小基）[1，2,4]***[l，5-a]嘧咬、 N-[2-[4-[[3-(4-氯苯基)-2-丙快-1-基]氧]_3_甲氧苯基]乙 基]-3-甲基-2-[(曱磺醯基)胺]丁醯胺、N-[2-[4-[[3-(4-氣笨 151284.doc •13· 201117722 基)-2-丙炔_ι_基]氧]_3_曱氧苯基]乙基]_3_甲基_2_[(乙磺 醯）胺]丁醯胺、2-丁氧基-6-碘-3-丙基-4H-1-苯并哌喃-4-_、3_[5-(4-氯笨基)_2,3-二甲基-3-異噁唑烷基]漠扯啶、 4-氟苯基N-[l-[[[l-(4-氰基苯基）乙基]磺醯基]曱基]丙基] 胺曱酸醋、N-[[(環丙基甲氧基)胺基][6-(二氟甲氧基)-2,3-二氟苯基]曱烯]苯乙醯胺、曱基亞胺）_N_甲基 -2-[[[1-[3-(三氟曱基）苯基]乙氧]亞胺基]曱基]苯乙醯 胺、Ν’-[4·[4·氣-3_(三亂甲基)苯氧基]-2,5-二曱基苯基]-N-乙基-N-雙曱脒、n-(4-氯-2-硝基苯基)-N-乙基-4-甲基苯 確醯胺、2_[[[[H2,6-二氣苯基H-曱基_2_丙烯-1-亞基]胺] 氧基]甲基]-α-(曱氧亞胺基)-Ν·甲基苯乙醯胺、1_[(2_丙烯 硫基）羰基]-2-( 1 -曱基乙基)-4-(2-曱基苯基)_5_胺-1Η-。比 峻-3-_、5-乙基_6_辛基-[1，2,4]三唾[i，5-a]苯胺嘧啶-7-烧 基胺、戊基N-[4-[[[[(l-曱基-1H-四唾_5_基）苯基亞甲基] 胺]氧基]曱基]-2-噻唑基]胺曱酸酯及戊基N-[6-[[[[(l-曱 基-1H·四哇_5_基）苯基亞甲基]胺]氧基]曱基]_2咬基]胺 曱酸醋。 12. —種組合物包括： (a)至少一化合物，選自如請求項第丨項所定義之 式1化合物、其N_氧化物及其鹽類；以及至少一無脊椎 害蟲防治化合物或藥劑。 13. 一種組合物，包含請求項第1項至第12項中任一項所述 之組合物及至少-種附加的組分，該組分係選自於由^ 面活性劑、固體稀釋劑以及液體稀釋劑所組成的群組。| 14. =㈣-植物或植物種子免受真菌病原體所致疾病 、方法，包含施予該植物或植物種子—殺真菌有效^ 151284.doc 201117722 項至第13項中任 量之組合物，該組合物係如請求項第ι 一項所述之組合物。 15. 種保漠Μ物免焚斑枯病侵襲 物-殺真菌有效劑量之心物⑼/ 施予该植 項至第^心組合物係如請求項第1 ^第8項t任-销狀組合物，其巾組分 種選自於⑽胺/嗎福林類殺真_之殺真菌化 16·=Γ自如請求項第1項所定義之式ι化合物、其队氧 化物及其鹽類；其限制條件為 當Q1係苯基、噻吩基、噻唑基、吡唑基咪唑基、 吼咬基、0基、錢基、料基或苯基，各 視情況以多達4個獨立選自R3a的取代基在碳原 子環員上取代及選自R4a的取代基在氮原子環 員上取代；其中 各R分別係鹵素、氰基、羥基、硝基、Ci_c7 烧基、c2-c7稀基、C2-C7块基、Q-C； i烷基、 C2_C7 _婦基、c3-c7環烧基、c3-c7 ii環炫基、 C4_C1Q燒環烷基、C4_CiG環烷烷基、C6_Ci4環烷 環烧基、C3-C7環烷氧基、c3-C7鹵環烷氧基、 CrC7：^氧基、crc7鹵烷氧基、Crc6烷硫基、 C1-C7 4燒硫基、Q-C7烧亞績驢基、C^-C?院續 醯基、crc7鹵烷亞磺醯基、crC7鹵烷磺醯基、 CrC7烷胺基、c2-C7二烷胺基、（：2-(：7烷羰基、 C2_C7院氧基羰基、c2-C7烧羰胺基、C3-C10三 烷基曱矽基、-SCN、C(=S)NH2或-X-U-Z ;以及 151284.doc 201117722 各R4a分別係氰基、CrC6烷基、C3-C6烯基、 C3-C6快基、C3-C6環烧基、Ci_C6烧氧基、C2-C6 烧氧烧基、C2-C6烧幾基、C2-C6烧氧幾基、C2-C6 烷胺烷基或c3-c6雙烷胺烷基； 則Q2係苯基、°塞吩基、嗟β坐基、吼唾基、°米唾基、 σ比咬基、塔ρ井基、σ密咬基、喧琳基或节基，各 經1至4個獨立選自R5的取代基在碳原子環員 上取代及選自R6的取代基在氮原子環員上取 代；其限制條件為至少一碳原子環員上之取代 基係C2-C7氰烷基、C2-C7氰烷氧基、胺羰基、 C2-C7烷胺羰基或C3-C7二烷胺羰基，或氮原子 環員上之取代基係crc6 _烧基。 151284.doc -16- 201117722 四、指定代表圖·· (一） 本案指定代表圖為：（無） (二) 本代表圖之元件符號簡單說明： 五、本案若有化學式時，請揭示最能顯示發明特徵的化學式：I Q2 wherein Q1 is phenyl, thienyl, thiazolyl, pyrazolyl, imidazolyl, pyridyl, hydrazine, pyrimidinyl, quinolinyl or a benzyl group, each optionally up to 4 independently selected from R3 a substituent substituted on a carbon atom ring member, and a substituent selected from R4 is substituted at a nitrogen atom ring; Q2 is a phenyl group, a thienyl group, a thiazolyl group, a pyrazolyl group, an imidazolyl group, a pyridyl group, a ruthenium group a pyrimidinyl 'quinolinyl or benzyl group, each optionally substituted with up to 4 substituents independently selected from R5 on a carbon atom ring, and a substituent selected from R6 substituted at the nitrogen atom; R and R2 is independently halogen, cyano, nitro, crc3 alkyl, C2-C3 alkenyl, c2-c3 alkynyl, cyclopropyl, crc3 _ burnt, c2-c3-alkenyl, (^(^ alkoxy) Base, CrC3 haloalkoxy-CrC3 alkylthio, CrC: 3 haloalkylthio or Ci_C7 hydroxyalkyl; 15I284.doc 201117722 Each R3 and R5 are independently halogen, cyano, hydroxy, nitro, CrC7 炫, C2 -C7 dilute, C2-C7 fast radical, C2-C7 chaotic alkyl, C1-C7 haloalkyl, C2-C7 haloalkenyl, C3-C7 • Institute, cyclization, C4-C1Q Base, C4-C1Q ring furnace base C6-c14 cycloalkylcycloalkyl, c3-c7 cycloalkoxy, c3-c7 halocycloalkoxy, crc7 alkoxy, c2-c7 cyanoalkoxy, crc7 south oxy, C1-C6 sulphur Base, C1-C7 halogen-burning sulfur group, C1-C7-sintering sulfhydryl group, C1-C7-spinning sulfhydryl group, C1-C7 halogen-sintering sulfhydryl group, C1-C7 halogen-burning continuation base, C1-C7 - Amino, C2-C7 dialkylamino, c2-c7 alkylcarbonyl, c2-c7 alkoxycarbonyl, amine carbonyl, C2-C7 acrylamine, C3-C7 diamined amine, C2-C7 Amino, C3-C1()trialkylsulfonyl, -SCN, C(=S)NH2 or -XUZ; each R4 and R6 is independently cyano, CVC6 alkyl, C3-C6 alkenyl, C3-C6 alkyne , CVC6 haloalkyl, c3-c6 cycloalkyl, crc6 alkoxy, c2-c6 alkoxyalkyl, c2-c6 alkylcarbonyl, c2-c6 oxynitride, C2-C6 amphoteric or C3 -C6 diamined amine; each X system is independently Ο, S(=0)n, NR7 or a direct bond; each U is independently crc6 alkyl, c2-c6 extended alkenyl, c3-c6 Alkynyl, c3-c6 cycloalkyl or c3-c6 cycloalkenyl, wherein up to 3 carbon atoms are independently selected from C(=0), optionally up to 5 independently selected from halogen, cyanide Base, nitro, hydroxyl, CrC6 alkyl, C1-C6 _ burning Substituted by a C1-C6 alkoxy group and a C1-C6 halogenated alkoxy group; each Z series is independently NR8aR8b, OR9 or S(=0)nR1G; 151284.doc 201117722 Each R7 is independently Η, crc6 alkane , crc6 haloalkyl, C2-C6 alkylcarbonyl, c2-c6 alkoxycarbonyl, c2-c6(alkylthio)carbonyl, C2**C6 alkoxy (thiol), c4-C8 cycloalkyl a C4-C8 ring-fired oxycarbonyl group, a C4-C8 (cycloalkylthio)carbonyl group or a C4-C8 cycloalkoxy group (thiocarbonyl group); each of R8a and R8b is independently H, Crc6 alkyl, CrC6 haloalkyl , c2-c6 alkenyl, c3-C6 alkynyl, c3-c6 cycloalkyl, c3-c6 halocycloalkyl, c2-c6 alkylcarbonyl, c2-c6 alkoxycarbonyl, c2-c6(decylthio)carbonyl , c2-c6 alkoxy (thiocarbonyl), c4-c8 cycloalkyl, C4-C8 cycloalkoxycarbonyl, C4-C8(cycloalkylthio) or 匸4&lt;8 cycloalkoxy ( Thiocarbonyl); each R9 and R10 are independently H, CrC6 alkyl, Ci_C6 haloalkyl, c2-c6 alkenyl, c3_c6 alkynyl, c3_Cpf alkyl, c3_c6 halocycloalkyl, cvc6 alkyl, C2_C6 alkoxy Carbonyl, C2-C6 (thiol)carbonyl, Cz-C6 alkoxy (thiocarbonyl), c4-C8 cycloalkylcarbonyl, Q-C8 cycloalkoxycarbonyl, C4_C8 (ring Thio) carbonyl, or Q-C8 cycloalkoxy (thiocarbonyl); each independently square based η, 1 or 2; &gt;, and to an additional fungicidal compound. 2. The composition according to claim 1, wherein component (4) comprises a compound or a salt thereof, wherein in the formula, Q is a phenyl group, a porphinyl group, a fluorenyl group, a mercapto group, an amidine, an anthracene. A thiol group, a ^3 group, a hydroxy group or a benzyl group, each optionally substituted with up to three independently selected substituents, wherein the substituent from the oxime is substituted on the nitrogen atom ring; 151284.doc 201117722 Q2 is a phenyl group, a porphinyl group, a fluorene 11 sitting group, a ° ratio π sitting group, a 0 metre sitting group, a D bite base, a sorghum base, a pyrimidinyl group or a benzyl group, as many as three depending on the case. Substituents independently selected from R5 are substituted on a carbon atom ring, and substituents selected from R6 are substituted on a nitrogen ring ring; and R1 and R2 are independently halogen, cyano, vinyl, ethynyl, oxime Or a thiol group; or a fluorenyl group is optionally substituted with a substituent selected from the group consisting of halogen, -OH and anthracenyl. 3. The composition of claim 2, wherein in formula 1, Q1 is phenyl, pyridyl or benzyl, each optionally having up to 3 substituents independently selected from R3 in the ring of carbon atoms. Substituted; Q2 is phenyl, pyridyl or benzyl, each optionally substituted with up to 3 substituents independently selected from R5 on a carbon atom ring; and each R3 and R5 is independently a cyano, cyano group , CrC3 alkyl, C2-C3 alkenyl, C2-C3 alkynyl, (VC3 haloalkyl, cyclopropyl, CVC3 alkoxy, CVQ haloalkoxy, CrC3 alkylthio, CrC3 alkylamino, C2- A C4 dialkylamino group, a C2-C4 alkylcarbonyl group, a C2-C4 alkoxycarbonyl group or a C2-C4 alkylcarbonylamino group. The composition of claim 3, wherein in the formula 1, the Q1 is a phenyl group. Or a 3-pyridine ring, optionally substituted with up to 3 substituents independently selected from R3 on the carbon atom ring; and Q2 is a phenyl or 3-pyridine ring, optionally up to 3 independently selected from the group The substituent of R5 is substituted on the carbon atom ring. 5. The composition of claim 4, wherein R1 and R2 are independently halogen, cyano or decyloxy; or fluorenyl, Depending on the situation, one is selected from F Substituent substitution of C1 or fluorenyl; and 151284.doc -4 - 201117722 C1-C3 alkyl, C2-C3 dilute R3 and R5 are independently halogen, cyano, c]-c3 i alkyl, Cl_c3^ An oxy group, a Ci_C3 functional alkoxy group, a Ci_C3 alkylthio group or a (^-(3 alkylamino) group. The composition of claim 5, wherein, in the formula, R1 and R2 are independently α. , Βγ, ί or Crc2 alkyl; each R3 and R5 are independently F, C, Br, cyano, Ci_c2 alkyl, Cl-C2 1 f, crc2 alkoxy or hydrazine; Any one of Q and Q is substituted with 2 or 3 substituents, and the other ring of Q1 and Q2 is substituted with 1 or 2 substituents. The composition of claim 6, wherein in the formula, R1 and R2 are independently α, valence or fluorenyl; any ring of Q1 and Q2 is a stupid or 3-pyridine ring, and is at a meta or para position selected from F, C1, methyl, methoxy and fluorine. The substitution of the methoxy group takes 1 generation j and is replaced by a F at the remaining position; and the ring benzene ring of the other of Q and Q2 is substituted by F in both ortho positions, and a position or a para position selected from a substituent selected from a cyano group and a CrC2 alkoxy group 8. The composition of claim 1, wherein component (a) comprises - a compound selected from the group consisting of: 4-gas 5-(2,6-difluoro + anthraquinone) Base H_(3-fluorophenyl)-2-mercapto-1H-mi[4 gas 1-(4-chlorophenyl) 2 fluorenyl-1H imidazolium-5-yl]_2,4-difluorobenzonitrile, Bromo-β^(2,6-difluoro_4·decyloxyphenyl)-5-(3-fluorophenyl)-4-methyl-1H-imi 151284.doc 201117722 4-[2-gas-1 -(6-Gas-3-pyridyl)-4-mercapto-1H-imidazol-5-yl]-3,5-difluorobenzonitrile, 2-bromo-4-chloro-5-(4-B Oxy-2,6-difluorophenyl)-1-(3-fluorophenyl)-1Η-miso, 4-chloro-5-(4-ethoxy-2,6-diphenyl) 2-mercapto-1-(4-mercaptophenyl)-1Η-imidazole, 4-chloro-5-(4-ethoxy-2,6-difluorophenyl)-1-(4- Fluorophenyl)-2-mercapto_1H- σ m saliva, 4-gas-5-(4-ethoxy-2,6-difluorophenyl)-1-(3-fluorophenyl)-2-曱基-1Η- 口米0坐, 2-&gt; odoryl-4-chloro-1-[3-(dioxadecyloxy)phenyl]-5-(4-ethoxy-2,6- Difluorophenyl)-1Η-imidazole, 2,4-dichloro-1-[3-(difluorodecyloxy)phenyl]-5-(4-ethoxy-2,6-di-phenylene )-1Η-imidazole, 4-[2-chloro-1-(6-decyloxy-3-pyridyl)-4-anthracene -1H-imidazole-5-yl]-3,5-difluorobenzonitrile, 4-[2-bromo-1-(6-decyloxy-3-pyridyl)-4-mercapto-1H-imidazole -5-yl]-3,5-difluorobenzonitrile, 4-[2-bromo-4-chloro-1-(4-mercaptophenyl)-1Η-imidazole-5-yl]-3,5 -difluorobenzonitrile, 4-chlorosodium [3-(difluorodecyloxy)phenyl]-5-(4-ethoxy-2,6-difluorophenyl)-2-mercapto-1H -imidazole, 4-[2-bromo-4-chloro-1-(3-fluorophenyl)-1Η-imidazol-5-yl]-3,5-difluorobenzonitrile, 4-[4-chloro- L-(3,4-Difluorophenyl)-2-mercapto-1H-imidazol-5-yl]-3,5-difluorobenzonitrile, 151284.doc -6- 201117722 4_[4_气小(3·fluorophenyl)-2-mercapto-1H-imidazol-5-yl]-3,5-difluorobenzoquinone, 4-[2_ desert-4-gas small (4-fluorophenyl; ) Η 咪唑 - imidazole _5 _ group; | _ 3,5-difluoro benzophenone, 2-gas small [4 · (difluoromethoxy) phenyl] _ 5 · (2 6 _ difluoro _ 4- methoxy Stupid base) methyl-1Η-ρmβ sit, 4-[2_chlorine small (4-chlorophenylidene-methyl-1Η-imidazole-5-yl)-3,5-difluoro 4_[2-Chloro-1·(3-fluorophenyl)_4_methyl·m_imidazole-5-yl]_3,5-difluoro-accumulate, 4-[4-chloro-1_(2,4 _Difluorophenyl)_2_methyl_1Η_imidazolyl]_3,5-difluorobenzonitrile, 4_[2_chloro-1_[3-(difluoromethoxy) Phenyl]-4-methyl-1Η-imidazol-5-yl]-3,5-difluorobenzonitrile, 4_[2'4-dichlorodifluoromethoxy)phenyl]-1Η-imidazole -5-yl; h3,5-difluorobenzonitrile, 4 [4-gaso(2-fluoro-4-indolyl)_2_indolyl_ih imidazole_5_yl]_3,5_two Fluorobenzonitrile, 4 [4 / odor-1-(2-fluoro_4_nonylphenyl)_2_indolyl-1H imidazolyl]_3,5 digas chitocarbonitrile, and 4_[^4- Dibromo-1-(3-fluorophenyl)-111-imidazol-5-yl]-3,5-difluorobenzonitrile. The composition of any one of clauses 1 to 8, wherein I, at least one of the agents, is selected from the group consisting of (bl) methyl strepamine Formate fungicide (b2) dicarboxyguanamine fungicide; 15l284.doc 201117722 (b3) demethylation inhibiting surface fungicide; (b4) aniline fungicide; (b5) version /? Folin fungicide; (b6) dish lipid biosynthesis inhibitor fungicide; (b7) several g of basket amine fungicide; (b8) hydroxy (2-amino) pyrimidine fungicide; (b9) aniline pyrimidine fungicide; (blO) N-phenylamine formate fungicide; (bll) bismuth inhibitor fungicide; (M2) phenyl steroid fungicide; Bl3) quinoline fungicide; (bl4) lipid peroxidation inhibitor fungicide; (bl5) melanin biosynthesis inhibitor _ reductase fungicide; (bl6) melanin biosynthesis inhibitor _ dehydratase kill Fungal agent; (bl7) hydroxyaniline fungicide; (M8) squalene-epoxidase inhibitor fungicide; (bl9) polyoxin (p〇iyoxin) fungicide; (b20) benzene Urea fungicide (b21) Inhibitor fungicides in the sputum; (b22) Benzoamide fungicides; (b23) «Antipyricides of uronic acid antibiotics; (b24) Hexopyranosyl antibiotics Fungicides; (b25) 0 glucosinolate (glUC〇pyran〇Syl) antibiotics: protein synthesis fungicides; (b26) glucopyranosides antibiotics: indolease and inositol Fungicide; σ 151284.doc 201117722 (b27) cyanoguanamine fungicide; (b28) amine phthalate fungicide; (b29) oxidative phosphorylation decoupling fungicide; (b30) organic Tin fungicide; (b31) carboxylic acid fungicide; (b32) aromatic heterocyclic fungicide; (b33) phosphonate fungicide; (b34) o-amine methotrexate fungicide (b35) Benzotriazine (benzotriazine) fungicide; (b36) Benzene-sulfonamide amine fungicide; (b37) Hydrazine ketone fungicide; (b38) Thiophene-carboxyguanamine a fungicide; (b39) a pyrimidin fungicide; (b40) a guanamine amide fungicide; (b41) a tetracycline antibiotic a fungicide; (b42) a thioaminyl phthalate fungicide; (b43) a benzoguanamine fungicide; (b44) a host plant defense fungicide; (b45) a multiplex fungicide (b46) the remaining non-component (a) and the fungicides of components (b1) to (b45); and the salts of the compounds (b1) to (b46). 10. The composition of claim 9 wherein component (b) comprises at least one fungicide and the fungicide is from each of two different groups selected from (bl) to (b46) Fungicide. 11. The composition of claim 1 wherein component (b) comprises at least one compound selected from the group consisting of phenyl-S-mercapto 151284.doc 201117722 (acibenzolar-S-methyl), Bataan (aldimoirph), amytoctradin, amisulbrom, anilazine, azaconazole, azoxystrobin, 右本达乐 ( Benalaxyl), benalaxyl-M, benodanil, benomyl, benthiavalicarb, benthiavalicarb-isopropyl , bethoxazin, binapacryl, biphenyl, bitertanol, bixafen, blasticidin-S, boscalid ), bromuconazole, bupirimate, carboxin, carpropamid, captafol, captan, carbendazim, Chlorogenb, chlorothalonil, chlozolinate, Clotrimazole, copper salts, cyazofamid, cyflufenamid, cymoxanil, cyproconazole, cyprodinil, proliferative Dichlofluanid, dilococymet, diclomezine, dicloran, diethofencarb, difenoconazole, diflumetorim, diterpenoid Dimethirimol, dimethomorph, dimoxystrobin, diniconazole, diniconazole-M, dinocap, dithianon ), dodemorph, dodine, edifenphos, enestroburin, ep. 151284.doc .10-201117722 (epoxiconazole), ethaboxam ( Ethaboxam ), ethirimol, etridiazole, famoxadone, fenamid〇ne, fenarimol, fenbuconazole, A0 Fenfuram, ring 醯Amine (fenhexamid), fenoxanil, seed dressing p (fenpiclonil), fenpropidin, fenpropimorph, fenpyrazamine, fentin acetate, triphenyltin chloride (fentin chloride), fentin hydroxide, ferbam, ferimzone, fluazinam, fludioxonil, flumetover, Flumorph, fluopicolide, fluoride. Fluopyram, fluoroimide, fluoxastrobin, fluquinconazole, flusilazole, flusulfamide, flutianil ), flutolanil, flutriafol, fluxapyroxad, folfet, fosetyl-aluminum, fuberidazole, bite creamer Furalaxy ), furametpyr, hexaconazole, hymexazol, guazatine, imazalil, imibenconazole, iminoctadine , iodocarb, ipconazole, iprobenfos, iprodione, iprovalicarb, isoprothiolane, isopyrazam Isotianil, gibberellin 151284.doc 201117722 (kasugamycin), kresoxim-methyl, manganzeb, mandipropamid, manganese (maneb), mepronil Meptyldinocap, metalaxyl, metalaxyl-M, metconazole, methasulfocarb, metiram, phenoxystrobin Metominostrobin), mepanipyrim, metrafenone, myclobutanil, naftifme, neo-asozin (ferric methanearsonate), nuarimol, Octilinone, ofurace, oressastrobin, oxadixyl, oxolinic acid, oxpoconazole, oxycarboxin ), oxytetracycline, penconazole, pencycuron, penflufen, 0-beta-penthiopyrad, pefurazoate, squaraine and Phosphorous acid and salts, phthalide, picoxystrobin, piperalin, polyoxin, probenazole, prochloraz Fighting (procymidon) e), propamocarb, propamocarb-hydrochloride, propiconazole, propineb, proquinazid, prothiocarb, Prothioconazole, pyraclostrobin, pyrametostrobin, pyraoxystrobin, pyrazophos 'pyribencarb, pyributicarb , Bifino 151284.doc -12· 201117722 (pyrifenox ), pyrimethan (pyrimethanil), pyriofenone, pyroquilon, pyrrinidin (pyrr〇lnitrin) quinomethionate, quinoxyfen ), quintozene, sedaxane, silthiofam, shixi fluoride. Simeconazole 'spiroxamine, streptomycin, sulfur, tebuconazole, tebufloquin, tecloftalam, tetrachloronitrobenzene (tecnazene), terbinafine, tetraconazole, thiabendazole, thifluzamide, thiophanate, thiophanate-methyl Thiram, tiadinil, tolclofos-methyl, t〇iyifluanid, triadimefon, triadimenol, imidazol (triazoxide), tricyclazole, tridemorph, triflumizole, tricyclazole, trifloxystrobin, triforine, urate (trimorphamide), triticonazole, uniconazole, validamycin, vaiifenaiate, vinclozolin, Zineb, thiram ( Ziram) Amine (zoxamide), N'-[4-[4-chloro-3-(trifluoromethyl)phenoxy]_2,5-diamidinophenyl]-N-ethyl-N-indenyl Amine amine, 5-gas-6-(2,4,6-trifluorophenyl)-7-(4-methylpiperidinyl)[1,2,4]triazole [l,5-a Pyrimidine, N-[2-[4-[[3-(4-chlorophenyl)-2-propan-1-yl]oxy]_3_methoxyphenyl]ethyl]-3-methyl -2-[(oxasulfonyl)amine]butanamine, N-[2-[4-[[3-(4-气笨151284.doc •13· 201117722 基)-2-propyne_ι_ Oxy]_3_indolylphenyl]ethyl]_3_methyl_2_[(ethanesulfonyl)amine]butanamine, 2-butoxy-6-iodo-3-propyl-4H-1 -benzopiperine-4-_,3_[5-(4-chlorophenyl)_2,3-dimethyl-3-isoxazolidinyl]difluoropyridine, 4-fluorophenyl N-[l -[[[l-(4-cyanophenyl)ethyl]sulfonyl]hydrazino]propyl]amine phthalic acid vinegar, N-[[(cyclopropylmethoxy)amino][6- (difluoromethoxy)-2,3-difluorophenyl]decene] phenethylamine, mercaptoimine)_N_methyl-2-[[[1-[3-(trifluoromethyl) Phenyl]ethoxy]imino]indenyl]phenethylamine, Ν'-[4·[4·gas-3_(tri-chaotic methyl)phenoxy]-2,5-dimercaptobenzene ]]-N-ethyl-N-biguanide, n-(4-chloro-2-nitrophenyl)-N-ethyl-4-methylbenzene Amine, 2_[[[[H2,6-diphenylphenyl H-indenyl-2-propen-1-yl]amine]oxy]methyl]-α-(nonoxyimino)-Ν· Methyl phenethylamine, 1_[(2-propenylthio)carbonyl]-2-(1-indolylethyl)-4-(2-indolylphenyl)-5-amine-1Η-.峻君-3-_, 5-ethyl-6-octyl-[1,2,4]tris[i,5-a]anilinium-7-alkylamine, pentyl N-[4-[ [[[(l-fluorenyl-1H-tetrasyl-5-yl)phenylmethylene]amine]oxy]indolyl]-2-thiazolyl]amine decanoate and pentyl N-[6- [[[[(l-曱基-1H·四哇_5_yl)phenylmethylene]amine]oxy]indenyl]_2 octa]] amide vinegar. 12. A composition comprising: (a) at least one compound selected from the group consisting of a compound of formula 1 as defined in claim 3, an N-oxide thereof and a salt thereof; and at least one invertebrate pest control compound or agent. 13. A composition comprising the composition of any one of claims 1 to 12 and at least one additional component selected from the group consisting of surfactants, solid diluents And a group of liquid diluents. 14. = (d) - a disease or method caused by a fungal pathogen of a plant or plant seed, comprising the administration of the plant or plant seed - a composition effective for fungicidal action 151284.doc 201117722 through item 13, which The composition is a composition as claimed in claim 1 . 15. Protecting Moistures from Burning Spot Blight Invasives - Fungicidal Effective Dosing Hearts (9) / Applying the Planting to the Heart Composition as Request Item 1 ^ Item 8 t-pin The composition, the towel component of which is selected from the group consisting of (10) amine/fosfolin-like fungicides, the fungicidal compound, the compound of the formula ι as defined in claim 1, the group oxide and the salt thereof. The restriction condition is that when Q1 is a phenyl group, a thienyl group, a thiazolyl group, a pyrazolyl imidazolyl group, a thiol group, a yl group, a benzyl group, a benzyl group or a phenyl group, each of which is optionally independently selected from 4 or more The substituent of R3a is substituted on the carbon atom ring member and the substituent selected from R4a is substituted on the nitrogen atom ring member; wherein each R is halogen, cyano group, hydroxyl group, nitro group, Ci_c7 alkyl group, c2-c7 group , C2-C7 block group, QC; i alkyl group, C2_C7 _ mentyl group, c3-c7 cycloalkyl group, c3-c7 ii cyclodyl group, C4_C1Q alkyl group, C4_CiG cycloalkyl group, C6_Ci4 cycloalkane ring Base, C3-C7 cycloalkoxy, c3-C7 halocycloalkoxy, CrC7:oxy, crc7 haloalkoxy, Crc6 alkylthio, C1-C7 4 sulfur-burning, Q-C7驴基, C^-C? Institute continued 醯, crc7 halogen Sulfosyl, crC7 halosulfonyl, CrC7 alkylamino, c2-C7 dialkylamino, (: 2-(:7-alkylcarbonyl, C2_C7-homoyloxycarbonyl, c2-C7-carcinylcarbonyl, C3 -C10 trialkylsulfonyl, -SCN, C(=S)NH2 or -XUZ; and 151284.doc 201117722 Each R4a is a cyano group, a CrC6 alkyl group, a C3-C6 alkenyl group, a C3-C6 fast group, C3-C6 cycloalkyl, Ci_C6 alkoxy, C2-C6 alkoxyalkyl, C2-C6 alkyl, C2-C6 alkoxy, C2-C6 alkylamino or c3-c6 bisalkylamine Base; then Q2 is phenyl, ° thiophene, 嗟β, 吼, 吼, 米, σ, σ, σ, 塔, σ, σ, 节, 节Substituents of 1 to 4 substituents independently selected from R 5 are substituted on a carbon atom ring member and a substituent selected from R 6 is substituted on a nitrogen atom ring member; the limitation is that the substituent group C2 on at least one carbon atom ring member a C7 cyanoalkyl group, a C2-C7 cyanoalkoxy group, an amine carbonyl group, a C2-C7 alkylamine carbonyl group or a C3-C7 dialkylamine carbonyl group, or a substituent on the nitrogen atom ring member is a crc6-alkyl group. 151284.doc -16- 201117722 IV. Designation of Representative Representatives (1) The representative representative of the case is: (none) (2) A brief description of the symbol of the representative figure: 5. If there is a chemical formula in this case, please disclose the chemical formula that best shows the characteristics of the invention: 151284.doc151284.doc