WO2015032280A1 - Aryl pyridine (pyrimidine) compound and use thereof - Google Patents

Aryl pyridine (pyrimidine) compound and use thereof Download PDF

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WO2015032280A1
WO2015032280A1 PCT/CN2014/084992 CN2014084992W WO2015032280A1 WO 2015032280 A1 WO2015032280 A1 WO 2015032280A1 CN 2014084992 W CN2014084992 W CN 2014084992W WO 2015032280 A1 WO2015032280 A1 WO 2015032280A1
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group
alkyl
halogenated
alkyloxy
hydrogen
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PCT/CN2014/084992
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French (fr)
Chinese (zh)
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刘长令
谢勇
宋玉泉
徐英
李轲轲
关爱莹
杨吉春
杨帆
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中国中化股份有限公司
沈阳化工研究院有限公司
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C07D213/85—Nitriles in position 3
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/60—1,4-Diazines; Hydrogenated 1,4-diazines
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/54—1,3-Diazines; Hydrogenated 1,3-diazines
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A01N43/74—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,3
    • A01N43/78—1,3-Thiazoles; Hydrogenated 1,3-thiazoles
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
    • A01N47/02—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having no bond to a nitrogen atom
    • A01N47/06—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having no bond to a nitrogen atom containing —O—CO—O— groups; Thio analogues thereof
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
    • A01N47/40—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having a double or triple bond to nitrogen, e.g. cyanates, cyanamides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/62—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to atoms of the carbocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Definitions

  • the invention belongs to the field of agricultural insecticide and acaricide.
  • it relates to an arylpyrimidine compound and the use thereof as an insecticidal and acaricidal agent in agriculture or other fields.
  • Chinese patent CN1938292 relates to acaricides such as:
  • U.S. Patent No. 2007004,750 relates to the following compounds as insecticidal and fungicides:
  • X is selected from an oxygen or nitrogen atom.
  • the object of the present invention is to provide an arylpyrimidine compound which can control pests and diseases at a small dose, which can be applied to agriculture to control crop pests, or in other fields.
  • the present invention provides an aromatic (pyrimidine) compound as shown in the general formula (I):
  • ⁇ selected from hydrogen, halogen, CN, N0 2 , fluorenyl, -C 12 fluorenyl, halogenated C r C 12 fluorenyl, 12 decyloxy, halo 12 decyloxy, cyano 12 decyloxy, 12 fluorene Sulfur, 3 ⁇ 4 generation, 12 thiol, -C 12 decyloxy Ci-Ci2 3 ⁇ 4 ⁇ 3 ⁇ 4 ⁇ ⁇ Ci-Ci2 C1-C12 3 ⁇ 4 ⁇ 3 ⁇ 4 Ci-Cn 3 ⁇ 4 ⁇ 43 ⁇ 43 ⁇ 43 ⁇ 4 C1-C12 3 ⁇ 4 ⁇ 3 ⁇ 4 ⁇ ⁇ Ci-Cn 3 ⁇ 43 ⁇ 43 ⁇ 43 ⁇ 4 -C 12 ⁇ , halogen -C 12 mercaptoamino, piperidinyl, tetrahydropyrrolyl, N-methylpiperazinyl, morpholinyl, C 2 -C 12 alkenyl, halogenated
  • R 2 is selected from the group consisting of hydrogen, halogen, cyano-C 12 fluorenyl, -C 12 fluorenyl, halo-C 12 fluorenyl, 12 decyloxy, halo 12 decyloxy, cyano 12 embankment oxy, thio embankment 12, substituting 12 3 ⁇ 4 thio embankment, embankment -C 12 group Ci-Ci2 3 ⁇ 4 ⁇ 3 ⁇ 4 ⁇ ⁇ Ci- Ci2 C1-C12 3 ⁇ 4 ⁇ 3 ⁇ 4 Ci-Cn 3 ⁇ 43 ⁇ 43 ⁇ 43 ⁇ 4 C1-C12 3 ⁇ 4 ⁇ 3 ⁇ 4 ⁇ ⁇ Ci-Cn 3 ⁇ 43 ⁇ 43 ⁇ 43 ⁇ 43 ⁇ 4 dC 12 fluorenyl, 12 fluorenylsulfinyl, -C 12 decylsulfonyl, C 3 -C 6 cyclodecyl or R 6;
  • R a, R b, R c , R d, R e R f, R g and R h each independently represents a hydrogen atom, alkyl with C r C 4, C r C 4 embankment halo, halo C r C 4 methoxy or -C 4 ⁇ oxycarbonyl; together with R c and R f may combine to form a saturated five-membered ring, six-membered ring or seven-membered ring;
  • Xi is selected from N or CR 3;
  • X 2 is selected from (CR 7 R 8 ) k , CO(CR 7 R 8 ) p , (CR 7 R 8 ) p CO, SOq(CR 7 R 8 )p or (CR 7 R 8 )pSOq;
  • Q is selected from phenyl or heteroaryl substituted by n each independently R 5 ;
  • R 5 is selected from the group consisting of halogen, CN, N0 2 , dC 12 fluorenyl, halogenated CC 12 fluorenyl, C 3 -C 12 cyclodecyl, 12 decyloxy, halo 12 decyloxy, 12 fluorenyl thio, halo a 12- thiol group, a C 2 -C 12 alkenyl group, a halogenated C 2 -C 12 alkyl group, a C 2 -C 12 alkynyl group, a halogenated C 2 -C 12 alkynyl group, a C 2 -C 12 alkenyloxy group , halo-C 2 -C 12 alkenyloxy, C 2 -C 12 alkynyl group, a halo-C 2 -C 12 alkynyloxy, alkylsulfinyl embankment 12, 12 on behalf of the embankment 3 ⁇ 4 alkyl
  • n is an integer selected from 0 to 5 (when n is 0, the corresponding position of R 5 is hydrogen, the same below); when n is greater than 1, it may be the same or different;
  • R 6 is selected from phenyl, benzoyl, phenoxycarbonyl, phenylaminocarbonyl, phenyl-C 6 fluorenyl, naphthyl which are unsubstituted or further substituted by 1 to 5 groups independently selected from the group consisting of , naphthyl dC 6 fluorenyl, heteroaryl, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroarylaminocarbonyl or heteroaryl C r C 6 fluorenyl: halogen, nitro, cyano, fluorenyl -C 12 fluorenyl, halogenated dC 12 fluorenyl, C 3 -C 12 cyclodecyl, 12 decyloxy, halo 12 decyloxy, 12 fluorenylthio, halo 1 2 thiol, C 2 -C 12 alkenyl, halo C 2 -C 12 alkenyl, C 2 -C
  • R 7, R 8 may be the same or different, are independently selected from hydrogen, cyano, SCN, formyl, embankment -C 12 group, a -C 12 alkyl with halo, alkoxy embankment 12, 12 3 ⁇ 4 embankment substituting group, 12 Sulfhydryl, 3 ⁇ 4 generation 12 thiol, -C 12 decylcarbonyl, -C 12 decyloxycarbonyl, C r C 12 decyloxycarbonyl-C 12 fluorenyl, 12 fluorenylsulfinyl, 12 fluorenyl Sulfonyl, cyano C r C 12 fluorenyl, hydroxy-C 12 fluorenyl, C 3 -C 12 cyclodecyl or -C 12 decylamino.
  • Preferred compounds in the present invention are: in the formula (I)
  • R 2 is selected from the group consisting of hydrogen, halogen, cyano dC 8 fluorenyl, dC 8 fluorenyl, halogenated CC 8 fluorenyl, CC 8 decyloxy, halogenated CC 8 decyloxy, cyano dC 8 decyloxy, CC 8 ⁇ thio, 3 ⁇ 4 ⁇ -03 ⁇ 4 ⁇ thio, CC 8 oxime CC 8 fluorenyl, 3 ⁇ 4 generation -03 ⁇ 4 ⁇ oxy CC 8 fluorenyl, dC 8 thiol CC 8 fluorenyl, ⁇ generation dC 8 ⁇ Sulfhydryl CC 8 fluorenyl, dC 8 decylsulfinyl, dC 8 decylsulfonyl, C 3 -C 8 cyclodecyl or R 6;
  • R a , R b , R c , R d , R e R f , R g and R h each independently represent a hydrogen atom, a CC 4 fluorenyl group, a halogenated CC 4 fluorenyl group, a halogenated CC 4 decyloxy group or dC. 4 ⁇ oxycarbonyl; ⁇ with R h or R c and R f together can form a saturated five-membered ring, six-membered ring or seven-membered ring;
  • Xi is selected from N or CR 3;
  • X 2 is selected from (CR 7 R 8 ) k , CO(CR 7 R 8 ) p , (CR 7 R 8 ) p CO, SOq(CR 7 R 8 )p or (CR 7 R 8 )pSOq;
  • R4 is selected from the group consisting of hydrogen, NH 2 , -C 8 fluorenyl, C r C 8 halodecyl, C r C 8 decyloxy, -C 8 halodecyloxy, phenyl or heteroaryl, said The phenyl or heteroaryl ring may also contain from 1 to 3 of the following substituent groups: F, Cl, Br, I, CN, N0 2 , CH 3 , C(CH 3 ) 3 , OCH 3 , C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 , OCH 2 CF 3 , CF 3 or OCF 3;
  • Q is selected from phenyl or heteroaryl groups which are independently substituted by n;
  • R 5 is selected from the group consisting of halogen, CN, N0 2 , -C 8 fluorenyl, halo-C 8 fluorenyl, 3 ⁇ 4-cyclodecyl, -C 8 decyloxy, halo dC 8 decyloxy, -C 8 ⁇ Thio, halogeno-C 8 thiol, C 2 -C 8 alkenyl, halogenated C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, halogenated C 2 -C 8 alkynyl, 3 ⁇ 4- Alkenyloxy, halogenated C 2 -Q ⁇ oxy, 3 ⁇ 4 8 alkynyloxy, halogenated C 2 -C 8 alkyne , -C 8 decylsulfinyl, dC 8 decylsulfinyl, dC 8 decylsulfonyl, 3 ⁇ 4 -C
  • n is selected from an integer from 0 to 5; when n is greater than 1, it may be the same or different;
  • R 6 is selected from phenyl, benzoyl, phenoxycarbonyl, phenylaminocarbonyl, phenyl-C 6 fluorenyl, naphthyl which are unsubstituted or further substituted by 1 to 5 groups independently selected from the group consisting of , naphthyl dC 6 fluorenyl, heteroaryl, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroarylaminocarbonyl or heteroaryl C r C 6 fluorenyl: halogen, nitro, cyano, fluorenyl , dC 8 fluorenyl, halogenated dC 8 fluorenyl, 3 ⁇ 4 8 cyclodecyl, 8 methoxy, ⁇ methoxy, 8 thiol, ⁇ thiol, C 2 - C 8 alkenyl, halo C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, halo C 2
  • R 7, R 8 may be the same or different, are independently selected from hydrogen, cyano, SCN, formyl, alkyl with the CC 8, 8-halo alkyl with the CC, the CC 8 embankment group, substituting 8 3 ⁇ 4 embankment group, dC 8 Sulfhydryl, 3 ⁇ 4th generation 8 thiol, dC 8 fluorenylcarbonyl, dC 8 decyloxycarbonyl, dC 8 decyloxycarbonyl dC 8 fluorenyl, dC 8 decylsulfinyl, dC 8 decylsulfonyl, Cyano dC 8 fluorenyl, hydroxy dC 8 fluorenyl, C 3 -C 8 cyclodecyl or CC 8 decylamino.
  • R 2 is selected from the group consisting of hydrogen, halogen, CN, N0 2 , CONH 2 , cyano C r C 4 fluorenyl, -C 4 fluorenyl, halogenated C r C 4 fluorenyl, -C 4 decyloxy, halo- C 4 embankment, cyano group C r C 4 embankment, dC 4 embankment alkylthio, halo embankment -C 4 alkylthio, Ci-C 4 Ci-C 4 3 ⁇ 4 ⁇ 3 ⁇ 4 ⁇ ⁇ Ci-C 4 3 ⁇ 43 ⁇ 43 ⁇ 4, 3 ⁇ 4 Ci -C 4 3 ⁇ 43 ⁇ 43 ⁇ 4 Ci-C 4 3 ⁇ 43 ⁇ 43 ⁇ 4 Ci-C 4 3 ⁇ 43 ⁇ 43 ⁇ 43 ⁇ 4 Ci-C 4 3 ⁇ 43 ⁇ 43 ⁇ 4 Ci-C 4 3 ⁇ 43 ⁇ 43 ⁇ 4 Ci-C 4 3 ⁇ 43 ⁇ 43 ⁇ 4 Ci-C 4 3 ⁇ 43 ⁇ 43 ⁇ 4 Ci-C 4 3 ⁇ 43 ⁇ 43 ⁇ 4
  • R a, R b, R c , R d, R e R f, R g and R h each independently represents a hydrogen atom, alkyl with C r C 4, C r C 4 embankment halo, halo C r C 4 methoxy or -C 4 ⁇ oxycarbonyl; together with R c and R f may combine to form a saturated five-membered ring, six-membered ring or seven-membered ring;
  • Xi is selected from N or CR 3;
  • X 2 is selected from (CR 7 R 8 ) k , CO(CR 7 R 8 ) p , (CR 7 R 8 ) p CO, SOq(CR 7 R 8 )p or (CR 7 R 8 )pSOq;
  • R4 is selected from the group consisting of hydrogen, NH 2 , C r C 4 fluorenyl, dC 4 halo fluorenyl, C r C 4 decyloxy, -C 4 halodecyloxy, phenyl or heteroaryl, said benzene
  • the base or heteroaryl ring may also contain from 1 to 3 of the following substituent groups: F, Cl, Br, I, CN, N0 2 , CH 3 , C(CH 3 ) 3 , OCH 3 , C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 , OCH 2 CF 3 , CF 3 or OCF 3 ;
  • Q is selected from phenyl or heteroaryl groups which are independently substituted by n;
  • R 5 is selected from the group consisting of halogen, CN, N0 2 , dC 4 fluorenyl, halo-C 4 fluorenyl, C 3 -C 6 cyclodecyl, C r C 4 decyloxy, halogenated C r C 4 decyloxy -C 4 thiol, halo-C 4 thiol, C 2 -C 4 alkenyl, halogenated C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, halogenated C 2 -C 4 Alkynyl, C 2 -C 4 alkenyloxy, halo C 2 -C 4 alkenyloxy, C 2 -C 4 alkynyloxy, halo C 2 -C 4 alkynyloxy, C r C 4 fluorenyl Sulfonyl, halogenated C r C 4 fluorenylsulfinyl, C r
  • n is selected from an integer from 0 to 5; when n is greater than 1, R 5 may be the same or different;
  • R 6 is selected from phenyl, benzoyl, phenoxycarbonyl, phenylaminocarbonyl, phenyl CC 6 fluorenyl, naphthyl, which are unsubstituted or further substituted by 1 to 5 groups independently selected from the group consisting of Naphthyl dC 6 fluorenyl, heteroaryl, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroarylaminocarbonyl or heteroaryl dC 6 fluorenyl: halogen, nitro, cyano, fluorenyl, dC 4 Mercapto, halogenated dC 4 fluorenyl, C 3 -C 6 cyclodecyl, dC 4 decyloxy, 3 ⁇ 4 generation 4 methoxy, dC 4 thiol, ⁇ CC 4 thiol, C 2 -C 4 alkenyl, halo C 2 -C 4 alkenyl, C 2 -C
  • R 7 and R 8 may be the same or different and are respectively selected from the group consisting of hydrogen, cyano, SCN, formyl, C r C 4 fluorenyl, halogeno-C 4 fluorenyl, -C 4 decyloxy, ⁇ methoxy , -C 4 thiol, 3 ⁇ 4 thiol, C r C 4 fluorenylcarbonyl, -C 4 decyloxycarbonyl, -C 4 decyloxycarbonyl-C 4 fluorenyl, -C 4 fluorenyl Sulfonyl, -C 4 decylsulfonyl, cyano C r C 4 fluorenyl, hydroxy-C 4 fluorenyl, C 3 -C 6 cyclodecyl or -C 4 decylamino.
  • ! ⁇ selected from hydrogen, halogen, CN, N0 2 , C r C 4 fluorenyl, halogenated C r C 4 fluorenyl, C r C 4 decyloxy, halo-C 4 # ⁇ 3 ⁇ 4 Ci-C 4 Ci-C 4 3 ⁇ 43 ⁇ 43 ⁇ 4,3 ⁇ 4 Ci-C 4 3 ⁇ 43 ⁇ 43 ⁇ 4 ⁇ ⁇ Ci-C 4 Ci-C 4 C 3 -C 6 ring fluorenyl or R 6; m is selected from an integer from 0 to 5; when m is greater than 1, ! ⁇ can be the same or different;
  • R 2 is selected from the group consisting of hydrogen, halogen, CN, C r C 4 fluorenyl, halo-C 4 fluorenyl, C r C 4 decyloxy, halogenated C r C 4 decyloxy, Cyano C r C 4 decyloxy, C r C 4 decyloxy C r C 4 fluorenyl, 3 ⁇ 4 generation 14 4 oxy-C 4 fluorenyl, C 3 -C 6 cyclodecyl or R 6 ;
  • R a, R b, R c , R d, R e R f, R g and R h each independently represents a hydrogen atom, alkyl with C r C 4, C r C 4 embankment halo, halo C r C 4 methoxy or -C 4 ⁇ oxycarbonyl; together with R c and R f may combine to form a saturated five-membered ring, six-membered ring or seven-membered ring;
  • Xi is selected from N or CR 3 ;
  • X 2 is selected from (CR 7 R 8 ) k , CO(CR 7 R 8 ) p , (CR 7 R 8 ) p CO, SOq(CR 7 R 8 )p or (CR 7 R 8 )pSOq;
  • Q is selected from phenyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, quinolinyl, thienyl, benzothienyl, furyl, benzofuranyl, substituted by n each independently R 5 , Mercapto, pyrrolyl, oxazolyl, imidazolyl, benzoxazolyl, benzothiazolyl, benzimidazolyl, benzopyrazinyl, thiazolyl, pyrazolyl, triazolopyrimidinyl, imidazole And pyridazinyl, imidazopyridyl or pyridazinone;
  • R 5 is selected from the group consisting of halogen, CN, N0 2 , CC 4 fluorenyl, C 3 -C 6 cyclodecyl, CC 4 halodecyl, CC 4 decyloxy, CC 4 halodecyloxy, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 2 -C 4 alkenyloxy, C 2 -C 4 alkynyloxy, COCH 3 , COC 2 H 5 , C0 2 CH 3 , C0 2 C 2 H 5 , S0 2 CH 3 or S0 2 C 2 H 5 ;
  • n is selected from an integer from 0 to 5; when n is greater than 1, R 5 may be the same or different;
  • R 6 is selected from the group consisting of phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl, 2,6- Dichloro-4-trifluoromethylphenyl, benzyl, 4-chlorobenzyl, 4-tert-butylbenzyl, 4-trifluoromethylbenzyl, phenethyl, 2-pyridyl, 3-chloro -2-pyridyl, 3,5-dichloro-2-pyridyl, 3,5,6-trichloro-2-pyridyl, 5-trifluoromethyl-2-pyridyl, 5-methyl-2 Pyridyl, 3-chloro-5-cyano-2-pyridyl, 3-chloro-5-trifluoromethyl-2-pyridyl, 2-pyridylmethyl, 2-chloro-5-pyridinemethyl, 3-Chloro-5-trifluoromethyl-2-
  • R 7 and R 8 may be the same or different and are respectively selected from the group consisting of hydrogen, cyano, SCN, formyl, C r C 4 fluorenyl, halogeno-C 4 fluorenyl, -C 4 decyloxy, ⁇ methoxy , -C 4 thiol, 3 ⁇ 4 thiol, C r C 4 fluorenylcarbonyl, -C 4 decyloxycarbonyl, -C 4 decyloxycarbonyl-C 4 fluorenyl, -C 4 fluorenyl Sulfonyl, -C 4 decylsulfonyl, cyano C r C 4 fluorenyl, hydroxy-C 4 fluorenyl, C 3 -C 6 cyclodecyl or -C 4 decylamino.
  • Still further preferred compounds of the invention are: in formula (I)
  • R 2 is selected from the group consisting of hydrogen, F, Cl, Br, I, CN, C r C 4 fluorenyl, halogenated dC 4 fluorenyl, C r C 4 decyloxy, halo-C 4 ⁇ Oxy, C 3 -C 6 cyclodecyl or R6;
  • R a, R b, R c , R d, R e R f, R g and R h each independently represents a hydrogen atom, alkyl with C r C 4, C r C 4 embankment halo, halo C r C 4 methoxy or -C 4 ⁇ oxycarbonyl; together with R c and R f may combine to form a saturated five-membered ring, six-membered ring or seven-membered ring; Xi is selected from N or CR 3 ;
  • X 2 is selected from the group consisting of CH 2 , CO, S0 2 , CH(CH 3 ), CH(CN), COCH 2 , CH 2 CH 2 , CH 2 CO or SO 2 CH 2 ;
  • R 4 is selected from the group consisting of hydrogen, NH 2 , C r C 4 fluorenyl or C r C 4 halogenated fluorenyl
  • Y is selected from -CO-, -S0 2 -, -CH 2 - or -COCH(CH(CH 3 ) 2 )- ;
  • x is selected from 0 or 1;
  • Q is selected from phenyl, pyridyl, pyrimidinyl, thiazolyl, benzoxazolyl, benzopyrazinyl or pyridazinone groups substituted by n each independently R 5 ;
  • R 5 is selected from the group consisting of F, Cl, Br, I, CN, N0 2 , C r C 4 fluorenyl, halogenated C r C 4 fluorenyl, C r C 4 decyloxy, halo-C 4 decyloxy, C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 or OCH 2 CF 3 ;
  • R 6 is selected from the group consisting of phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl, 2,6- Dichloro-4-trifluoromethylphenyl, benzyl, 4-chlorobenzyl, 4-tert-butylbenzyl, 4-trifluoromethylbenzyl, phenethyl, 2-pyridyl, 3-chloro -2-pyridyl, 3,5-dichloro-2-pyridyl, 3,5,6-trichloro-2-pyridyl, 5-trifluoromethyl-2-pyridyl, 5-methyl-2 Pyridyl, 3-chloro-5-cyano-2-pyridyl, 3-chloro-5-trifluoromethyl-2-pyridyl, 2-pyridylmethyl, 2-chloro-5-pyridinemethyl, 3-Chloro-5-trifluoromethyl-2-
  • n is selected from 1, 2, 3, 4 or 5;
  • n is selected from 1, 2, 3 or 4;
  • n is selected from 1, 2 or 3;
  • n is selected from 1 or 2;
  • R 5 may be the same or different
  • the mercapto group described by R 2 and R 5 may further preferably be methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl or t-butyl, halofluorenyl.
  • a trifluoromethyl group, a difluoromethyl group, a monofluoromethyl group or a chloromethyl group may be further preferred
  • a methoxy group may further preferably be a methoxy group
  • a halogenated fluorenyloxy group may further preferably be a trifluoromethoxy group or a trifluoroethoxy group.
  • the cyclo or fluoromethoxy group, the cyclodecyl group may further preferably be a cyclopropyl group, a cyclobutyl group, a cyclopentyl group or a cyclohexyl group.
  • Ri is selected from the group consisting of hydrogen, F, Cl, Br, I, CN, N0 2 , CC 4 fluorenyl, halogenated CC 4 fluorenyl, CC 4 decyloxy or halogenated CC 4 decyloxy; m is selected from 0 to 5 Integer; when m is greater than 1, ! ⁇ can be the same or different;
  • R 2 is selected from the group consisting of hydrogen, F, Cl, Br, I, CN, CC 4 fluorenyl, halogenated CC 4 fluorenyl, CC 4 decyloxy, halogenated CC 4 methoxy _R6;
  • R a , R b , R c , R d , R e R f , R g and R h each independently represent a hydrogen atom, a CC 4 fluorenyl group, a halogenated CC 4 fluorenyl group, a halogenated CC 4 decyloxy group or dC. 4 ⁇ oxycarbonyl; ⁇ together with R h or R c and R f together can form a saturated six-membered ring;
  • Xi is selected from N or CR 3 ;
  • R3 is selected from hydrogen or CN
  • X 2 is selected from CH 2 or CO;
  • Y is selected from -CO- or -CH 2 - ;
  • X is selected from 0 or 1;
  • Q is selected from phenyl, pyridyl, pyrimidinyl or thiazolyl substituted by n each independently R 5 ;
  • R 5 is selected from the group consisting of F, Cl, Br, I, CN, N0 2 , dC 4 fluorenyl, halo-C 4 fluorenyl, -C 4 decyloxy, halo dC 4 decyloxy, C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 or OCH 2 CF 3 ;
  • R 6 is selected from the group consisting of phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl, 2,6- Dichloro-4-trifluoromethylphenyl, benzyl, 4-chlorobenzyl, 4-tert-butylbenzyl, 4-trifluoromethylbenzyl or phenethyl, 2-pyridyl, 3-chloro -2-pyridyl, 3,5-dichloro-2-pyridyl, 3,5,6-trichloro-2-pyridyl, 5-trifluoromethyl-2-pyridyl, 5-methyl-2-pyridyl, 3-chloro-5-cyano-2-pyridyl, 3-chloro-5-trifluoromethyl-2-pyridyl, 2-pyridylmethyl, 2-chloro- 5-pyridylmethyl, 3-chloro-5-triflu
  • n is selected from 1, 2, 3 or 4 or 5;
  • n is selected from 1, 2 or 3 or 4;
  • n is selected from 1, 2 or 3;
  • n is selected from 1 or 2;
  • R 5 may be the same or different
  • the mercapto group described by R 2 and R 5 may further preferably be methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl or t-butyl, halofluorenyl.
  • a trifluoromethyl group, a difluoromethyl group, a monofluoromethyl group or a chloromethyl group may be further preferred
  • a methoxy group may further preferably be a methoxy group
  • a halogenated fluorenyloxy group may further preferably be a trifluoromethoxy group or a trifluoroethoxy group. Base or monofluoromethoxy.
  • ! ⁇ selected from hydrogen, F, Cl, Br, I, CN, N0 2 , C r C 4 fluorenyl or halogenated C r C 4 fluorenyl C r C 4 decyloxy or halogenated C r C 4 decyloxy m is selected from an integer from 0 to 5; when m is greater than 1, ! ⁇ can be the same or different;
  • R 2 is selected from the group consisting of hydrogen, F, Cl, Br, I, CN, C r C 4 fluorenyl, halogenated C r C 4 fluorenyl or R 6;
  • R a , R b , R c R d , R e , R f , R g and R h each independently represent a hydrogen atom
  • Xi is selected from CR 3 ;
  • R 3 is selected from CN
  • X 2 is selected from CH 2 or CO;
  • Y is selected from -CO- or -CH 2 - ; x is selected from 0 or 1;
  • Q is selected from phenyl, pyridyl, pyrimidinyl or thiazolyl substituted by n each independently R 5 ;
  • R 5 is selected from the group consisting of F, Cl, Br, I, CN, N0 2 , CC 4 fluorenyl or halogenated CC 4 fluorenyl, CC 4 decyloxy, halogenated dC 4 decyloxy, C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 or OCH 2 CF 3 ;
  • R 6 is selected from phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl or 2,6- Dichloro-4-trifluoromethylphenyl, benzyl, 4-chlorobenzyl, 4-tert-butylbenzyl, 4-trifluoromethylbenzyl or phenethyl; wherein, when Q is selected from phenyl When n is selected from 1, 2, 3, 4 or 5;
  • n is selected from 1 or 2, 3 or 4;
  • n is selected from 1 or 2 or 3;
  • n is selected from 1 or 2;
  • R 5 may be the same or different
  • the fluorenyl group described by R 2 and R 5 may further preferably be a methyl group, an ethyl group or a tert-butyl group, and the halogenated fluorenyl group may further preferably be a trifluoromethyl group, a difluoromethyl group, a monofluoromethyl group or a chloro group.
  • the methoxy group may further preferably be a methoxy group, and the halogenated methoxy group may further preferably be a trifluoromethoxy group.
  • ! ⁇ selected from hydrogen, F, Cl, Br, I, CN, N0 2 , C r C 4 fluorenyl or halogenated C r C 4 fluorenyl C r C 4 decyloxy or halogenated C r C 4 decyloxy m is selected from an integer from 0 to 5; when m is greater than 1, ! ⁇ can be the same or different;
  • R 2 is selected from the group consisting of hydrogen, F, Cl, Br, I, CN, C r C 4 fluorenyl, halogenated C r C 4 fluorenyl or R 6;
  • R a , R b , R c R d , R e , R f , R g and R h each independently represent a hydrogen atom
  • Xi is selected from CR 3 ;
  • R 3 is selected from CN
  • X 2 is selected from CH 2 or CO;
  • Y is selected from -CO- or -CH 2 - ; x is selected from 0 or 1; Q is selected from phenyl, pyridyl, pyrimidinyl or thiazolyl substituted by n each independently R 5 ;
  • R 5 is selected from the group consisting of F, Cl, Br, I, CN, N0 2 , C r C 4 fluorenyl, halogenated C r C 4 fluorenyl, C r C 4 decyloxy, halogenated dC 4 decyloxy, S0 2 CH 3 or OCH 2 CF 3 ;
  • R 6 is selected from phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl or 2,6- Dichloro-4-trifluoromethylphenyl.
  • n is selected from 1, 2 or 3;
  • n is selected from 1 or 2 or 3;
  • n is selected from 1 or 2;
  • n is selected from 1 or 2;
  • R 5 may be the same or different
  • the fluorenyl group described by R 2 and R 5 may further preferably be a methyl group, an ethyl group or a tert-butyl group, and the halogenated fluorenyl group may further preferably be a trifluoromethyl group, a difluoromethyl group, a monofluoromethyl group or a chloro group.
  • the methoxy group may further preferably be a methoxy group, and the halogenated methoxy group may further preferably be a trifluoromethoxy group.
  • m is selected from an integer from 0 to 5; when m is greater than 1, ! ⁇ can be the same or different;
  • R 2 is selected from the group consisting of hydrogen, CC 4 fluorenyl, halogenated CC 4 fluorenyl or R 6;
  • Xi is selected from CR 3 ;
  • R 3 is selected from CN
  • X 2 is selected from CO;
  • Y is selected from -CO- or -CH 2 - ; x is selected from 0;
  • Q is selected from pyridyl substituted by 1 R 5 ;
  • R 5 is selected from the group consisting of hydrogen, F, Cl, Br, I, CN, N0 2 , CC 4 fluorenyl or halogenated CC 4 fluorenyl;
  • R 6 is selected from phenyl
  • the fluorenyl group described by R 2 and R 5 may further preferably be a methyl group, an ethyl group or a tert-butyl group, and the halogenated fluorenyl group may further preferably be a trifluoromethyl group, a difluoromethyl group, a monofluoromethyl group or a chloro group. base.
  • Halogen refers to fluorine, chlorine, bromine or iodine.
  • Mercapto A linear or branched fluorenyl group such as methyl, ethyl, propyl, isopropyl, n-butyl or t-butyl.
  • Cyclodecyl a substituted or unsubstituted cyclic fluorenyl group such as cyclopropyl, cyclopentyl or cyclohexyl. Substituents such as methyl, halogen and the like.
  • Halogenated fluorenyl a straight or branched fluorenyl group in which a hydrogen atom may be partially or completely replaced by a halogen atom, for example, chloromethyl, dichloromethyl, trichloromethyl, fluoromethyl , difluoromethyl, trifluoromethyl and the like.
  • Cyano fluorenyl a linear or branched fluorenyl group, the hydrogen atom on these fluorenyl groups may be partially substituted by a cyano group, for example, -CH 2 CN, -CH 2 CH 2 CN, -CH 2 C(CH 3 2 CN -CH 2 CH(CN) 2 and the like.
  • Alkoxy A linear or branched fluorenyl group attached to the structure via an oxygen atom.
  • Cyanomethoxy group The cyanoguanidino group is bonded to the structure via an oxygen atom bond.
  • Alkoxyalkyl A decyloxy group is attached to the structure via a thiol group.
  • Halogenated fluorenyl fluorenyl The hydrogen atom on the fluorenyl group of the fluorenyl fluorenyl group may be partially or completely substituted by a halogen atom. Such as ClCH 2 CH 2 OCH 2 -.
  • Alkoxycarbonyl a decyloxy group is attached to the structure via a carbonyl group. Such as CH 3 OCO-, CH 3 CH 2 OCO-.
  • Halogenated methoxy group a linear or branched decyloxy group, and a hydrogen atom on these decyloxy groups may be partially or completely substituted by a halogen atom.
  • Thiothio group A linear or branched fluorenyl group bonded to a structure via a sulfur atom bond.
  • Thiothio group The sulfonium group is attached to the structure via a thiol group. Such as CH 3 SCH 2 -.
  • Halogenated thiol group a linear or branched thiol group, and a hydrogen atom on these fluorenyl groups may be partially or completely substituted by a halogen atom.
  • Halogenated sulfhydryl fluorenyl The halo sulfhydryl group is attached to the structure via a fluorenyl group.
  • Mercaptoamino a linear or branched fluorenyl group bonded to the structure via a nitrogen atom.
  • Mercaptoaminocarbonyl such as CH 3 NHCO-, CH 3 CH 2 NHCO-.
  • Halogenated fluorenylaminocarbonyl The hydrogen atom on the fluorenyl group of the fluorenylaminocarbonyl group may be partially or completely substituted by a halogen atom. Such as CF 3 NHCO-.
  • Halogenated mercaptoamino group a linear or branched mercaptoamino group, and a hydrogen atom on these mercapto groups may be partially or completely substituted by a halogen atom.
  • Alkenyl a linear or branched olefin such as a vinyl group, a 1-propenyl group, a 2-propenyl group and a different butenyl, pentenyl and hexenyl isomer.
  • Alkenyl groups also include polyenes such as 1,2-propadienyl and 2,4-hexadienyl.
  • Haloalkenyl group a linear or branched olefin in which a hydrogen atom on these alkenyl groups may be partially or completely substituted by a halogen atom.
  • Alkynyl a straight or branched acetylenic group such as ethynyl, 1-propynyl, 2-propynyl and the different butynyl, pentynyl and hexynyl isomers.
  • the alkynyl group also includes a group consisting of a plurality of triple bonds, such as 2,5-hexadiynyl.
  • Haloalkynyl group a linear or branched alkyne, and a hydrogen atom on these alkynyl groups may be partially or completely substituted by a halogen atom.
  • Alkenyloxy A linear or branched olefin that is bonded to the structure via an oxygen atom.
  • Haloalkenyloxy a linear or branched alkenyloxy group, and a hydrogen atom on these alkenyloxy groups may be partially or completely substituted by a halogen atom.
  • Alkynyloxy A linear or branched acetylenic group attached to the structure via an oxygen atom.
  • Haloalkynyloxy a straight or branched alkynyloxy group in which a hydrogen atom may be partially or completely substituted by a halogen atom.
  • Mercaptocarbonyl The fluorenyl group is attached to the structure via a carbonyl group such as CH 3 CO-, CH 3 CH 2 0-.
  • Halogenated fluorenylcarbonyl The hydrogen atom on the fluorenyl group of the fluorenylcarbonyl group may be partially or completely substituted by a halogen atom such as CF 3 CO-.
  • Mercaptosulfinyl A linear or branched fluorenyl group is attached to the structure via a sulfinyl group (-SO-), such as a methylsulfinyl group.
  • Halogenated fluorenylsulfinyl a linear or branched fluorenylsulfinyl group in which a hydrogen atom on the fluorenyl group may be partially or completely substituted by a halogen atom.
  • Mercaptosulfonyl A linear or branched fluorenyl group is attached to the structure via a sulfonyl group (-S0 2 -), such as a methylsulfonyl group.
  • Halogenated fluorenylsulfonyl a linear or branched fluorenylsulfonyl group in which a hydrogen atom on the fluorenyl group may be partially or completely substituted by a halogen atom.
  • Phenoxycarbonyl A phenoxy group is attached to the structure via a carbonyl group, such as PhOCO-.
  • Phenylaminocarbonyl A phenylamino group is attached to the structure via a carbonyl group, such as PhNHCO-.
  • Phenylfluorenyl A phenyl group is attached to the structure via a thiol group, such as benzyl, phenethyl, and the like.
  • Naphthylfluorenyl A naphthyl group is attached to the structure via a fluorenyl group, such as naphthylmethyl, naphthylethyl, and the like.
  • Heteroaryl The heteroaryl group referred to in the present invention is a five-membered or six-membered ring aryl group having one or more N, 0, S hetero atoms.
  • heteroarylcarbonyl A heteroaryl group is attached to the structure via a carbonyl group, such as a picolinyl group, a pyrimidinyl group, a pyrazolyl group.
  • Heteroaryloxycarbonyl A heteroaryloxy group is attached to the structure via a carbonyl group.
  • Heteroarylaminocarbonyl A heteroarylamino group is attached to the structure via a carbonyl group.
  • Heteroaryl fluorenyl A heteroaryl group is attached to the structure via a thiol group, such as furylmethyl, pyridylethyl, and the like.
  • 1-261 of 17 represents the compound number 3133-.3393.
  • Table 38 In the general formula (1-17), when (R n ⁇ -Cl- ⁇ CFg, the substituent (R 5 ) n is shown in Table 35, which in turn corresponds to 4699-4781 of Table 35, and represents the compound number 4948- 5030.
  • Table 41 In the formula (1-17), when (R m 4-CN, the substituent (R 5 ) n is shown in Table 35, which in turn corresponds to 4699-4781 of Table 35, and represents the compound number 5197-5279.
  • Table 99 which in turn corresponds to 6623-6630 of Table 99, represents the compound number 7039-7046.
  • Table 162 General formula (1 The substituent Xi is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 7127-7150.
  • Table 169 In the formula (1-24), when (R ⁇ n ⁇ H, the substituent (R 5 ) n is shown in Table 17, which in turn corresponds to 1-261 of Table 17, and represents the compound number 8006-8266.
  • Table 171 In the general formula (1-24), when (R m ⁇ CFg, the substituent (R 5 ) n is shown in Table 17, which in turn corresponds to Table 17 1-261, representing compound number 8528-8788.
  • Table 187: In the formula (1-26), when (R n ⁇ A-CF ⁇ (R 5 ) n 2-Cl, the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, representing a compound The number is 9356-9379.
  • the compound number is 12748-12768.
  • R 2 CF 3
  • R 4 H
  • X 1 C-CN
  • X 2 CO
  • Y CH 2
  • the compound of the formula (I) of the present invention can be produced by the following method, and each group has the same meaning as defined above unless otherwise stated.
  • the compound of the formula (I) can be obtained by reacting the formula (II) with the formula (III) in a suitable solvent under basic conditions.
  • L is a leaving group selected from halogen, methanesulfonyl or p-toluenesulfonyl.
  • the reaction is carried out in a suitable solvent, and is suitably acetonitrile, toluene, xylene, benzene, hydrazine, hydrazine-dimethylformamide, methylene chloride, trichloromethane or acetone.
  • Suitable bases may be selected from, for example, potassium hydroxide, sodium hydroxide, sodium carbonate, potassium carbonate, sodium hydrogencarbonate, triethylamine or pyridine.
  • the reaction temperature may range from room temperature to the boiling point of the solvent, usually from 20 to 130 °C.
  • the reaction time is from 30 minutes to 20 hours, usually from 1 to 10 hours.
  • the compound of the formula (II) can be obtained by reacting a compound represented by the formula (IV) with (V) N-Boc-piperazine (commercially available) to obtain a compound (11-1), which is obtained by de Boc.
  • the formula (IV) is commercially available or prepared according to known methods.
  • the preparation method of the intermediate ⁇ -2 mainly has the following two types:
  • the compounds of the general formula (I) exhibit high activity against harmful insects and mites in the fields of agriculture, civil and animal technology. Therefore, another technical solution of the present invention relates to the use of a compound of the general formula (I) as an insecticidal and acaricidal agent in agriculture and other fields - the use of the compound of the general formula (I) for the preparation of an insecticide and acaricide use.
  • the compounds of the general formula (I) are active against important species of the following families: Plutella xylostella, Mythimna, Myzus persicae, Aphis citrifolia, T. cinnabarinus, T. cinnabarinus, C. citrifolia, Citrus grandiflora, etc. ⁇ , ⁇ , etc.
  • the compounds of formula (I) are less toxic to many beneficial insects and aphids, mammals, fish, birds, and are not phytotoxic.
  • the above compounds are advantageously used to protect crops, livestock and stocks important in agriculture and horticulture, as well as the environment in which humans are often exposed to pests and mites.
  • the amount of the compound varies depending on various factors such as the compound used, the pre-protected crop, the type of the pest, the degree of infection, the climatic conditions, the method of application, and the dosage form employed.
  • a dose of 10 grams to 5 kilograms of compound per hectare provides adequate control.
  • composition comprising one or more compounds of formula (I). Therefore, another technical solution of the present invention further comprises an insecticidal and acaricidal composition comprising as an active ingredient a compound of the formula (I) and an agriculturally acceptable carrier, the weight of the active ingredient in the composition The content of the fraction is 0.5-90%.
  • the composition may be used in the form of a dry powder, a wettable powder, an emulsifiable concentrate, a microemulsion, a paste, a granule, a solution, a suspending agent, etc.:
  • the choice of the type of composition depends on the particular application.
  • composition is prepared in a known manner, for example by diluting or dissolving the active substance with a solvent medium and/or a solid diluent, optionally in the presence of a surfactant.
  • Useful solid diluents or carriers are, for example, silica, kaolin, bentonite, talc, diatomaceous earth, dolomite, calcium carbonate, magnesium oxide, chalk, clay, synthetic silicate, attapulgite, sepiolite.
  • useful liquid diluents are, for example, aromatic organic solvents (mixtures of xylene or mercaptobenzene, chlorobenzene, etc.), paraffin (petroleum), alcohols (methanol, propanol, butanol, octanol) , glycerol), esters (ethyl acetate, isobutyl acetate, etc.), ketones (cyclohexanone, acetone, acetophenone, isophorone, ethyl amyl ketone, etc.), amides ( ⁇ , ⁇ - dimethylformamide, hydrazine-methylpyrrolidone, etc.).
  • aromatic organic solvents mixture of xylene or mercaptobenzene, chlorobenzene, etc.
  • paraffin paraffin
  • alcohols methanol, propanol, butanol, octanol
  • esters ethyl acetate, isobuty
  • Useful surfactants are sodium, calcium, triethylamine, such as mercaptosulfonate, mercaptoarylsulfonate, polyoxyethylene nonylphenol, polyoxyethylene ester of sorbitol, lignosulfonate, and the like. Or triethanolamine salt.
  • composition may also contain special additives for specific purposes such as binders such as gum arabic, polyvinyl alcohol, polyvinylpyrrolidone and the like.
  • binders such as gum arabic, polyvinyl alcohol, polyvinylpyrrolidone and the like.
  • the concentration of the active ingredient in the above composition may vary widely depending on the active ingredient, its intended use, environmental conditions, and the type of preparation employed. Generally, the concentration of the active ingredient ranges from 1 to 90%, preferably from 5 to 50%.
  • compositions may be added to the compositions, such as other acaricides/insecticides, fungicides, plant growth regulators, antibiotics, herbicides, fertilizers.
  • active ingredients compatible with the compounds of formula (I) may be added to the compositions, such as other acaricides/insecticides, fungicides, plant growth regulators, antibiotics, herbicides, fertilizers.
  • suspending agent The active ingredient content in the commonly used formula is 5%-35%.
  • the water, the main drug, the dispersing agent, the suspending agent and the antifreezing agent are added to a sand mill and ground to prepare a suspension.
  • Preparation of water emulsion The original drug, solvent and emulsifier are added together to dissolve into a uniform oil phase. Water, antifreeze, and the like are mixed together to form a uniform aqueous phase. The aqueous phase is added to the oil phase or the oil phase is added to the aqueous phase under high-speed agitation to form a water-dispersible water emulsion.
  • the aqueous emulsion active ingredient of the present invention is generally present in an amount of from 5% to 15%.
  • the compound of the present invention can be dissolved in one or several mixed solvents, and an emulsifier is added to enhance the dispersion of the compound in water.
  • Preparation of wettable powder According to the formulation requirements, the original drug, various surfactants and solid diluents are thoroughly mixed and pulverized by an ultrafine pulverizer to obtain a wettable property of a predetermined content (for example, 10% to 40%). Powder products.
  • the compounds of the present invention can be combined with finely divided solid powders such as clays, inorganic silicates, carbonates, and A mixture of wetting agents, binders and/or dispersing agents.
  • Preparation of water-dispersible granules mixing and pulverizing the original drug with powdered solid diluent, wetting spreader and binder, adding water and kneading, adding granulator with 10 to 100 mesh screen Granulation is carried out, followed by drying and sieving (by sieve range).
  • the original drug, dispersing agent, disintegrating agent and wetting agent and solid diluent may also be added to a sand mill, ground with water as a suspending agent, and then spray-dried and granulated, usually in a content of 20%. — 30% granulated product.
  • Potassium carbonate weighed 13.9 g (0.089 mol) of p-chlorophenylboronic acid into it, added a catalytic amount of tetrakistriphenylphosphine palladium, heated to reflux, reaction for 4 h, after TLC monitoring reaction, cooled to room temperature, pumping After filtration, the cake was washed three times with 100 mL of toluene, and the filtrate was evaporated to dryness to give a brown solid, 18.3 g, yield: 68.3%.
  • Example 8 30% wettable powder
  • the compound 5035 and the other components are thoroughly mixed, and the resulting suspension concentrate is diluted with water to obtain a desired concentration of the diluent.
  • Example 10 60% water dispersible granules
  • Kaolin is made up to 100%
  • a mixed solvent of 2.5 mL of acetone/methanol (1:1) was added to a weighing flask containing 3 mg of the test compound (100% purity), and the mixture was thoroughly dissolved by stirring, and 2.5 mL was added to contain 2%.
  • the Tween 80 was allowed to stand in tap water, and after stirring, a solution of 600 mg/L of the test compound was obtained in 5 mL.
  • the test targets were: armyworm, diamondback moth, peach aphid.
  • the test insects were sprayed by Airbrush spray method, in which the mortality of the test insects was investigated 3 days after the treatment of the armyworm and the diamondback moth; the mortality of the test insects was investigated within 2 days of the spray treatment.
  • the lethal rate of 9155 and other insects is more than 70%.
  • the lethal rate of compounds 5573, 5769, 13775, 13796, 13826 and so on is 100%; 5705, 5789, 13456, 13435, 13477, 13645, 13871, 14128, etc.
  • the mortality rate is greater than 70%.
  • Example 12 Determination of virulence in the cinnabar
  • the mother liquor was made of acetone, and the concentration of the series was diluted according to the experimental design with static tap water containing 0.1% Tween 80.
  • Two leaves of true leafy bean seedlings were inoculated, and the cinnabar was inoculated into a sputum and the base was investigated.
  • the mixture was sprayed with a hand-held sprayer, and each treatment was repeated three times. After treatment, it was placed in a standard observation room. After 72 hours, the survival number was counted and the mortality was calculated.
  • the lethal rate of 13435, 13456, 13477, 13624 and other cinnabar mites was 100%, the lethal rate of 4869 to cinnabarinus was 95%, and the lethal rate of 5510 to cinnabarinus was 97%.
  • the mortality rate of the compounds 4891, 5035, 5053, 5057, 5706, 5552, 5663, 5664, 5684, 5685, 5705, 5789, 13414, 13624, etc. on the cinnabar leafhopper is 100%. 5573 pairs of cinnabar leaves The mortality rate of cockroach was 98%, and the lethal rate of compound 5041 to cinnabarinus was 95%.
  • the activity comparison test of some compounds with the control agents and intermediates was carried out, and the test results are shown in Table 288.
  • the control compounds KCl to KC25 were all made by the inventors, among which KC1, KC3, KC4, KC5, KC7, KC8, KC10, KC17, KC18 and KC19 are similar to some compounds in US2013072497, and KC15 is a compound reported in CN102015627.
  • KC20, KC21, and KC22 are compounds reported in CN101381342.

Abstract

Disclosed in the present invention is aryl pyridine (pyrimidine) compound having a structure as shown by the general formula (I) below, wherein the substituents in the formula are as defined in the description. The compound of formula I displays relatively high activities on harmful insects, mites and eggs in the fields of agriculture, and civil and animal technology, especially having better activities on harmful mites such as Tetranychus cinnabarinus etc., and can obtain very good effects at a very low dose.

Description

芳基吡 (嘧)啶类化合物及其用途  Arylpyrimidine compounds and uses thereof
技术领域 Technical field
本发明属农用杀虫杀螨剂领域。 具体地涉及一种芳基吡 (嘧)啶类化合物， 以及使用它们 在农业或其他领域中作为杀虫杀螨剂的用途。  The invention belongs to the field of agricultural insecticide and acaricide. In particular, it relates to an arylpyrimidine compound and the use thereof as an insecticidal and acaricidal agent in agriculture or other fields.
背景技术 Background technique
中国专利 CN1938292涉及如 杀螨剂：  Chinese patent CN1938292 relates to acaricides such as:
Figure imgf000002_0001
Figure imgf000002_0001
美国专利 US2007004750涉及如下 的化合物作为杀虫、 杀菌剂:
Figure imgf000002_0002
U.S. Patent No. 2007004,750 relates to the following compounds as insecticidal and fungicides:
Figure imgf000002_0002
中国专利 CN101332198报道了一种 6-芳基 -3-取代羰基 -吡啶类化合物及其盐作为抗肿瘤 药物的应用， 其通式为：  Chinese patent CN101332198 reports the use of a 6-aryl-3-substituted carbonyl-pyridine compound and a salt thereof as an antitumor drug, which has the general formula:
Figure imgf000002_0003
Figure imgf000002_0003
其中， X选自氧或氮原子。  Wherein X is selected from an oxygen or nitrogen atom.
现有技术中报道的化合物， 与本发明的化合物结构有很大差别。  The compounds reported in the prior art are quite different from the structures of the compounds of the present invention.
发明内容 Summary of the invention
本发明的目的在于提供一种在很小的剂量下就可以控制虫害螨害的芳基吡 (嘧)啶类化合 物， 它可应用于农业上以防治作物虫害螨害， 或在其他领域中作为杀虫杀螨剂的用途。  The object of the present invention is to provide an arylpyrimidine compound which can control pests and diseases at a small dose, which can be applied to agriculture to control crop pests, or in other fields. The use of insecticides and acaricides.
本发明的技术方案如下：  The technical solution of the present invention is as follows:
本发明提供一种芳 (嘧)啶类化合物， 如通式 (I)所示：  The present invention provides an aromatic (pyrimidine) compound as shown in the general formula (I):
Figure imgf000002_0004
Figure imgf000002_0004
式中:  In the formula:
！^选自氢、 卤素、 CN、 N02、 巯基、 -C12垸基、 卤代 CrC12垸基、 12垸氧基、 卤 代 12垸氧基、 氰基 12垸氧基、 12垸硫基、 ¾代 12垸硫基、 -C12垸氧基 Ci-Ci2 ¾υ¾ \ ί Ci-Ci2 C1-C12 ¾υ¾ Ci-Cn ¾¾¾¾¾ C1-C12 ¾υ¾ \ ί Ci-Cn ¾¾¾¾¾ -C12垸基、 卤代 -C12垸基氨基、 哌啶基、 四氢吡咯基、 N-甲基哌嗪基、 吗啉基、 C2-C12 烯基、 卤代 C2-C12烯基、 ¾ 12烯氧基、 卤代 ¾ 12烯氧基、 C2-C12炔基、 卤代 C2-C12炔基、 ¾ 12炔氧基、 卤代 ¾ 12炔氧基、 12垸基亚磺酰基、 -C12垸基磺酰基、 C3-C12环垸 基、 ¾代 12垸基亚磺酰基、 ¾代 -C12垸基磺酰基、 d-C12垸氧基羰基、 ¾代 -C12 垸基羰基、 12垸基羰基氧基、 12垸基羰基氨基、 d-C12垸基磺酰基氧基、 12垸 氧基 12垸氧基、 -C12垸氧基羰基 -C12垸基、 d-C12垸氧基羰基氨基、 CrC12垸氧基 羰基 ^垸氧基、 CHO、 C02H、 C02Na、 C02NH4、 NR7R8、 C(=0)NR7R8、 OC(=0)NR7R8、 C(=S)NR7R8、 S02NR7R8或 R6; m选自 0至 5的整数； 当 m大于 1时， ！^可相同或不同； R2选自氢、 卤素、 氰基 -C12垸基、 -C12垸基、 卤代 -C12垸基、 12垸氧基、 卤 代 12垸氧基、 氰基 12垸氧基、 12垸硫基、 ¾代 12垸硫基、 -C12垸氧基 Ci-Ci2 ¾υ¾ \ ί Ci-Ci2 C1-C12 ¾υ¾ Ci-Cn ¾¾¾¾¾ C1-C12 ¾υ¾ \ ί Ci-Cn ¾¾¾¾¾ d-C12垸基、 12垸基亚磺酰基、 -C12垸基磺酰基、 C3-C6环垸基或 R6; ! ^ selected from hydrogen, halogen, CN, N0 2 , fluorenyl, -C 12 fluorenyl, halogenated C r C 12 fluorenyl, 12 decyloxy, halo 12 decyloxy, cyano 12 decyloxy, 12 fluorene Sulfur, 3⁄4 generation, 12 thiol, -C 12 decyloxy Ci-Ci2 3⁄4υ3⁄4 \ ί Ci-Ci2 C1-C12 3⁄4υ3⁄4 Ci-Cn 3⁄4⁄43⁄43⁄43⁄4 C1-C12 3⁄4υ3⁄4 \ ί Ci-Cn 3⁄43⁄43⁄43⁄43⁄4 -C 12垸, halogen -C 12 mercaptoamino, piperidinyl, tetrahydropyrrolyl, N-methylpiperazinyl, morpholinyl, C 2 -C 12 alkenyl, halogenated C 2 -C 12 alkenyl, 3⁄4 12 olefin Oxy, halo 3⁄4 12 alkenyloxy, C 2 -C 12 alkynyl, halo C 2 -C 12 alkynyl, 3⁄4 12 alkynyloxy, halo 3⁄4 12 alkynyloxy, 12 fluorenylsulfinyl, embankment -C 12 arylsulfonyl group, C 3 -C 12 cyclic alkyl with, ¾ substituting embankment 12 alkylsulfinyl, ¾ behalf -C 12 alkyl with a sulfonyl group, dC 12 embankment butoxycarbonyl, ¾ -C 12 generations Mercaptocarbonyl, 12 fluorenylcarbonyloxy, 12 fluorenylcarbonylamino, dC 12 decylsulfonyloxy, 12 decyloxy 12 decyloxy, -C 12 decyloxycarbonyl-C 12 decyl, dC 12垸oxycarbonylamino, C r C 12 methoxycarbonylcarbonyl, CHO, C0 2 H, C0 2 Na, C0 2 NH 4 , NR 7 R 8 , C(=0)NR 7 R 8 , OC (=0)NR 7 R 8 , C(=S)NR 7 R 8 , S0 2 NR 7 R 8 or R 6; m is selected from an integer from 0 to 5; when m is greater than 1, ! ^ may be the same or different; R 2 is selected from the group consisting of hydrogen, halogen, cyano-C 12 fluorenyl, -C 12 fluorenyl, halo-C 12 fluorenyl, 12 decyloxy, halo 12 decyloxy, cyano 12 embankment oxy, thio embankment 12, substituting 12 ¾ thio embankment, embankment -C 12 group Ci-Ci2 ¾υ¾ \ ί Ci- Ci2 C1-C12 ¾υ¾ Ci-Cn ¾¾¾¾¾ C1-C12 ¾υ¾ \ ί Ci-Cn ¾¾¾¾¾ dC 12 fluorenyl, 12 fluorenylsulfinyl, -C 12 decylsulfonyl, C 3 -C 6 cyclodecyl or R 6;
Ra、 Rb、 Rc、 Rd、 Re Rf、 Rg和 Rh各自独立的表示氢原子、 CrC4垸基、 卤代 CrC4垸 基、 卤代 CrC4垸氧基或 -C4垸氧羰基； 与 一起或者 Rc与 Rf—起可以结合形成饱和 的五元环、 六元环或者七元环； R a, R b, R c , R d, R e R f, R g and R h each independently represents a hydrogen atom, alkyl with C r C 4, C r C 4 embankment halo, halo C r C 4 methoxy or -C 4垸 oxycarbonyl; together with R c and R f may combine to form a saturated five-membered ring, six-membered ring or seven-membered ring;
Xi选自 N或 CR3; Xi is selected from N or CR 3;
R3选自氢、 CN、 N02、 CONHNH2、 C(=0)NR7R8、 C(=S)NR7R8、 -C12垸氧基羰基、 C(=0)N=CR7R8、 C02NR7R8、 C02N=CR7R8、 CONHN=CR7NR7R8或 C(=0)NR7N=CR7R8; R3 is selected from the group consisting of hydrogen, CN, N0 2 , CONHNH 2 , C(=0)NR 7 R 8 , C(=S)NR 7 R 8 , -C 12垸oxycarbonyl, C(=0)N=CR 7 R 8 , C0 2 NR 7 R 8 , C0 2 N=CR 7 R 8 , CONHN=CR 7 NR 7 R 8 or C(=0)NR 7 N=CR 7 R 8 ;
X2选自 (CR7R8)k、 CO(CR7R8)p、 （CR7R8)pCO、 SOq(CR7R8)p或 (CR7R8)pSOq; X 2 is selected from (CR 7 R 8 ) k , CO(CR 7 R 8 ) p , (CR 7 R 8 ) p CO, SOq(CR 7 R 8 )p or (CR 7 R 8 )pSOq;
k选自 1、 2或 3; p选自 0、 1、 2或 3; q选自 0、 1或 2;  k is selected from 1, 2 or 3; p is selected from 0, 1, 2 or 3; q is selected from 0, 1 or 2;
选自氢、 NH2、 C C12垸基、 C C12卤代垸基、 12垸氧基、 d-C12卤代垸氧基、 苯基或杂芳基， 所述的苯基或杂芳基环上还可以含有 1-3个下述取代基团： F、 Cl、 Br、 I、 CN、 N02、 CH3、 C(CH3)3、 OCH3、 C02CH3、 C02CH2CH3、 S02CH3、 OCH2CF3、 CF3或 OCF3; Selected from hydrogen, NH 2 , CC 12 fluorenyl, CC 12 halodecyl, 12 decyloxy, dC 12 halodecyloxy, phenyl or heteroaryl, on the phenyl or heteroaryl ring It may also contain 1-3 substituent groups: F, Cl, Br, I, CN, N0 2 , CH 3 , C(CH 3 ) 3 , OCH 3 , C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 , OCH 2 CF 3 , CF 3 or OCF 3;
Y 选自 -CO-、 -SO2-、 -(CR7R8)t-、 -CH=CHCHR7-、 - (CR7R8)tCO-、 -CH=CHCO-、Y is selected from -CO-, -SO2-, -(CR 7 R 8 ) t -, -CH=CHCHR 7 -, - (CR 7 R 8 ) t CO-, -CH=CHCO-,
-S(CR7R8)tCO-、 -N(CR7R8)tCO-、 -0(CR7R8)tCO-、 -S(CR7R8)tS02-、 -N(CR7R8)tS02-、 -0(CR7R8)tS02-、 -CONR7CO-、 -S02NR7C(=S) -、 -S02NR7C(=0)-、 -CONR7C(=S) -、 -NR7CO (CR7R8)t- -CO(CR7R8)t- -NR7CO-或 -NR7C(=S)-; t选自 0、 1或 2; x选自 0或 1; -S(CR 7 R 8 ) t CO-, -N(CR 7 R 8 ) t CO-, -0(CR 7 R 8 ) t CO-, -S(CR 7 R 8 ) t S0 2 -, - N(CR 7 R 8 ) t S0 2 -, -0(CR 7 R 8 ) t S0 2 -, -CONR 7 CO-, -S0 2 NR 7 C(=S) -, -S0 2 NR 7 C( =0) -, -CONR 7 C(=S) -, -NR 7 CO (CR 7 R 8 )t- -CO(CR 7 R 8 )t- -NR 7 CO- or -NR 7 C(=S - t is selected from 0, 1 or 2; x is selected from 0 or 1;
Q选自被 n个各自独立的 R5取代的苯基或杂芳基； Q is selected from phenyl or heteroaryl substituted by n each independently R 5 ;
R5选自卤素、 CN、 N02、 d-C12垸基、 卤代 C C12垸基、 C3-C12环垸基、 12垸氧基、 卤代 12垸氧基、 12垸硫基、卤代 12垸硫基、 C2-C12烯基、卤代 C2-C12録基、 C2-C12 炔基、 卤代 C2-C12炔基、 C2-C12烯氧基、 卤代 C2-C12烯氧基、 C2-C12炔氧基、 卤代 C2-C12炔 氧基、 12垸基亚磺酰基、 ¾代 12垸基亚磺酰基、 d-C12垸基磺酰基、 ¾代 12垸 基磺酰基、 d-C12垸基羰基、 ¾代 d-C12垸基羰基、 12垸基羰基氧基、 12垸基羰基 氨基、 d-C12垸基磺酰基氧基、 C C12垸氧基羰基、 C C12垸氧基 C C12垸氧基、 12垸 氧基羰基 d-C12垸基、 d-C12垸氧基羰基氨基、 C C12垸氧基羰基 C C12垸氧基、 COR8、 C02R7、 CONR7R8、 NR7R8、 NR7COR8、 NR7COR8、 NR8C02R7、 SOqR8、 S02NR7R8、 芳基、 杂芳基、 芳胺基、 芳垸基氧基、 芳氧基或杂芳胺基， 所述的芳基、 杂芳基、 芳胺基、 芳垸基 氧基、芳氧基或杂芳胺基环上的氢还可以进一步被 1-4个下述基团所取代： 卤素、 CN、 N02、 d-C12垸基、 CrC12卤代垸基、 d-C12卤代垸氧基、 d-C12垸氧基、 -C12垸氧基羰基或 -C12 垸基磺酰基； R 5 is selected from the group consisting of halogen, CN, N0 2 , dC 12 fluorenyl, halogenated CC 12 fluorenyl, C 3 -C 12 cyclodecyl, 12 decyloxy, halo 12 decyloxy, 12 fluorenyl thio, halo a 12- thiol group, a C 2 -C 12 alkenyl group, a halogenated C 2 -C 12 alkyl group, a C 2 -C 12 alkynyl group, a halogenated C 2 -C 12 alkynyl group, a C 2 -C 12 alkenyloxy group , halo-C 2 -C 12 alkenyloxy, C 2 -C 12 alkynyl group, a halo-C 2 -C 12 alkynyloxy, alkylsulfinyl embankment 12, 12 on behalf of the embankment ¾ alkylsulfinyl, dC 12 embankment arylsulfonyl group, ¾ 12 generations embankment arylsulfonyl, dC 12 alkyl with a carbonyl group, ¾ substituting dC 12 alkyl with a carbonyl group, 12 embankment carbonyl group, 12 embankment arylcarbonylamino, dC 12 embankment sulfonyloxy group, the CC 12垸 oxycarbonyl, CC 12 decyloxy CC 12 decyloxy, 12 methoxycarbonyl dC 12 fluorenyl, dC 12 decyloxycarbonylamino, CC 12 decyloxycarbonyl CC 12 decyloxy, COR 8 , C0 2 R 7 , CONR 7 R 8 , NR 7 R 8 , NR 7 COR 8 , NR 7 COR 8 , NR 8 C0 2 R 7 , SOqR 8 , S0 2 NR 7 R 8 , aryl, heteroaryl, aromatic An amino group, an arylmethyloxy group, an aryloxy group or a heteroarylamino group, said aryl group, heteroaryl group, arylamino group, aryl fluorenyl group Group, aryloxy or heteroaryl amine hydrogens on the ring may further be substituted with 1-4 of the following radicals: halogen, CN, N0 2, dC 12 embankment group, C r C 12 alkyl with haloalkyl, dC 12 halomethoxy, dC 12 decyloxy, -C 12 decyloxycarbonyl or -C 12 decylsulfonyl;
n选自 0至 5的整数 （当 n为 0时， R5的相应位置为氢， 下同）； 当 n大于 1时， 可 相同或不同； n is an integer selected from 0 to 5 (when n is 0, the corresponding position of R 5 is hydrogen, the same below); when n is greater than 1, it may be the same or different;
R6选自未取代的或被 1-5个独立选自以下基团进一步取代的苯基、苯甲酰基、苯氧基羰 基、 苯基胺基羰基、 苯基 -C6垸基、 萘基、 萘基 d-C6垸基、 杂芳基、 杂芳基羰基、 杂芳 基氧基羰基、 杂芳基胺基羰基或杂芳基 CrC6垸基： 卤素、 硝基、 氰基、 巯基、 -C12垸基、 卤代 d-C12垸基、 C3-C12环垸基、 12垸氧基、 卤代 12垸氧基、 12垸硫基、 卤代 12垸硫基、 C2-C12烯基、 卤代 C2-C12烯基、 C2-C12炔基、 卤代 C2-C12炔基、 C2-C12烯氧 基、 卤代 C2-C12烯氧基、 C2-C12炔氧基、 卤代 C2-C12炔氧基、 -C12垸基亚磺酰基、 卤代 12垸基亚磺酰基、 -C12垸基磺酰基、 ¾代 CrC12垸基磺酰基、 -C12垸基羰基、 卤代 d-C12垸基羰基、 12垸基羰基氧基、 12垸基羰基氨基、 -C12垸基磺酰基氧基、 d-C12 垸氧基羰基、 -C12垸氧基 12垸氧基、 d-C12垸氧基羰基 -C12垸基、 Q-C12垸氧基羰 基氨基、 CrC12垸氧基羰基 CrC12垸氧基、 CHO、C02H、C02Na、C02NH4、NR7R8、C(=0)NR7R8、 OC(=0)NR7R8、 C(=S)NR7R8或 S02NR7R8; R 6 is selected from phenyl, benzoyl, phenoxycarbonyl, phenylaminocarbonyl, phenyl-C 6 fluorenyl, naphthyl which are unsubstituted or further substituted by 1 to 5 groups independently selected from the group consisting of , naphthyl dC 6 fluorenyl, heteroaryl, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroarylaminocarbonyl or heteroaryl C r C 6 fluorenyl: halogen, nitro, cyano, fluorenyl -C 12 fluorenyl, halogenated dC 12 fluorenyl, C 3 -C 12 cyclodecyl, 12 decyloxy, halo 12 decyloxy, 12 fluorenylthio, halo 1 2 thiol, C 2 -C 12 alkenyl, halo C 2 -C 12 alkenyl, C 2 -C 12 alkynyl, halo C 2 -C 12 alkynyl, C 2 -C 12 alkenyloxy, halo C 2 -C 12 Alkenyloxy, C 2 -C 12 alkynyloxy, halogenated C 2 -C 12 alkynyloxy, -C 12 -mercaptosulfinyl, halogenated 12 embankment sulfinyl group, a sulfonyl group -C 12 alkyl with, ¾ substituting C r C 12 alkyl with a sulfonyl group, a carbonyl group -C 12 alkyl with, dC 12 alkyl with haloalkyl carbonyl, carbonyloxy group embankment 12, 12 embankment Carbocarbonylamino, -C 12 decylsulfonyloxy, dC 12 decyloxycarbonyl, -C 12 decyloxy 12 decyloxy, dC 12 decyloxycarbonyl-C 12 fluorenyl, QC 12 decyloxycarbonyl Amino, C r C 12 decyloxycarbonyl C r C 12 decyloxy, CHO, C0 2 H, C0 2 Na, C0 2 NH 4 , NR 7 R 8 , C(=0)NR 7 R 8 , OC( =0) NR 7 R 8 , C(=S)NR 7 R 8 or S0 2 NR 7 R 8 ;
R7、 R8可相同或不同， 分别选自氢、 氰基、 SCN、 甲酰基、 -C12垸基、 卤代 -C12 垸基、 12垸氧基、 ¾代 12垸氧基、 12垸硫基、 ¾代 12焼硫基、 -C12垸基 羰基、 -C12垸氧基羰基、 CrC12垸氧基羰基 -C12垸基、 12垸基亚磺酰基、 12垸 基磺酰基、 氰基 CrC12垸基、 羟基 -C12垸基、 C3-C12环垸基或 -C12垸基氨基。 R 7, R 8 may be the same or different, are independently selected from hydrogen, cyano, SCN, formyl, embankment -C 12 group, a -C 12 alkyl with halo, alkoxy embankment 12, 12 ¾ embankment substituting group, 12 Sulfhydryl, 3⁄4 generation 12 thiol, -C 12 decylcarbonyl, -C 12 decyloxycarbonyl, C r C 12 decyloxycarbonyl-C 12 fluorenyl, 12 fluorenylsulfinyl, 12 fluorenyl Sulfonyl, cyano C r C 12 fluorenyl, hydroxy-C 12 fluorenyl, C 3 -C 12 cyclodecyl or -C 12 decylamino.
本发明中较为优选的化合物为： 通式 (I)中  Preferred compounds in the present invention are: in the formula (I)
！^选自氢、 卤素、 CN、 N02、 巯基、 CrC8垸基、 卤代 -C8垸基、 -C8垸氧基、 卤 代 ^-^垸氧基、 氰基 -0¾垸氧基、 -C8^硫基、 ¾代 8垸硫基、 -C8垸氧基 -C8 垸基、 ^代^-^垸氧基 -C8垸基、 -C8垸硫基 -C8垸基、 ^代^-^焼硫基 8垸 基、 卤代 CrC8垸基氨基、 哌啶基、 四氢吡咯基、 N-甲基哌嗪基、 吗啉基、 C2-C8烯基、 卤 代 C2-C8烯基、 ¾ 8烯氧基、 卤代 C2-C 氧基、 C2-C8炔基、 卤代 C2-C8炔基、 C2-C8炔氧 基、 卤代 ^-^炔氧基、 ^-^垸基亚磺酰基、 d-C8垸基磺酰基、 ¾ 8环垸基、 卤代 -C8 垸基亚磺酰基、 代 d-C8垸基磺酰基、 d-C8垸氧基羰基、 ¾代 d-C8垸基羰基、 d-C8垸 基羰基氧基、 d-C8垸基羰基氨基、 d-C8垸基磺酰基氧基、 C C8垸氧基 C C8垸氧基、 d-C8 垸氧基羰基 d-C8垸基、 d-C8垸氧基羰基氨基、 d-C8垸氧基羰基 8垸氧基、 CHO、C02H、 C02Na、 C02NH4、 NR7R8、 C(=0)NR7R8、 OC(=0)NR7R8、 C(=S)NR7R8、 S02NR7R8或 R6; m选自 0至 5的整数； 当 m大于 1时， 可相同或不同； ! ^Selected from hydrogen, halogen, CN, N0 2 , fluorenyl, C r C 8 fluorenyl, halo-C 8 fluorenyl, -C 8 decyloxy, halo^-oxycarbonyl, cyano-03⁄4垸alkoxy, ^ -C 8 alkylthio, thio embankment ¾ substituting 8, -C 8 group -C 8 alkyl with embankment, substituting ^ ^ - ^ embankment embankment -C 8 alkoxy group, alkylthio embankment -C 8 - C 8 fluorenyl, ^^^^ thiol 8 fluorenyl, halogenated C r C 8 decylamino, piperidinyl, tetrahydropyrrolyl, N-methylpiperazinyl, morpholinyl, C 2 -C 8 alkenyl, halo C 2 -C 8 alkenyl, 3⁄8 alkenyloxy, halo C 2 -Coxy, C 2 -C 8 alkynyl, halo C 2 -C 8 alkynyl, C 2 -C 8 alkynyl group, a halo ^ - ^ alkynyloxy, ^ - ^ embankment sulfinyl, dC 8-ylsulfonyl embankment, ¾ 8 cycloalkyl group embankment, halo embankment -C 8 alkylsulfinyl, Generation dC 8 alkyl with sulfonyl group, dC 8 embankment butoxycarbonyl, ¾ substituting dC 8 alkyl with a carbonyl group, dC 8 alkyl with carbonyl group, dC 8 embankment arylcarbonylamino, dC 8 embankment sulfonyloxy group, CC 8 embankment Oxyl CC 8 decyloxy, dC 8 decyloxycarbonyl dC 8 fluorenyl, dC 8 decyloxycarbonylamino, dC 8 decyloxycarbonyl 8 decyloxy, CHO, C0 2 H, C0 2 Na, C0 2 NH 4 , NR 7 R 8 , C(=0)NR 7 R 8 , OC(=0)NR 7 R 8 , C(=S)NR 7 R 8 , S0 2 NR 7 R 8 or R 6 ; m is selected from an integer from 0 to 5; when m is greater than 1, it may be the same or different ;
R2选自氢、 卤素、 氰基 d-C8垸基、 d-C8垸基、 卤代 C C8垸基、 C C8垸氧基、 卤代 C C8垸氧基、 氰基 d-C8垸氧基、 C C8垸硫基、 ¾代 -0¾垸硫基、 C C8垸氧基 C C8垸 基、 ¾代 -0¾垸氧基 C C8垸基、 d-C8垸硫基 C C8垸基、 ^代 d-C8垸硫基 C C8垸基、 d-C8垸基亚磺酰基、 d-C8垸基磺酰基、 C3-C8环垸基或 R6; R 2 is selected from the group consisting of hydrogen, halogen, cyano dC 8 fluorenyl, dC 8 fluorenyl, halogenated CC 8 fluorenyl, CC 8 decyloxy, halogenated CC 8 decyloxy, cyano dC 8 decyloxy, CC 8垸thio, 3⁄4代-03⁄4垸thio, CC 8 oxime CC 8 fluorenyl, 3⁄4 generation -03⁄4 垸oxy CC 8 fluorenyl, dC 8 thiol CC 8 fluorenyl, ^ generation dC 8垸Sulfhydryl CC 8 fluorenyl, dC 8 decylsulfinyl, dC 8 decylsulfonyl, C 3 -C 8 cyclodecyl or R 6;
Ra、 Rb、 Rc、 Rd、 Re Rf、 Rg和 Rh各自独立的表示氢原子、 C C4垸基、 卤代 C C4垸 基、 卤代 C C4垸氧基或 d-C4垸氧羰基； ！^与 Rh—起或者 Rc与 Rf—起可以结合形成饱和 的五元环、 六元环或者七元环； R a , R b , R c , R d , R e R f , R g and R h each independently represent a hydrogen atom, a CC 4 fluorenyl group, a halogenated CC 4 fluorenyl group, a halogenated CC 4 decyloxy group or dC. 4垸 oxycarbonyl; ^ with R h or R c and R f together can form a saturated five-membered ring, six-membered ring or seven-membered ring;
Xi选自 N或 CR3; Xi is selected from N or CR 3;
R3选自氢、 CN、 N02、 CONHNH2、 C(=0)NR7R8、 C(=S)NR7R8、 d-C12垸氧基羰基、R 3 is selected from the group consisting of hydrogen, CN, N0 2 , CONHNH 2 , C(=0)NR 7 R 8 , C(=S)NR 7 R 8 , dC 12 decyloxycarbonyl,
C(=0)N=CR7R8、 C02NR7R8、 C02N=CR7R8、 CONHN=CR7NR7R8或 C(=0)NR7N=CR7R8; C(=0)N=CR 7 R 8 , C0 2 NR 7 R 8 , C0 2 N=CR 7 R 8 , CONHN=CR 7 NR 7 R 8 or C(=0)NR 7 N=CR 7 R 8 ;
X2选自 (CR7R8)k、 CO(CR7R8)p、 （CR7R8)pCO、 SOq(CR7R8)p或 (CR7R8)pSOq; X 2 is selected from (CR 7 R 8 ) k , CO(CR 7 R 8 ) p , (CR 7 R 8 ) p CO, SOq(CR 7 R 8 )p or (CR 7 R 8 )pSOq;
k选自 1、 2或 3; p选自 0、 1、 2或 3; q选自 0、 1或 2;  k is selected from 1, 2 or 3; p is selected from 0, 1, 2 or 3; q is selected from 0, 1 or 2;
R4选自氢、 NH2、 -C8垸基、 CrC8卤代垸基、 CrC8垸氧基、 -C8卤代垸氧基、 苯基 或杂芳基， 所述的苯基或杂芳基环上还可以含有 1-3个下述取代基团： F、 Cl、 Br、 I、 CN、 N02、 CH3、 C(CH3)3、 OCH3、 C02CH3、 C02CH2CH3、 S02CH3、 OCH2CF3、 CF3或 OCF3; R4 is selected from the group consisting of hydrogen, NH 2 , -C 8 fluorenyl, C r C 8 halodecyl, C r C 8 decyloxy, -C 8 halodecyloxy, phenyl or heteroaryl, said The phenyl or heteroaryl ring may also contain from 1 to 3 of the following substituent groups: F, Cl, Br, I, CN, N0 2 , CH 3 , C(CH 3 ) 3 , OCH 3 , C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 , OCH 2 CF 3 , CF 3 or OCF 3;
Y 选自 -CO-、 -S02-、 -(CR7R8)t-、 -CH=CHCHR7-、 - (CR7R8)tCO-、 -CH=CHCO-、 -S(CR7R8)tCO-、 -N(CR7R8)tCO-、 -0(CR7R8)tCO-、 -S(CR7R8)tS02-、 -N(CR7R8)tS02-、 -0(CR7R8)tS02-、 -CONR7CO-、 -S02NR7C(=S) -、 -S02NR7C(=0)-、 -CONR7C(=S) -、 -NR7CO (CR7R8)t-、 -CO(CR7R8)t- -NR7CO-或 -NR7C(=S)-; t分别选自 0、 1或 2; x选自 0或 1; Y is selected from -CO-, -S0 2 -, -(CR 7 R 8 ) t -, -CH=CHCHR 7 -, - (CR 7 R 8 ) t CO-, -CH=CHCO-, -S(CR 7 R 8 ) t CO-, -N(CR 7 R 8 ) t CO-, -0(CR 7 R 8 ) t CO-, -S(CR 7 R 8 ) t S0 2 -, -N (CR 7 R 8 ) t S0 2 -, -0(CR 7 R 8 ) t S0 2 -, -CONR 7 CO-, -S0 2 NR 7 C(=S) -, -S0 2 NR 7 C(=0)- -CONR 7 C(=S) -, -NR 7 CO (CR 7 R 8 ) t -, -CO(CR 7 R 8 ) t - -NR 7 CO- or -NR 7 C(=S)- ; t is selected from 0, 1 or 2, respectively; x is selected from 0 or 1;
Q选自被 n个各自独立的 取代的苯基或杂芳基；  Q is selected from phenyl or heteroaryl groups which are independently substituted by n;
R5选自卤素、 CN、 N02、 -C8垸基、 卤代 -C8垸基、 ¾- 环垸基、 -C8垸氧基、 卤代 d-C8垸氧基、 -C8垸硫基、 卤代 -C8垸硫基、 C2-C8烯基、 卤代 C2-C8烯基、 C2-C8 炔基、 卤代 C2-C8炔基、 ¾- 烯氧基、 卤代 C2-Q^ 氧基、 ¾ 8炔氧基、 卤代 C2-C8炔氧 基、 -C8垸基亚磺酰基、 代 d-C8垸基亚磺酰基、 d-C8垸基磺酰基、 ¾代 -C8垸基磺 酰基、 -C8垸基羰基、 ¾代 -C8垸基羰基、 8垸基羰基氧基、 - 垸基羰基氨基、 C Cs垸基磺酰基氧基、 d-C8垸氧基羰基、 -C8垸氧基 -C8垸氧基、 CrC8垸氧基羰基 -C8 垸基、 -C8垸氧基羰基氨基、 CrC8垸氧基羰基 8垸氧基、 COR8、 C02R7、 CONR7R8、 NR7R8、 NR8COR7、 NR7COR8、 NR8C02R7、 SOqR8、 S02NR7R8、 芳基、 杂芳基、 芳胺基、 芳垸基氧基、 芳氧基或杂芳胺基， 所述的芳基、 杂芳基、 芳胺基、 芳垸基氧基、 芳氧基或杂 芳胺基环上的氢还可以进一步被 1-4个下述基团所取代： 卤素、 CN、 N02、 d-C8垸基、 d-C8 卤代垸基、 -C8¾代垸氧基、 8垸氧基、 d-C8垸氧基羰基或 -C8垸基磺酰基； R 5 is selected from the group consisting of halogen, CN, N0 2 , -C 8 fluorenyl, halo-C 8 fluorenyl, 3⁄4-cyclodecyl, -C 8 decyloxy, halo dC 8 decyloxy, -C 8垸Thio, halogeno-C 8 thiol, C 2 -C 8 alkenyl, halogenated C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, halogenated C 2 -C 8 alkynyl, 3⁄4- Alkenyloxy, halogenated C 2 -Q^oxy, 3⁄4 8 alkynyloxy, halogenated C 2 -C 8 alkyne , -C 8 decylsulfinyl, dC 8 decylsulfinyl, dC 8 decylsulfonyl, 3⁄4 -C 8 decylsulfonyl, -C 8 decylcarbonyl, 3⁄4 -C 8垸Carbocarbonyl, 8 -mercaptocarbonyloxy, -fluorenylcarbonylamino, C Cs decylsulfonyloxy, dC 8 decyloxycarbonyl, -C 8 decyloxy-C 8 decyloxy, C r C 8垸Oxycarbonyl-C 8 fluorenyl, -C 8 decyloxycarbonylamino, C r C 8 decyloxycarbonyl 8 decyloxy, COR 8 , C0 2 R 7 , CONR 7 R 8 , NR 7 R 8 , NR 8 COR 7 , NR 7 COR 8 , NR 8 C0 2 R 7 , SOqR 8 , S0 2 NR 7 R 8 , aryl, heteroaryl, arylamino, aryl methoxy, aryloxy or heteroarylamine The hydrogen on the aryl, heteroaryl, arylamino, arylalkyloxy, aryloxy or heteroarylamino ring may be further substituted with from 1 to 4 of the following groups: , CN, N0 2 , dC 8 fluorenyl, dC 8 halodecyl, -C 8 3⁄4 decyloxy, 8 decyloxy, dC 8 decyloxycarbonyl or -C 8 decylsulfonyl;
n选自 0至 5的整数； 当 n大于 1时， 可相同或不同；  n is selected from an integer from 0 to 5; when n is greater than 1, it may be the same or different;
R6选自未取代的或被 1-5个独立选自以下基团进一步取代的苯基、苯甲酰基、苯氧基羰 基、 苯基胺基羰基、 苯基 -C6垸基、 萘基、 萘基 d-C6垸基、 杂芳基、 杂芳基羰基、 杂芳 基氧基羰基、 杂芳基胺基羰基或杂芳基 CrC6垸基： 卤素、 硝基、 氰基、 巯基、 d-C8垸基、 卤代 d-C8垸基、 ¾ 8环垸基、 8垸氧基、 ^代^-^垸氧基、 8垸硫基、 ^代^-^ 垸硫基、 C2-C8烯基、 卤代 C2-C8烯基、 C2-C8炔基、 卤代 C2-C8炔基、 C2-C8烯氧基、 卤代 C2-C8烯氧基、 C2-C8炔氧基、 卤代 C2-C8炔氧基、 -C8垸基亚磺酰基、 卤代 -C8垸基亚磺 酰基、 -C8垸基磺酰基、 ¾代 d-C8垸基磺酰基、 d-C8垸基羰基、 ¾代 d-C8垸基羰基、 d-C8垸基羰基氧基、 d-C8垸基羰基氨基、 d-C8垸基磺酰基氧基、 d-C8垸氧基羰基、 d-C8 垸氧基 C C8垸氧基、 d-C8垸氧基羰基 d-C8垸基、 d-C8垸氧基羰基氨基、 d-C8垸氧基羰 基^-^垸氧基、 CHO、 C02H、 C02Na、 C02NH4、 NR7R8、 C(=0)NR7R8、 OC(=0)NR7R8、 C(=S)NR7R8或 S02NR7R8; R 6 is selected from phenyl, benzoyl, phenoxycarbonyl, phenylaminocarbonyl, phenyl-C 6 fluorenyl, naphthyl which are unsubstituted or further substituted by 1 to 5 groups independently selected from the group consisting of , naphthyl dC 6 fluorenyl, heteroaryl, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroarylaminocarbonyl or heteroaryl C r C 6 fluorenyl: halogen, nitro, cyano, fluorenyl , dC 8 fluorenyl, halogenated dC 8 fluorenyl, 3⁄4 8 cyclodecyl, 8 methoxy, ^^^ methoxy, 8 thiol, ^^^ thiol, C 2 - C 8 alkenyl, halo C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, halo C 2 -C 8 alkynyl, C 2 -C 8 alkenyloxy, halo C 2 -C 8 alkene Oxy, C 2 -C 8 alkynyloxy, halo C 2 -C 8 alkynyloxy, -C 8 decylsulfinyl, halo-C 8 decylsulfinyl, -C 8 decylsulfonyl , ¾ behalf dC 8 alkyl with sulfonyl group, dC 8 alkyl with a carbonyl group, ¾ substituting dC 8 alkyl with a carbonyl group, dC 8 alkyl with carbonyl group, dC 8 embankment arylcarbonylamino, dC 8 embankment sulfonyloxy group, dC 8 Oxyloxycarbonyl, dC 8 decyloxy CC 8 decyloxy, dC 8 decyloxycarbonyl dC 8 fluorenyl, dC 8 decyloxycarbonylamino, dC 8 decyloxy Carbonyl group - CHO, C0 2 H, C0 2 Na, C0 2 NH 4 , NR 7 R 8 , C(=0)NR 7 R 8 , OC(=0)NR 7 R 8 , C( =S) NR 7 R 8 or S0 2 NR 7 R 8 ;
R7、 R8可相同或不同， 分别选自氢、 氰基、 SCN、 甲酰基、 C C8垸基、 卤代 C C8垸 基、 C C8垸氧基、 ¾代 8垸氧基、 d-C8垸硫基、 ¾代 8垸硫基、 d-C8垸基羰基、 d-C8垸氧基羰基、 d-C8垸氧基羰基 d-C8垸基、 d-C8垸基亚磺酰基、 d-C8垸基磺酰基、 氰基 d-C8垸基、 羟基 d-C8垸基、 C3-C8环垸基或 C C8垸基氨基。 R 7, R 8 may be the same or different, are independently selected from hydrogen, cyano, SCN, formyl, alkyl with the CC 8, 8-halo alkyl with the CC, the CC 8 embankment group, substituting 8 ¾ embankment group, dC 8 Sulfhydryl, 3⁄4th generation 8 thiol, dC 8 fluorenylcarbonyl, dC 8 decyloxycarbonyl, dC 8 decyloxycarbonyl dC 8 fluorenyl, dC 8 decylsulfinyl, dC 8 decylsulfonyl, Cyano dC 8 fluorenyl, hydroxy dC 8 fluorenyl, C 3 -C 8 cyclodecyl or CC 8 decylamino.
本发明进一步优选的化合物为： 通式 (I)中  Further preferred compounds of the invention are: in formula (I)
选自氢、 卤素、 CN、 N02、 巯基、 C C4垸基、 卤代 C C4垸基、 C C4垸氧基、 卤 代 d-C4垸氧基、 氰基 C C4垸氧基、 C C4焼硫基、 卤代 C C4垸硫基、 C C4垸氧基 d-C4 \ ί Ci-C4 Ci-C4 ¾υ¾ Ci-C4 ¾¾¾¾¾ Ci-C4¾¾¾ \ ί Ci-C4 ¾¾¾¾¾ Ci-C4 i 基、 卤代 C C4垸基氨基、 哌啶基、 四氢吡咯基、 N-甲基哌嗪基、 吗啉基、 C2-C4烯基、 卤 代 C2-C4烯基、 C2-C4烯氧基、 卤代 C2-C4烯氧基、 C2-C4炔基、 卤代 C2-C4炔基、 C2-C4炔氧 基、 卤代 C2-C4炔氧基、 d-C4垸基亚磺酰基、 d-C4垸基磺酰基、 C3-C6环垸基、 卤代 d-C4 垸基亚磺酰基、 ¾代 d-C4垸基磺酰基、 d-C4垸氧基羰基、 ¾代 d-C4垸基羰基、 d-C4垸 基羰基氧基、 CrC4垸基羰基氨基、 -C4垸基磺酰基氧基、 -C4垸氧基 -C4垸氧基、 C C4 垸氧基羰基 CrC4垸基、 -C4垸氧基羰基氨基、 -C4垸氧基羰基 -C4垸氧基、 CHO、C02H、 C02Na、 C02NH4、 NR7R8、 C(=0)NR7R8、 OC(=0)NR7R8、 C(=S)NR7R8、 S02NR7R8或 R6; m选自 0至 5的整数； 当 m大于 1时， ！^可相同或不同； Selected from hydrogen, halogen, CN, N0 2 , fluorenyl, CC 4 fluorenyl, halogenated CC 4 fluorenyl, CC 4 decyloxy, halogenated dC 4 decyloxy, cyano CC 4 decyloxy, CC 4焼Thio, halogenated CC 4 thiol group, CC 4 decyloxy dC 4 \ ί Ci-C 4 Ci-C 4 3⁄4 υ 3⁄4 Ci-C 4 3⁄43⁄43⁄43 ⁄ Ci-C 4 3⁄43⁄43⁄4 \ ί Ci-C 4 3⁄43⁄43⁄43⁄43⁄4 Ci-C 4 i group, halogenated CC 4 decylamino, piperidinyl, tetrahydropyrrolyl, N-methylpiperazinyl, morpholinyl, C 2 -C 4 alkenyl, halogenated C 2 -C 4 alkenyl, C 2 -C 4 alkenyloxy, halo C 2 -C 4 alkenyloxy, C 2 -C 4 alkynyl, halo C 2 -C 4 alkynyl, C 2 -C 4 alkynyloxy, halo C 2- C 4 alkynyloxy, dC 4 decylsulfinyl, dC 4 decylsulfonyl, C 3 -C 6 cyclodecyl, halogenated dC 4 decylsulfinyl, 3⁄4 dC 4 decylsulfonyl , dC 4 methoxycarbonyl, 3⁄4 dC 4 fluorenylcarbonyl, dC 4 fluorenylcarbonyloxy, C r C 4 fluorenylcarbonylamino, -C 4 decylsulfonyloxy, -C 4 decyloxy- C 4 methoxy, CC 4 methoxycarbonyl C r C 4 fluorenyl, -C 4 methoxycarbonylamino, -C 4 methoxycarbonyl-C 4 decyloxy, CHO, C0 2 H, C0 2 Na, C0 2 NH 4 , NR 7 R 8 , C(=0)NR 7 R 8 , OC(=0)NR 7 R 8 , C(=S)NR 7 R 8 , S0 2 NR 7 R 8 or R 6 ; m is selected from An integer from 0 to 5; when m is greater than 1, ! ^ can be the same or different;
R2选自氢、 卤素、 CN、 N02、 CONH2、 氰基 CrC4垸基、 -C4垸基、 卤代 CrC4垸基、 -C4垸氧基、 卤代 -C4垸氧基、 氰基 CrC4垸氧基、 d-C4垸硫基、 卤代 -C4垸硫基、 Ci-C4 Ci-C4 ¾υ¾ \ ί Ci-C4¾¾¾,¾ Ci-C4¾¾¾ Ci-C4¾¾¾¾¾ Ci-C4¾¾¾ Ci-C4 垸硫基 CrC4垸基、 -C4垸基亚磺酰基、 -C4垸基磺酰基、 C3-C6环垸基或 R6; R 2 is selected from the group consisting of hydrogen, halogen, CN, N0 2 , CONH 2 , cyano C r C 4 fluorenyl, -C 4 fluorenyl, halogenated C r C 4 fluorenyl, -C 4 decyloxy, halo- C 4 embankment, cyano group C r C 4 embankment, dC 4 embankment alkylthio, halo embankment -C 4 alkylthio, Ci-C 4 Ci-C 4 ¾υ¾ \ ί Ci-C 4 ¾¾¾, ¾ Ci -C 4 ¾¾¾ Ci-C 4 ¾¾¾¾¾ Ci-C 4 ¾¾¾ Ci-C 4 alkylthio C r C 4 embankment embankment group, -C 4 embankment sulfinyl, -C 4 alkyl with a sulfonyl group, C 3 -C 6 Cyclodecyl or R 6;
Ra、 Rb、 Rc、 Rd、 Re Rf、 Rg和 Rh各自独立的表示氢原子、 CrC4垸基、 卤代 CrC4垸 基、 卤代 CrC4垸氧基或 -C4垸氧羰基； 与 一起或者 Rc与 Rf—起可以结合形成饱和 的五元环、 六元环或者七元环； R a, R b, R c , R d, R e R f, R g and R h each independently represents a hydrogen atom, alkyl with C r C 4, C r C 4 embankment halo, halo C r C 4 methoxy or -C 4垸 oxycarbonyl; together with R c and R f may combine to form a saturated five-membered ring, six-membered ring or seven-membered ring;
Xi选自 N或 CR3; R3选自氢、 CN、 N02、 CONHNH2、 C(=0)NR7R8、 C(=S)NR7R8、 -C12垸氧基羰基、 C(=0)N=CR7R8、 C02NR7R8、 C02N=CR7R8、 CONHN=CR7NR7R8或 C(=0)NR7N=CR7R8; Xi is selected from N or CR 3; R 3 is selected from the group consisting of hydrogen, CN, N0 2 , CONHNH 2 , C(=0)NR 7 R 8 , C(=S)NR 7 R 8 , -C 12 decyloxycarbonyl, C(=0)N=CR 7 R 8 , C0 2 NR 7 R 8 , C0 2 N=CR 7 R 8 , CONHN=CR 7 NR 7 R 8 or C(=0)NR 7 N=CR 7 R 8 ;
X2选自 (CR7R8)k、 CO(CR7R8)p、 （CR7R8)pCO、 SOq(CR7R8)p或 (CR7R8)pSOq; X 2 is selected from (CR 7 R 8 ) k , CO(CR 7 R 8 ) p , (CR 7 R 8 ) p CO, SOq(CR 7 R 8 )p or (CR 7 R 8 )pSOq;
k选自 1、 2或 3; p选自 0、 1、 2或 3; q选自 0、 1或 2;  k is selected from 1, 2 or 3; p is selected from 0, 1, 2 or 3; q is selected from 0, 1 or 2;
R4选自氢、 NH2、 CrC4垸基、 d-C4卤代垸基、 CrC4垸氧基、 -C4卤代垸氧基、 苯基 或杂芳基， 所述的苯基或杂芳基环上还可以含有 1-3个下述取代基团： F、 Cl、 Br、 I、 CN、 N02、 CH3、 C(CH3)3、 OCH3、 C02CH3、 C02CH2CH3、 S02CH3、 OCH2CF3、 CF3或 OCF3 ; R4 is selected from the group consisting of hydrogen, NH 2 , C r C 4 fluorenyl, dC 4 halo fluorenyl, C r C 4 decyloxy, -C 4 halodecyloxy, phenyl or heteroaryl, said benzene The base or heteroaryl ring may also contain from 1 to 3 of the following substituent groups: F, Cl, Br, I, CN, N0 2 , CH 3 , C(CH 3 ) 3 , OCH 3 , C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 , OCH 2 CF 3 , CF 3 or OCF 3 ;
Y 选自 -CO-、 -S02-、 -(CR7R8)t-、 -CH=CHCHR7-、 - (CR7R8)tCO-、 -CH=CHCO-、 -S(CR7R8)tCO- 、 -N(CR7R8)tCO-、 -0(CR7R8)tCO- 、 -S(CR7R8)tS02- 、 -N(CR7R8)tS02-、 -0(CR7R8)tS02-、 -CONR7CO-、 -S02NR7C(=S) -、 -S02NR7C(=0)-、 -CONR7C(=S) -、 -NR7CO (CR7R8)t -、 -CO(CR7R8)t -、 -NR7CO-或 -NR7C(=S)-; t分别选自 0、 1或 2; x选自 0或 1 ; Y is selected from -CO-, -S0 2 -, -(CR 7 R 8 ) t -, -CH=CHCHR 7 -, - (CR 7 R 8 ) t CO-, -CH=CHCO-, -S(CR 7 R 8 ) t CO- , -N(CR 7 R 8 ) t CO-, -0(CR 7 R 8 ) t CO- , -S(CR 7 R 8 ) t S0 2 - , -N(CR 7 R 8 ) t S0 2 -, -0(CR 7 R 8 ) t S0 2 -, -CONR 7 CO-, -S0 2 NR 7 C(=S) -, -S0 2 NR 7 C(=0)- -CONR 7 C(=S) -, -NR 7 CO (CR 7 R 8 ) t -, -CO(CR 7 R 8 ) t -, -NR 7 CO- or -NR 7 C(=S)- ; t are each selected from 0, 1 or 2; x is selected from 0 or 1;
Q选自被 n个各自独立的 取代的苯基或杂芳基；  Q is selected from phenyl or heteroaryl groups which are independently substituted by n;
R5选自卤素、 CN、 N02、 d-C4垸基、 卤代 -C4垸基、 C3-C6环垸基、 CrC4垸氧基、 卤代 CrC4垸氧基、 -C4垸硫基、 卤代 -C4垸硫基、 C2-C4烯基、 卤代 C2-C4烯基、 C2-C4 炔基、 卤代 C2-C4炔基、 C2-C4烯氧基、 卤代 C2-C4烯氧基、 C2-C4炔氧基、 卤代 C2-C4炔氧 基、 CrC4垸基亚磺酰基、 卤代 CrC4垸基亚磺酰基、 CrC4垸基磺酰基、 卤代 CrC4垸基磺 酰基、 d-C4垸基羰基、 ¾代 d-C4垸基羰基、 d-C4垸基羰基氧基、 d-C4垸基羰基氨基、 d-C4垸基磺酰基氧基、 d-C4垸氧基羰基、 d-C4垸氧基 d-C4垸氧基、 d-C4垸氧基羰基 d-C4 垸基、 d-C4垸氧基羰基氨基、 d-C4垸氧基羰基 d-C4垸氧基、 COR8、 C02R7、 CONR7R8、 NR7R8、 NR8COR7、 NR7COR8、 NR8C02R7、 SOqR8、 S02NR7R8、 芳基、 杂芳基、 芳胺基、 芳垸基氧基、 芳氧基或杂芳胺基， 所述的芳基、 杂芳基、 芳胺基、 芳垸基氧基、 芳氧基或杂 芳胺基环上的氢还可以进一步被 1-4个下述基团所取代： 卤素、 CN、 N02、 d-C4垸基、 d-C4 卤代垸基、 d-C4卤代垸氧基、 d-C4垸氧基、 d-C4垸氧基羰基或 d-C4垸基磺酰基； R 5 is selected from the group consisting of halogen, CN, N0 2 , dC 4 fluorenyl, halo-C 4 fluorenyl, C 3 -C 6 cyclodecyl, C r C 4 decyloxy, halogenated C r C 4 decyloxy -C 4 thiol, halo-C 4 thiol, C 2 -C 4 alkenyl, halogenated C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, halogenated C 2 -C 4 Alkynyl, C 2 -C 4 alkenyloxy, halo C 2 -C 4 alkenyloxy, C 2 -C 4 alkynyloxy, halo C 2 -C 4 alkynyloxy, C r C 4 fluorenyl Sulfonyl, halogenated C r C 4 fluorenylsulfinyl, C r C 4 decylsulfonyl, halogenated C r C 4 fluorenylsulfonyl, dC 4 fluorenylcarbonyl, 3⁄4 dC 4 fluorenylcarbonyl, dC 4 -mercaptocarbonyloxy, dC 4 decylcarbonylamino, dC 4 decylsulfonyloxy, dC 4 decyloxycarbonyl, dC 4 decyloxy dC 4 decyloxy, dC 4 decyloxycarbonyl dC 4垸a group, dC 4 methoxycarbonylamino group, dC 4 decyloxycarbonyl dC 4 decyloxy group, COR 8 , C0 2 R 7 , CONR 7 R 8 , NR 7 R 8 , NR 8 COR 7 , NR 7 COR 8 , NR 8 C0 2 R 7 , SOqR 8 , S0 2 NR 7 R 8 , aryl, heteroaryl, arylamino, arylmethyloxy, aryloxy or heteroarylamino, said aryl, hetero Aryl, aromatic The hydrogen on the amine, aryl aryloxy, aryloxy or heteroarylamino ring may be further substituted with from 1 to 4 groups: halogen, CN, N0 2 , dC 4 fluorenyl, dC 4 Halogenated fluorenyl, dC 4 halodecyloxy, dC 4 decyloxy, dC 4 decyloxycarbonyl or dC 4 decylsulfonyl;
n选自 0至 5的整数； 当 n大于 1时， R5可相同或不同； n is selected from an integer from 0 to 5; when n is greater than 1, R 5 may be the same or different;
R6选自未取代的或被 1-5个独立选自以下基团进一步取代的苯基、苯甲酰基、苯氧基羰 基、 苯基胺基羰基、 苯基 C C6垸基、 萘基、 萘基 d-C6垸基、 杂芳基、 杂芳基羰基、 杂芳 基氧基羰基、 杂芳基胺基羰基或杂芳基 d-C6垸基： 卤素、 硝基、 氰基、 巯基、 d-C4垸基、 卤代 d-C4垸基、 C3-C6环垸基、 d-C4垸氧基、 ¾代 4垸氧基、 d-C4垸硫基、 ^代 C C4 垸硫基、 C2-C4烯基、 卤代 C2-C4烯基、 C2-C4炔基、 卤代 C2-C4炔基、 C2-C4烯氧基、 卤代 C2-C4烯氧基、 C2-C4炔氧基、 卤代 C2-C4炔氧基、 CrC4垸基亚磺酰基、 卤代 CrC4垸基亚磺 酰基、 d-C4垸基磺酰基、 ¾代 d-C4垸基磺酰基、 d-C4垸基羰基、 ¾代 d-C4垸基羰基、 d-C4垸基羰基氧基、 d-C4垸基羰基氨基、 d-C4垸基磺酰基氧基、 d-C4垸氧基羰基、 d-C4 垸氧基 d-C4垸氧基、 -C4垸氧基羰基 -C4垸基、 -C4垸氧基羰基氨基、 -C4垸氧基羰 基^ 垸氧基、 CHO、 C02H、 C02Na、 C02NH4、 NR7R8、 C(=0)NR7R8、 OC(=0)NR7R8、 C(=S)NR7R8或 S02NR7R8; R 6 is selected from phenyl, benzoyl, phenoxycarbonyl, phenylaminocarbonyl, phenyl CC 6 fluorenyl, naphthyl, which are unsubstituted or further substituted by 1 to 5 groups independently selected from the group consisting of Naphthyl dC 6 fluorenyl, heteroaryl, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroarylaminocarbonyl or heteroaryl dC 6 fluorenyl: halogen, nitro, cyano, fluorenyl, dC 4 Mercapto, halogenated dC 4 fluorenyl, C 3 -C 6 cyclodecyl, dC 4 decyloxy, 3⁄4 generation 4 methoxy, dC 4 thiol, ^ CC 4 thiol, C 2 -C 4 alkenyl, halo C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, halo C 2 -C 4 alkynyl, C 2 -C 4 alkenyloxy, halo C 2 -C 4 olefin , C 2 -C 4 alkynyloxy, halogenated C 2 -C 4 alkynyloxy, CrC 4 fluorenylsulfinyl, halogenated CrC 4 fluorenylsulfinyl, dC 4 decylsulfonyl, 3⁄4 dC 4 embankment arylsulfonyl group, dC 4 alkyl with a carbonyl group, ¾ substituting dC 4 alkyl with a carbonyl group, dC 4 alkyl with a carbonyl group, dC 4 alkyl with a carbonyl group, dC 4 embankment sulfonyloxy group, dC 4 embankment oxycarbonyl , dC 4 embankment embankment dC 4 alkoxy group, group -C 4 embankment -C 4 alkyl with a carbonyl group, -C 4 embankment oxycarbonyl group, -C 4 Embankment ^ butoxycarbonyl group, CHO, C0 2 H, C0 2 Na, C0 2 NH 4, NR 7 R 8, C (= 0) NR 7 R 8, OC (= 0) NR 7 R 8, C ( =S) NR 7 R 8 or S0 2 NR 7 R 8 ;
R7、 R8可相同或不同， 分别选自氢、 氰基、 SCN、 甲酰基、 CrC4垸基、 卤代 -C4垸 基、 -C4垸氧基、 ^代^ 垸氧基、 -C4垸硫基、 ¾代 4垸硫基、 CrC4垸基羰基、 -C4垸氧基羰基、 -C4垸氧基羰基 -C4垸基、 -C4垸基亚磺酰基、 -C4垸基磺酰基、 氰基 CrC4垸基、 羟基 -C4垸基、 C3-C6环垸基或 -C4垸基氨基。 R 7 and R 8 may be the same or different and are respectively selected from the group consisting of hydrogen, cyano, SCN, formyl, C r C 4 fluorenyl, halogeno-C 4 fluorenyl, -C 4 decyloxy, ^ methoxy , -C 4 thiol, 3⁄4 thiol, C r C 4 fluorenylcarbonyl, -C 4 decyloxycarbonyl, -C 4 decyloxycarbonyl-C 4 fluorenyl, -C 4 fluorenyl Sulfonyl, -C 4 decylsulfonyl, cyano C r C 4 fluorenyl, hydroxy-C 4 fluorenyl, C 3 -C 6 cyclodecyl or -C 4 decylamino.
本发明更进一步优选的化合物为： 通式 (I)中  Further preferred compounds of the invention are: in formula (I)
！^选自氢、 卤素、 CN、 N02、 CrC4垸基、 卤代 CrC4垸基、 CrC4垸氧基、 卤代 -C4 #ΐ¾ Ci-C4 Ci-C4 ¾¾¾,¾ Ci-C4 ¾¾¾ \ ί Ci-C4 Ci-C4 C3-C6 环垸基或 R6; m选自 0至 5的整数； 当 m大于 1时， ！^可相同或不同； ! ^ selected from hydrogen, halogen, CN, N0 2 , C r C 4 fluorenyl, halogenated C r C 4 fluorenyl, C r C 4 decyloxy, halo-C 4 #ΐ3⁄4 Ci-C 4 Ci-C 4 3⁄43⁄43⁄4,3⁄4 Ci-C 4 3⁄43⁄43⁄4 \ ί Ci-C 4 Ci-C 4 C 3 -C 6 ring fluorenyl or R 6; m is selected from an integer from 0 to 5; when m is greater than 1, ! ^ can be the same or different;
R2选自氢、 卤素、 CN、 CrC4垸基、 卤代 -C4垸基、 CrC4垸氧基、 卤代 CrC4垸氧基、 氰基 CrC4垸氧基、 CrC4垸氧基 CrC4垸基、 ¾代 1 4垸氧基 -C4垸基、 C3-C6环垸基或 R6; 一 R 2 is selected from the group consisting of hydrogen, halogen, CN, C r C 4 fluorenyl, halo-C 4 fluorenyl, C r C 4 decyloxy, halogenated C r C 4 decyloxy, Cyano C r C 4 decyloxy, C r C 4 decyloxy C r C 4 fluorenyl, 3⁄4 generation 14 4 oxy-C 4 fluorenyl, C 3 -C 6 cyclodecyl or R 6 ;
Ra、 Rb、 Rc、 Rd、 Re Rf、 Rg和 Rh各自独立的表示氢原子、 CrC4垸基、 卤代 CrC4垸 基、 卤代 CrC4垸氧基或 -C4垸氧羰基； 与 一起或者 Rc与 Rf—起可以结合形成饱和 的五元环、 六元环或者七元环； R a, R b, R c , R d, R e R f, R g and R h each independently represents a hydrogen atom, alkyl with C r C 4, C r C 4 embankment halo, halo C r C 4 methoxy or -C 4垸 oxycarbonyl; together with R c and R f may combine to form a saturated five-membered ring, six-membered ring or seven-membered ring;
Xi选自 N或 CR3 ; Xi is selected from N or CR 3 ;
R3选自氢、 CN、 N02、 CONHNH2、 C(=0)NR7R8、 C(=S)NR7R8、 -C12垸氧基羰基、 C(=0)N=CR7R8、 C02NR7R8、 C02N=CR7R8、 CONHN=CR7NR7R8或 C(=0)NR7N=CR7R8; R 3 is selected from the group consisting of hydrogen, CN, N0 2 , CONHNH 2 , C(=0)NR 7 R 8 , C(=S)NR 7 R 8 , -C 12 decyloxycarbonyl, C(=0)N=CR 7 R 8 , C0 2 NR 7 R 8 , C0 2 N=CR 7 R 8 , CONHN=CR 7 NR 7 R 8 or C(=0)NR 7 N=CR 7 R 8 ;
X2选自 (CR7R8)k、 CO(CR7R8)p、 （CR7R8)pCO、 SOq(CR7R8)p或 (CR7R8)pSOq; X 2 is selected from (CR 7 R 8 ) k , CO(CR 7 R 8 ) p , (CR 7 R 8 ) p CO, SOq(CR 7 R 8 )p or (CR 7 R 8 )pSOq;
k选自 1、 2或 3; p选自 0、 1、 2或 3; q选自 0、 1或 2;  k is selected from 1, 2 or 3; p is selected from 0, 1, 2 or 3; q is selected from 0, 1 or 2;
选自氢、 NH2、 CrC4垸基、 CrC4卤代垸基、 CrC4垸氧基、 -C4卤代垸氧基、 未取 代或被 1-3个下述基团进一步取代的苯基、 吡啶基、 噻吩基、 呋喃基、 吡咯基、 咪唑基、 噻 唑基或吡唑基： F、 Cl、 Br、 I、 CN、 N02、 CH3、 C(CH3)3、 OCH3、 C02CH3、 C02CH2CH3、 S02CH3、 OCH2CF3、 CF3或 OCF3 ; Selected from hydrogen, NH 2 , C r C 4 fluorenyl, C r C 4 halodecyl, C r C 4 decyloxy, -C 4 halodecyloxy, unsubstituted or 1-3 a further substituted phenyl, pyridyl, thienyl, furyl, pyrrolyl, imidazolyl, thiazolyl or pyrazolyl group: F, Cl, Br, I, CN, N0 2 , CH 3 , C (CH 3 3 , OCH 3 , C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 , OCH 2 CF 3 , CF 3 or OCF 3 ;
Y选自 -CO-、 -S02-、 -CH2-、 -CH=CHCHR7-、 - (CR7R8)tCO-、 -CH=CHCO-、 -S(CR7R8)tCO-、Y is selected from -CO-, -S0 2 -, -CH 2 -, -CH=CHCHR 7 -, -(CR 7 R 8 ) t CO-, -CH=CHCO-, -S(CR 7 R 8 ) t CO-,
-N(CR7R8)tCO-、 -0(CR7R8)tCO-、 -S(CR7R8)tS02-、 -N(CR7R8)tS02-、 -0(CR7R8)tS02-、 -CONR7CO-、 -S02NR7C(=S)-、 -S02NR7C(=0)-、 -CONR7C(=S)-、 -NR7CO (CR7R8)t-、 -CO(CR7R8)t- -NR7CO-或 -NR7C(=S)-; t分别选自 0、 1或 2; x选自 0或 1 ; -N(CR 7 R 8 ) t CO-, -0(CR 7 R 8 ) t CO-, -S(CR 7 R 8 ) t S0 2 -, -N(CR 7 R 8 ) t S0 2 -, -0(CR 7 R 8 ) t S0 2 -, -CONR7CO-, -S0 2 NR 7 C(=S)-, -S0 2 NR 7 C(=0)-, -CONR 7 C(=S)- -NR 7 CO (CR 7 R 8 ) t -, -CO(CR 7 R 8 ) t - -NR 7 CO- or -NR 7 C(=S)- ; t are each selected from 0, 1 or 2; x is selected from 0 or 1;
Q选自被 n个各自独立的 R5取代的苯基、 吡啶基、 嘧啶基、 哒嗪基、 吡嗪基、 喹啉基、 噻吩基、 苯并噻吩基、 呋喃基、 苯并呋喃基、 吲哚基、 吡咯基、 恶唑基、 咪唑基、 苯并恶唑 基、 苯并噻唑基、 苯并咪唑基、 苯并吡嗪基、 噻唑基、 吡唑基、 ***并嘧啶基、 咪唑并哒嗪 基、 咪唑并吡啶基或哒嗪酮基； Q is selected from phenyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, quinolinyl, thienyl, benzothienyl, furyl, benzofuranyl, substituted by n each independently R 5 , Mercapto, pyrrolyl, oxazolyl, imidazolyl, benzoxazolyl, benzothiazolyl, benzimidazolyl, benzopyrazinyl, thiazolyl, pyrazolyl, triazolopyrimidinyl, imidazole And pyridazinyl, imidazopyridyl or pyridazinone;
R5选自卤素、 CN、 N02、 C C4垸基、 C3-C6环垸基、 C C4卤代垸基、 C C4垸氧基、 C C4卤代垸氧基、 C2-C4烯基、 C2-C4炔基、 C2-C4烯氧基、 C2-C4炔氧基、 COCH3、 COC2H5、 C02CH3、 C02C2H5、 S02CH3或 S02C2H5 ; R 5 is selected from the group consisting of halogen, CN, N0 2 , CC 4 fluorenyl, C 3 -C 6 cyclodecyl, CC 4 halodecyl, CC 4 decyloxy, CC 4 halodecyloxy, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 2 -C 4 alkenyloxy, C 2 -C 4 alkynyloxy, COCH 3 , COC 2 H 5 , C0 2 CH 3 , C0 2 C 2 H 5 , S0 2 CH 3 or S0 2 C 2 H 5 ;
n选自 0至 5的整数； 当 n大于 1时， R5可相同或不同； n is selected from an integer from 0 to 5; when n is greater than 1, R 5 may be the same or different;
R6选自苯基、 4-氯苯基、 2,4-二氯苯基、 4-甲基苯基、 4-三氟甲基苯基、 4-甲氧基苯基、 2,6-二氯 -4-三氟甲基苯基、 苄基、 4-氯苄基、 4-叔丁基苄基、 4-三氟甲基苄基、 苯乙基、 2- 吡啶基、 3-氯 -2-吡啶基、 3,5-二氯 -2-吡啶基、 3,5,6-三氯 -2-吡啶基、 5-三氟甲基 -2-吡啶基、 5-甲基 -2-吡啶基、 3-氯 -5-氰基 -2-吡啶基、 3-氯 -5-三氟甲基 -2-吡啶基、 2-吡啶甲基、 2-氯 -5- 吡啶甲基、 3-氯 -5-三氟甲基 -2-吡啶甲基、 2-吡啶乙基、 3-氯 -5-三氟甲基 -2-吡啶乙基、噻唑 -2- 基、 2-氯 -5-噻唑基甲基或 2-嘧啶基； R 6 is selected from the group consisting of phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl, 2,6- Dichloro-4-trifluoromethylphenyl, benzyl, 4-chlorobenzyl, 4-tert-butylbenzyl, 4-trifluoromethylbenzyl, phenethyl, 2-pyridyl, 3-chloro -2-pyridyl, 3,5-dichloro-2-pyridyl, 3,5,6-trichloro-2-pyridyl, 5-trifluoromethyl-2-pyridyl, 5-methyl-2 Pyridyl, 3-chloro-5-cyano-2-pyridyl, 3-chloro-5-trifluoromethyl-2-pyridyl, 2-pyridylmethyl, 2-chloro-5-pyridinemethyl, 3-Chloro-5-trifluoromethyl-2-pyridylmethyl, 2-pyridylethyl, 3-chloro-5-trifluoromethyl-2-pyridylethyl, thiazol-2-yl, 2-chloro- 5-thiazolylmethyl or 2-pyrimidinyl;
R7、 R8可相同或不同， 分别选自氢、 氰基、 SCN、 甲酰基、 CrC4垸基、 卤代 -C4垸 基、 -C4垸氧基、 ^代^ 垸氧基、 -C4垸硫基、 ¾代 4垸硫基、 CrC4垸基羰基、 -C4垸氧基羰基、 -C4垸氧基羰基 -C4垸基、 -C4垸基亚磺酰基、 -C4垸基磺酰基、 氰基 CrC4垸基、 羟基 -C4垸基、 C3-C6环垸基或 -C4垸基氨基。 R 7 and R 8 may be the same or different and are respectively selected from the group consisting of hydrogen, cyano, SCN, formyl, C r C 4 fluorenyl, halogeno-C 4 fluorenyl, -C 4 decyloxy, ^ methoxy , -C 4 thiol, 3⁄4 thiol, C r C 4 fluorenylcarbonyl, -C 4 decyloxycarbonyl, -C 4 decyloxycarbonyl-C 4 fluorenyl, -C 4 fluorenyl Sulfonyl, -C 4 decylsulfonyl, cyano C r C 4 fluorenyl, hydroxy-C 4 fluorenyl, C 3 -C 6 cyclodecyl or -C 4 decylamino.
本发明再进一步优选的化合物为： 通式 (I)中  Still further preferred compounds of the invention are: in formula (I)
选自氢、 F、 Cl、 Br、 I、 CN、 N02、 CrC4垸基、 卤代 CrC4垸基、 CrC4垸氧基、 卤 代 d-C4垸氧基或¾-0>环垸基； m选自 1至 5的整数； 当 m大于 1时， ！^可相同或不同； R2选自氢、 F、 Cl、 Br、 I、 CN、 CrC4垸基、 卤代 d-C4垸基、 CrC4垸氧基、 卤代 -C4 垸氧基、 C3-C6环垸基或 R6; Selected from hydrogen, F, Cl, Br, I, CN, N0 2 , C r C 4 fluorenyl, halogenated C r C 4 fluorenyl, C r C 4 decyloxy, halogenated dC 4 decyloxy or 3⁄4 -0>cycloalkyl; m is selected from an integer from 1 to 5; when m is greater than 1, ! ^ may be the same or different; R 2 is selected from the group consisting of hydrogen, F, Cl, Br, I, CN, C r C 4 fluorenyl, halogenated dC 4 fluorenyl, C r C 4 decyloxy, halo-C 4垸Oxy, C 3 -C 6 cyclodecyl or R6;
Ra、 Rb、 Rc、 Rd、 Re Rf、 Rg和 Rh各自独立的表示氢原子、 CrC4垸基、 卤代 CrC4垸 基、 卤代 CrC4垸氧基或 -C4垸氧羰基； 与 一起或者 Rc与 Rf—起可以结合形成饱和 的五元环、 六元环或者七元环； Xi选自 N或 CR3 ; R a, R b, R c , R d, R e R f, R g and R h each independently represents a hydrogen atom, alkyl with C r C 4, C r C 4 embankment halo, halo C r C 4 methoxy or -C 4垸 oxycarbonyl; together with R c and R f may combine to form a saturated five-membered ring, six-membered ring or seven-membered ring; Xi is selected from N or CR 3 ;
R3选自氢、 CN、 N02、 CONH2、 CSNH2、 C02CH3、 CONHCH3、 CONHCN、 C02N=C(CH3)2、 CONHNH2、 CONHN(CH3)2、 CONHN=CHOCH3或 CONHN=CHN(CH3)2; R 3 is selected from the group consisting of hydrogen, CN, NO 2 , CONH 2 , CSNH 2 , C0 2 CH 3 , CONHCH 3 , CONHCN, C0 2 N=C(CH 3 ) 2 , CONHNH 2 , CONHN(CH 3 ) 2 , CONHN= CHOCH 3 or CONHN=CHN(CH 3 ) 2 ;
X2选自 CH2、 CO、 S02、 CH(CH3)、 CH(CN)、 COCH2、 CH2CH2、 CH2CO或 S02CH2; R4选自氢、 NH2、 CrC4垸基或 CrC4卤代垸基 X 2 is selected from the group consisting of CH 2 , CO, S0 2 , CH(CH 3 ), CH(CN), COCH 2 , CH 2 CH 2 , CH 2 CO or SO 2 CH 2 ; R 4 is selected from the group consisting of hydrogen, NH 2 , C r C 4 fluorenyl or C r C 4 halogenated fluorenyl
Y选自 -CO-、 -S02-、 -CH2-或 -COCH(CH(CH3)2)-; x选自 0或 1 ; Y is selected from -CO-, -S0 2 -, -CH 2 - or -COCH(CH(CH 3 ) 2 )- ; x is selected from 0 or 1;
Q选自被 n个各自独立的 R5取代的苯基、 吡啶基、 嘧啶基、 噻唑基、 苯并恶唑基、 苯 并吡嗪基或哒嗪酮基； Q is selected from phenyl, pyridyl, pyrimidinyl, thiazolyl, benzoxazolyl, benzopyrazinyl or pyridazinone groups substituted by n each independently R 5 ;
R5选自 F、 Cl、 Br、 I、 CN、 N02、 CrC4垸基、 卤代 CrC4垸基、 CrC4垸氧基、 卤代 -C4垸氧基、 C02CH3、 C02CH2CH3、 S02CH3或 OCH2CF3 ; R 5 is selected from the group consisting of F, Cl, Br, I, CN, N0 2 , C r C 4 fluorenyl, halogenated C r C 4 fluorenyl, C r C 4 decyloxy, halo-C 4 decyloxy, C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 or OCH 2 CF 3 ;
R6选自苯基、 4-氯苯基、 2,4-二氯苯基、 4-甲基苯基、 4-三氟甲基苯基、 4-甲氧基苯基、 2,6-二氯 -4-三氟甲基苯基、 苄基、 4-氯苄基、 4-叔丁基苄基、 4-三氟甲基苄基、 苯乙基、 2- 吡啶基、 3-氯 -2-吡啶基、 3,5-二氯 -2-吡啶基、 3,5,6-三氯 -2-吡啶基、 5-三氟甲基 -2-吡啶基、 5-甲基 -2-吡啶基、 3-氯 -5-氰基 -2-吡啶基、 3-氯 -5-三氟甲基 -2-吡啶基、 2-吡啶甲基、 2-氯 -5- 吡啶甲基、 3-氯 -5-三氟甲基 -2-吡啶甲基、 2-吡啶乙基、 3-氯 -5-三氟甲基 -2-吡啶乙基、噻唑 -2- 基、 2-氯 -5-噻唑基甲基或 2-嘧啶基； R 6 is selected from the group consisting of phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl, 2,6- Dichloro-4-trifluoromethylphenyl, benzyl, 4-chlorobenzyl, 4-tert-butylbenzyl, 4-trifluoromethylbenzyl, phenethyl, 2-pyridyl, 3-chloro -2-pyridyl, 3,5-dichloro-2-pyridyl, 3,5,6-trichloro-2-pyridyl, 5-trifluoromethyl-2-pyridyl, 5-methyl-2 Pyridyl, 3-chloro-5-cyano-2-pyridyl, 3-chloro-5-trifluoromethyl-2-pyridyl, 2-pyridylmethyl, 2-chloro-5-pyridinemethyl, 3-Chloro-5-trifluoromethyl-2-pyridylmethyl, 2-pyridylethyl, 3-chloro-5-trifluoromethyl-2-pyridylethyl, thiazol-2-yl, 2-chloro- 5-thiazolylmethyl or 2-pyrimidinyl;
其中， 当 Q选自苯基或苯并吡嗪基时， n选自 1、 2、 3、 4或 5 ;  Wherein when Q is selected from phenyl or benzopyrazinyl, n is selected from 1, 2, 3, 4 or 5;
当 Q选自吡啶或苯并恶唑基时， n选自 1、 2、 3或 4;  When Q is selected from pyridine or benzoxazolyl, n is selected from 1, 2, 3 or 4;
当 Q选自嘧啶或哒嗪酮基时， n选自 1、 2或 3 ;  When Q is selected from pyrimidine or pyridazinone, n is selected from 1, 2 or 3;
当 Q选自噻唑基时， n选自 1或 2;  When Q is selected from thiazolyl, n is selected from 1 or 2;
当 n大于 1时， R5可相同或不同； When n is greater than 1, R 5 may be the same or different;
此时 、 R2 、 R5所述的垸基可进一步优选甲基、 乙基、 正丙基、 异丙基、 正丁基、 仲丁基、异丁基或叔丁基， 卤代垸基可进一步优选三氟甲基、二氟甲基、一氟甲基或氯甲基， 垸氧基可进一步优选甲氧基， 卤代垸氧基可进一步优选三氟甲氧基、三氟乙氧基或一氟甲氧 基， 环垸基可进一步优选环丙基、 环丁基、 环戊基或环己基。 In this case, the mercapto group described by R 2 and R 5 may further preferably be methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl or t-butyl, halofluorenyl. Further, a trifluoromethyl group, a difluoromethyl group, a monofluoromethyl group or a chloromethyl group may be further preferred, a methoxy group may further preferably be a methoxy group, and a halogenated fluorenyloxy group may further preferably be a trifluoromethoxy group or a trifluoroethoxy group. The cyclo or fluoromethoxy group, the cyclodecyl group may further preferably be a cyclopropyl group, a cyclobutyl group, a cyclopentyl group or a cyclohexyl group.
本发明更进一步优选的化合物为： 通式 (I)中  Further preferred compounds of the invention are: in formula (I)
Ri选自氢、 F、 Cl、 Br、 I、 CN、 N02、 C C4垸基、 卤代 C C4垸基、 C C4垸氧基或卤 代 C C4垸氧基； m选自 0至 5的整数； 当 m大于 1时， ！^可相同或不同； Ri is selected from the group consisting of hydrogen, F, Cl, Br, I, CN, N0 2 , CC 4 fluorenyl, halogenated CC 4 fluorenyl, CC 4 decyloxy or halogenated CC 4 decyloxy; m is selected from 0 to 5 Integer; when m is greater than 1, ! ^ can be the same or different;
R2选自氢、 F、 Cl、 Br、 I、 CN、 C C4垸基、 卤代 C C4垸基、 C C4垸氧基、 卤代 C C4 垸氧基 _R6; R 2 is selected from the group consisting of hydrogen, F, Cl, Br, I, CN, CC 4 fluorenyl, halogenated CC 4 fluorenyl, CC 4 decyloxy, halogenated CC 4 methoxy _R6;
Ra、 Rb、 Rc、 Rd、 Re Rf、 Rg和 Rh各自独立的表示氢原子、 C C4垸基、 卤代 C C4垸 基、 卤代 C C4垸氧基或 d-C4垸氧羰基； ！^与 Rh—起或者 Rc与 Rf—起可以结合形成饱和 的六元环； R a , R b , R c , R d , R e R f , R g and R h each independently represent a hydrogen atom, a CC 4 fluorenyl group, a halogenated CC 4 fluorenyl group, a halogenated CC 4 decyloxy group or dC. 4垸 oxycarbonyl; ^ together with R h or R c and R f together can form a saturated six-membered ring;
Xi选自 N或 CR3 ; Xi is selected from N or CR 3 ;
R3选自氢或 CN;  R3 is selected from hydrogen or CN;
X2选自 CH2或 CO; X 2 is selected from CH 2 or CO;
选自氢、 CH3或 CF3 ; Selected from hydrogen, CH 3 or CF 3 ;
Y选自 -CO-或 -CH2-; X选自 0或 1 ; Y is selected from -CO- or -CH 2 - ; X is selected from 0 or 1;
Q选自被 n个各自独立的 R5取代的苯基、 吡啶基、 嘧啶基或者噻唑基； Q is selected from phenyl, pyridyl, pyrimidinyl or thiazolyl substituted by n each independently R 5 ;
R5选自 F、 Cl、 Br、 I、 CN、 N02、 d-C4垸基、 卤代 -C4垸基、 -C4垸氧基、 卤代 d-C4垸氧基、 C02CH3、 C02CH2CH3、 S02CH3或 OCH2CF3 ; R 5 is selected from the group consisting of F, Cl, Br, I, CN, N0 2 , dC 4 fluorenyl, halo-C 4 fluorenyl, -C 4 decyloxy, halo dC 4 decyloxy, C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 or OCH 2 CF 3 ;
R6选自苯基、 4-氯苯基、 2,4-二氯苯基、 4-甲基苯基、 4-三氟甲基苯基、 4-甲氧基苯基、 2,6-二氯 -4-三氟甲基苯基、 苄基、 4-氯苄基、 4-叔丁基苄基、 4-三氟甲基苄基或苯乙基、 2- 吡啶基、 3-氯 -2-吡啶基、 3,5-二氯 -2-吡啶基、 3,5,6-三氯 -2-吡啶基、 5-三氟甲基 -2-吡啶基、 5-甲基 -2-吡啶基、 3-氯 -5-氰基 -2-吡啶基、 3-氯 -5-三氟甲基 -2-吡啶基、 2-吡啶甲基、 2-氯 -5- 吡啶甲基、 3-氯 -5-三氟甲基 -2-吡啶甲基、 2-吡啶乙基或 3-氯 -5-三氟甲基 -2-吡啶乙基； R 6 is selected from the group consisting of phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl, 2,6- Dichloro-4-trifluoromethylphenyl, benzyl, 4-chlorobenzyl, 4-tert-butylbenzyl, 4-trifluoromethylbenzyl or phenethyl, 2-pyridyl, 3-chloro -2-pyridyl, 3,5-dichloro-2-pyridyl, 3,5,6-trichloro-2-pyridyl, 5-trifluoromethyl-2-pyridyl, 5-methyl-2-pyridyl, 3-chloro-5-cyano-2-pyridyl, 3-chloro-5-trifluoromethyl-2-pyridyl, 2-pyridylmethyl, 2-chloro- 5-pyridylmethyl, 3-chloro-5-trifluoromethyl-2-pyridylmethyl, 2-pyridylethyl or 3-chloro-5-trifluoromethyl-2-pyridylethyl;
其中， 当 Q选自苯基时， n选自 1、 2、 3或 4或 5;  Wherein, when Q is selected from phenyl, n is selected from 1, 2, 3 or 4 or 5;
当 Q选自吡啶时， n选自 1、 2或 3或 4;  When Q is selected from pyridine, n is selected from 1, 2 or 3 or 4;
当 Q选自嘧啶时， n选自 1、 2或 3;  When Q is selected from pyrimidine, n is selected from 1, 2 or 3;
当 Q选自噻唑时， n选自 1或 2;  When Q is selected from thiazole, n is selected from 1 or 2;
当 n大于 1时， R5可相同或不同； When n is greater than 1, R 5 may be the same or different;
此时 、 R2 、 R5所述的垸基可进一步优选甲基、 乙基、 正丙基、 异丙基、 正丁基、 仲丁基、异丁基或叔丁基， 卤代垸基可进一步优选三氟甲基、二氟甲基、一氟甲基或氯甲基， 垸氧基可进一步优选甲氧基， 卤代垸氧基可进一步优选三氟甲氧基、三氟乙氧基或一氟甲氧 基。 In this case, the mercapto group described by R 2 and R 5 may further preferably be methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl or t-butyl, halofluorenyl. Further, a trifluoromethyl group, a difluoromethyl group, a monofluoromethyl group or a chloromethyl group may be further preferred, a methoxy group may further preferably be a methoxy group, and a halogenated fluorenyloxy group may further preferably be a trifluoromethoxy group or a trifluoroethoxy group. Base or monofluoromethoxy.
再进一步地， 本发明更优选的化合物为： 通式 (I)中  Still further, more preferred compounds of the invention are: in formula (I)
！^选自氢、 F、 Cl、 Br、 I、 CN、 N02、 CrC4垸基或卤代 CrC4垸基 CrC4垸氧基或卤代 CrC4垸氧基； m选自 0至 5的整数； 当 m大于 1时， ！^可相同或不同； ! ^ selected from hydrogen, F, Cl, Br, I, CN, N0 2 , C r C 4 fluorenyl or halogenated C r C 4 fluorenyl C r C 4 decyloxy or halogenated C r C 4 decyloxy m is selected from an integer from 0 to 5; when m is greater than 1, ! ^ can be the same or different;
R2选自氢、 F、 Cl、 Br、 I、 CN、 CrC4垸基、 卤代 CrC4垸基或 R6; R 2 is selected from the group consisting of hydrogen, F, Cl, Br, I, CN, C r C 4 fluorenyl, halogenated C r C 4 fluorenyl or R 6;
Ra、 Rb、 Rc Rd、 Re、 Rf、 Rg和 Rh各自独立的表示氢原子； R a , R b , R c R d , R e , R f , R g and R h each independently represent a hydrogen atom;
Xi选自 CR3 ; Xi is selected from CR 3 ;
R3选自 CN; R 3 is selected from CN;
X2选自 CH2或 CO; X 2 is selected from CH 2 or CO;
选自氢；  Selected from hydrogen;
Y选自 -CO-或 -CH2-; x选自 0或 1 ; Y is selected from -CO- or -CH 2 - ; x is selected from 0 or 1;
Q选自被 n个各自独立的 R5取代的苯基、 吡啶基、 嘧啶基或者噻唑基； Q is selected from phenyl, pyridyl, pyrimidinyl or thiazolyl substituted by n each independently R 5 ;
R5选自 F、 Cl、 Br、 I、 CN、 N02、 C C4垸基或卤代 C C4垸基、 C C4垸氧基、 卤代 d-C4垸氧基、 C02CH3、 C02CH2CH3、 S02CH3或 OCH2CF3 ; R 5 is selected from the group consisting of F, Cl, Br, I, CN, N0 2 , CC 4 fluorenyl or halogenated CC 4 fluorenyl, CC 4 decyloxy, halogenated dC 4 decyloxy, C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 or OCH 2 CF 3 ;
R6选自苯基、 4-氯苯基、 2,4-二氯苯基、 4-甲基苯基、 4-三氟甲基苯基、 4-甲氧基苯基或 2,6-二氯 -4-三氟甲基苯基、 苄基、 4-氯苄基、 4-叔丁基苄基、 4-三氟甲基苄基或苯乙基； 其中， 当 Q选自苯基时， n选自 1、 2、 3、 4或 5; R 6 is selected from phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl or 2,6- Dichloro-4-trifluoromethylphenyl, benzyl, 4-chlorobenzyl, 4-tert-butylbenzyl, 4-trifluoromethylbenzyl or phenethyl; wherein, when Q is selected from phenyl When n is selected from 1, 2, 3, 4 or 5;
当 Q选自吡啶时， n选自 1或 2、 3或 4;  When Q is selected from pyridine, n is selected from 1 or 2, 3 or 4;
当 Q选自嘧啶时， n选自 1或 2或 3;  When Q is selected from pyrimidine, n is selected from 1 or 2 or 3;
当 Q选自噻唑时， n选自 1或 2;  When Q is selected from thiazole, n is selected from 1 or 2;
当 n大于 1时， R5可相同或不同； When n is greater than 1, R 5 may be the same or different;
此时 、 R2 、 R5所述的垸基可进一步优选甲基、 乙基或叔丁基， 卤代垸基可进一步 优选三氟甲基、 二氟甲基、 一氟甲基或氯甲基， 垸氧基可进一步优选甲氧基， 卤代垸氧基可 进一步优选三氟甲氧基。 In this case, the fluorenyl group described by R 2 and R 5 may further preferably be a methyl group, an ethyl group or a tert-butyl group, and the halogenated fluorenyl group may further preferably be a trifluoromethyl group, a difluoromethyl group, a monofluoromethyl group or a chloro group. The methoxy group may further preferably be a methoxy group, and the halogenated methoxy group may further preferably be a trifluoromethoxy group.
再进一步地， 本发明更优选的化合物为： 通式 (I)中  Still further, more preferred compounds of the invention are: in formula (I)
！^选自氢、 F、 Cl、 Br、 I、 CN、 N02、 CrC4垸基或卤代 CrC4垸基 CrC4垸氧基或卤代 CrC4垸氧基； m选自 0至 5的整数； 当 m大于 1时， ！^可相同或不同； ! ^ selected from hydrogen, F, Cl, Br, I, CN, N0 2 , C r C 4 fluorenyl or halogenated C r C 4 fluorenyl C r C 4 decyloxy or halogenated C r C 4 decyloxy m is selected from an integer from 0 to 5; when m is greater than 1, ! ^ can be the same or different;
R2选自氢、 F、 Cl、 Br、 I、 CN、 CrC4垸基、 卤代 CrC4垸基或 R6; R 2 is selected from the group consisting of hydrogen, F, Cl, Br, I, CN, C r C 4 fluorenyl, halogenated C r C 4 fluorenyl or R 6;
Ra、 Rb、 Rc Rd、 Re、 Rf、 Rg和 Rh各自独立的表示氢原子； R a , R b , R c R d , R e , R f , R g and R h each independently represent a hydrogen atom;
Xi选自 CR3 ; Xi is selected from CR 3 ;
R3选自 CN; R 3 is selected from CN;
X2选自 CH2或 CO; X 2 is selected from CH 2 or CO;
选自氢；  Selected from hydrogen;
Y选自 -CO-或 -CH2-; x选自 0或 1 ; Q选自被 n个各自独立的 R5取代的苯基、 吡啶基、 嘧啶基或噻唑基； Y is selected from -CO- or -CH 2 - ; x is selected from 0 or 1; Q is selected from phenyl, pyridyl, pyrimidinyl or thiazolyl substituted by n each independently R 5 ;
R5选自 F、 Cl、 Br、 I、 CN、 N02、 CrC4垸基、 卤代 CrC4垸基、 CrC4垸氧基、 卤代 d-C4垸氧基、 S02CH3或 OCH2CF3 ; R 5 is selected from the group consisting of F, Cl, Br, I, CN, N0 2 , C r C 4 fluorenyl, halogenated C r C 4 fluorenyl, C r C 4 decyloxy, halogenated dC 4 decyloxy, S0 2 CH 3 or OCH 2 CF 3 ;
R6选自苯基、 4-氯苯基、 2,4-二氯苯基、 4-甲基苯基、 4-三氟甲基苯基、 4-甲氧基苯基或 2,6-二氯 -4-三氟甲基苯基。 R 6 is selected from phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl or 2,6- Dichloro-4-trifluoromethylphenyl.
其中， 当 Q选自苯基时， n选自 1、 2或 3 ;  Wherein, when Q is selected from phenyl, n is selected from 1, 2 or 3;
当 Q选自吡啶时， n选自 1或 2或 3 ;  When Q is selected from pyridine, n is selected from 1 or 2 or 3;
当 Q选自嘧啶时， n选自 1或 2;  When Q is selected from pyrimidine, n is selected from 1 or 2;
当 Q选自噻唑时， n选自 1或 2;  When Q is selected from thiazole, n is selected from 1 or 2;
当 n大于 1时， R5可相同或不同； When n is greater than 1, R 5 may be the same or different;
此时 、 R2 、 R5所述的垸基可进一步优选甲基、 乙基或叔丁基， 卤代垸基可进一步 优选三氟甲基、 二氟甲基、 一氟甲基或氯甲基， 垸氧基可进一步优选甲氧基， 卤代垸氧基可 进一步优选三氟甲氧基。 In this case, the fluorenyl group described by R 2 and R 5 may further preferably be a methyl group, an ethyl group or a tert-butyl group, and the halogenated fluorenyl group may further preferably be a trifluoromethyl group, a difluoromethyl group, a monofluoromethyl group or a chloro group. The methoxy group may further preferably be a methoxy group, and the halogenated methoxy group may further preferably be a trifluoromethoxy group.
本发明更优选的化合物为： 通式 (I)中  More preferred compounds of the invention are: in formula (I)
选自氢、 F、 Cl、 Br、 I、 CN、 N02、 CrC4垸基或卤代 CrC4垸基； m选自 0至 5的 整数； 当 m大于 1时， ！^可相同或不同； Selected from hydrogen, F, Cl, Br, I, CN, N0 2 , C r C 4 fluorenyl or halogenated C r C 4 fluorenyl; m is selected from an integer from 0 to 5; when m is greater than 1, ! ^ can be the same or different;
R2选自氢、 C C4垸基、 卤代 C C4垸基或 R6; R 2 is selected from the group consisting of hydrogen, CC 4 fluorenyl, halogenated CC 4 fluorenyl or R 6;
Ra、 Rb、 Rc Rd、 Re、 Rf、 Rg和 各自独立的表示氢原子； R a , R b , Rc R d , R e , R f , R g and each independently represent a hydrogen atom;
Xi选自 CR3 ; Xi is selected from CR 3 ;
R3选自 CN; R 3 is selected from CN;
X2选自 CO; X 2 is selected from CO;
选自氢；  Selected from hydrogen;
Y选自 -CO-或 -CH2-; x选自 0; Y is selected from -CO- or -CH 2 - ; x is selected from 0;
Q选自被 1个 R5取代的吡啶基； Q is selected from pyridyl substituted by 1 R 5 ;
R5选自氢、 F、 Cl、 Br、 I、 CN、 N02、 C C4垸基或卤代 C C4垸基； R 5 is selected from the group consisting of hydrogen, F, Cl, Br, I, CN, N0 2 , CC 4 fluorenyl or halogenated CC 4 fluorenyl;
R6选自苯基； R 6 is selected from phenyl;
此时 、 R2 、 R5所述的垸基可进一步优选甲基、 乙基或叔丁基， 卤代垸基可进一步 优选三氟甲基、 二氟甲基、 一氟甲基或氯甲基。 In this case, the fluorenyl group described by R 2 and R 5 may further preferably be a methyl group, an ethyl group or a tert-butyl group, and the halogenated fluorenyl group may further preferably be a trifluoromethyl group, a difluoromethyl group, a monofluoromethyl group or a chloro group. base.
上面给出的通式 (I)化合物的定义中， 汇集所用术语一般定义如下：  In the definitions of the compounds of the general formula (I) given above, the terms used in the collection are generally defined as follows:
卤素： 指氟、 氯、 溴或碘。 垸基： 直链或支链垸基， 例如甲基、 乙基、 丙基、 异丙基、 正丁基或叔丁基。 环垸基： 取代或未取代的环状垸基， 例如环丙基、 环戊基或环己基。 取代 基如甲基、 卤素等。 卤代垸基： 直链或支链垸基， 在这些垸基上的氢原子可部分或全部被卤 原子所取代， 例如， 氯甲基、 二氯甲基、 三氯甲基、 氟甲基、 二氟甲基、 三氟甲基等。 氰基 垸基： 直链或支链垸基， 在这些垸基上的氢原子可部分被氰基所取代， 例如， -CH2CN、 -CH2CH2CN、 -CH2C(CH3)2CN -CH2CH(CN)2等。 垸氧基： 直链或支链垸基， 经氧原子键连 接到结构上。 氰基垸氧基： 氰基垸基经氧原子键连接到结构上。 如 CNCH20-。 垸氧基垸基: 垸氧基经垸基连接到结构上。 如 CH3OCH2-， CH3CH2OCH2-。 卤代垸氧基垸基： 垸氧基垸基 的垸基上的氢原子可部分或全部被卤原子所取代。如 ClCH2CH2OCH2-。垸氧基羰基： 垸氧基 经羰基连接到结构上。 如 CH3OCO-， CH3CH2OCO-。 垸氧基羰基垸基： 垸氧基羰基再经过垸 基连接到结构上。 卤代垸氧基： 直链或支链垸氧基， 在这些垸氧基上的氢原子可部分或全部 被卤原子所取代。 例如， 氯甲氧基、 二氯甲氧基、 三氯甲氧基、 氟甲氧基、 二氟甲氧基、 三 氟甲氧基、 氯氟甲氧基、 三氟乙氧基等。 垸硫基： 直链或支链垸基， 经硫原子键连接到结构 上。 垸硫基垸基： 垸硫基经垸基连接到结构上。 如 CH3SCH2-。 卤代垸硫基： 直链或支链垸 硫基，在这些垸基上的氢原子可部分或全部被卤原子所取代。例如， 氯甲硫基、二氯甲硫基、 三氯甲硫基、 氟甲硫基、 二氟甲硫基、 三氟甲硫基、 氯氟甲硫基等。 卤代垸硫基垸基： 卤代 垸硫基经垸基连接到结构上。 垸基氨基： 直链或支链垸基， 经氮原子键连接到结构上。 垸基 氨基羰基： 如 CH3NHCO-， CH3CH2NHCO-。 卤代垸基氨基羰基： 垸基氨基羰基的垸基上的 氢原子可部分或全部被卤原子所取代。如 CF3NHCO-。 卤代垸基氨基： 直链或支链垸基氨基， 在这些垸基上的氢原子可部分或全部被卤原子所取代。烯基：直链或支链烯类，例如乙烯基、 1-丙烯基、 2-丙烯基和不同的丁烯基、 戊烯基和己烯基异构体。 烯基还包括多烯类， 如 1,2- 丙二烯基和 2,4-己二烯基。 卤代烯基： 直链或支链烯类， 在这些烯基上的氢原子可部分或全 部被卤原子所取代。 炔基： 直链或支链炔类， 例如乙炔基、 1-丙炔基、 2-丙炔基和不同的丁 炔基、 戊炔基和己炔基异构体。 炔基还包括由多个三键组成的基团， 如 2,5-己二炔基。 卤代 炔基： 直链或支链炔类， 在这些炔基上的氢原子可部分或全部被卤原子所取代。 烯氧基： 直 链或支链烯类， 经氧原子键连接到结构上。 卤代烯氧基： 直链或支链烯氧基， 在这些烯氧基 上的氢原子可部分或全部被卤原子所取代。 炔氧基： 直链或支链炔类， 经氧原子键连接到结 构上。 卤代炔氧基： 直链或支链炔氧基， 在这些炔氧基上的氢原子可部分或全部被卤原子所 取代。 垸基羰基： 垸基经羰基连接到结构上， 如 CH3CO-， CH3CH20-。 卤代垸基羰基： 垸基 羰基的垸基上的氢原子可部分或全部被卤原子所取代， 如 CF3CO-。 垸基亚磺酰基： 直链或 支链垸基经亚磺酰基（-SO-)连接到结构上， 如甲基亚磺酰基。 卤代垸基亚磺酰基： 直链或 支链垸基亚磺酰基， 其垸基上的氢原子可部分或全部被卤原子所取代。 垸基磺酰基： 直链或 支链垸基经磺酰基 （-S02-) 连接到结构上， 如甲基磺酰基。 卤代垸基磺酰基： 直链或支链 垸基磺酰基， 其垸基上的氢原子可部分或全部被卤原子所取代。 苯氧基羰基： 苯氧基经羰基 连接到结构上， 如 PhOCO-。 苯基氨基羰基： 苯基氨基经羰基连接到结构上， 如 PhNHCO-。 苯基垸基： 将苯基经垸基连接到结构上， 如苄基， 苯乙基等。 萘基垸基： 将萘基经垸基连接 到结构上， 如萘甲基， 萘乙基等。 杂芳基： 本发明中所指杂芳基是含 1个或多 N、 0、 S杂原 子的五元环或六元环芳基。 例如吡啶基、 嘧啶基、 吡嗪基、 哒嗪基、 呋喃基、 噻唑基、 喹啉 基、 异噻唑基、 恶唑基、 异恶唑基、 吡唑基、 苯并噻唑基、 苯并呋喃基等。 杂芳基羰基： 杂 芳基经羰基连接到结构上， 如吡啶甲酰基、 嘧啶甲酰基、 吡唑甲酰基。 杂芳基氧基羰基： 杂 芳基氧基经羰基连接到结构上。 杂芳基氨基羰基： 杂芳基氨基经羰基连接到结构上。 杂芳基 垸基： 将杂芳基经垸基连接到结构上， 如呋喃甲基， 吡啶乙基等。 Halogen: Refers to fluorine, chlorine, bromine or iodine. Mercapto: A linear or branched fluorenyl group such as methyl, ethyl, propyl, isopropyl, n-butyl or t-butyl. Cyclodecyl: a substituted or unsubstituted cyclic fluorenyl group such as cyclopropyl, cyclopentyl or cyclohexyl. Substituents such as methyl, halogen and the like. Halogenated fluorenyl: a straight or branched fluorenyl group in which a hydrogen atom may be partially or completely replaced by a halogen atom, for example, chloromethyl, dichloromethyl, trichloromethyl, fluoromethyl , difluoromethyl, trifluoromethyl and the like. Cyano fluorenyl: a linear or branched fluorenyl group, the hydrogen atom on these fluorenyl groups may be partially substituted by a cyano group, for example, -CH 2 CN, -CH 2 CH 2 CN, -CH 2 C(CH 3 2 CN -CH 2 CH(CN) 2 and the like. Alkoxy: A linear or branched fluorenyl group attached to the structure via an oxygen atom. Cyanomethoxy group: The cyanoguanidino group is bonded to the structure via an oxygen atom bond. Such as CNCH 2 0-. Alkoxyalkyl: A decyloxy group is attached to the structure via a thiol group. For example, CH 3 OCH 2 -, CH 3 CH 2 OCH 2 -. Halogenated fluorenyl fluorenyl: The hydrogen atom on the fluorenyl group of the fluorenyl fluorenyl group may be partially or completely substituted by a halogen atom. Such as ClCH 2 CH 2 OCH 2 -. Alkoxycarbonyl: a decyloxy group is attached to the structure via a carbonyl group. Such as CH 3 OCO-, CH 3 CH 2 OCO-. Anthracenylcarbonylcarbonyl: A decyloxycarbonyl group is attached to the structure via a thiol group. Halogenated methoxy group: a linear or branched decyloxy group, and a hydrogen atom on these decyloxy groups may be partially or completely substituted by a halogen atom. For example, chloromethoxy, dichloromethoxy, trichloromethoxy, fluoromethoxy, difluoromethoxy, trifluoromethoxy, chlorofluoromethoxy, trifluoroethoxy, and the like. Thiothio group: A linear or branched fluorenyl group bonded to a structure via a sulfur atom bond. Thiothio group: The sulfonium group is attached to the structure via a thiol group. Such as CH 3 SCH 2 -. Halogenated thiol group: a linear or branched thiol group, and a hydrogen atom on these fluorenyl groups may be partially or completely substituted by a halogen atom. For example, chloromethylthio, dichloromethylthio, Trichloromethylthio, fluoromethylthio, difluoromethylthio, trifluoromethylthio, chlorofluoromethylthio and the like. Halogenated sulfhydryl fluorenyl: The halo sulfhydryl group is attached to the structure via a fluorenyl group. Mercaptoamino: a linear or branched fluorenyl group bonded to the structure via a nitrogen atom. Mercaptoaminocarbonyl: such as CH 3 NHCO-, CH 3 CH 2 NHCO-. Halogenated fluorenylaminocarbonyl: The hydrogen atom on the fluorenyl group of the fluorenylaminocarbonyl group may be partially or completely substituted by a halogen atom. Such as CF 3 NHCO-. Halogenated mercaptoamino group: a linear or branched mercaptoamino group, and a hydrogen atom on these mercapto groups may be partially or completely substituted by a halogen atom. Alkenyl: a linear or branched olefin such as a vinyl group, a 1-propenyl group, a 2-propenyl group and a different butenyl, pentenyl and hexenyl isomer. Alkenyl groups also include polyenes such as 1,2-propadienyl and 2,4-hexadienyl. Haloalkenyl group: a linear or branched olefin in which a hydrogen atom on these alkenyl groups may be partially or completely substituted by a halogen atom. Alkynyl: a straight or branched acetylenic group such as ethynyl, 1-propynyl, 2-propynyl and the different butynyl, pentynyl and hexynyl isomers. The alkynyl group also includes a group consisting of a plurality of triple bonds, such as 2,5-hexadiynyl. Haloalkynyl group: a linear or branched alkyne, and a hydrogen atom on these alkynyl groups may be partially or completely substituted by a halogen atom. Alkenyloxy: A linear or branched olefin that is bonded to the structure via an oxygen atom. Haloalkenyloxy: a linear or branched alkenyloxy group, and a hydrogen atom on these alkenyloxy groups may be partially or completely substituted by a halogen atom. Alkynyloxy: A linear or branched acetylenic group attached to the structure via an oxygen atom. Haloalkynyloxy: a straight or branched alkynyloxy group in which a hydrogen atom may be partially or completely substituted by a halogen atom. Mercaptocarbonyl: The fluorenyl group is attached to the structure via a carbonyl group such as CH 3 CO-, CH 3 CH 2 0-. Halogenated fluorenylcarbonyl: The hydrogen atom on the fluorenyl group of the fluorenylcarbonyl group may be partially or completely substituted by a halogen atom such as CF 3 CO-. Mercaptosulfinyl: A linear or branched fluorenyl group is attached to the structure via a sulfinyl group (-SO-), such as a methylsulfinyl group. Halogenated fluorenylsulfinyl: a linear or branched fluorenylsulfinyl group in which a hydrogen atom on the fluorenyl group may be partially or completely substituted by a halogen atom. Mercaptosulfonyl: A linear or branched fluorenyl group is attached to the structure via a sulfonyl group (-S0 2 -), such as a methylsulfonyl group. Halogenated fluorenylsulfonyl: a linear or branched fluorenylsulfonyl group in which a hydrogen atom on the fluorenyl group may be partially or completely substituted by a halogen atom. Phenoxycarbonyl: A phenoxy group is attached to the structure via a carbonyl group, such as PhOCO-. Phenylaminocarbonyl: A phenylamino group is attached to the structure via a carbonyl group, such as PhNHCO-. Phenylfluorenyl: A phenyl group is attached to the structure via a thiol group, such as benzyl, phenethyl, and the like. Naphthylfluorenyl: A naphthyl group is attached to the structure via a fluorenyl group, such as naphthylmethyl, naphthylethyl, and the like. Heteroaryl: The heteroaryl group referred to in the present invention is a five-membered or six-membered ring aryl group having one or more N, 0, S hetero atoms. For example, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, furyl, thiazolyl, quinolinyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazolyl, benzothiazolyl, benzofuran Base. Heteroarylcarbonyl: A heteroaryl group is attached to the structure via a carbonyl group, such as a picolinyl group, a pyrimidinyl group, a pyrazolyl group. Heteroaryloxycarbonyl: A heteroaryloxy group is attached to the structure via a carbonyl group. Heteroarylaminocarbonyl: A heteroarylamino group is attached to the structure via a carbonyl group. Heteroaryl fluorenyl: A heteroaryl group is attached to the structure via a thiol group, such as furylmethyl, pyridylethyl, and the like.
本发明的通式 (I)中， 当 Ra、 Rb、 Rc Rd Re Rf、 Rg和 为氢时， 优选 Q基团上的取 代基如下： In the general formula (I) of the present invention, when R a , R b , Rc R d R e Rf, R g and hydrogen are hydrogen, the substituent on the Q group is preferably as follows:
当 Q为吡啶基时， 吡啶环上的取代基见表 1-表 3; 当 Q为苯基时， 苯环上的取代基见表 4； 当 Q为嘧啶基时， 嘧啶环上的取代基见表 5-表 6; 当 Q为吡嗪时， 吡嗪环上的取代基见 表 7; 当 Q为哒嗪时， 哒嗪环上的取代基见表 8; 当 Q为吡唑基时， 吡唑环上的取代基见表 9-表 10; 当 Q为噻唑、 恶唑或咪唑时， 噻唑、 恶唑或咪唑环上的取代基见表 11-表 12; 当 Q 为噻吩、 吡咯或呋喃时， 噻吩、 吡咯或呋喃环上的取代基见表 13-表 14; 当 Q为喹啉时， 喹 啉环上的取代基见表 15; 当 Q为哒嗪酮时， 哒嗪酮环上的取代基见表 16。
Figure imgf000011_0001
When Q is a pyridyl group, the substituents on the pyridine ring are shown in Table 1 - Table 3; when Q is a phenyl group, the substituent on the benzene ring is shown in Table 4; when Q is a pyrimidinyl group, the substituent on the pyrimidine ring See Table 5 - Table 6; when Q is pyrazine, the substituent on the pyrazine ring is shown in Table 7; when Q is pyridazine, the substituent on the pyridazine ring is shown in Table 8; when Q is pyrazolyl , the substituents on the pyrazole ring are shown in Table 9 - Table 10; when Q is thiazole, oxazole or imidazole, the substituents on the thiazole, oxazole or imidazole ring are shown in Table 11 - Table 12; when Q is thiophene, pyrrole Or furan, the substituents on the thiophene, pyrrole or furan ring are shown in Table 13 - Table 14; when Q is quinoline, the substituent on the quinoline ring is shown in Table 15; when Q is pyridazinone, pyridazinone The substituents on the ring are shown in Table 16.
Figure imgf000011_0001
Figure imgf000011_0002
4- CI 5- Br 5-OCH3 3-N02-5-Br 5-CN-6-CH3
Figure imgf000011_0002
4- CI 5- Br 5-OCH3 3-N0 2 -5-Br 5-CN-6-CH3
5- CI 6- Br 3,5- 2C1 3- Br- 5- N02 3- CN- 4,6- 2C15- CI 6- Br 3,5- 2C1 3- Br- 5- N0 2 3- CN- 4,6- 2C1
6- CI 5-1 3,5- 2Br 3- Br- 5- CH3 3,5- 2Br- 6- CH3 6- CI 5-1 3,5- 2Br 3- Br- 5- CH 3 3,5- 2Br- 6- CH 3
3-CH3 5-F 3,5,6- 3C1 5- Br- 6- CH3 3-CN-4-CH3-6-CI3-CH 3 5-F 3,5,6- 3C1 5- Br- 6- CH 3 3-CN-4-CH3-6-CI
4-CH3 6-F 3-CO2CH3 3- CH3- 5- Br 3-CN-4-CF3-6-CI4-CH3 6-F 3-CO2CH3 3- CH 3 - 5- Br 3-CN-4-CF3-6-CI
5-CH3 3-CN 5-CO2CH3 3-CF3-6-CI 4-CH3-5-CN-6-C15-CH3 3-CN 5-CO2CH3 3-CF3-6-CI 4-CH3-5-CN-6-C1
6-CH3 4-CN 3-OCH2Ph 3-CH3-5-NO2 4-CF3-5-CN-6-CI6-CH3 4-CN 3-OCH 2 Ph 3-CH3-5-NO2 4-CF3-5-CN-6-CI
3-CF3 5-CN 5-CF3-6-CI 3-NO2-4-CH3 3-CO2CH3-6-CI3-CF3 5-CN 5-CF3-6-CI 3-NO2-4-CH3 3-CO2CH3-6-CI
4-CF3 6-CN 3-CN-6-C1 4-CH3-5-NO2 5-CO2CH3-6-CI4-CF3 6-CN 3-CN-6-C1 4-CH3-5-NO2 5-CO2CH3-6-CI
5-CF3 3-NO2 3-CI-5-CF3 3-NO2-5-CH3 3,6- 2C1- 5- CF3 5-CF3 3-NO2 3-CI-5-CF3 3-NO2-5-CH3 3,6- 2C1- 5- CF 3
6-CF3 5-N02 3-C1-5-CN 4-NO2-6-CH3 3- CONH2- 4,6- 2C16-CF3 5-N0 2 3-C1-5-CN 4-NO2-6-CH3 3- CONH 2 - 4,6- 2C1
3- Br 6- N02 3-CI-5-CH3 5-NO2-6-CH3 3- Br- 4- CH3- 5- N02 3- Br 6- N0 2 3-CI-5-CH3 5-NO2-6-CH3 3- Br- 4- CH 3 - 5- N0 2
3,5- 2C1- 6- OCH3 3,5- 2C1- 6- (0- Ph- 4- CI) 3,5- 2C1- 6- OCH 3 3,5- 2C1- 6- (0- Ph- 4- CI)
Figure imgf000012_0001
Figure imgf000012_0003
Figure imgf000012_0002
Figure imgf000012_0001
Figure imgf000012_0003
Figure imgf000012_0002
Figure imgf000012_0004
Figure imgf000012_0004
表 4
Figure imgf000013_0001
Table 4
Figure imgf000013_0001
Figure imgf000013_0002
2-N02 2,3,6- 3F 2-CH3-5-CI 2-CI-5-CF3 2- Br- 4- COOCH3
Figure imgf000013_0002
2-N0 2 2,3,6- 3F 2-CH3-5-CI 2-CI-5-CF3 2- Br- 4- COOCH 3
3-N02 2,4,5- 3F 2- CH3- 5- Br 2- Br- 5- CF3 2,4,6- 3CH(CH3)2 3-N0 2 2,4,5- 3F 2- CH 3 - 5- Br 2- Br- 5- CF 3 2,4,6- 3CH(CH 3 ) 2
4-N02 2,4,6- 3F 2-CH3-6-CI 2-CN-3-F 2,4,6- 3C(CH3)3 4-N0 2 2,4,6- 3F 2-CH3-6-CI 2-CN-3-F 2,4,6- 3C(CH 3 ) 3
3-SCF3 2,3- 2N02 2- Br- 3- CH3 2- CN- 3- CI 2,3- 2CH3- 6- N02 3-SCF3 2,3- 2N0 2 2- Br- 3- CH 3 2- CN- 3- CI 2,3- 2CH 3 - 6- N0 2
4-SCF3 2,4- 2N02 3-CH3-4-C1 2-CN-4-N02 2,4- 20CH3- 5- CI4-SCF3 2,4- 2N0 2 3-CH3-4-C1 2-CN-4-N02 2,4- 20CH 3 - 5- CI
2-OC2H5 2,5- 2N02 3- CH3- 4- Br 2- CN- 4- CI 2-CI-5-CONH22-OC2H5 2,5- 2N0 2 3- CH 3 - 4- Br 2- CN- 4- CI 2-CI-5-CONH2
3-OC2H5 2,6- 2N02 3-CH3-4-I 2- CN- 4- Br 2-N02-4-N(CH3)2 3-OC2H5 2,6- 2N0 2 3-CH3-4-I 2- CN- 4- Br 2-N0 2 -4-N(CH 3 ) 2
4- OC2H5 3,4- 2N02 2-CH3-4-I 2-CF3-4-CN 2-N02-5-N(CH3)2 4- OC 2 H 5 3,4- 2N0 2 2-CH3-4-I 2-CF3-4-CN 2-N0 2 -5-N(CH 3 ) 2
2-COCH3 3,5- 2N02 2-C1-4-F 2- CI- 4- CN 2- N02- 4,5- 2CH3 2-COCH3 3,5-2N0 2 2-C1-4-F 2- CI- 4- CN 2- N0 2 - 4,5- 2CH 3
3-COCH3 3,5- 20CH3 2- CI- 4- Br 2-N02-4-CN 2-N02-4-F-5-C13-COCH3 3,5- 20CH 3 2- CI- 4- Br 2-N02-4-CN 2-N02-4-F-5-C1
4-COCH3 2-OCH2Ph 2-C1-4-I 2-F-5-CH3 2-CN-4-N02-6-C14-COCH3 2-OCH 2 Ph 2-C1-4-I 2-F-5-CH3 2-CN-4-N02-6-C1
2-CH2Ph 3-OCH2Ph 3-C1-4-I 2-NO2-4-CH3 2- CN- 4- N02- 6- Br2-CH 2 Ph 3-OCH 2 Ph 3-C1-4-I 2-NO2-4-CH3 2- CN- 4- N0 2 - 6- Br
3-CH2Ph 4-OCH2Ph 2- Br- 4- CI 3-NO2-4-CH3 2- OCH2CH=CH2 3-CH 2 Ph 4-OCH 2 Ph 2- Br- 4- CI 3-NO2-4-CH3 2- OCH 2 CH=CH 2
4-CH2Ph 3-CONH2 3,4,5- 3F 2-CN-5-CH3 3-OCH2CH=CH2 4-CH 2 Ph 3-CONH 2 3,4,5- 3F 2-CN-5-CH3 3-OCH 2 CH=CH 2
2- C(CH3)3 4-CONH2 2,3,4- 3C1 2-F-5-N02 4- OCH2CH=CH2 2- C(CH 3 ) 3 4-CONH 2 2,3,4- 3C1 2-F-5-N0 2 4- OCH 2 CH=CH 2
3- C(CH3)3 2- N(CH3)2 2,3,5- 3C1 2- CF3- 4,6- 2C1 3-OCH2Ph-4-CH3 3- C(CH 3 ) 3 2- N(CH 3 ) 2 2,3,5- 3C1 2-CF 3 - 4,6- 2C1 3-OCH 2 Ph-4-CH 3
4- C(CH3)3 3-N(CH3)2 2,3,6- 3C1 2- CF3- 4,6- 2Br 2- CH2C(CH3)=CH2 4- C(CH 3 ) 3 3-N(CH 3 ) 2 2,3,6- 3C1 2-CF 3 -4,6- 2Br 2- CH 2 C(CH 3 )=CH 2
2- COC2H5 4-N(CH3)2 2,4,5- 3C1 3- CH3- 2,6- 2C1 3-CH2C(CH3)=CH2 2-COC 2 H 5 4-N(CH 3 ) 2 2,4,5- 3C1 3- CH 3 - 2,6- 2C1 3-CH 2 C(CH 3 )=CH 2
3-COC2H5 2-N(C2H5)2 2,4,6- 3C1 2- CH3- 4,6- 2Br 2- CH3- 5- CONH2 3-COC 2 H 5 2-N(C 2 H 5 ) 2 2,4,6- 3C1 2- CH 3 - 4,6- 2Br 2- CH 3 - 5-CONH 2
4- COC2H5 3-N(C2H5)2 3,4,5- 3C1 2,4,6- 30CH3 2-CI-5-NHCOCH34-COC 2 H 5 3-N(C 2 H 5 ) 2 3,4,5- 3C1 2,4,6- 30CH 3 2-CI-5-NHCOCH3
2-SOCH3 4-N(C2H5)2 2,3,4- 3Br 3,4,5- 30CH3 2,6- 2Br- 3- CI- 4- F2-SOCH3 4-N(C 2 H 5 ) 2 2,3,4- 3Br 3,4,5- 30CH 3 2,6- 2Br- 3- CI- 4- F
3-SOCH3 2 -20CH3 2,3,5- 3Br 2,4,6- 3SCH3 2,3- (CH2CH2CH2- )3-SOCH3 2 -20CH3 2,3,5- 3Br 2,4,6- 3SCH 3 2,3- (CH 2 CH 2 CH 2 - )
4-SOCH3 2,4- 20CH3 2,3,6- 3Br 2,4,6- 30CF3 4- 0(CH2)3CH3 4-SOCH3 2,4- 20CH 3 2,3,6- 3Br 2,4,6- 30CF 3 4- 0(CH 2 ) 3 CH 3
2-SO2CH3 2,5- 20CH3 2,4,5- 3Br 2,4,6- 3SCF3 4- 0(CH2)2N(CH3)2 2-SO2CH3 2,5-20CH 3 2,4,5- 3Br 2,4,6- 3SCF 3 4- 0(CH 2 ) 2 N(CH 3 ) 2
3-SO2CH3 2,6- 20CH3 2,4,6- 3Br 2- CH2C≡CH 3-CH3-4-NHCOCH33-SO2CH3 2,6- 20CH 3 2,4,6- 3Br 2- CH 2 C≡CH 3-CH3-4-NHCOCH3
4-SO2CH3 3,4- 20CH3 3,4,5- 3Br 3-CH2C≡CH 3-NHSO2CH3-4-CH34-SO2CH3 3,4- 20CH 3 3,4,5- 3Br 3 -CH 2 C≡CH 3-NHSO2CH3-4-CH3
2-SOC2H5 4- C02C2H5 3-F-4-CH3 4- CH2C≡CH 3- OCH2Ph- 4- CH3- 6- Br2-SOC2H5 4- C0 2 C 2 H 5 3-F-4-CH3 4- CH 2 C≡CH 3- OCH 2 Ph- 4- CH 3 - 6- Br
3-SOC2H5 2 -2OCF3 3-CI-4-CH3 2-F-3-C1 2-OCH3-5-CH3-4-CI3-SOC2H5 2 -2OCF3 3-CI-4-CH3 2-F-3-C1 2-OCH3-5-CH3-4-CI
4- SOC2H5 2,4- 20CF3 3- Br- 4- CH3 2-CI-3-CH3 2,6- 2C1- 4- COCH3 4- SOC 2 H 5 2,4- 20CF 3 3- Br- 4- CH 3 2-CI-3-CH3 2,6- 2C1- 4-COCH 3
2- OCHF2 2,5- 20CF3 2,4,6- 3CF3 4- (4- F- Ph) 2-NHCOCH3-5-CF32- OCHF 2 2,5- 20CF 3 2,4,6- 3CF 3 4- (4-F- Ph) 2-NHCOCH3-5-CF3
3-OCHF2 2,6- 20CF3 2-CH3-3-F 4- (4- N02- Ph) 2-CH3-4-NO2-6-CI3-OCHF 2 2,6- 20CF 3 2-CH3-3-F 4- (4- N0 2 - Ph) 2-CH3-4-NO2-6-CI
4-OCHF2 3,4- 20CF3 2-CH3-3-CI 4- (3- CI- Ph) 2- CH3- 4- N02- 6- Br4-OCHF2 3,4- 20CF 3 2-CH3-3-CI 4- (3- CI- Ph) 2- CH 3 - 4- N0 2 - 6- Br
2-CO2CH3 3,5- 20CF3 2-CH3-4-F 4- (2- CI- Ph) 2-CH3-4-CI-6-NO22-CO2CH3 3,5-20CF 3 2-CH3-4-F 4- (2- CI- Ph) 2-CH3-4-CI-6-NO2
3-CO2CH3 2,3-2SCF3 2-CH3-4-C1 4- (4- CI- Ph) 2- CH3- 4- Br- 6- N02 3-CO2CH3 2,3-2SCF 3 2-CH3-4-C1 4- (4- CI- Ph) 2- CH 3 - 4- Br- 6- N0 2
4- C02CH3 2,4- 2SCF3 2- CH3- 4- Br 4- (4- CH3- Ph) 2,5- 20CH3- 4- N02 4- C0 2 CH 3 2,4- 2SCF 3 2- CH 3 - 4- Br 4- (4-CH 3 - Ph) 2,5- 20CH 3 - 4- N0 2
2- C02C2H5 2,5- 2SCF3 2- Br- 4- CH3 2- OCH2C≡CH 2,6- 2CH3- 4- C(CH3)3 2- C0 2 C 2 H 5 2,5- 2SCF 3 2- Br- 4- CH 3 2- OCH 2 C≡CH 2,6- 2CH 3 - 4- C(CH 3 ) 3
4- (4- Br- Ph) 2- Br- 5- N02 2- Br- 4- OCF3 3-OCH2C≡CH 4- CH2C(CH3)=CH2 4-(4-Br- Ph) 2-Br- 5- N0 2 2- Br- 4- OCF 3 3-OCH 2 C≡CH 4- CH 2 C(CH 3 )=CH 2
4- (4- CN- Ph) 2-OCH3-5-CI 2,3,5,6- 4F 4- OCH2C≡CH 2- N02- 4- 0(CH2)3CH3 - 0(Ph- 4- Br) 3-F-4-OCH3 2- CN- 4,6- 2C1 5-NO2-2-OCH3 3- OCH3- 4- C02CH3- 0(Ph- 4- CH3) 3-C1-4-OCH3 2- CN- 4,6- 2Br 2-OCH3-5-CH3 2,5- 2C1- 4- N02- (4- OCH3- Ph) 3-N02-4-F 2,6- 2C1- 4- CN 2,6- 2C1- 4- N02 2- N02- 4- CF3- 6- Br - (2- CH3- Ph) 2-OCF3-4-CN 2,6- 2C1- 4- CF3 2-NO2-4-OCF3 2-N02-4-CF3-5-C14- (4- CN- Ph) 2-OCH3-5-CI 2,3,5,6- 4F 4- OCH 2 C≡CH 2- N0 2 - 4- 0(CH 2 ) 3 CH 3 - 0( Ph- 4-Br) 3-F-4-OCH3 2- CN- 4,6- 2C1 5-NO2-2-OCH3 3- OCH 3 - 4- C0 2 CH 3 - 0(Ph- 4- CH 3 ) 3-C1-4-OCH3 2- CN- 4,6- 2Br 2-OCH3-5-CH3 2,5- 2C1- 4- N0 2 - (4- OCH 3 - Ph) 3-N02-4-F 2 ,6- 2C1- 4- CN 2,6- 2C1- 4- N0 2 2- N0 2 - 4-CF 3 - 6- Br - (2-CH 3 - Ph) 2-OCF3-4-CN 2,6 - 2C1- 4- CF 3 2-NO2-4-OCF3 2-N02-4-CF3-5-C1
2-OCF3-4-CI 2,6- 2Br- 4- CF3 2,3,4- 3F- 6- N02 2- CONH2- 5- CH3 2-NO2-4-CF3-6-CI
Figure imgf000015_0001
Figure imgf000015_0002
2-OCF3-4-CI 2,6- 2Br- 4- CF 3 2,3,4- 3F- 6- N0 2 2 -CONH 2 - 5- CH 3 2-NO2-4-CF3-6-CI
Figure imgf000015_0001
Figure imgf000015_0002
(R5)„ (R5)„ (R5)„ (R5)„ (R5)„(R 5 )„ (R 5 )„ (R 5 )„ (R 5 )„ (R 5 )„
5- Br 5-Cl 6-Cl 3-Cl 5-CH35- Br 5-Cl 6-Cl 3-Cl 5-CH3
5-NH2 5-CN 6-CN 5-OCH3 6-OCH35-NH 2 5-CN 6-CN 5-OCH3 6-OCH3
5-SCH3 6-SCH3 6-OPh 5-OPh 5-SPh 5-SCH3 6-SCH3 6-OPh 5-OPh 5-SPh
Figure imgf000016_0001
Figure imgf000016_0001
Figure imgf000016_0004
Figure imgf000016_0002
Figure imgf000016_0005
Figure imgf000016_0003
Figure imgf000016_0006
Figure imgf000016_0004
Figure imgf000016_0002
Figure imgf000016_0005
Figure imgf000016_0003
Figure imgf000016_0006
表 11
Figure imgf000017_0001
Table 11
Figure imgf000017_0001
Figure imgf000018_0001
Figure imgf000018_0001
(Rs)„ (Rs)„ (Rs)„ (Rs)„ (Rs)„ -CN 5-NO2 4- C(CH3)3 4- (Ph- 3,4- 2F) 3-CH2C02C2H5 (Rs)„ (Rs)„ (Rs)„ (Rs)„ (Rs)„ -CN 5-NO2 4- C(CH 3 ) 3 4- (Ph- 3,4- 2F) 3-CH 2 C0 2 C 2 H 5
5- CI 5-OPh 5- (Ph- 4- CI) 3-CF3-5-CN 4- Ph- 5- C02C2H5-CH3 5-OCH3 3,4- 2CH3 3- (Ph- 3,4- 2F) 4-CH3-5-CO2C2H55- CI 5-OPh 5- (Ph- 4- CI) 3-CF3-5-CN 4- Ph- 5- C0 2 C 2 H 5 -CH3 5-OCH3 3,4- 2CH 3 3- (Ph- 3,4- 2F) 4-CH3-5-CO2C2H5
4- CI 3-CH3 3,5- 2CH3 3- CF3- 5- C02C2H5 4- CF3- 5- C02C2H5 4- CI 3-CH3 3,5- 2CH 3 3- CF 3 - 5- C0 2 C 2 H 5 4- CF 3 - 5- C0 2 C 2 H 5
3- CI 3-OCH3 4- (Ph- 4- CI) 5- Ph- 4- C02C2H5 5- CH3- 4- C02C2H5 3- CI 3-OCH3 4- (Ph- 4- CI) 5- Ph- 4- C0 2 C 2 H 5 5- CH 3 - 4- C0 2 C 2 H 5
5- Br 4,5- 2C1 4-C02C2H5 3- C02C2H5- 4- CF3 4-CF3-5-CONHCH35- Br 4,5-2C1 4-C0 2 C 2 H 5 3- C0 2 C 2 H 5 - 4- CF 3 4-CF3-5-CONHCH3
3- Br 3-OPh 3-C02C2H5 4- CH2C02C2H5 4-CF3-5-CONHOCH3-CH3 4,5- 2CH3 3- (Ph- 4- CI) 4-CH3-5-COCH3 4-CH3-5-CONHCH3 - Ph 3-N02 4-CF3-5-CN 3-COCH3-4-CH3 4- (Ph- 4- CI)- 5- C02C2H5 - Ph 3- Ph 4- (Ph- 4- Br) 3-CH3-5-COCH3 4- (Ph- 4- CI)- 5- CONHCH3 表 14 3- Br 3-OPh 3-C0 2 C 2 H 5 4- CH 2 C0 2 C 2 H 5 4-CF3-5-CONHOCH3-CH3 4,5- 2CH 3 3- (Ph- 4- CI) 4- CH3-5-COCH3 4-CH3-5-CONHCH3 - Ph 3-N0 2 4-CF3-5-CN 3-COCH3-4-CH3 4- (Ph- 4- CI)- 5- C0 2 C 2 H 5 - Ph 3- Ph 4- (Ph- 4- Br) 3-CH3-5-COCH3 4- (Ph- 4- CI)- 5- CONHCH 3 Table 14
Figure imgf000018_0002
Figure imgf000019_0001
Figure imgf000019_0004
Figure imgf000019_0002
Figure imgf000019_0005
Figure imgf000018_0002
Figure imgf000019_0001
Figure imgf000019_0004
Figure imgf000019_0002
Figure imgf000019_0005
表 16
Figure imgf000019_0003
Table 16
Figure imgf000019_0003
Figure imgf000019_0006
1-CH3-5-C1 1- C(CH3)3- 5- SCH2- (Ph- 4- CI) 1- (3- CI- 5- CF3- 2- Py- )- 5- CI
Figure imgf000019_0006
1-CH3-5-C1 1- C(CH 3 ) 3 - 5- SCH 2 - (Ph- 4- CI) 1- (3- CI- 5- CF 3 - 2- Py- )- 5- CI
1- (Ph- 4- CI) -5 -CI 1- (Ph- 4- CI) - 5- SCH2- (Ph- 4- CI) 1- (3- CI- 5- CN- 2- Py- )- 5- CI 1- (Ph- 4- CI) -5 -CI 1- (Ph- 4- CI) - 5- SCH 2 - (Ph- 4- CI) 1- (3- CI- 5- CN- 2- Py- )- 5- CI
1- (2- Py- )- 5- CI 1- (2- Py- ) - SCH2- (Ph- 4- CI) 1- (3,5- 2C1- 2- Py- )- 5- CI 1-(2- Py- )- 5- CI 1- (2- Py- ) - SCH 2 - (Ph- 4- CI) 1- (3,5- 2C1- 2- Py- )- 5- CI
1- H- 5- SCH2- Ph 1- (Ph- 2,4- 2C1) - SCH2- (Ph- 4- CI) 1- (3,5- 2C1- 2- Py- )- 5- CI 1- H- 5- SCH 2 - Ph 1- (Ph- 2,4- 2C1) - SCH 2 - (Ph- 4- CI) 1- (3,5- 2C1- 2- Py- )- 5- CI
1- Ph- 5- SCH2- Ph 1- Ph- 5- SCH2- (Ph- 4- CI) 1- (3- CI- 5- CH3- 2- Py- )- 5- CI 1- Ph- 5- SCH 2 - Ph 1- Ph- 5- SCH 2 - (Ph- 4- CI) 1- (3- CI- 5- CH 3 - 2- Py- )- 5- CI
1- CH3- 5- SCH2- Ph 1- H- 5- SCH2- (Ph- 4- CI) 1- (5- CF3- 2- Py- )- 5- CI 1- CH 3 - 5- SCH 2 - Ph 1- H- 5- SCH 2 - (Ph- 4- CI) 1- (5- CF 3 - 2- Py- )- 5- CI
1- (Ph- 2,4- 2C1) -5 -CI 1- (Ph- 4- CI) - 5- SCH2- Ph 1- (Ph- 4- N02) -5- CI 1-(Ph- 2,4- 2C1) -5 -CI 1- (Ph- 4- CI) - 5- SCH 2 - Ph 1- (Ph- 4- N0 2 ) -5- CI
1- CH3- 5- Br 1- (Ph- 4- CF3- 2,6- 2C1) -5 -Br 1- (Ph- 2,6- 2C1) -5 -CI 1- CH 3 - 5- Br 1- (Ph- 4- CF 3 - 2,6-2C1) -5 -Br 1- (Ph- 2,6-2C1) -5 -CI
1- C(CH3)3- 5- Br 1- (Ph- 4- CF3- 2,6- 2C1) -5 -CI 1- (CH2Ph- 4- CI)- 5- CI 本发明的部分化合物可以用表 17—表 270中列出的具体化合物来说明， 但并不限定本 当通式 (1-1 ) 中， R4=H， R2=CF3， Xi=C-CN, X2=CO， x=0时， 结构如通式 (1-17) 所 1-C(CH 3 ) 3 - 5- Br 1-(Ph- 4-CF 3 - 2,6-2C1) -5 -CI 1-(CH 2 Ph- 4- CI)- 5- CI Some of the compounds can be illustrated by the specific compounds listed in Tables 17 to 270, but are not limited to the formula (1-1), R 4 = H, R 2 = CF 3 , Xi = C-CN, X 2 =CO, when x=0, the structure is as shown in the general formula (1-17)
Figure imgf000020_0001
在通式 （1-17) 中， 当 (R5)n =3-Cl时， 取代基 (R m见表 17， 代表化合物编号为 1-261 , 表 17
Figure imgf000020_0001
In the general formula (1-17), when (R 5 ) n = 3-Cl, the substituent (R m is shown in Table 17, represents the compound number 1-261, Table 17
Figure imgf000020_0002
3-N02 107 2-CH3-4-CI 194 2- CI- 3- C(CH3)3
Figure imgf000020_0002
3-N0 2 107 2-CH3-4-CI 194 2- CI- 3- C(CH 3 ) 3
2,3- 2F 108 2-N02-4-C1 195 2- CI- 5- C(CH3)3 2,3- 2F 108 2-N02-4-C1 195 2- CI- 5- C(CH 3 ) 3
2,4- 2F 109 2-CN-4-C1 196 2- C(CH3)3- 4- CF3 2,4- 2F 109 2-CN-4-C1 196 2- C(CH 3 ) 3 - 4- CF 3
2,5- 2F 110 2- C(CH3)3 197 2- Br- 4- C(CH3)3 2,5- 2F 110 2- C(CH 3 ) 3 197 2- Br- 4- C(CH 3 ) 3
2,6- 2F 111 3- C(CH3)3 198 2- F- 4- C(CH3)3 2,6- 2F 111 3- C(CH 3 ) 3 198 2- F- 4- C(CH 3 ) 3
3,4- 2F 112 4- C(CH3)3 199 3-OC2H5-4-CF33,4- 2F 112 4- C(CH 3 ) 3 199 3-OC2H5-4-CF3
3,5- 2F 113 3-F-4-C1 200 3-NHCH3-4-CF33,5-2F 113 3-F-4-C1 200 3-NHCH3-4-CF3
2,3- 2C1 114 3- Br- 4- CI 201 3-COCH3-4-CF32,3- 2C1 114 3- Br- 4- CI 201 3-COCH3-4-CF3
2,5- 2C1 115 3-CH3-4-C1 202 2-CI-4-NCH32,5- 2C1 115 3-CH3-4-C1 202 2-CI-4-NCH3
2,6- 2C1 116 3-N02-4-C1 203 2-CI-4-COCH32,6- 2C1 116 3-N02-4-C1 203 2-CI-4-COCH3
3,4- 2C1 117 3-CN-4-C1 204 2- CI- 4- OC02CH3 3,4- 2C1 117 3-CN-4-C1 204 2- CI- 4- OC0 2 CH 3
3,5- 2C1 118 3-OCF3-4-CI 205 2-OCF3-4-CF33,5- 2C1 118 3-OCF3-4-CI 205 2-OCF3-4-CF3
2,3- Br 119 2-F-4-CF3 206 2- OC2H5- 4- CF3 2,3- Br 119 2-F-4-CF3 206 2- OC 2 H 5 - 4- CF 3
2,4- 2Br 120 2- Br- 4- CF3 207 2-NHCH3-4-CF32,4- 2Br 120 2- Br- 4- CF 3 207 2-NHCH3-4-CF3
2,5- 2Br 121 2-CH3-4-CF3 208 2-COCH3-4-CF32,5- 2Br 121 2-CH3-4-CF3 208 2-COCH3-4-CF3
2,6- 2Br 122 2-NO2-4-CF3 209 2,5- 2C1- 4- CF3 2,6- 2Br 122 2-NO2-4-CF3 209 2,5- 2C1- 4- CF 3
3,4- 2Br 123 2-CN-4-CF3 210 2,5- 2C1- 4- CN3,4- 2Br 123 2-CN-4-CF3 210 2,5- 2C1- 4- CN
3,5- 2Br 124 2- COC2H5 211 2,6- 2C1- 4- CH3 3,5- 2Br 124 2- COC 2 H 5 211 2,6- 2C1- 4- CH 3
2-SCH3 125 3-COC2H5 212 2-CH3-3-CI -4-CF32-SCH 3 125 3-COC 2 H 5 212 2-CH3-3-CI -4-CF3
3-SCH3 126 4- COC2H5 213 2-CH3-3-CI-6-CN3-SCH3 126 4- COC 2 H 5 213 2-CH3-3-CI-6-CN
4-SCH3 127 2- S02CH3 214 2,4,6- 3N02 4-SCH3 127 2- S0 2 CH 3 214 2,4,6- 3N0 2
2-SCF3 128 3-S02CH3 215 2- Br- 4- N02 2-SCF3 128 3-S0 2 CH 3 215 2- Br- 4- N0 2
3-SCF3 129 4-SO2CH3 216 2-NO2-4-CH33-SCF3 129 4-SO2CH3 216 2-NO2-4-CH3
4-SCF3 130 2-OCHF2 217 2-NO2-4-OCH34-SCF3 130 2-OCHF2 217 2-NO2-4-OCH3
2-OCF3 131 3-OCHF2 218 2-NO2-4-SCH32-OCF3 131 3-OCHF 2 218 2-NO2-4-SCH3
3-OCF3 132 4-OCHF2 219 2-NO2-4-NCH33-OCF3 132 4-OCHF2 219 2-NO2-4-NCH3
4-OCF3 133 2- S02C2H5 220 3-COCH3-4-CI4-OCF3 133 2- S0 2 C 2 H 5 220 3-COCH3-4-CI
2-OCH3 134 3-S02C2H5 221 2- OCOCH2CH3 2-OCH3 134 3-S0 2 C 2 H 5 221 2- OCOCH 2 CH 3
3-OCH3 135 4- S02C2H5 222 3-OCOCH2CH3 3-OCH3 135 4- S0 2 C 2 H 5 222 3-OCOCH 2 CH 3
4-OCH3 136 2- C02CH3 223 4- OCOCH2CH3 4-OCH3 136 2- C0 2 CH 3 223 4- OCOCH 2 CH 3
2,3,4- 3F 137 3-C02CH3 224 2-CI-4-COOCH32,3,4- 3F 137 3-C0 2 CH 3 224 2-CI-4-COOCH3
2,3,5- 3F 138 4-CO2CH3 225 2-CI-4-SO2CH32,3,5- 3F 138 4-CO2CH3 225 2-CI-4-SO2CH3
2,4,5- 3F 139 2- C02C2H5 226 2,6- 2C1- 4- COCH3 2,4,5- 3F 139 2- C0 2 C 2 H 5 226 2,6- 2C1- 4-COCH 3
2,3,6- 3F 140 3-C02C2H5 227 2,6- 2C1- 4- CONH2 2,3,6- 3F 140 3-C0 2 C 2 H 5 227 2,6- 2C1- 4-CONH 2
2,4,6- 3F 141 4- C02C2H5 228 2,6- 2Br- 4- CF3 2,4,6- 3F 141 4- C0 2 C 2 H 5 228 2,6- 2Br- 4- CF 3
3,4,5- 3F 142 2- CH2OCH3 229 2,4- 2C1- 6- SCH3 3,4,5- 3F 142 2- CH 2 OCH 3 229 2,4- 2C1- 6- SCH 3
2,3,4- 3C1 143 3-CH2OCH3 230 2,4- 2C1- 6- NCH3 2,3,4- 3C1 143 3-CH 2 OCH 3 230 2,4- 2C1- 6- NCH 3
2,3,5- 3C1 144 4- CH2OCH3 231 2- N02- 4- COCH3 2,3,5- 3C1 144 4- CH 2 OCH 3 231 2- N0 2 - 4- COCH 3
2,4,5- 3C1 145 2-OCOCH3 232 2-N02-4-CONH2 2,4,5- 3C1 145 2-OCOCH3 232 2-N0 2 -4-CONH 2
2,3,6- 3C1 146 3-OCOCH3 233 2-CH3-4-CI-6-CN2,3,6- 3C1 146 3-OCOCH3 233 2-CH3-4-CI-6-CN
2,4,6- 3C1 147 4-OCOCH3 234 2-CH3-4-C1-5-CN2,4,6- 3C1 147 4-OCOCH3 234 2-CH3-4-C1-5-CN
3,4,5- 3C1 148 2-CI-3-CH3 235 2-NCH3-4-C1-6-CN3,4,5- 3C1 148 2-CI-3-CH3 235 2-NCH3-4-C1-6-CN
2,3,4- 3Br 149 2-CI-5-CH3 236 2-SCH3-4-C1-5-CN 63 2,3,5- 3Br 150 2-CI-6-CH3 237 2,4- 2C1- 6- S02CH3 2,3,4- 3Br 149 2-CI-5-CH3 236 2-SCH3-4-C1-5-CN 63 2,3,5- 3Br 150 2-CI-6-CH3 237 2,4- 2C1- 6- S0 2 CH 3
64 2,4,5- 3Br 151 2-C1-3-CN 238 2,6- 2C1- 4- C02CH3 64 2,4,5- 3Br 151 2-C1-3-CN 238 2,6- 2C1- 4- C0 2 CH 3
65 2,3,6- 3Br 152 2-C1-5-CN 239 2,6- 2Br- 4- OCF3 65 2,3,6- 3Br 152 2-C1-5-CN 239 2,6- 2Br- 4- OCF 3
66 2,4,6- 3Br 153 2-C1-6-CN 240 2- CI- 4- CF3- 6- N02 66 2,4,6- 3Br 153 2-C1-6-CN 240 2- CI- 4- CF 3 - 6- N0 2
67 3,4,5- 3Br 154 2-CONHPh 241 2-CI-4-CF3-5-CN67 3,4,5- 3Br 154 2-CONHPh 241 2-CI-4-CF3-5-CN
68 2,4- 2N02 155 3-CONHPh 242 2,3,5- 3C1- 4,6- 2CN68 2,4- 2N0 2 155 3-CONHPh 242 2,3,5- 3C1- 4,6-2CN
69 2,3- 2CH3 156 4-CONHPh 243 3-C1-4-CF3-5-CN69 2,3- 2CH 3 156 4-CONHPh 243 3-C1-4-CF3-5-CN
70 2,4- 2CH3 157 2-OCO2CH3 244 3-CI-4-CF3-6-NO270 2,4- 2CH 3 157 2-OCO2CH3 244 3-CI-4-CF3-6-NO2
71 2,5- 2CH3 158 3-OCO2CH3 245 2,6- 2C1- 4- S02CH3 71 2,5- 2CH 3 158 3-OCO2CH3 245 2,6- 2C1- 4- S0 2 CH 3
72 2,6- 2CH3 159 4-OCO2CH3 246 2-CI-3-CH3-4-CF372 2,6- 2CH 3 159 4-OCO2CH3 246 2-CI-3-CH3-4-CF3
73 3,4- 2CH3 160 2- OCH2OCH3 247 2-CI-3-CH3-6-CN73 3,4- 2CH 3 160 2- OCH 2 OCH 3 247 2-CI-3-CH3-6-CN
74 3,5- 2CH3 161 3-OCH2OCH3 248 2-CH3-4-CF3-6-CN74 3,5- 2CH 3 161 3-OCH 2 OCH 3 248 2-CH3-4-CF3-6-CN
75 2- OC2H5 162 4- OCH2OCH3 249 2-CH3-4-CF3-5-CN75 2- OC 2 H 5 162 4- OCH 2 OCH 3 249 2-CH3-4-CF3-5-CN
76 3-OC2H5 163 2-COCH2Ph 250 2-CI-4-CF3-6-OCH376 3-OC 2 H 5 163 2-COCH 2 Ph 250 2-CI-4-CF3-6-OCH3
77 4- OC2H5 164 3-COCH2Ph 251 2-CI-4-NO2-6-OCH377 4- OC 2 H 5 164 3-COCH 2 Ph 251 2-CI-4-NO2-6-OCH3
78 2-NHCH3 165 4-COCH2Ph 252 2-CI-4-NO2-6-SCH378 2-NHCH 3 165 4-COCH 2 Ph 252 2-CI-4-NO2-6-SCH3
79 3-NHCH3 166 2-CI-4-OCF3 253 2-CI-4-CF3-5-OCH379 3-NHCH3 166 2-CI-4-OCF3 253 2-CI-4-CF3-5-OCH3
80 4-NHCH3 167 2-CI-4-SCH3 254 2,4- 2C1- 3- CH3- 6- N02 80 4-NHCH3 167 2-CI-4-SCH3 254 2,4- 2C1- 3- CH 3 - 6- N0 2
81 2-N(CH3)2 168 2-CI-4-OCH3 255 2- CI- 3- CH3- 4,6- 2N02 81 2-N(CH 3 ) 2 168 2-CI-4-OCH3 255 2- CI- 3- CH 3 - 4,6- 2N0 2
82 3-N(CH3)2 169 2-OCF3-4-CI 256 2,6- 2C1- 4- CONHCH3 82 3-N(CH 3 ) 2 169 2-OCF3-4-CI 256 2,6- 2C1- 4-CONHCH 3
83 4-N(CH3)2 170 2- OC2H5- 4- CI 257 2,6- 2C1- 4- CON(CH3)2 83 4-N(CH 3 ) 2 170 2- OC 2 H 5 - 4- CI 257 2,6- 2C1- 4-CON(CH 3 ) 2
84 2-COCH3 171 2-NHCH3-4-CI 258 2-CI-4-NO2-6-NHCH384 2-COCH3 171 2-NHCH3-4-CI 258 2-CI-4-NO2-6-NHCH3
85 3-COCH3 172 2-COCH3-4-CI 259 2-CI-4-NO2-6-SO2CH385 3-COCH3 172 2-COCH3-4-CI 259 2-CI-4-NO2-6-SO2CH3
86 4-COCH3 173 3-OC2H5-4-CI 260 2-CI-4-CF3-5-NHCH386 4-COCH3 173 3-OC2H5-4-CI 260 2-CI-4-CF3-5-NHCH3
87 2-F-4-N02 174 3-NHCH3-4-C1 261 2-CI-4-CF3-6-NHCH3 表 18: 通式 （1-17 ) 中， 当 (R5)n=5-Cl时， 取代基 (RL)m与表 17—致， 依次对应表 17的 1-261， 代表化合物编号为 262-522。 87 2-F-4-N02 174 3-NHCH3-4-C1 261 2-CI-4-CF3-6-NHCH3 Table 18: In the general formula (1-17), when (R 5 ) n =5-Cl When the substituent (RL) m is consistent with Table 17, it corresponds to 1-261 of Table 17, which represents the compound number 262-522.
表 19: 通式 （1-17 ) 中， 当 (R5)n=3-CN时， 取代基 (R^m与表 17—致， 依次对应表 17 的 1-261， 代表化合物编号为 523-783。 Table 19: In the general formula (1-17), when (R 5 ) n = 3-CN, the substituent (R^m is the same as Table 17 and corresponds to 1-261 of Table 17 in turn, representing the compound number 523). -783.
表 20: 通式 (1-17 ) 中， 当 (R5)n =4-CN时， 取代基 (Ri)m与表 17 依次对应表 17 的 1-261， 代表化合物编号为 784-1044。 Table 20: In the formula (1-17), when (R 5 ) n = 4-CN, the substituent (Ri) m and Table 17 correspond to 1-261 of Table 17 in order, and represent the compound number 784-1044.
表 21 : 通式 （1-17 ) 中， 当 (R5)n =3-CF3时， 取代基 (R m与表 17 依次对应表 17 的 1-261， 代表化合物编号为 1045-1305。 Table 21: In the general formula (1-17), when (R 5 ) n = 3-CF 3 , the substituent (R m and Table 17 correspond to 1-261 of Table 17 in order, and the compound number is 1045-1305.
表 22: 通式 （1-17 ) 中， 当 (R5)n =5-CF3时， 取代基 (R m与表 17 依次对应表 17 的 1-261， 代表化合物编号为 1306-1566。 Table 22: In the formula (1-17), when (R 5 ) n = 5-CF 3 , the substituent (R m and Table 17 correspond to 1-261 of Table 17 in order, and the compound number is 1306-1566.
表 23 : 通式 （1-17 ) 中， 当 (R5)n =3,5-2Cl时 取代基 (R m与表 17 依次对应表 17 的 1-261， 代表化合物编号为 1567-1827。 Table 23: In the general formula (1-17), when (R 5 ) n = 3, 5-2Cl, the substituent (R m and Table 17 correspond to 1-261 of Table 17 in order, and the compound number is 1567-1827.
表 24: 通式 （1-17 ) 中， 当 (R5)n =3,5-2Br时 取代基 (R m与表 17 依次对应表 17 的 1-261， 代表化合物编号为 1828-2088。 Table 24: In the general formula (1-17), when (R 5 ) n = 3, 5-2Br, the substituent (R m and Table 17 correspond to 1-261 of Table 17 in order, representing the compound number 1828-2088).
表 25: 通式 （1-17 ) 中， 当 (R5)n =3-Cl-5-F时， 取代基 (R^m与表 17—致， 依次对应表 17的 1-261， 代表化合物编号为 2089-2349。 Table 25: In the general formula (1-17), when (R 5 ) n = 3-Cl-5-F, the substituent (R^m is the same as Table 17 and corresponds to 1-261 of Table 17 in turn, representing The compound number is 2089-2349.
表 26: 通式 （1-17 ) 中， 当 (R5)n =3-Cl-5-Br时， 取代基 (R^m与表 17—致， 依次对应表 17的 1-261， 代表化合物编号为 2350-2610。 表 27: 通式 （1-17) 中， 当 (R5)n = 3-C1-5-CN时， 取代基 (Ri)m与表 17 - -致， 依次对应表 17的 1-261， 代表化合物编号为 2611-■2871。 Table 26: In the general formula (1-17), when (R 5 ) n = 3-Cl-5-Br, the substituent (R^m is the same as Table 17 and corresponds to 1-261 of Table 17 in turn, representing The compound number is 2350-2610. Table 27: In the general formula (1-17), when (R 5 ) n = 3-C1-5-CN, the substituent (Ri) m and the table 17 - are sequentially corresponding to 1-261 of Table 17, The representative compound number is 2611 - ■ 2871.
表 28: 通式 （1-17) 中， 当 (R5)n = 3-Cl-5-CF3时， 取代基 (Ri)m与表 17 - -致， 依次对应表 17的 1-261， 代表化合物编号为 2872- .3132。 Table 28: In the formula (1-17), when (R 5 ) n = 3-Cl-5-CF 3 , the substituent (Ri) m and the table 17 - are in turn, corresponding to 1-261 of Table 17 , represents the compound number 2872-.3132.
表 29: 通式 （1-17) 中， 当 (R5)n =5-Cl-3-F时， 取代基 (Ri)m与表 17― '致， 依次对应表Table 29: In the general formula (1-17), when (R 5 ) n =5-Cl-3-F, the substituent (Ri) m and the table 17-', respectively, correspond to the table
17的 1-261， 代表化合物编号为 3133- .3393。 1-261 of 17 represents the compound number 3133-.3393.
表 30: 通式 (1-17) 中， 当 (R5)n ： =3-Br-5-Cl时， 取代基 (Ri)m与表 17 .致， 依次对应表 17的 1-261， 代表化合物编号为 3394- .3654。 Table 30: In the formula (1-17), when (R 5 ) n : =3-Br-5-Cl, the substituent (Ri) m and Table 17 are in turn, correspondingly to 1-261 of Table 17, The representative compound number is 3394-.3654.
表 31: 通式 （1-17) 中， 当 (R5)n = 3-Br-5-CN时， 取代基 (Ri)m与表 17 - -致， 依次对应表 17的 1-261， 代表化合物编号为 3655- .3915。 Table 31: In the formula (1-17), when (R 5 ) n = 3-Br-5-CN, the substituent (Ri) m and the table 17 - are sequentially corresponding to 1-261 of Table 17, The representative compound number is 3655-.3915.
表 32: 通式 （1-17) 中， 当 (R5)n = 3-CN-5-C1时， 取代基 (Ri)m与表 17 -致， 依次对应表 17的 1-261， 代表化合物编号为 3916-■4176ο Table 32: In the general formula (1-17), when (R 5 ) n = 3-CN-5-C1, the substituent (Ri) m is related to Table 17 and corresponds to 1-261 of Table 17, which represents The compound number is 3916-■4176ο
表 33: 通式 （1-17) 中， 当 (R5)n = 3-CN-5-Br时， 取代基 (Ri)m与表 17 -致， 依次对应表 17的 1-261， 代表化合物编号为 4177-■4437 ο Table 33: In the general formula (1-17), when (R 5 ) n = 3-CN-5-Br, the substituent (Ri) m is in the same manner as in Table 17 and corresponds to 1-261 in Table 17, which represents The compound number is 4177-■4437 ο
表 34: 通式 （1-17) 中， 当 (R5)n : =3,5,6-3Cl时， 取代基 (R m与表 17 致， 依次对应表Table 34: In the general formula (1-17), when (R 5 ) n : =3,5,6-3Cl, the substituent (R m and Table 17)
17的 1-261， 代表化合物编号为 4438- -4698。 1-261 of 17 represents the compound number 4438- -4698.
通式 （1-17) 中， 当 （！^；^二！！时 ， 取代基 (R5)n见表 35， 代表化合物 号为 4699-4781 ο 表 35 In the general formula (1-17), when (!^;^二!!, the substituent (R 5 ) n is shown in Table 35, representing the compound number 4699-4781 ο Table 35
Figure imgf000023_0001
4723 5-CN 4751 3-CH3-5-CI 4779 4-CH3-5-CN-6-CI
Figure imgf000023_0001
4723 5-CN 4751 3-CH3-5-CI 4779 4-CH3-5-CN-6-CI
4724 6-CN 4752 3-CH3-5-NO2 4780 3- CN- 5- C02C2H5- 6- CF3 4724 6-CN 4752 3-CH3-5-NO2 4780 3- CN- 5- C0 2 C 2 H 5 - 6- CF 3
4725 3,5- 2C1 4753 4- CH3- 5- Br 4781 3,5- 2C1- 6- (0- Ph- 4- CI)4725 3,5- 2C1 4753 4- CH 3 - 5- Br 4781 3,5- 2C1- 6- (0- Ph- 4- CI)
4726 6-CH3 4754 4-CH3-5-NO2 4726 6-CH 3 4754 4-CH3-5-NO2
"表示无取代基 表 36: 通式 （1-17) 中， 当 （R^m =2-Cl时， 取代基 (R5)n见表 35， 依次对应表 35 的 4699-4781 , 代表化合物编号为 4782-4864。 "Indicating no substituents Table 36: In the general formula (1-17), when (R^m = 2-Cl, the substituent (R 5 ) n is shown in Table 35, which in turn corresponds to 4699-4781 of Table 35, represents a compound The number is 4782-4864.
表 37: 通式 （1-17) 中， 当 （R^m =4-Cl时， 取代基 (R5)n见表 35， 依次对应表 35 的Table 37: In the general formula (1-17), when (R^m = 4-Cl, the substituent (R 5 ) n is shown in Table 35, which in turn corresponds to Table 35
4699-4781 , 代表化合物编号为 4865-4947。 4699-4781, the representative compound number is 4865-4947.
表 38: 通式 （1-17) 中， 当 （R n^ -Cl-^CFg时， 取代基 (R5)n见表 35， 依次对应表 35 的 4699-4781， 代表化合物编号为 4948-5030。 Table 38: In the general formula (1-17), when (R n^ -Cl-^CFg, the substituent (R 5 ) n is shown in Table 35, which in turn corresponds to 4699-4781 of Table 35, and represents the compound number 4948- 5030.
表 39: 通式 （1-17) 中， 当 （R^m =4-CF3时， 取代基 (R5)n见表 35， 依次对应表 35的 4699-4781 , 代表化合物编号为 5031-5113。 Table 39: In the general formula (1-17), when (R^m = 4-CF 3 , the substituent (R 5 ) n is shown in Table 35, which in turn corresponds to 4699-4781 of Table 35, representing the compound number 5031- 5113.
表 40: 通式 （1-17) 中，
Figure imgf000024_0001
=2-CF3-4-Cl时， 取代基 (R5)n见表 35， 依次对应表 35 的 4699-4781， 代表化合物编号为 5114-5196。 Table 40: In the general formula (1-17),
Figure imgf000024_0001
For the case of =2-CF 3 -4-Cl, the substituent (R 5 ) n is shown in Table 35, which in turn corresponds to 4699-4781 of Table 35, and represents the compound number 5114-5196.
表 41 : 通式 （1-17) 中， 当 （R m 4-CN时， 取代基 (R5)n见表 35， 依次对应表 35的 4699-4781 , 代表化合物编号为 5197-5279。 Table 41: In the formula (1-17), when (R m 4-CN, the substituent (R 5 ) n is shown in Table 35, which in turn corresponds to 4699-4781 of Table 35, and represents the compound number 5197-5279.
表 42: 通式 （1-17) 中， 当 （!^;^ =2,4-20时， 取代基 (R5)n见表 35， 依次对应表 35的Table 42: In the general formula (1-17), when (!^;^ = 2, 4-20, the substituent (R 5 ) n is shown in Table 35, which in turn corresponds to Table 35
4699-4781 , 代表化合物编号为 5280-5362。 4699-4781, the representative compound number is 5280-5362.
当通式 （1-1 ) 中 R4=H， X1=C-CN, X2=CO， x=0时， 结构如通式 （1-18) 所示。 When R 4 = H, X 1 = C-CN, X 2 = CO, x = 0 in the formula (1-1), the structure is as shown in the formula (1-18).
Figure imgf000024_0002
通式 （1-18) 中， 当 （^;^ =11、 （R5)n =3-Cl时， 取代基 R2见表 43， 代表化合物编号为 5363-5383。 表 43
Figure imgf000024_0002
In the formula (1-18), when (^; ^ = 11, (R 5 ) n = 3-Cl, the substituent R 2 is shown in Table 43, and the compound number is 5363-5383.
Figure imgf000024_0004
Figure imgf000024_0004
表 44: 通式 （1-18) 中，
Figure imgf000024_0003
(R5)n =3-CN时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 5384-5404。 Table 44: In the general formula (1-18),
Figure imgf000024_0003
When (R 5 ) n = 3-CN, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, and represents the compound number 5384-5404.
表 45: 通式 （1-18) 中， 当 （R m :!^ (R5)n =3,5-2C1时， 取代基 R2见表 43， 依次对应 表 43的 5363-5383， 代表化合物编号为 5405-5425。 Table 45: In the general formula (1-18), when (R m :!^ (R 5 ) n = 3,5-2C1, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and represents The compound number is 5405-5425.
表 46: 通式 (1-18) 中， ¾(R M =H (R5)n =3-Cl-5-CF3时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 5426-5446。 Table 46: In the general formula (1-18), when 3⁄4 (R M =H (R 5 ) n =3-Cl-5-CF 3 , the substituent R 2 is shown in Table 43, It should be 5363-5383 of Table 43 and represents the compound number 5426-5446.
表 47: 通式 (1-18) 中， ¾(R m =H (R5)n =3,5,6-3Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 5447-5467。 Table 47: In the general formula (1-18), when 3⁄4 (R m = H (R 5 ) n = 3, 5 , 6-3Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 The representative compound number is 5447-5467.
表 48: 通式 （1-18) 中， 当 (1 ^ =11、 （R5)n =3-CF3时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 5468-5488。 Table 48: In the formula (1-18), when (1 ^ =11, (R 5 ) n = 3-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and represents a compound The number is 5468-5488.
表 49: 通式 (1-18) 中， 当 (R m =H、 (R5)n =5-CF3时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 5489-5509。 Table 49: In the general formula (1-18), when (R m = H, (R 5 ) n = 5-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and represents a compound The number is 5489-5509.
表 50: 通式 (1-18) 中， 当 (Ri)m =4-CL (R5)n=3-Cl时， 取代基 R2见表 43， 依次对应 表 43的 5363-5383， 代表化合物编号为 5510-5530。 Table 50: In the general formula (1-18), when (Ri) m = 4-CL (R 5 ) n = 3-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, The compound number is 5510-5530.
表 51 : 通式 （1-18) 中， 当 (!^;^ =4 1、 （R5)n=3-CN时， 取代基 R2见表 43， 依次对应 表 43的 5363-5383， 代表化合物编号为 5531-5551。 Table 51: In the general formula (1-18), when (!^; ^ = 4 1 , (R 5 ) n = 3-CN, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 The representative compound number is 5531-5551.
表 52: 通式 （1-18) 中，
Figure imgf000025_0001
=4-Cl、 （R5)n=3,5-2C1时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 5552-5572。 Table 52: In the general formula (1-18),
Figure imgf000025_0001
When 4-4-Cl, (R 5 ) n = 3, 5-2C1, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, and represents the compound number 5552-5572.
表 53: 通式 (1-18) 中， ¾(R m =4-CL (R5)n=3-Cl-5-CF3时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 5573-5593。 Table 53: In the general formula (1-18), when 3⁄4 (R m = 4-CL (R 5 ) n = 3-Cl-5-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363 of Table 43 -5383, represents the compound number 5573-5593.
表 54: 通式 (1-18) 中， ¾(R m =4-CL (R5)n=3,5,6-3C1时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 5594-5614。 Table 54: In the general formula (1-18), when 3⁄4 (R m = 4-CL (R 5 ) n = 3, 5 , 6-3C1, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363 of Table 43 5383, representing compound number 5594-5614.
表 55: 通式 （1-18) 中， (R5)n=3-CF3时， 取代基 R2见表 43， 依次对应 表 43的 5363-5383， 代表化合 -5635。 Table 55: In the formula (1-18), when (R 5 ) n = 3-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and represents a compound of -5635.
表 56: 通式 （1-18) 中，
Figure imgf000025_0002
(R5)n=5-CF3时， 取代基 R2见表 43， 依次对应 表 43的 5363-5383， 代表化合物编号为 5636-5656。 Table 56: In the general formula (1-18),
Figure imgf000025_0002
When (R 5 ) n = 5-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, and represents the compound number 5636-5656.
表 57: 通式 （1-18) 中， 当 （R^m =4-CF3、 （R5)n=3-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 5657-5677。 Table 57: In the formula (1-18), when (R^m = 4-CF 3 , (R 5 ) n = 3-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 , represents the compound number 5657-5677.
表 58: 通式 （1-18) 中，
Figure imgf000025_0003
=4-CF3、 （R5)n=3-CN时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 5678-5698。 Table 58: In the general formula (1-18),
Figure imgf000025_0003
When 4-CF 3 and (R 5 ) n = 3-CN, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, and represents the compound number 5678-5698.
表 59: 通式 (1-18) 中， ¾(R m =4-CF3 (R5)n=3,5-2C1时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 5699-5719。 Table 59: In the general formula (1-18), 3⁄4 (R m = 4-CF 3 (R 5 ) n = 3, 5-2C1, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 , represents the compound number 5699-5719.
表 60: 通式 (1-18) 中，
Figure imgf000025_0004
=4-CF3、 （R5)n=3-Cl-5-CF3时， 取代基 R2见表 43， 依 次对应表 43的 5363-5383， 代表化合物编号为 5720-5740。 Table 60: In the general formula (1-18),
Figure imgf000025_0004
When 4-CF 3 and (R 5 ) n = 3-Cl-5-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, and represents the compound number 5720-5740.
表 61 : 通式 （1-18) 中，
Figure imgf000025_0005
(R5)n=3,5,6-3C1时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 5741-5761。 Table 61: In the general formula (1-18),
Figure imgf000025_0005
When (R 5 ) n = 3, 5 , 6-3C1, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, and represents the compound number 5741-5761.
表 62: 通式 （1-18) 中， =4-CF3、 （R5)n=3-CF3时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化 为 5762-5782。 Table 62: In the formula (1-18), when =4-CF 3 and (R 5 ) n =3-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and is represented as 5762-5782.
表 63: 通式 （1-18) 中，
Figure imgf000025_0006
=4-CF3、 （R5)n=5-CF3时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 5783-5803。 Table 63: In the general formula (1-18),
Figure imgf000025_0006
When 4-CF 3 and (R 5 ) n = 5-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, and represents the compound number 5783-5803.
表 64: 通式 (1-18) 中， 当 (Ri)m =2,4-2Cl、 (R5)„ =3-Cl时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 5804-5824。 Table 64: In the general formula (1-18), when (Ri) m = 2, 4-2Cl, (R 5 ) „ = 3-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363 of Table 43 5383, represents the compound number 5804-5824.
表 65: 通式 （1-18) 中，
Figure imgf000025_0007
(R5)n =3-CN时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 5825-5845。 Table 65: In the general formula (1-18),
Figure imgf000025_0007
When (R 5 ) n = 3-CN, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, and represents the compound number 5825-5845.
表 66: 通式 (1-18) 中， ¾(Ri)m =2,4-2CL (R5)n =3,5-2Cl时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 5846-5866。 Table 66: In the general formula (1-18), when 3⁄4(Ri) m = 2, 4-2CL (R 5 ) n = 3, 5-2Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363 of Table 43 -5383, represents the compound number 5846-5866.
表 67: 通式 (1-18) 中， ¾(Ri)m =2,4-2CL (R5)n =3-Cl-5-CF3时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 5867-5887。 Table 67: In the general formula (1-18), when 3⁄4(Ri) m = 2, 4-2CL (R 5 ) n = 3-Cl-5-CF 3 , the substituent R 2 is shown in Table 43, 5363-5383 of 43 represents the compound number 5867-5887.
表 68: 通式 (1-18) 中， ¾(Ri)m =2,4-2CL (R5)n =3,5,6-3Cl时， 取代基 R2见表 43， 依 次对应表 43的 5363-5383， 代表化合物编号为 5888-5908。 Table 68: In the general formula (1-18), when 3⁄4(Ri) m = 2, 4-2CL (R 5 ) n = 3, 5 , 6-3Cl, the substituent R 2 is shown in Table 43 Sub-corresponding to 5363-5383 of Table 43, the representative compound number is 5888-5908.
表 69: 通式 (1-18) 中， ¾(Ri)m =2,4-2CL (R5)n =3-CF3时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 5909-5929。 Table 69: In the general formula (1-18), when 3⁄4(Ri) m = 2, 4-2CL (R 5 ) n = 3-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363 of Table 43 5383, representing compound number 5909-5929.
表 70: 通式 (1-18) 中， ¾(Ri)m =2,4-2CL (R5)n =5-CF3时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 5930-5950。 Table 70: In the general formula (1-18), when 3⁄4(Ri) m = 2,4-2CL (R 5 ) n =5-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363 of Table 43 5383, the representative compound number is 5930-5950.
当通式 (1-1) 中， R2=CF3， R4=H， X2=CO， x=0时， 结构如通式 (1-19) 所示。 When R 2 = CF 3 , R4 = H, X 2 = CO, and x = 0 in the formula (1-1), the structure is as shown in the formula (1-19).
Figure imgf000026_0001
通式 （1-19) 中，
Figure imgf000026_0002
=H、 (R5)„ =3-Cl时， 取代基 见表 71， 代表化合物编号为 5951-5974。
Figure imgf000026_0001
In the general formula (1-19),
Figure imgf000026_0002
When =H, (R 5 ) „ = 3-Cl, the substituents are shown in Table 71, and the compound number is 5951-5974.
表 71  Table 71
Figure imgf000026_0006
表 72: 通式 （1-19) 中， 当 (1 ^=11、 （R5)n=3-CN时， 取代基 X 见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 5975-5998。
Figure imgf000026_0006
Table 72: In the general formula (1-19), when (1^=11, (R 5 ) n =3-CN, the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, which represents the compound number 5975-5998.
表 73: 通式 （1-19) 中，
Figure imgf000026_0003
(R5)n=3,5-2C1时， 取代基 X 见表 71， 依次对应 表 71的 5951-5974， 代表化合物编号为 5999-6022。 Table 73: In the general formula (1-19),
Figure imgf000026_0003
When (R 5 ) n = 3,5-2C1, the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 5999-6022.
表 74: 通式 (1-19) 中， ¾(R m =H (R5)n=3-Cl-5-CF3时， 取代基 X 见表 71， 依次对 应表 71的 5951-5974， 代表化合物编号为 6023-6046。 Table 74: In the general formula (1-19), when 3⁄4 (R m = H (R 5 ) n = 3-Cl-5-CF 3 , the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, The representative compound number is 6023-6046.
表 75: 通式 (1-19) 中， ¾(R m =H (R5)n =3,5,6-3Cl时， 取代基 X 见表 71， 依次对 应表 71的 5951-5974， 代表化合物编号为 6047-6070。 Table 75: In the general formula (1-19), when 3⁄4 (R m = H (R 5 ) n = 3, 5 , 6-3Cl, the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, representing The compound number is 6047-6070.
表 76: 通式 （1-19) 中， 当 (1 ^=11、 （R5)n=3-CF3时， 取代基 X 见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 6071-6094。 Table 76: In the general formula (1-19), when (1^11, (R 5 ) n = 3-CF 3 , the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, representing the compound number. It is 6071-6094.
表 77: 通式 （1-19) 中， 当 (1 ^=11、 （R5)n=5-CF3时， 取代基 X 见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 6095-6118。 Table 77: In the general formula (1-19), when (1^=11, (R 5 ) n =5-CF 3 , the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, representing the compound number. It is 6095-6118.
表 78: 通式 （1-19) 中，
Figure imgf000026_0004
(R5)n=3-Cl时， 取代基 Xi见表 71， 依次对应 表 71的 5951-5974， 代表化合物编号为 6119-6142。 Table 78: In the general formula (1-19),
Figure imgf000026_0004
When (R 5 ) n = 3-Cl, the substituent Xi is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 6119-6142.
表 79: 通式 （1-19) 中， 当 (^;^=4 1、 （R5)n=3-CN时， 取代基 Xi见表 71， 依次对应 表 71的 5951-5974， 代表化合物编号为 6143-6166。 Table 79: In the general formula (1-19), when (^; ^=4 1 , (R 5 ) n = 3-CN, the substituent Xi is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, representing a compound The number is 6143-6166.
表 80: 通式 （1-19) 中， 当 (^;^=4 1、 （R5)n=3,5-2C1时， 取代基 Xi见表 71， 依次对 应表 71的 5951-5974， 代表化合物编号为 6167-6190。 Table 80: In the general formula (1-19), when (^; ^=4 1 , (R 5 ) n = 3, 5-2C1, the substituent Xi is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, The representative compound number is 6167-6190.
表 81: 通式 （1-19) 中，
Figure imgf000026_0005
(R5)n=3-Cl-5-CF3时， 取代基 Xi见表 71， 依次 对应表 71的 5951-5974， 代表化合物编号为 6191-6214。 Table 81: In the general formula (1-19),
Figure imgf000026_0005
When (R 5 ) n = 3-Cl-5-CF 3 , the substituent Xi is shown in Table 71, in order Corresponding to 5951-5974 of Table 71, the representative compound number is 6191-6214.
表 82: 通式 （1-19) 中，
Figure imgf000027_0001
(R5)n =3,5,6-3Cl时， 取代基 X 见表 71， 依次 对应表 71的 5951-5974， 代表化合物编号为 6215-6238。 Table 82: In the general formula (1-19),
Figure imgf000027_0001
When (R 5 ) n = 3,5,6-3Cl, the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 6215-6238.
表 83: 通式 （1-19) 中， 当 (!^;^ =4 1、 （R5)n =3-CF3时， 取代基 X 见表 71， 依次对应 表 71的 5951-5974， 代表化合物编号为 6239-6262。 Table 83: In the general formula (1-19), when (!^;^ =4 1 , (R 5 ) n =3-CF 3 , the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, The representative compound number is 6239-6262.
表 84: 通式 （1-19) 中， 当 (!^;^ =4 1、 （R5)n =5-CF3时， 取代基 X 见表 71， 依次对应 表 71的 5951-5974， 代表化合物编号为 6263-6286。 Table 84: In the general formula (1-19), when (!^;^ =4 1 , (R 5 ) n =5-CF 3 , the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, The representative compound number is 6263-6286.
表 85: 通式 （1-19) 中， =2-N02、 （R5)n =3-Cl时， 取代基 表 ^ 依次对应 表 71的 5951-5974， 代表化合 6287-6310。 Table 85: In the formula (1-19), when =2-N0 2 and (R 5 ) n = 3-Cl, the substituent table ^ corresponds to 5951-5974 of Table 71 in turn, and represents the compound 6287-6310.
表 86: 通式 （1-19) 中， =4-CF3、 （R5)n =3-CN时， 取代基 X 见表 71， 依次对 应表 71的 5951-5974， 代表化 为 6311-6334。 Table 86: In the general formula (1-19), when =4-CF 3 and (R 5 ) n =3-CN, the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and is represented as 6311- 6334.
表 87: 通式 （1-19) 中，
Figure imgf000027_0002
=4-CF3、 （R5)n =3,5-2Cl时， 取代基 X 见表 71， 依次 对应表 71的 5951-5974， 代表化合物编号为 6335-6358。 Table 87: In the general formula (1-19),
Figure imgf000027_0002
When 4-CF 3 , (R 5 ) n = 3 , 5-2Cl, the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 6335-6358.
表 88: 通式 （1-19) 中，
Figure imgf000027_0003
(R5)n =3-Cl-5-CF3时， 取代基 X 见表 71， 依 次对应表 71的 5951-5974， 代表化合物编号为 6359-6382。 Table 88: In the general formula (1-19),
Figure imgf000027_0003
When (R 5 ) n = 3-Cl-5-CF 3 , the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 6359-6382.
表 89: 通式 （1-19) 中，
Figure imgf000027_0004
(R5)n =3,5,6-3Cl时， 取代基 X 见表 71， 依次 对应表 71的 5951-5974， 代表化合物编号为 6383-6406。 Table 89: In the general formula (1-19),
Figure imgf000027_0004
When (R 5 ) n = 3,5,6-3Cl, the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 6383-6406.
表 90: 通式 （1-19) 中， (R5)n =3-CF3时， 取代基 Xi见表 71， 依次对 应表 71的 5951-5974， 代表化 -6430。 Table 90: In the formula (1-19), when (R 5 ) n = 3-CF 3 , the substituent Xi is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, representing -6430.
表 91 : 通式 （1-19) 中，
Figure imgf000027_0005
(R5)n =5-CF3时， 取代基 Xi见表 71， 依次对 应表 71的 5951-5974， 代表化合物编号为 6431-6454。 Table 91: In the general formula (1-19),
Figure imgf000027_0005
When (R 5 ) n = 5 - CF 3 , the substituent Xi is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 6431-6454.
表 92: 通式 （1-19) 中， =2,4-2Cl、 （R5)n =3-Cl时， 取代基 Xi见表 71， 依次对 应表 71的 5951-5974， 代表化 为 6455-6478。 Table 92: In the general formula (1-19), when =2,4-2Cl, (R 5 ) n =3-Cl, the substituent Xi is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and is represented as 6455. -6478.
表 93: 通式 （1-19) 中，
Figure imgf000027_0006
=2,4-2Cl、 （R5)n =3-CN时， 取代基 Xi见表 71， 依次 对应表 71的 5951-5974， 代表化合物编号为 6479-6502。 Table 93: In the general formula (1-19),
Figure imgf000027_0006
When 2,4-2Cl, (R 5 ) n =3-CN, the substituent Xi is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 6479-6502.
表 94: 通式 (1-19) 中， ¾(Ri)m =2,4-2CL (R5)n =3,5-2Cl时， 取代基 Xi见表 71， 依次 对应表 71的 5951-5974， 代表化合物编号为 6503-6526。 Table 94: In the general formula (1-19), when 3⁄4(Ri) m = 2, 4-2CL (R 5 ) n = 3, 5-2Cl, the substituent Xi is shown in Table 71, which in turn corresponds to the 5951 of Table 71. 5974, representing compound number 6503-6526.
表 95: 通式 （1-19) 中，
Figure imgf000027_0007
=2,4-2Cl、 （R5)n =3-Cl-5-CF3时， 取代基 Xi见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 6527-6550。 Table 95: In the general formula (1-19),
Figure imgf000027_0007
When 2,4-2Cl, (R 5 ) n =3-Cl-5-CF 3 , the substituent Xi is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 6527-6550.
表 96: 通式 (1-19) 中， ¾(Ri)m =2,4-2CL (R5)n =3,5,6-3Cl时， 取代基 Xi见表 71， 依 次对应表 71的 5951-5974， 代表化合物编号为 6551-6574。 Table 96: In the general formula (1-19), when 3⁄4(Ri) m = 2, 4-2CL (R 5 ) n = 3, 5 , 6-3Cl, the substituent Xi is shown in Table 71, which in turn corresponds to Table 71. 5951-5974, representing compound number 6551-6574.
表 97: 通式 （1-19) 中， =2,4-2Cl、 （R5)n =3-CF3时， 取代基 Xi见表 71， 依次 对应表 71的 5951-5974， 代表 号为 6575-6598。 Table 97: In the formula (1-19), when =2,4-2Cl, (R 5 ) n =3-CF 3 , the substituent Xi is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and the representative number is 6575-6598.
表 98: 通式 （1-19) 中，
Figure imgf000027_0008
=2,4-2Cl、 （R5)n =5-CF3时， 取代基 X 见表 71， 依次 对应表 71的 5951-5974， 代表化合物编号为 6599-6622。 Table 98: In the general formula (1-19),
Figure imgf000027_0008
When 2,4-2Cl, (R 5 ) n =5-CF 3 , the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 6599-6622.
当通式 (1-1 ) 中， R =CF3， R4=H， X1=C-CN, x=0时， 结构如通式 (1-20) 所示。 When R = CF 3 , R4 = H, X 1 = C-CN, and x = 0 in the formula (1-1), the structure is as shown in the formula (1-20).
Figure imgf000027_0009
通式 （1-20) 中， 当 (R m =H、 (R5)„ =3-Cl时， 取代基 X2见表 99， 代表化合物编号为 6623-6630。 表 99
Figure imgf000027_0009
In the formula (1-20), when (R m = H, (R 5 ) „ = 3-Cl, the substituent X 2 is shown in Table 99, and the compound number is 6623-6630. Table 99
Figure imgf000028_0009
Figure imgf000028_0009
表 100: 通式 （1-20) 中， 当 (R m :^ (R5)n =3-CN时， 取代基 X2见表 99， 依次对应 表 99的 6623-6630， 代表化合物编号为 6631-6638。 Table 100: In the formula (1-20), when (R m :^ (R 5 ) n =3-CN, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, representing the compound number 6631-6638.
表 101 : 通式 (1-20) 中， ¾(Ri)m =H (R5)n =3,5-2Cl时， 取代基 X2见表 99， 依次对 应表 99的 6623-6630， 代表化合物编号为 6639-6646。 Table 101: In the general formula (1-20), when 3⁄4(Ri) m =H (R 5 ) n =3,5-2Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, representing The compound number is 6639-6646.
表 102: 通式 （1-20) 中，
Figure imgf000028_0001
(R5)n =3-Cl-5-CF3时， 取代基 X2见表 99， 依次 对应表 99的 6623-6630， 代表化合物编号为 6647-6654。 Table 102: In the general formula (1-20),
Figure imgf000028_0001
When (R 5 ) n = 3-Cl-5-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, and represents the compound number 6647-6654.
表 103: 通式 (1-20) 中， ¾(Ri)m =H (R5)n =3,5,6-3C1时， 取代基 X2见表 99， 依次对 应表 99的 6623-6630， 代表化合物编号为 6655-6662。 Table 103: In the general formula (1-20), when 3⁄4(Ri) m =H (R 5 ) n =3,5,6-3C1, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99. , represents the compound number 6555-6662.
表 104: 通式 （1-20) 中，
Figure imgf000028_0002
(R5)n =3-CF3时， 取代基 X2见表 99， 依次对应 表 99的 6623-6630， 代表化合物编号为 6663-6670。 Table 104: In the general formula (1-20),
Figure imgf000028_0002
When (R 5 ) n = 3-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, and represents the compound number 6663-6670.
表 105: 通式 （1-20) 中， 当 (1 ^ =11、 （R5)n =5-CF3时， 取代基 X2见表 99， 依次对应 表 99的 6623-6630， 代表化合物编号为 6671-6678。 Table 105: In the formula (1-20), when (1 ^ =11, (R 5 ) n =5-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, representing a compound The number is 6671-6678.
表 106: 通式 （1-20) 中，
Figure imgf000028_0003
(R5)n =3-Cl时， 取代基 X2见表 99， 依次对应 表 99的 6623-6630， 代表化合物编号为 6679-6686。 Table 106: In the general formula (1-20),
Figure imgf000028_0003
When (R 5 ) n = 3-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, and represents the compound number 6679-6686.
表 107: 通式 （1-20) 中， 当 (!^;^ =4 1、 （R5)n =3-CN时， 取代基 X2见表 99， 依次对 应表 99的 6623-6630， 代表化合物编号为 6687-6694。 Table 107: In the general formula (1-20), when (!^;^ =4 1 , (R 5 ) n =3-CN, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, The representative compound number is 6687-6694.
表 108: 通式 (1-20) 中， ¾(R M =4-CL (R5)n =3,5-2Cl时， 取代基 X2见表 99， 依次 对应表 99的 6623-6630， 代表化合物编号为 6695-6702。 Table 108: In the general formula (1-20), 3⁄4 (R M = 4-CL (R 5 ) n = 3, 5-2Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, The representative compound number is 6695-6702.
表 109: 通式 （1-20) 中， 当 (!^;^ =4 1、 （R5)n =3-Cl-5-CF3时， 取代基 X2见表 99， 依 次对应表 99的 6623-6630， 代表化合物编号为 6703-6710。 Table 109: In the general formula (1-20), when (!^;^ =4 1 , (R 5 ) n =3-Cl-5-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to Table 99 6623-6630, representing the compound number 6703-6710.
表 110: 通式 (1-20) 中， ¾(R M =4-CL (R5)n =3,5,6-3Cl时， 取代基 X2见表 99， 依次 对应表 99的 6623-6630， 代表化合物编号为 6711-6718。 Table 110: In the general formula (1-20), when 3⁄4 (R M = 4-CL (R 5 ) n = 3, 5 , 6-3Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to the 6623 of Table 99 6630, the representative compound number is 6711-6718.
表 111 : 通式 （1-20) 中， (R5)n =3-CF3时， 取代基 X2见表 99， 依次对 应表 99的 6623-6630， 代表化 9-6726。 In the formula (1-20), when (R 5 ) n = 3-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, and represents 9-6726.
表 112: 通式 （1-20) 中，
Figure imgf000028_0004
(R5)n =5-CF3时， 取代基 X2见表 99， 依次对 应表 99的 6623-6630， 代表化合物编号为 6727-6734。 Table 112: In the general formula (1-20),
Figure imgf000028_0004
When (R 5 ) n = 5-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, and represents the compound number 6727-6734.
表 113: 通式 (1-20) 中，
Figure imgf000028_0005
=4-CF3、 （R5)n =3-Cl时， 取代基 X2表 99， 依次对应 表 99的 6623-6630， 代表化合物编号为 6735-6742。 Table 113: In the general formula (1-20),
Figure imgf000028_0005
When 4-CF 3 and (R 5 ) n = 3-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, and represents the compound number 6735-6742.
表 114: 通式 （1-20) 中， (R5)n =3-CN时， 取代基 X2见表 99， 依次对 应表 99的 6623-6630， 代表化 -6750。 Table 114: In the formula (1-20), when (R 5 ) n = 3-CN, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, representing -6750.
表 115: 通式 （1-20) 中，
Figure imgf000028_0006
(R5)n =3,5-2Cl时， 取代基 X2见表 99， 依次 对应表 99的 6623-6630， 代表化合物编号为 6751-6758。 Table 115: In the general formula (1-20),
Figure imgf000028_0006
When (R 5 ) n = 3,5-2Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, and represents the compound number 6751-6758.
表 116: 通式 (1-20) 中， =4-CF3、 （R5)n =3-Cl-5-CF3时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 物编号为 6759-6766。 Table 116: In the formula (1-20), when =4-CF 3 , (R 5 ) n =3-Cl-5-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99. , item number is 6759-6766.
表 117: 通式 (1-20) 中，
Figure imgf000028_0007
=4-CF3、 （R5)n =3,5,6-3Cl时， 取代基 X2见表 99， 依 次对应表 99的 6623-6630， 代表化合物编号为 6767-6774。 Table 117: In the general formula (1-20),
Figure imgf000028_0007
When 4-CF 3 and (R 5 ) n = 3,5,6-3Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, and represents the compound number 6767-6774.
表 118: 通式 （1-20) 中，
Figure imgf000028_0008
(R5)n =3-CF3时， 取代基 X2见表 99, 依次对 应表 99的 6623-6630， 代表化合物编号为 6775-6782。 表 119: 通式 (1-20) 中， ¾(R m =4-CF3 (R5)n =5-CF3时， 取代基 X2见表 99， 依次对 应表 99的 6623-6630， 代表化合物编号为 6783-6790。 Table 118: In the general formula (1-20),
Figure imgf000028_0008
When (R 5 ) n = 3-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, and represents the compound number 6775-6782. Table 119: In the general formula (1-20), when 3⁄4 (R m = 4-CF 3 (R 5 ) n = 5-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, The representative compound number is 6783-6790.
表 120: 通式 (1-20) 中， ¾(Ri)m =2,4-2CL (R5)n =3-Cl时， 取代基 X2见表 99， 依次 对应表 99的 6623-6630， 代表化合物编号为 6791-6798。 Table 120: In the general formula (1-20), when 3⁄4(Ri) m = 2,4-2CL (R 5 ) n =3-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99. , represents the compound number 6791-6798.
表 121 : 通式 （1-20) 中， 当 (!^;^ =2,4-20、 （R5)n =3-CN时， 取代基 X2见表 99， 依次 对应表 99的 6623-6630， 代表化合物编号为 6799-6806。 Table 121: In the general formula (1-20), when (!^;^ =2,4-20, (R 5 ) n =3-CN, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623 of Table 99. -6630, representing compound number 6799-6806.
表 122: 通式 (1-20) 中， ¾(Ri)m =2,4-2CL (R5)n =3,5-2Cl时， 取代基 X2见表 99， 依 次对应表 99的 6623-6630， 代表化合物编号为 6807-6814。 Table 122: In the general formula (1-20), when 3⁄4(Ri) m = 2, 4-2CL (R 5 ) n = 3, 5-2Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623 of Table 99. -6630, representing compound number 6807-6814.
表 123: 通式 (1-20) 中， ¾(Ri)m =2,4-2CL (R5)n =3-Cl-5-CF3时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6815-6822。 Table 123: In the general formula (1-20), when 3⁄4(Ri) m = 2, 4-2CL (R 5 ) n = 3-Cl-5-CF 3 , the substituent X 2 is shown in Table 99, and the corresponding correspondence table 9923-6630 of 99, representing the compound number 6815-6822.
表 124: 通式 (1-20) 中， ¾(Ri)m =2,4-2CL (R5)n =3,5,6-3Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6823-6830。 Table 124: In the general formula (1-20), when 3⁄4(Ri) m = 2, 4-2CL (R 5 ) n = 3, 5 , 6-3Cl, the substituent X 2 is shown in Table 99, which corresponds to Table 99 in sequence. 6623-6630, representing the compound number 6823-6830.
表 125通式 （1-20) 中， 当 (!^;^ =2,4-20、 （R5)n =3-CF3时， 取代基 X2见表 99， 依次对 应表 99的 6623-6630， 代表化合物编号为 6831-6838。 In the formula (1-20), when (!^;^ = 2,4-20, (R 5 ) n =3-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to 6623 of Table 99. -6630, representing compound number 6831-6838.
表 126: 通式 (1-20) 中， ¾(Ri)m =2,4-2CL (R5)n =5-CF3时， 取代基 X2见表 99， 依次 对应表 99的 6623-6630， 代表化合物编号为 6839-6846。 Table 126: In the general formula (1-20), when 3⁄4(Ri) m = 2,4-2CL (R 5 ) n =5-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to the 6623 of Table 99 6630, the representative compound number is 6839-6846.
当通式 (1-1 ) 中， =Η， Xi=C-CN, x=0时， 结构如通式 (1-21 ) 所示。  When the formula (1-1), =Η, Xi=C-CN, x=0, the structure is as shown in the formula (1-21).
Figure imgf000029_0001
Figure imgf000029_0001
表 127: 通式 （1-21 ) 中， 当 R2=CH3、 （Ri)m =H、 （R5)n =3-Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6847-6854。 Table 127: In the general formula (1-21), when R 2 =CH 3 , (Ri) m =H, (R 5 ) n =3-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to Table 99. 6623-6630, the representative compound number is 6847-6854.
表 128: 通式 (1-21 ) 中， 当 R2=CHF2、 （Ri)m =H、 （R5)n =3-Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6855-6862。 Table 128: In the general formula (1-21), when R 2 =CHF 2 , (Ri) m =H, (R 5 ) n =3-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to Table 99. 6623-6630, the representative compound number is 6855-6862.
表 129: 通式（1-21 ) 中， 当 R2=CH3、 （Ri)m =H、 （R5)n =3,5-2Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6863-6870。 Table 129: In the general formula (1-21), when R 2 =CH 3 , (Ri) m =H, (R 5 ) n =3,5-2Cl, the substituent X 2 is shown in Table 99, and the corresponding correspondence table The 6623-6630 of 99 represents the compound number 6863-6870.
表 130: 通式 (1-21 ) 中， 当 R2=CH3、 （Ri)m =H、 （R5)n =3-Cl-5-CF3时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 6871-6878。 Table 130: In the formula (1-21), when R 2 =CH 3 , (Ri) m =H, (R 5 ) n =3-Cl-5-CF 3 , the substituent X 2 is shown in Table 99. Corresponding to 6623-6630 of Table 99, the representative compound number is 6871-6878.
表 131 : 通式 (1-21 ) 中， 当 R2= CHF2、 （Ri)m =H、 （R5)n =3,5-2Cl时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 6879-6886。 Table 131: In the general formula (1-21), when R 2 = CHF 2 , (Ri) m = H, (R 5 ) n = 3, 5-2Cl, the substituent X 2 is shown in Table 99, and the corresponding correspondence table 9923-6630 of 99, representing the compound number 6879-6886.
表 132: 通式 （1-21 ) 中， 当 R2=CH3、 (R m =H (R5)n =3-CF3时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6887-6894。 Table 132: In the general formula (1-21), when R 2 =CH 3 , (R m =H (R 5 ) n =3-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to 6623 of Table 99. -6630, representing the compound number 6887-6894.
表 133: 通式 (1-21 ) 中， 当 R2=CHF2、 (R m =H (R5)n =3-CF3时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6895-6902。 Table 133: In the general formula (1-21), when R 2 =CHF 2 , (R m =H (R 5 ) n =3-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to 6623 of Table 99. -6630, the representative compound number is 6895-6902.
表 134: 通式 (1-21 ) 中， 当 R2=CH3、 (R m =4-CL (R5)n =3-Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6903-6910。 Table 134: In the general formula (1-21), when R 2 =CH 3 , (R m =4-CL (R 5 ) n =3-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to Table 99 6623-6630, the representative compound number is 6903-6910.
表 135: 通式 (1-21 )中， 当 R2=CHF2、 (R m =4-CL (R5)n =3-Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6911-6918。 Table 135: In the general formula (1-21), when R 2 =CHF 2 , (R m =4-CL (R 5 ) n =3-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to Table 99 6623-6630, the representative compound number is 6911-6918.
表 136: 通式 (1-21 ) 中， 当 R2=CH3、 (R m =4-CL (R5)n =3,5-2Cl时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 6919-6926。 Table 136: In the general formula (1-21), when R 2 =CH 3 , (R m =4-CL (R 5 ) n =3,5-2Cl, the substituent X 2 is shown in Table 99, and the corresponding correspondence table 6623-6630 of 99, representing compound number 6919-6926.
表 137: 通式 (1-21 ) 中， 当 R2=CH3、 (R m =4-CL (R5)n =3-Cl-5-CF3时， 取代基 X2见 表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6927-6934。 Table 137: In the formula (1-21), when R 2 =CH 3 , (R m =4-CL (R 5 ) n =3-Cl-5-CF 3 , the substituent X 2 is found Table 99, which in turn corresponds to 6623-6630 of Table 99, represents the compound number 6927-6934.
表 138: 通式 (1-21 ) 中， 当 R2=CHF2、 (R m =4-CL (R5)n =3,5-2Cl时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 6935-6942。 Table 138: In the general formula (1-21), when R 2 =CHF 2 , (R m =4-CL (R 5 ) n =3,5-2Cl, the substituent X 2 is shown in Table 99, and the corresponding correspondence table The 6623-6630 of 99 represents the compound number 6935-6942.
表 139: 通式 (1-21 )中， 当 R2=CH3、 (R m =4-CL (R5)n =3-CF3时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6943-6950。 Table 139: In the general formula (1-21), when R 2 =CH 3 , (R m =4-CL (R 5 ) n =3-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to Table 99 6623-6630, representing the compound number 6943-6950.
表 140: 通式 (1-21 ) 中， 当 R2=CHF2、 (R m =4-CL (R5)n =3-CF3时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 6951-6958。 Table 140: In the general formula (1-21), when R 2 =CHF 2 , (R m =4-CL (R 5 ) n =3-CF 3 , the substituent X 2 is shown in Table 99, which in turn corresponds to Table 99 6623-6630, representing the compound number 6951-6958.
表 141 : 通式 （1-21 ) 中， 当 R2=CH3、 (R m =4-CF3 (R5)n =3-Cl时， 取代基 X2表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6959-6966。 Table 141: In the formula (1-21), when R 2 =CH 3 , (R m =4-CF 3 (R 5 ) n =3-Cl, the substituent X 2 is in Table 99, which in turn corresponds to Table 99 6623-6630, the representative compound number is 6959-6966.
表 142: 通式 （1-21 ) 中， 当 R2=CHF2、 (R m =4-CF3 (R5)n =3-Cl时， 取代基 X2见表Table 142: In the formula (1-21), when R 2 =CHF 2 , (R m =4-CF 3 (R 5 ) n =3-Cl, the substituent X 2 is shown in the table.
99, 依次对应表 99的 6623-6630， 代表化合物编号为 6967-6974。 99, which corresponds to 6623-6630 of Table 99 in turn, represents the compound number 6967-6974.
表 143: 通式 (1-21 ) 中， 当 R2=CH3、 (R m =4-CF3 (R5)n =3,5-2Cl时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 6975-6982。 Table 143: In the general formula (1-21), when R 2 =CH 3 , (R m =4-CF 3 (R 5 ) n =3,5-2Cl, the substituent X 2 is shown in Table 99, which corresponds to 6623-6630 of Table 99, representing the compound number 6975-6982.
表 144: 通式 (1-21 ) 中， 当 R2=CH3、 (R m =4-CF3 (R5)n =3-Cl-5-CF3时， 取代基 X2 见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6983-6990。 Table 144: In the formula (1-21), when R 2 =CH 3 , (R m =4-CF 3 (R 5 ) n =3-Cl-5-CF 3 , the substituent X 2 is shown in Table 99 , which corresponds to 6623-6630 of Table 99 in turn, and represents the compound number 6983-6990.
表 145: 通式 （1-21 ) 中， 当 R2=CHF2、 (R m =4-CF3 (R5)n =3,5-2Cl时， 取代基 X2见 表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 6991-6998。 Table 145: In the general formula (1-21), when R 2 =CHF 2 , (R m =4-CF 3 (R 5 ) n =3,5-2Cl, the substituent X 2 is shown in Table 99, which corresponds to 6623-6630 of Table 99, representing the compound number 6991-6998.
表 146: 通式 （1-21 ) 中， 当 R2=CH3、 (Ri)m =4-CF3 (R5)n =3-CF3时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 6999-7006。 Table 146: In the formula (1-21), when R 2 =CH 3 , (Ri) m =4-CF 3 (R 5 ) n =3-CF 3 , the substituent X 2 is shown in Table 99, which corresponds to 6623-6630 of Table 99, representing the compound number 6999-7006.
表 147: 通式 （1-21 ) 中， 当 R2=CHF2、 (Ri)m =4-CF3 (R5)n =3-CF3时， 取代基 X2见表Table 147: In the formula (1-21), when R 2 =CHF 2 , (Ri) m =4-CF 3 (R 5 ) n =3-CF 3 , the substituent X 2 is shown in the table.
99, 依次对应表 99的 6623-6630， 代表化合物编号为 7007-7014。 99, which corresponds to 6623-6630 of Table 99 in turn, represents the compound number 7007-7014.
表 148: 通式 （1-21 ) 中， 当 R2=CH3、 (Ri)m =2,4-2CL (R5)n =3-Cl时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 7015-7022。 Table 148: In the general formula (1-21), when R 2 =CH 3 , (Ri) m =2,4-2CL (R 5 ) n =3-Cl, the substituent X 2 is shown in Table 99, which corresponds to 6623-6630 of Table 99, representing the compound number 7015-7022.
表 149: 通式 (1-21 ) 中， 当 R2=CHF2、 (Ri)m =2,4-2CL (R5)n =3-Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 7023-7030。 Table 149: In the general formula (1-21), when R 2 =CHF 2 , (Ri) m =2,4-2CL (R 5 ) n =3-Cl, the substituent X 2 is shown in Table 99, which corresponds to 6623-6630 of Table 99, representing the compound number 7023-7030.
表 150: 通式 （1-21 ) 中， 当 R2=CH3、 (Ri)m =2,4-2CL (R5)n =3,5-2Cl时， 取代基 X2见 表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 7031-7038。 Table 150: In the formula (1-21), when R 2 =CH 3 , (Ri) m =2, 4-2CL (R 5 ) n =3,5-2Cl, the substituent X 2 is shown in Table 99, Corresponding to 6623-6630 of Table 99, the representative compound number is 7031-7038.
表 151 : 通式 (1-21 ) 中， 当 R2=CH3、 (Ri)m =2,4-2CL (R5)n =3-Cl-5-CF3时， 取代基 X2 见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 7039-7046。 Table 151: In the general formula (1-21), when R 2 =CH 3 , (Ri) m =2, 4-2CL (R 5 ) n =3-Cl-5-CF 3 , the substituent X 2 is found. Table 99, which in turn corresponds to 6623-6630 of Table 99, represents the compound number 7039-7046.
表 152: 通式 （1-21 ) 中， 当 R2=CHF2、 (Ri)m =2,4-2Cl、 (R5)„ =3,5-2Cl时， 取代基 X2 见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 7047-7054。 Table 152: In the formula (1-21), when R 2 =CHF 2 , (Ri) m =2,4-2Cl, (R 5 )„ =3,5-2Cl, the substituent X 2 is shown in Table 99 , which corresponds to 6623-6630 of Table 99 in turn, and represents the compound number 7047-7054.
表 153: 通式 (1-21 ) 中， 当 R2=CH3、 (Ri)m =2,4-2CL (R5)n =3-CF3时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 7055-7062。 Table 153: In the general formula (1-21), when R 2 =CH 3 , (Ri) m =2,4-2CL (R 5 ) n =3-CF 3 , the substituent X 2 is shown in Table 99, in turn Corresponding to 6623-6630 of Table 99, the representative compound number is 7055-7062.
表 154: 通式 (1-21 ) 中， 当 R2=CHF2、 (R m =2,4-2CL (R5)n =3-CF3时， 取代基 X2见 表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 7063-7070。 Table 154: In the general formula (1-21), when R 2 =CHF 2 , (R m =2,4-2CL (R 5 ) n =3-CF 3 , the substituent X 2 is shown in Table 99, which corresponds to 6623-6630 of Table 99, representing the compound number 7063-7070.
当通式 (1-1 ) 中 =CF3， R4=H， x=0时， 结构如通式 (1-22) 所示。 When the formula (1-1) = CF 3 , R 4 = H, x = 0, the structure is as shown in the formula (1-22).
表 155: 通式 （1-22) 中， 当 X1=N、 （Ri)m =H、 （R5)n =3-Cl时， 取代基 X2见表 99， 依 次对应表 99的 6623-6630， 代表化合物编号为 7071-7078。 Table 155: In the general formula (1-22), when X 1 = N, (Ri) m = H, (R 5 ) n = 3-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623 of Table 99. -6630, the representative compound number is 7071-7078.
表 156: 通式 （1-22) 中， 当 X1=N、 （Ri)m =H、 （R5)n =3,5-2Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 7079-7086。 Table 156: In the general formula (1-22), when X 1 = N, (Ri) m = H, (R 5 ) n = 3, 5-2Cl, the substituent X 2 is shown in Table 99, Corresponding to 6623-6630 of Table 99, the representative compound number is 7079-7086.
表 157 : 通式（1-22)中， 当 X1=N、（Ri)M =H、（R5)N =3-Cl-5-CF3时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 7087-7094。 Table 157: In the general formula (1-22), when X 1 = N, (Ri) M = H, (R 5 ) N = 3-Cl-5-CF 3 , the substituent X 2 is shown in Table 99, in turn Corresponding to 6623-6630 of Table 99, the representative compound number is 7087-7094.
表 158 : 通式 （1-22) 中， 当 XFC-CC^CH^ (R m =4-Cl、 (R5)„ =3-Cl时， 取代基 X2 见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 7095-7102。 Table 158: In the general formula (1-22), when XFC-CC^CH^ (R m = 4-Cl, (R 5 ) „ = 3-Cl, the substituent X 2 is shown in Table 99, which corresponds to Table 99 in sequence. 6623-6630, representing the compound number 7095-7102.
表 159: 通式 ( 1-22) 中， ¾ X!=C-CONH2 (Ri)m =4-CL (R5)N =3,5-2Cl时， 取代基 X2 见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 7103-7110。 Table 159: In the general formula (1-22), 3⁄4 X!=C-CONH 2 (Ri) m = 4-CL (R 5 ) N = 3,5-2Cl, the substituent X 2 is shown in Table 99, in turn Corresponding to 6623-6630 of Table 99, the representative compound number is 7103-7110.
表 160: 通式 ( 1-22) 中， ¾ X!=C-CONH2 (Ri)m =4-CF3、 (R5)„ =3,5-2Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 7111-7118。 Table 160: In the general formula (1-22), 3⁄4 X!=C-CONH 2 (Ri) m = 4-CF 3 , (R 5 ) „ =3,5-2Cl, the substituent X 2 is shown in Table 99 , which corresponds to 6623-6630 of Table 99 in turn, and represents the compound number 7111-7118.
表 161 : 通式 （1-22) 中， 当 X1= C-C02CH3、 (R M =2,4-2CL (R5)N =3-Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 7119-7126。 Table 161: In the formula (1-22), when X 1 = C-C0 2 CH 3 , (R M = 2 , 4-2CL (R 5 ) N = 3-Cl, the substituent X 2 is shown in Table 99 , which corresponds to 6623-6630 of Table 99 in turn, and represents the compound number 7119-7126.
当通式 （1- 1 ) 中 所示。  As shown in the general formula (1-1).
表 162: 通式 （1
Figure imgf000031_0001
， 取代基 Xi见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 7127-7150。 Table 162: General formula (1
Figure imgf000031_0001
The substituent Xi is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 7127-7150.
表 163: 通式 (1-23 )中， ¾(Ri)m =2-N02 (R5)„ =3-CL R2=CH3时， 取代基 Xi见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 7151-7174。 Table 163: In the general formula (1-23), when 3⁄4(Ri) m = 2-N0 2 (R 5 ) „ = 3-CL R 2 = CH 3 , the substituent Xi is shown in Table 71, which in turn corresponds to Table 71. 5951-5974, representing compound number 7151-7174.
表 164: 通式 (1-23 ) 中， ¾(R m =4-CL (R5)n =3,5-2Cl、 R2=CHF2时， 取代基 X 见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 7175-7198。 Table 164: In the general formula (1-23), when 3⁄4 (R m = 4-CL (R 5 ) n = 3, 5-2Cl, R 2 = CHF 2 , the substituent X is shown in Table 71, which corresponds to Table 71 in sequence. 5951-5974, representing the compound number 7175-7198.
表 165: 通式（1-23 ) 中，
Figure imgf000031_0002
R2=CH3时， 取代基 Xi见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 7199-7222。 Table 165: In the general formula (1-23),
Figure imgf000031_0002
When R 2 =CH 3 , the substituent Xi is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 7199-7222.
当通式 (1-4) 中， R2=CF3， R4=H， X2=CO， Xi=C-CN, x=0时， 结构如通式 (1-24)所 In the general formula (1-4), R 2 =CF 3 , R4=H, X 2 =CO, Xi=C-CN, x=0, the structure is as shown in the general formula (1-24)
Figure imgf000031_0003
Figure imgf000031_0003
表 166: 通式 （1-24) 中， (R5)„ =2-Cl (Ri)m见表 17 依次对应表 17的 1-261， 代表化 合物编号为 7223-7483。 Table 166: In the general formula (1-24), (R 5 ) „ = 2-Cl (Ri) m is shown in Table 17 and corresponds to 1-261 of Table 17, which represents the compound number 7223-7483.
表 167: 通式 （1-24) 中， （R5)n =4-Cl， （R^m见表 17， 依次对应表 17的 1-261， 代表化 合物编号为 7484-7744。 Table 167: In the formula (1-24), (R 5 ) n = 4-Cl, (R^m is shown in Table 17, which in turn corresponds to 1-261 of Table 17, and represents the compound number 7484-7744.
表 168: 通式 （1-24) 中， （R5)n =2,4-2Cl， （Ri)m见表 17， 依次对应表 17的 1-261， 代 表化合物编号为 7745-8005。 Table 168: In the formula (1-24), (R 5 ) n = 2, 4-2Cl, (Ri) m is shown in Table 17, which in turn corresponds to 1-261 of Table 17, and represents the compound number 7745-8005.
表 169:通式（1-24)中， 当 （R^n^H时， 取代基 (R5)n见表 17， 依次对应表 17的 1-261， 代表化合物编号为 8006-8266。 Table 169: In the formula (1-24), when (R^n^H, the substituent (R 5 ) n is shown in Table 17, which in turn corresponds to 1-261 of Table 17, and represents the compound number 8006-8266.
表 170: 通式 （1-24) 中， 当 （R^m =4-Cl时， 取代基 (R5)n见表 17， 依次对应表 17的 1-261， 代表化合物编号为 8267-8527。 Table 170: In the formula (1-24), when (R^m = 4-Cl, the substituent (R 5 ) n is shown in Table 17, which in turn corresponds to 1-261 of Table 17, representing the compound number 8267-8527 .
表 171 : 通式 （1-24) 中， 当 （R m ^CFg时， 取代基 (R5)n见表 17， 依次对应表 17的 1-261， 代表化合物编号为 8528-8788。 Table 171: In the general formula (1-24), when (R m ^CFg, the substituent (R 5 ) n is shown in Table 17, which in turn corresponds to Table 17 1-261, representing compound number 8528-8788.
表 172: 通式 （1-24) 中， 当 （R^m =2,4-2Cl时， 取代基 (R5)n见表 17， 依次对应表 17 的 1-261， 代表化合物编号为 8789-9049。 Table 172: In the general formula (1-24), when (R^m = 2, 4-2Cl, the substituent (R 5 ) n is shown in Table 17, which in turn corresponds to 1-261 of Table 17, representing the compound number 8789 -9049.
当通式 (1-4) 中， R4=H， X2=CO， Xi=C-CN, x=0时， 结构如通式 (1-25) 所示。 When R4 = H, X 2 = CO, Xi = C-CN, x = 0 in the formula (1-4), the structure is as shown in the formula (1-25).
Figure imgf000032_0001
Figure imgf000032_0001
表 173: 通式 （1-25) 中， 当 （R m :!^ (R5)n =2-Cl时， 取代基 R2见表 43， 依次对应 表 43的 5363-5383， 代表化合物编号为 9050-9070。 Table 173: In the general formula (1-25), when (R m :!^ (R 5 ) n = 2-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and represents the compound number. It is 9050-9070.
表 174: 通式 (1-25) 中， 当 （Ri)m=H、 （R5)n =2,4-2Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 9071-9091。 Table 174: In the general formula (1-25), when (Ri) m = H, (R 5 ) n = 2 , 4-2Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 The representative compound number is 9071-9091.
表 175: 通式 (1-25) 中， ¾(R M =H (R5)n =2-Cl-4-CF3时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 9092-9112。 Table 175: In the general formula (1-25), when 3⁄4 (R M =H (R 5 ) n =2-Cl-4-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 , represents the compound number is 9092-9112.
表 176: 通式 （1-25) 中， 当 （R n^A-CL (R5)n =2,4-2Cl时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 9113-9133。 Table 176: In the formula (1-25), when (R n^A-CL (R 5 ) n = 2 , 4-2Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 The representative compound number is 9113-9133.
表 177: 通式 (1-25) 中， 当 (Ri)m =4-CL (R5)n =2,6-2Cl-4-N02时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 9134-9154。 Table 177: In the general formula (1-25), when (Ri) m = 4-CL (R 5 ) n = 2 , 6-2Cl-4-N0 2 , the substituent R 2 is shown in Table 43, 5363-5383 of 43 represents the compound number 9134-9154.
表 178: 通式 (1-25) 中， 当 (Ri)m =4-CL (R5)n =2,3,5-3Cl-4,6-2CN时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 9155-9175。 Table 178: In the general formula (1-25), when (Ri) m = 4-CL (R 5 ) n = 2 , 3, 5-3Cl-4, 6-2CN, the substituent R 2 is shown in Table 43, Corresponding to 5363-5383 of Table 43, the representative compound number is 9155-9175.
表 179: 通式 (1-25)中， 当 (Ri)m =4-CF3 (R5)n =2,6-2Cl-4-N02时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 9176-9196。 Table 179: In the general formula (1-25), when (Ri) m = 4-CF 3 (R 5 ) n = 2 , 6-2Cl-4-N0 2 , the substituent R 2 is shown in Table 43, 5363-5383 of Table 43 represents the compound number 9176-9196.
表 180: 通式 (1-25) 中， 当 (Ri)m =4-CF3 (R5)n =4-CF3时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 9197-9217。 Table 180: In the general formula (1-25), when (Ri) m = 4-CF 3 (R 5 ) n = 4-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 , represents the compound number 9197-9217.
表 181: 通式 （1-25) 中， 当 （^;^ =2,4-20、 （R5)n =2,6-2Cl-4-N02时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 9218-9238。 Table 181: In the formula (1-25), when (^; ^ = 2, 4-20, (R 5 ) n = 2 , 6-2Cl-4-N0 2 , the substituent R 2 is shown in Table 43, Corresponding to 5363-5383 of Table 43, this represents the compound number 9218-9238.
表 182: 通式 (1-25) 中， 当 (Ri)m =2,4-2CL (R5)n =2,4-2Cl时， 取代基 R2见表 43， 依 次对应表 43的 5363-5383， 代表化合物编号为 9239-9259。 Table 182: In the general formula (1-25), when (Ri) m = 2, 4-2CL (R 5 ) n = 2 , 4-2Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363 of Table 43 -5383, represents the compound number 9239-9259.
当通式 (1-4) 中 式 (1-26) 所示。  When formula (1-4) is shown in formula (1-26).
Figure imgf000032_0002
Figure imgf000032_0002
表 183: 通式 （1-26) 中， 当 （Ri)m=H、 （R5)n =2-Cl时， 取代基 X 见表 71， 依次对应 表 71的 5951-5974， 代表化合物编号为 9260-9283。 Table 183: In the general formula (1-26), when (Ri) m = H, (R 5 ) n = 2-Cl, the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, representing the compound number. It is 9260-9283.
表 184: 通式 （1-26) 中，
Figure imgf000032_0003
(R5)n =2-Cl-4-CF3时， 取代基 X 见表 71， 依次 对应表 71的 5951-5974， 代表化合物编号为 9284-9307。 Table 184: In the general formula (1-26),
Figure imgf000032_0003
When (R 5 ) n = 2-Cl-4-CF 3 , the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, and represents the compound number 9284-9307.
表 185: 通式 （1-26) 中， 当 （R n^A-CL (R5)n =2-Cl时， 取代基 X 见表 71， 依次对 应表 71的 5951-5974， 代表化合物编号为 9308-9331。 Table 185: In the formula (1-26), when (R n^A-CL (R 5 ) n = 2-Cl, the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, representing the compound number. It is 9308-9331.
表 186: 通式 （1-26) 中， 当 （R n^A-CL (R5)n =2,6-2Cl-4-N02时， 取代基 见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 9332-9355。 表 187: 通式 （1-26) 中， 当 （R n^A-CF^ (R5)n =2-Cl时， 取代基 X 见表 71， 依次对 应表 71的 5951-5974， 代表化合物编号为 9356-9379。 Table 186: In the general formula (1-26), when (R n^A-CL (R 5 ) n = 2 , 6-2Cl-4-N0 2 , the substituents are shown in Table 71, which in turn correspond to the 5591 of Table 71. -5974, representing compound number 9332-9355. Table 187: In the formula (1-26), when (R n^A-CF^(R 5 ) n = 2-Cl, the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, representing a compound The number is 9356-9379.
表 188: 通式 （1-26) 中， 当 （R^m =4-CF3、 (R5)„ =2,6-2Cl-4-N02时， 取代基 X 见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 9380-9403。 Table 188: In the general formula (1-26), when (R^m = 4-CF 3 , (R 5 ) „ 2,6-2Cl-4-N0 2 , the substituent X is shown in Table 71, which corresponds to 5951-5974 of Table 71, representing the compound number 9380-9403.
表 189: 通式 (1-26) 中， 当 (Ri)m =2,4-2CL (R5)n =2-Cl时， 取代基 X 见表 71， 依次 对应表 71的 5951-5974， 代表化合物编号为 9404-9427。 Table 189: In the general formula (1-26), when (Ri) m = 2, 4-2CL (R 5 ) n = 2-Cl, the substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, The representative compound number is 9404-9427.
当通式 (1-4) 中， R =CF3， R4=H， X1=C-CN, x=0时， 结构如通式 (1-27) 所示。 When R = CF 3 , R4 = H, X 1 = C-CN, and x = 0 in the formula (1-4), the structure is as shown in the formula (1-27).
Figure imgf000033_0001
Figure imgf000033_0001
表 190: 通式 （1-27) 中， 当 （R m :!^ (R5)n =2-Cl时， 取代基 X2见表 99， 依次对应 表 99的 6623-6630， 代表化合物编号为 9428-9435。 Table 190: In the general formula (1-27), when (R m :!^ (R 5 ) n = 2-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, representing the compound number. It is 9428-9435.
表 191 : 通式 (1-27) 中， ¾(R M =H (R5)n =2,6-2Cl-4-N02时， 取代基 X2见表 99， 依 次对应表 99的 6623-6630， 代表化合物编号为 9436-9443。 Table 191: In the general formula (1-27), when 3⁄4 (R M =H (R 5 ) n = 2,6-2Cl-4-N0 2 , the substituent X 2 is shown in Table 99, which in turn corresponds to 6623 of Table 99. -6630, the representative compound number is 9436-9443.
表 192: 通式 （1-27) 中， 当 （R n^A-CL (R5)n =2-Cl时， 取代基 X2见表 99， 依次对 应表 99的 6623-6630， 代表化合物编号为 9444-9451。 Table 192: In the formula (1-27), when (R n^A-CL (R 5 ) n = 2-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, representing a compound The number is 9444-9451.
表 193: 通式 （1-27) 中， 当 （R m =4-CF3、 (R5)„ =2,6-2Cl-4-N02时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 9452-9459。 Table 193: In the general formula (1-27), when (R m = 4-CF 3 , (R 5 ) „ 2 , 6-2Cl-4-N0 2 , the substituent X 2 is shown in Table 99, which corresponds to 6623-6630 of Table 99, representing the compound number 9452-9459.
表 194: 通式 (1-27) 中， 当 (Ri)m =4-CF3 (R5)n =2,4-2Cl时， 取代基 X2见表 99， 依 次对应表 99的 6623-6630， 代表化合物编号为 9460-9467。 Table 194: In the general formula (1-27), when (Ri) m = 4-CF 3 (R 5 ) n = 2 , 4-2Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623 of Table 99. 6630, representing the compound number 9460-9467.
表 195: 通式 （1-27) 中， 当 （!^;^ =2,4-20、 （R5)n =2-Cl时， 取代基 X2见表 99， 依次 对应表 99的 6623-6630， 代表化合物编号为 9468-9475。 Table 195: In the general formula (1-27), when (!^;^ =2,4-20, (R 5 ) n =2-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623 of Table 99. -6630, representing compound number 9468-9475.
表 196: 通式 （1-27) 中， 当 （R n^S^JCL (R5)n =2,4-2Cl时， 取代基 X2见表 99， 依 次对应表 99的 6623-6630， 代表化合物编号为 9476-9483。 Table 196: In the general formula (1-27), when (R n^S^JCL (R 5 ) n = 2 , 4-2Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, The representative compound number is 9476-9483.
当通式 (1-4) 中， R =H， Xi=C-CN, x=0时， 结构如通式 (1-28) 所示。  When R = H, Xi = C-CN, x = 0 in the formula (1-4), the structure is as shown in the formula (1-28).
Figure imgf000033_0002
Figure imgf000033_0002
表 197: 通式 （1-28) 中， 当 （Ri)m =H、 R2=CH3、 （R5)n =2-Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 9484-9491。 Table 197: In the general formula (1-28), when (Ri) m = H, R 2 = CH 3 , (R 5 ) n = 2-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to Table 99. 6623-6630, the representative compound number is 9484-9491.
表 198: 通式 （1-28) 中，
Figure imgf000033_0003
R2=CHF2、 （R5)n =2-Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 9492-9499。 Table 198: In the general formula (1-28),
Figure imgf000033_0003
When R 2 =CHF 2 and (R 5 ) n =2-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, and represents the compound number 9492-9499.
表 199: 通式 (1-28) 中， 当 (Ri)m =4-CL R2=CH3、 （R5)n =2-Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 9500-9507。 Table 199: In the general formula (1-28), when (Ri) m = 4-CL R 2 =CH 3 , (R 5 ) n = 2-Cl, the substituent X 2 is shown in Table 99, which corresponds to Table 99 in sequence. 6623-6630, representing the compound number 9500-9507.
表 200: 通式 （1-28) 中， 当 （R^m =4-Cl、 R2=CHF2、 (R5)„ =2-Cl时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 9508-9515。 Table 200: In the general formula (1-28), when (R^m = 4-Cl, R 2 =CHF 2 , (R 5 ) „ = 2-Cl, the substituent X 2 is shown in Table 99, and the corresponding correspondence table 9923-6630 of 99, representing the compound number 9508-9515.
表 201 : 通式 (1-28) 中， 当 (Ri)m =4-CF3、 R2=CH3、 (R5)„ =2-Cl时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 9516-9523。 Table 201: In the general formula (1-28), when (Ri) m = 4-CF 3 , R 2 = CH 3 , (R 5 ) „ = 2-Cl, the substituent X 2 is shown in Table 99, which corresponds to 6623-6630 of Table 99, representing the compound number 9516-9523.
表 202: 通式 （1-28) 中， 当 （R n^^CF^ R2=CHF2、 （R5)n =2-Cl时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 9524-9531。 表 203: 通式 (1-28) 中， 当 (Ri)m =2,4-2CL R2=CH3、 (R5)n =2-Cl时， 取代基 X2见表 99, 依次对应表 99的 6623-6630， 代表化合物编号为 9532-9539。 Table 202: In the general formula (1-28), when (R n^^CF^ R 2 =CHF 2 , (R 5 ) n =2-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to Table 99. 6623-6630, the representative compound number is 9524-9531. Table 203: In the general formula (1-28), when (Ri) m = 2, 4-2CL R 2 = CH 3 , (R 5 ) n = 2-Cl, the substituent X 2 is shown in Table 99, which corresponds to 6623-6630 of Table 99, representing the compound number 9532-9539.
表 204: 通式 （1-28) 中， 当 （^;^ =2,4-20、 R2=CHF2、 （R5)n =2-Cl时， 取代基 X2见 表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 9540-9547。 Table 204: In the general formula (1-28), when (^; ^ = 2 , 4-20, R 2 =CHF 2 , (R 5 ) n = 2-Cl, the substituent X 2 is shown in Table 99, in order Corresponding to 6623-6630 of Table 99, the representative compound number is 9540-9547.
当通式 (1-4) 中， R2=CF3， R4=H， x=0时， 结构如通式 (1-29) 所示。 When R 2 = CF 3 and R4 = H, x = 0 in the formula (1-4), the structure is as shown in the formula (1-29).
Figure imgf000034_0001
Figure imgf000034_0001
表 205: 通式 (1-29) 中， 当 （Ri)m =H、 X1=N (R5)n =2-Cl时， 取代基 X2见表 99， 依 次对应表 99的 6623-6630， 代表化合物编号为 9548-9555。 Table 205: In the general formula (1-29), when (Ri) m = H, X 1 = N (R 5 ) n = 2-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623 of Table 99. 6630, the representative compound number is 9548-9555.
表 206: 通式 (1-29) 中， 当 （Ri)m =H、 X1=N (R5)n =2,4-2Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 9556-9563。 Table 206: In the general formula (1-29), when (Ri) m = H, X 1 = N (R 5 ) n = 2 , 4-2Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to Table 99. 6623-6630, the representative compound number is 9556-9563.
表 207: 通式 （1-29) 中，
Figure imgf000034_0002
(R5)n =2,4-2Cl时， 取代基 X2见 表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 9564-9571。 Table 207: In the general formula (1-29),
Figure imgf000034_0002
When (R 5 ) n = 2 , 4-2Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623-6630 of Table 99, and represents the compound number 9564-9571.
表 208: 通式 (1-29) 中， 当 (Ri)m =4-CL Xi=N (R5)n =2-Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 9572-9579。 Table 208: In the general formula (1-29), when (Ri) m = 4-CL Xi=N (R 5 ) n = 2-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to 6623 of Table 99. 6630, the representative compound number is 9572-9579.
表 209: 通式 (1-29) 中， 当 (Ri)m =4-Cl、 Xi=C-C02CH3 (R5)„ =2,4-2Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 9580-9587。 Table 209: In the general formula (1-29), when (Ri) m = 4-Cl, Xi=C-C0 2 CH 3 (R 5 ) „ = 2 , 4-2Cl, the substituent X 2 is shown in Table 99 , which in turn correspond to 6623-6630 of Table 99, representing the compound number 9580-9587.
表 210: 通式 (1-29) 中， 当 (Ri)m =4-CF3 Xi=N、 （R5)n =2-Cl时， 取代基 X2见表 99， 依次对应表 99的 6623-6630， 代表化合物编号为 9588-9595。 Table 210: In the general formula (1-29), when (Ri) m = 4-CF 3 Xi=N, (R 5 ) n = 2-Cl, the substituent X 2 is shown in Table 99, which in turn corresponds to Table 99. 6623-6630, the representative compound number is 9858-9595.
当通式 （1-4) 中， 示。  When the formula (1-4) is shown.
表 211 : 通式 (1-3
Figure imgf000034_0003
R2=CH3时， 取代 基 见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 9596-9619。 Table 211: General formula (1-3
Figure imgf000034_0003
When R 2 =CH 3 , the substituents are shown in Table 71, which in turn correspond to 5951-5974 of Table 71, and represent the compound number 9596-9619.
表 212: 通式 (1-30) 中， ¾(Ri)m =2-N02 (R5)„ =2,3,5-3Cl-4,6-2CN R2=CH3时， 取代 基 X 见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 9620-9643。 Table 212: In the general formula (1-30), 3⁄4(Ri) m = 2-N0 2 (R 5 ) „ = 2,3,5-3Cl-4, 6-2CN R 2 =CH 3 , substituent X is shown in Table 71, which in turn corresponds to 5951-5974 of Table 71, representing the compound number 9620-9643.
表 213: 通式 (1-30) 中， ¾(R m =3-CF3 (R5)„ =2,3,5-3Cl-4,6-2CN R2=CH3时， 取代 基 见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 9644-9667。 Table 213: In the general formula (1-30), when 3⁄4(R m =3-CF 3 (R 5 )„ =2,3,5-3Cl-4,6-2CN R 2 =CH 3 , the substituents are as seen Table 71, which corresponds in turn to 5951-5974 of Table 71, represents the compound number 9644-9667.
表 214: 通式 (1-30) 中， ¾(Ri)m =4-Cl、 (R5)„ =2,6-2Cl-4-N02、 X1=N时， 取代基 R2 见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 9668-9688。 Table 214: In the general formula (1-30), when 3⁄4(Ri) m = 4-Cl, (R 5 ) „ = 2,6-2Cl-4-N0 2 , X 1= N, the substituent R 2 is as seen Table 43, which in turn corresponds to 5363-5383 of Table 43, represents the compound number 9668-9688.
表 215: 通式 （1-30) 中，
Figure imgf000034_0004
Χι=Ν时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 9689-9709。 Table 215: In the general formula (1-30),
Figure imgf000034_0004
When Χι=Ν, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, and represents the compound number 9689-9709.
当通式 (1-4) 中， R2=CF3， R4=H， X1=C-CN, X2=CO， Y=CH2， x=l 时， 结构如通式 (1-31 ) 所示。
Figure imgf000035_0001
When R 2 =CF 3 , R 4 =H, X 1= C-CN, X 2 =CO, Y=CH 2 , x=l in the formula (1-4), the structure is as in the formula (1- 31) shown.
Figure imgf000035_0001
通式 （1-31 ) 中， （R5)n =2-Cl， （R^m见表 216， 依次对应表 216的 9710-9741， 代表化 合物编号为 9710-9741。 表 216 In the formula (1-31), (R 5 ) n = 2-Cl, (R^m is shown in Table 216, which in turn corresponds to 9710-9741 of Table 216, and represents the compound number 9710-9741. Table 216
Figure imgf000035_0003
表 217: 通式 (1-31 ) 中， (R5)„ =2-CN, (R 见表 216， 依次对应表 216的 9710-9741， 代表化合物编号为 9742-9773。
Figure imgf000035_0003
Table 217: In the formula (1-31), (R 5 ) „=2-CN, (R is shown in Table 216, which corresponds to 9710-9741 of Table 216 in turn, and represents the compound number 9472-9773.
表 218: 通式 (1-31 ) 中， (R5)„ =4-Cl, (R^m见表 216， 依次对应表 216的 9710-9741， 代表化合物编号为 9774-9805。 Table 218: In the formula (1-31), (R 5 ) „ = 4-Cl, (R^m is shown in Table 216, which in turn corresponds to 9710-9741 of Table 216, and represents the compound number 9774-9805.
表 219: 通式 (1-31 ) 中， (R5)„ =H, (R^m见表 216， 依次对应表 216的 9710-9741， 代 表化合物编号为 9806-9837。 Table 219: In the formula (1-31), (R 5 ) „ = H, (R^m is shown in Table 216, which in turn corresponds to 9710-9741 of Table 216, and represents the compound number 9806-9837.
表 220：通式（1-31 )中， (R5)„ =4-C(CH3)3，（R^m见表 216，依次对应表 216的 9710-9741 , 代表化合物编号为 9838-9869。 Table 220: In the formula (1-31), (R 5 ) „=4-C(CH 3 ) 3 , (R^m is shown in Table 216, which in turn corresponds to 9710-9741 of Table 216, representing the compound number 9838- 9869.
当通式 （1-4) 中， R4=H， Xi=C-CN, X2=CO， Y=CH2， x=l时， 结构如通式 （1-32) 所 示。 When R 4 =H, Xi=C-CN, X 2 =CO, Y=CH 2 , x=l in the formula (1-4), the structure is as shown in the formula (1-32).
Figure imgf000035_0002
Figure imgf000035_0002
表 221 : 通式 （1-32) 中， 当 （1^:^ =4 1、 （R5)n =2-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 9870-9890。 Table 221: In the formula (1-32), when (1^:^ = 4 1 , (R 5 ) n = 2-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 The representative compound number is 9870-9890.
表 222: 通式 (1-32) 中， 当 (R m =4-CL (R5)n =4-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 9891-9911。 Table 222: In the formula (1-32), when (R m = 4-CL (R 5 ) n = 4-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and represents a compound The number is 9991-9911.
表 223: 通式 （1-32) 中， 当 （1 ^ =4 1、 （R5)n =H时， 取代基 R2见表 43， 依次对应 表 43的 5363-5383， 代表化合物编号为 9912-9932。 Table 223: In the formula (1-32), when (1 ^ = 4 1 , (R 5 ) n = H, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, representing the compound number 9912-9932.
表 224: 通式 (1-32) 中， 当 (R m =4-CL (R5)n =4-C(CH3)3时， 取代基 R2见表 43， 依 次对应表 43的 5363-5383， 代表化合物编号为 9933-9953。 Table 224: In the formula (1-32), when (R m = 4-CL (R 5 ) n = 4-C(CH 3 ) 3 , the substituent R 2 is shown in Table 43 Sub-corresponding to 5363-5383 of Table 43, represents the compound number 9933-9953.
表 225: 通式 （1-32) 中， 当 （R n^^CF^ (R5)n =2-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 9954-9974。 Table 225: In the formula (1-32), when (R n^^CF^(R 5 ) n = 2-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and represents a compound The number is 9954-9974.
表 226: 通式 (1-32) 中， 当 (R m =4-CF3 (R5)n =4-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 9975-9995。 Table 226: In the general formula (1-32), when (R m = 4-CF 3 (R 5 ) n = 4-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, The compound number is 9975-9995.
通式（1-4)中， R2=CF3， R4=H, X1=C-CN, X2=CO， Y=CO x=l时，结构如通式（1-33 ) In the general formula (1-4), R 2 =CF 3 , R4=H, X 1= C-CN, X 2 =CO, Y=CO x=l, the structure is as shown in the formula (1-33)
Figure imgf000036_0001
Figure imgf000036_0001
表 227: 通式 (1-33 ) 中， (R5)„ =2-Cl, (R^m见表 216， 依次对应表 216的 9710-9741， 代表化合物编号为 9996-10027。 Table 227: In the formula (1-33), (R 5 ) „ = 2-Cl, (R^m is shown in Table 216, which in turn corresponds to 9710-9741 of Table 216, and represents the compound number of 9996-10027.
表 228: 通式 (1-33 ) 中， （R5)n =2-CF3， （R^m见表 216， 依次对应表 216的 9710-9741， 代表化合物编号为 10028-10059。 Table 228: In the formula (1-33), (R 5 ) n = 2-CF 3 , (R^m is shown in Table 216, which in turn corresponds to 9710-9741 of Table 216, and represents the compound number 10028-10059.
表 229: 通式 (1-33 ) 中， (R5)„ =4-Cl, (R^m见表 216， 依次对应表 216的 9710-9741， 代表化合物编号为 10060-10091。 Table 229: In the formula (1-33), (R 5 ) „ = 4-Cl, (R^m is shown in Table 216, which in turn corresponds to 9710-9741 of Table 216, and represents the compound number 10060-10091.
表 230: 通式 (1-33 )中， (R5)„ =2,4-2Cl, (R m见表 216， 依次对应表 216的 9710-9741， 代表化合物编号为 10092-10123。 Table 230: In the formula (1-33), (R 5 ) „ = 2, 4-2Cl, (R m is shown in Table 216, which in turn corresponds to 9710-9741 of Table 216, and represents the compound number 10092-10123.
表 231 :通式（1-33 )中，（R5)n =2-Cl-4-CF3，（R 见表 216，依次对应表 216的 9710-9741 , 代表化合物编号为 10124-10155。 Table 231: In the formula (1-33), (R 5 ) n = 2-Cl-4-CF 3 , (R is shown in Table 216, which in turn corresponds to 9710-9741 of Table 216, and represents the compound number 10124-10155.
当通式 （1-4) 中， R4=H， Xi=C-CN, X2=CO， Y=CO， x=l时， 结构如通式 （1-34) 所 When in the formula (1-4), R4=H, Xi=C-CN, X 2 =CO, Y=CO, x=l, the structure is as shown in the formula (1-34)
Figure imgf000036_0002
Figure imgf000036_0002
表 232: 通式 （1-34) 中， 当 （!^;^ =4 1、 （R5)n =2-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 10156-10176。 Table 232: In the general formula (1-34), when (!^; ^ = 4 1 , (R 5 ) n = 2-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 The representative compound number is 10156-10176.
表 233: 通式 (1-34) 中， 当 (Ri)m =4-CL (R5)n =4-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 10177-10197。 Table 233: In the general formula (1-34), when (Ri) m = 4-CL (R 5 ) n = 4-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, The compound number is 10177-10197.
表 234: 通式 (1-34) 中， 当 (R m =4-CL (R5)n =2,4-2Cl时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 10198-10218。 Table 234: In the formula (1-34), when (R m = 4-CL (R 5 ) n = 2 , 4-2Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 The representative compound number is 10198-10218.
表 235: 通式 （1-34) 中， 当 （R n^^CF^ (R5)n =2-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 10219-10239。 Table 235: In the formula (1-34), when (R n^^CF^ (R 5 ) n = 2-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and represents a compound The number is 10219-10239.
表 236: 通式 （1-34) 中， 当 （R n^A-CF^ (R5)n =4-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 10240-10260。 Table 236: In the formula (1-34), when (R n^A-CF^(R 5 ) n = 4-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and represents The compound number is 10240-10260.
表 237: 通式 (1-34) 中， 当 (R m =4-CF3 (R5)n =2,4-2Cl时， 取代基 R2见表 43， 依 次对应表 43的 5363-5383， 代表化合物编号为 10261-10281。 Table 237: In the formula (1-34), when (R m = 4-CF 3 (R 5 ) n = 2 , 4-2Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 , represents the compound number 10261-10281.
当通式 (1-5) 中， R2=CF3， R4=H， X1=C-CN, X2=CO， x=0时， 结构如通式 (1-35)所 示。
Figure imgf000037_0001
In the formula (1-5), R 2 = CF 3 , R 4 = H, X 1 = C-CN, X 2 = CO, and x = 0, the structure is as shown in the formula (1-35).
Figure imgf000037_0001
表 238: 通式 （1-35) 中， 当 (R5)n=2-Cl时， 取代基 (R^m与表 17—致， 依次对应表 17 的 1-261， 代表化合物编号为 10282-10542。 Table 238: In the formula (1-35), when (R 5 ) n = 2-Cl, the substituent (R^m is the same as Table 17 and corresponds to 1-261 of Table 17, which represents the compound number 10282). -10542.
表 239: 通式 （1-35) 中， 当 (R5)n=5-Cl时， 取代基 (R 与表 17—致， 依次对应表 17 的 1-261， 代表化合物编号为 10543-10803。 Table 239: In the formula (1-35), when (R 5 ) n = 5-Cl, the substituent (R and Table 17 correspond to 1-261 in Table 17, which represents the compound number 10543-10803 .
表 240: 通式 （1-35) 中， 当 (R5)n=5-CN时， 取代基 (R 与表 17—致， 依次对应表 17 的 1-261， 代表化合物编号为 10804-11064。 Table 240: In the general formula (1-35), when (R 5 ) n = 5-CN, the substituent (R corresponds to Table 17 and corresponds to 1-261 of Table 17 in sequence, representing the compound number 10804-11064 .
表 241: 通式 （1-35) 中， 当 (R5)n=2-CF3时， 取代基 (R^m与表 17—致， 依次对应表 17 的 1-261， 代表化合物编号为 11065-11325。 Table 241: In the formula (1-35), when (R 5 ) n = 2-CF 3 , the substituent (R^m is the same as Table 17 and corresponds to 1-261 of Table 17 in turn, representing the compound number as 11065-11325.
通式（1-35)中，当 （Ri)m=H时，取代基 (R5)n见表 242，依次对应表 242的 11326-11377， 代表化合物编号为 11326-11377。 In the formula (1-35), when (Ri) m = H, the substituent (R 5 ) n is shown in Table 242, which in turn corresponds to 11326-11377 of Table 242, and represents the compound number 11326-11377.
表 242 Table 242
Figure imgf000037_0002
Figure imgf000037_0002
注： " "表示无取代基  Note: " " means no substituent
表 243: 通式 （1-35) 中， 当 （R^m =4-Cl时， 取代基 (R5)n见表 242， 依次对应表 242 的 11326-11377, 代表化合物编号为 11378-11429。 Table 243: In the formula (1-35), when (R^m = 4-Cl, the substituent (R 5 ) n is shown in Table 242, which in turn corresponds to 11326-11377 of Table 242, representing the compound number 11378-11429 .
表 244: 通式 (1-35) 中， 当 （R^m =4-CF3时， 取代基 (R5)n见表 242， 依次对应表 242 的 11326-11377, 代表化合物编号为 11430-11481。 Table 244: In the formula (1-35), when (R^m = 4-CF 3 , the substituent (R 5 ) n is shown in Table 242, which in turn corresponds to 11326-11377 of Table 242, representing the compound number 11430- 11481.
当通式 (1-5) 中， =Η， Xi=C-CN, X2=CO， x=0时， 结构如通式 (1-36) 所示。
Figure imgf000038_0001
When in the formula (1-5), =Η, Xi=C-CN, X 2 =CO, x=0, the structure is as shown in the formula (1-36).
Figure imgf000038_0001
表 245: 通式 （1-36) 中， 当 （R^m =4-Cl、 （R5)n=2-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 11482-11502。 Table 245: In the formula (1-36), when (R^m = 4-Cl, (R 5 ) n = 2-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 The representative compound number is 11482-11502.
表 246: 通式 （1-36) 中，
Figure imgf000038_0002
(R5)n=5-Cl时， 取代基 R2见表 43， 依次对应 表 43的 5363-5383， 代表化合物编号为 11503-11523。 Table 246: In the general formula (1-36),
Figure imgf000038_0002
When (R 5 ) n = 5-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, and represents the compound number 11503-11523.
表 247: 通式 （1-36) 中， 当 （R n^A-CF^ (R5)n=2-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 11524-11544。 Table 247: In the general formula (1-36), when (R n^A-CF^(R 5 ) n = 2-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and represents The compound number is 11524-11544.
表 248: 通式 （1-36) 中，
Figure imgf000038_0003
=4-CF3、 （R5)n=5-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 11545-11565。 Table 248: In the general formula (1-36),
Figure imgf000038_0003
When 4-CF 3 and (R 5 ) n = 5-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, and represents the compound number 11545-11565.
当通式 (1-6) 中， R2=CF3， R4=H, X1=C-CN, X2=CO， x=0时， 结构如通式 (1-37)所 In the general formula (1-6), R 2 =CF 3 , R4=H, X 1= C-CN, X 2 =CO, x=0, the structure is as shown in the formula (1-37)
Figure imgf000038_0004
Figure imgf000038_0004
表 249: 通式 （1-37) 中， 当 （R5)n=4-Cl时， 取代基 (R^m与表 17—致， 依次对应表 17 的 1-261， 代表化合物编号为 11566-11826。 Table 249: In the general formula (1-37), when (R 5 ) n = 4-Cl, the substituent (R^m is the same as Table 17 and corresponds to 1-261 of Table 17, which represents the compound number 11566). -11826.
表 250: 通式 （1-37) 中， 当 （R5)n=4,6-2C1时， 取代基 (R^m与表 17—致， 依次对应表 17的 1-261， 代表化合物编号为 11827-12087。 Table 250: In the general formula (1-37), when (R 5 ) n = 4, 6-2C1, the substituent (R^m is the same as Table 17 and corresponds to 1-261 of Table 17 in turn, representing the compound number It is 11827-12087.
通式（1-37)中，当 （R m H时，取代基 (R5)n见表 251，代表化合物编号为 12088-12103， 依次对应表 251的 12088-12103。 In the formula (1-37), when (R m H, the substituent (R 5 ) n is shown in Table 251, and the representative compound number is 12088-12103, which in turn corresponds to 12088-12103 of Table 251.
表 251  Table 251
Figure imgf000038_0005
Figure imgf000038_0005
注： " "表示无取代基  Note: " " means no substituent
表 252: 通式 （1-37) 中， 当 （R^m =4-Cl时， 取代基 (R5)n见表 251， 依次对应表 251 的 12088-12103， 代表化合物编号为 12104-12119。 Table 252: In the general formula (1-37), when (R^m = 4-Cl, the substituent (R 5 ) n is shown in Table 251, which in turn corresponds to 12088-12103 of Table 251, representing the compound number 12104-12119 .
表 253: 通式 （1-37) 中， 当 （R^m =4-CF3时， 取代基 (R5)n见表 251， 依次对应表 251 的 12088-12103， 代表化合物编号为 12120-12135。 Table 253: In the general formula (1-37), when (R^m = 4-CF 3 , the substituent (R 5 ) n is shown in Table 251, which in turn corresponds to 12088-12103 of Table 251, and represents the compound number 12120- 12135.
当通式 (1-6) 中， =Η， Xi=C-CN, X2=CO， x=0时， 结构如通式 (1-38 ) 所示。
Figure imgf000039_0001
When in the formula (1-6), =Η, Xi=C-CN, X 2 =CO, x=0, the structure is as shown in the formula (1-38).
Figure imgf000039_0001
表 254: 通式 (1-38) 中， 当 (Ri)m =4-CL (R5)n=4-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 12136-12156。 Table 254: In the general formula (1-38), when (Ri) m = 4-CL (R 5 ) n = 4-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, The compound number is 12136-12156.
表 255: 通式 (1-38) 中， 当 (Ri)m =4-CF3 (R5)n=4-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 12157-12177。 Table 255: In the general formula (1-38), when (Ri) m = 4-CF 3 (R 5 ) n = 4-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 The representative compound number is 12157-12177.
当通式 (1-11-1 ) 中， R2=CF3， R4=H, X1=C-CN, X2=CO， x=0时， 结构如通式 (1-39) 所示。 When the formula (1-11-1), R 2 =CF 3 , R4=H, X 1= C-CN, X 2 =CO, x=0, the structure is as shown in the formula (1-39) .
Figure imgf000039_0002
Figure imgf000039_0002
表 256: 通式 （1-39) 中， 当 （R5)n=4-Cl时， 取代基 (Ri)m与表 17 ¾ 依次对应表 17 的 1-261， 代表化合物编号为 12178-12438。 Table 256: In the general formula (1-39), when (R 5 ) n = 4-Cl, the substituent (Ri) m and Table 17 3⁄4 sequentially correspond to 1-261 of Table 17, representing the compound number 12178-12438 .
表 257: 通式 （1-39) 中， 当 （R5)n=4-C02CH3时， 取代基 (Ri)m与表 17
Figure imgf000039_0003
Table 257: In the formula (1-39), when (R 5 ) n = 4-C0 2 CH 3 , the substituent (Ri) m and Table 17
Figure imgf000039_0003
表 17的 1-261， 代表化合物编号为 12439-12699。 1-261 of Table 17, representing the compound number 12439-12699.
通式（1-39)中，当 （R m H时，取代基 (R5)n见表 258，代表化合物编号为 12700-1270 表 258 In the formula (1-39), when (R m H, the substituent (R 5 ) n is shown in Table 258, and the representative compound number is 12700-1270. Table 258
Figure imgf000039_0005
Figure imgf000039_0005
注： " '表示无取代基  Note: " ' indicates no substituent
表 259： 通式 (1-39) 中， 当 （R^m =4-Cl 取代基 (R5)n见表 258， 依次对应表 258 的 12700-12708， 代表化合物编号为 12709-12717。 Table 259: In the formula (1-39), when (R^m = 4-Cl substituent (R 5 ) n is shown in Table 258, which corresponds to 12700-12708 of Table 258 in turn, represents the compound number 12709-12717.
表 260: 通式 (1-39) 中， 当 (Ri)m =4-CF3时， 取代基 (R5)n见表 258， 依次对应表 258 的 12700-12708， 代表化合物编号为 12718-12726。 Table 260: In the general formula (1-39), when (Ri) m = 4-CF 3 , the substituent (R 5 ) n is shown in Table 258, which in turn corresponds to 12700-12708 of Table 258, representing the compound number 12718- 12726.
当通式 (1-11-1 ) 中， R4=H， Xi=C-CN, X2=CO， x=0时， 结构如通式 （1-40) 所示。 When R 4 =H, Xi=C-CN, X 2 =CO, x=0 in the formula (1-11-1), the structure is as shown in the formula (1-40).
表 261 : 通式 (1-4 Table 261 : General formula (1-4
应表 43的 5363-5383， Should be 5363-5383 of Table 43,
表 262: 通式 (1-4
Figure imgf000039_0004
Table 262: General formula (1-4
Figure imgf000039_0004
应表 43的 5363-5383， 代表化合物编号为 12748-12768。 当通式 (1-12) 中， R2=CF3， R4=H， X1=C-CN, X2=CO， Y=CH2， x=l时， 结构如通式 (1-41) 所示。 According to 5363-5383 of Table 43, the compound number is 12748-12768. When R 2 =CF 3 , R 4 =H, X 1= C-CN, X 2 =CO, Y=CH 2 , x=l in the formula (1-12), the structure is as in the formula (1- 41) As shown.
Figure imgf000040_0001
Figure imgf000040_0001
表 263: 通式 （1-41) 中， 当 (R5)n=2-Cl时， 取代基 (R^m与表 17—致， 依次对应表 17 的 1-261， 代表化合物编号为 12769-13029。 Table 263: In the general formula (1-41), when (R 5 ) n = 2-Cl, the substituent (R^m is the same as Table 17 and corresponds to 1-261 of Table 17, which represents the compound number 12769). -13029.
表 264: 通式 （1-41) 中， 当 (R5)n =2,4-2Cl时， 取代基 (R 与表 17—致， 依次对应表 17的 1-261， 代表化合物编号为 13030-13290。 Table 264: In the general formula (1-41), when (R 5 ) n = 2, 4-2Cl, the substituent (R corresponds to Table 17 and corresponds to 1-261 of Table 17 in turn, representing the compound number 13030 -13290.
通式 (1-41)中， 当 (R^H时，取代基 (R5)n见表 265，依次对应表 265的 13291-13308, 代表化合物编号为 13291-13308。 In the formula (1-41), when (R^H, the substituent (R 5 ) n is shown in Table 265, which in turn corresponds to 13291-13308 of Table 265, and represents the compound number 13291-13308.
表 265  Table 265
Figure imgf000040_0003
Figure imgf000040_0003
注： " "表示无取代基  Note: " " means no substituent
表 266： 通式 (1-41) 中， 当 (R m =4-Cl时， 取代基 (R5)n见表 265， 依次对应表 265 的 13291-13308, 代表化合物编号为 13309-13326。 Table 266: In the formula (1-41), when (R m = 4-Cl, the substituent (R 5 ) n is shown in Table 265, which in turn corresponds to 13291-13308 of Table 265, and represents the compound number 13309-13326.
表 267: 通式 （1-41) 中， 当 （R^m =4-CF3时 取代基 (R5)n见表 265， 依次对应表 265 的 13291-13308， 代表化合物编号为 13327-13344。 Table 267: In the formula (1-41), when (R^m = 4-CF 3 , the substituent (R 5 ) n is shown in Table 265, which in turn corresponds to 13291-13308 of Table 265, representing the compound number 13327-13344 .
当通式 (1-12) 中， R4=H, X1=C-CN, X2=CO Y=CH2， x=l 时， 结构如通式 (1-42) 所示。 When R4 = H, X 1 = C-CN, X 2 = CO Y = CH 2 , x = 1, in the formula (1-12), the structure is as shown in the formula (1-42).
Figure imgf000040_0002
Figure imgf000040_0002
表 268: 通式 (1-42) 中， 当 （Ri)m=H、 （R5)n=2-Cl时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 13345-13365。 Table 268: In the formula (1-42), when (Ri) m = H, (R 5 ) n = 2-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and represents a compound The number is 13345-13365.
表 269: 通式 (1-42) 中， 当 (Ri)m =4-CL (R5)n=2-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 13366-13386。 Table 269: In the formula (1-42), when (Ri) m = 4-CL (R 5 ) n = 2-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, The compound number is 13366-13386.
表 270: 通式 (1-42) 中， 当 (Ri)m =4-CF3 (R5)n=2-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 13387-13407。 Table 270: In the formula (1-42), when (Ri) m = 4-CF 3 (R 5 ) n = 2-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 The representative compound number is 13387-13407.
表 271: 通式 (1-18) 中， 当 (R m =3-CF3、 （R5)n =3-Cl-5-CF3时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 13408-13428。 Table 271: In the general formula (1-18), when (R m = 3-CF 3 , (R 5 ) n = 3-Cl-5-CF 3 , the substituent R 2 is shown in Table 43, and corresponds to Table 43 in order. 5363-5383, representing the compound number 13408-13428.
表 272: 通式 (1-18) 中， ¾(Ri)m =2-F-4-CL (R5)n =3-Cl-5-CF3时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 13429-13449。 Table 272: In the formula (1-18), when 3⁄4(Ri) m = 2-F-4-CL (R 5 ) n = 3-Cl-5-CF 3 , the substituent R 2 is shown in Table 43, Corresponding to 5363-5383 of Table 43, the compound number is 13429-13449.
表 273: 通式 (1-18) 中， ¾(Ri)m =2-F-4-CK (R5)n =3-Cl-5-Cl时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 13450-13470。 Table 273: In the formula (1-18), when 3⁄4(Ri) m = 2-F-4-CK (R 5 ) n = 3-Cl-5-Cl, the substituent R 2 is shown in Table 43, Corresponding to 5363-5383 of Table 43, the representative compound number is 13450-13470.
表 274: 通式 (1-18) 中， ¾(Ri)m =2,4-2CL (R5)n =3-CF3时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 13471-13491。 Table 274: In the general formula (1-18), when 3⁄4(Ri) m = 2, 4-2CL (R 5 ) n = 3-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363 of Table 43 5383, representing compound number 13471-13491.
表 275: 通式 （1-18) 中，
Figure imgf000041_0001
(R5)n =4-CN时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 13492-13512。 Table 275: In the general formula (1-18),
Figure imgf000041_0001
When (R 5 ) n = 4-CN, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, and represents the compound number 13492-13512.
表 276: 通式 (1-18) 中， ¾(Ri)m =2-F-4-CL (R5)n =3-Cl时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 13513-13533。 Table 276: In the general formula (1-18), when 3⁄4(Ri) m = 2-F-4-CL (R 5 ) n = 3-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363 of Table 43 -5383, the representative compound number is 13513-13533.
表 277: 通式 (1-18) 中， ¾(Ri)m =2-F-4-CL (R5)n =3-CF3时， 取代基 R2见表 43， 依 次对应表 43的 5363-5383， 代表化合物编号为 13534-13554。 Table 277: In the general formula (1-18), when 3⁄4(Ri) m = 2-F-4-CL (R 5 ) n = 3-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to Table 43 5363-5383, the representative compound number is 13534-13554.
表 278: 通式 (1-18) 中， ¾(Ri)m =2-F-4-CL (R5)n =3-CN时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 13555-13575。 Table 278: In the general formula (1-18), when 3⁄4(Ri) m = 2-F-4-CL (R 5 ) n = 3-CN, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363 of Table 43 -5383, represents the compound number 13555-13575.
表 279: 通式 (1-18) 中， ¾(Ri)m =2,4-2CL (R5)n =4-CN时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 13576-13596。 Table 279: In the general formula (1-18), when 3⁄4(Ri) m = 2, 4-2CL (R 5 ) n = 4-CN, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 , represents the compound number 13576-13596.
表 280: 通式 (1-18) 中， ¾(Ri)m =2-CF3 (R5)n =3-Cl时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 13597-13617。 Table 280: In the formula (1-18), when 3⁄4(Ri) m = 2-CF 3 (R 5 ) n = 3-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 The representative compound number is 13597-13617.
表 281 : 通式 （1-18) 中，
Figure imgf000041_0002
(R5)n =4-CF3时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化合物编号为 13618-13638。 Table 281: In the general formula (1-18),
Figure imgf000041_0002
When (R 5 ) n = 4-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, and represents the compound number 13618-13638.
表 282: 通式 (1-18) 中， ¾(R m =3-CF3 (R5)n =3,5-2Cl时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 13639-13659。 Table 282: In the general formula (1-18), when 3⁄4 (R m = 3-CF 3 (R 5 ) n = 3, 5-2Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 , represents the compound number 13639-13659.
表 283: 通式 (1-18) 中， ¾(R m =3-CF3 (R5)n =3,5-2Cl时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 13660-13680。 Table 283: In the general formula (1-18), when 3⁄4 (R m = 3-CF 3 (R 5 ) n = 3, 5-2Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 , represents the compound number 13660-13680.
表 284: 通式 (1-18) 中， ¾(R m =4-CN (R5)n =3,5-2Cl时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 13681-13701。 Table 284: In the general formula (1-18), when 3⁄4 (R m = 4-CN (R 5 ) n = 3, 5-2Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 The representative compound number is 13681-13701.
表 285: 通式 (1-18) 中， ¾(R m =4-CN (R5)n =3-Cl-5-CF3时， 取代基 R2见表 43， 依 次对应表 43的 5363-5383， 代表化合物编号为 13702-13722。 Table 285: In the formula (1-18), when 3⁄4 (R m = 4-CN (R 5 ) n = 3-Cl-5-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363 of Table 43 -5383, represents the compound number 13702-13722.
表 286: 通式 （1-18) 中， (R5)n =3-CN时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代表化 3-13753。 Table 286: In the formula (1-18), when (R 5 ) n = 3-CN, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and represents 3-13753.
表 287: 通式 （1-18) 中，
Figure imgf000041_0003
(R5)n =3-CF3时， 取代基 R2见表 43， 依次对 应表 43的 5363-5383， 代 Table 287: In the general formula (1-18),
Figure imgf000041_0003
When (R 5 ) n = 3-CF 3 , the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43
Figure imgf000041_0004
Figure imgf000041_0004
表 288: 通式 1-43中， 当 （R m =H、 （R5)n =4-Cl时， 取代基 R2见表 43， 依次对应表 43的 5363-5383， 代表化合物编号为 13775-13795。 Table 288: In the formula 1-43, when (R m = H, (R 5 ) n = 4-Cl, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43, representing the compound number 13775 -13795.
表 289: 通式 1-23中， 当 （Ri)m =H、 （R5)n =3-Cl时， R2=CH3时， 取代基 X 见表 71， 依次对应表 71的 5951-5974， 代表化合物编号为 13796-13819。 Table 289: In Formula 1-23, when (Ri) m = H, (R 5 ) n = 3-Cl, when R 2 = CH 3 , the substituent X is shown in Table 71, which in turn corresponds to 5951 of Table 71. 5974, representing compound number 13796-13819.
表 290: 通式 1-18中， ¾(Ri)m =2-CF3 (R5)n =4-CN时， 取代基 R2见表 43， 依次对应 表 43的 5363-5383， 代表化合物编号为 13820-13840。 Table 290: In the formula 1-18, when 3⁄4(Ri) m = 2-CF 3 (R 5 ) n = 4-CN, the substituent R 2 is shown in Table 43, which in turn corresponds to 5363-5383 of Table 43 and represents a compound The number is 13820-13840.
表 291 : 通式 1-35中， 当 (R5)n =2,6-2Cl时， 取代基 (R^m与表 17—致， 依次对应表 17 的 1-261， 代表化合物编号为 13862-14122。 Table 291: In the formula 1-35, when (R 5 ) n = 2, 6-2Cl, the substituent (R^m and Table 17 are the same, which in turn correspond to 1-261 of Table 17, representing the compound number 13862 -14122.
表 292: 通式 1-18中，
Figure imgf000041_0005
=2-F-4-Cl、 （R5)n =3,5-2Cl时， 取代基 R2见表 43， 依次 对应表 43的 5363-5383， 代表化合物编号为 14122-14142: 本发明通式 (I)化合物可用如下方法制备， 除另有说明的外， 各基团的定义同前。 Table 292: In Formula 1-18,
Figure imgf000041_0005
=2-F-4-Cl, (R 5 ) n =3,5-2Cl, the substituent R 2 is shown in Table 43, in turn Corresponding to 5363-5383 of Table 43, the compound number is 14122-14142: The compound of the formula (I) of the present invention can be produced by the following method, and each group has the same meaning as defined above unless otherwise stated.
通式 (I)化合物可以由通式 (II)与通式 (III)在适宜的溶剂以及碱性条件下反应制得。  The compound of the formula (I) can be obtained by reacting the formula (II) with the formula (III) in a suitable solvent under basic conditions.
Figure imgf000042_0001
Figure imgf000042_0001
L是离去基团， 选自卤素、 甲磺酰基或对甲苯磺酰基。  L is a leaving group selected from halogen, methanesulfonyl or p-toluenesulfonyl.
反应在适宜的溶剂中进行， 适宜 乙腈、 甲苯、 二甲苯、 苯、 Ν,Ν-二甲基甲酰胺、 二氯甲垸、 三氯甲垸或丙酮等。  The reaction is carried out in a suitable solvent, and is suitably acetonitrile, toluene, xylene, benzene, hydrazine, hydrazine-dimethylformamide, methylene chloride, trichloromethane or acetone.
适宜的碱可选自如氢氧化钾、氢氧化钠、碳酸钠、碳酸钾、碳酸氢钠、三乙胺或吡啶等。 反应温度可在室温至溶剂沸点温度之间， 通常为 20~130°C。  Suitable bases may be selected from, for example, potassium hydroxide, sodium hydroxide, sodium carbonate, potassium carbonate, sodium hydrogencarbonate, triethylamine or pyridine. The reaction temperature may range from room temperature to the boiling point of the solvent, usually from 20 to 130 °C.
反应时间为 30分钟至 20小时， 通常 1~10小时。  The reaction time is from 30 minutes to 20 hours, usually from 1 to 10 hours.
通式 (II)可由通式 (IV)所代表的化合物和 (V)N-Boc-哌嗪 (市售)反应得到化合物（11-1 )， 化 合物 （II-1 ) 再经脱 Boc得到。 其中通式 (IV)部分有市售或者按照已知方法制备。  The compound of the formula (II) can be obtained by reacting a compound represented by the formula (IV) with (V) N-Boc-piperazine (commercially available) to obtain a compound (11-1), which is obtained by de Boc. Wherein the formula (IV) is commercially available or prepared according to known methods.
通式 (II)具体制备方法参见文献 CN 102656163; CN 101128455; Tetrahedron Letters, 52(45), 5905-5909; Zhongguo Yaowu Huaxue Zazhi, 13(3), 142-145; Bioorganic & Medicinal Chemistry Letters, 22(17), 5545-5549; WO 2010118367; Bioorganic & Medicinal Chemistry Letters, 19(17), 5214-5217; European Journal of Medicinal Chemistry, 46(4), 1404-1414; CN 102481300。  For the specific preparation method of the general formula (II), see the literature CN 102656163; CN 101128455; Tetrahedron Letters, 52(45), 5905-5909; Zhongguo Yaowu Huaxue Zazhi, 13(3), 142-145; Bioorganic & Medicinal Chemistry Letters, 22( 17), 5545-5549; WO 2010118367; Bioorganic & Medicinal Chemistry Letters, 19(17), 5214-5217; European Journal of Medicinal Chemistry, 46(4), 1404-1414; CN 102481300.
Figure imgf000042_0002
Figure imgf000042_0002
根据 X2定义不同， 本发明较为优选的中间体 (III) (通式 (ΙΠ))， 即当 Χ2选自 CO或 CH2; 当 X2=CO中间体 III-1和 X2= CH2中间体 ΠΙ-2的制备方法主要有如下两种： According to the definition of X 2 , the intermediate (III) (formula) of the invention is preferred, that is, when Χ 2 is selected from CO or CH 2 ; when X 2 = CO intermediates III-1 and X 2 = CH 2 The preparation method of the intermediate ΠΙ-2 mainly has the following two types:
方法一：  method one:
可由通式 (VI) 与通式 (VII)在碱性条件下反应制得， 具体制备方法参见文献 Journal of Heterocyclic Chemistry, 27(2), 295-305; CN 101538246； CN 101538246。 It can be obtained by reacting the general formula (VI) with the general formula (VII) under basic conditions. For the specific preparation method, see Journal of Heterocyclic Chemistry, 27(2), 295-305; CN 101538246; CN 101538246.
Figure imgf000043_0001
Figure imgf000043_0001
III-b III-c  III-b III-c
Figure imgf000043_0002
Figure imgf000043_0002
III-l (X2=CO) III-2 (X2= CH2) III-l (X 2 =CO) III-2 (X 2 = CH 2 )
方法二：  Method Two:
可由通式 (VI) 与通式 (VIII)反应制得， 具体制备方法参见文献 Archives of Pharmacal Research, 35(9), 1543-1552; Tetrahedron, 63(52), 13024-13031; Journal of Heterocyclic Chemistry, 45(4), 1099-1102; Journal of Medicinal Chemistry, 53(14), 5129-5143; Russian Journal of Organic Chemistry, 41(9), 1367-1373; Journal of Chemical Research, (7), 440-445; CN 101511815。  It can be prepared by reacting the general formula (VI) with the general formula (VIII). For the specific preparation method, see Archives of Pharmacal Research, 35(9), 1543-1552; Tetrahedron, 63(52), 13024-13031; Journal of Heterocyclic Chemistry , 45(4), 1099-1102; Journal of Medicinal Chemistry, 53(14), 5129-5143; Russian Journal of Organic Chemistry, 41(9), 1367-1373; Journal of Chemical Research, (7), 440- 445; CN 101511815.
Figure imgf000043_0003
Figure imgf000043_0003
当 X2选自除 CO或 CH2以外的基团时， 中间体 III的具体制备方法参见文献 Journal of Heterocyclic Chemistry, 2006:43(2), 405-416; Bioorganic & Medicinal Chemistry, 2012:20(7), 2427-2434; WO2007026916; US 20050096336; WO 2009144473。 When X 2 is selected from a group other than CO or CH 2 , the specific preparation method of Intermediate III can be found in the literature Journal of Heterocyclic Chemistry, 2006: 43(2), 405-416; Bioorganic & Medicinal Chemistry, 2012: 20 ( 7), 2427-2434; WO2007026916; US 20050096336; WO 2009144473.
通式 （I) 化合物对农业、 民用和动物技术领域中有害的虫、 螨显示出高活性。 因此， 本发明的另一技术方案涉及通式 （I) 化合物在农业和其他领域中作为杀虫杀螨剂的用途一 ——将通式 （I) 化合物用于制备杀虫杀螨剂药物的用途。 尤其是， 通式 （I) 化合物对下列 科的重要品种有活性： 小菜蛾、 粘虫、 桃蚜、 叶螨科 (二斑叶螨、 朱砂叶螨、 苹果全爪螨、 柑橘全爪螨等)， 瘿螨科， 跗线螨科等。  The compounds of the general formula (I) exhibit high activity against harmful insects and mites in the fields of agriculture, civil and animal technology. Therefore, another technical solution of the present invention relates to the use of a compound of the general formula (I) as an insecticidal and acaricidal agent in agriculture and other fields - the use of the compound of the general formula (I) for the preparation of an insecticide and acaricide use. In particular, the compounds of the general formula (I) are active against important species of the following families: Plutella xylostella, Mythimna, Myzus persicae, Aphis citrifolia, T. cinnabarinus, T. cinnabarinus, C. citrifolia, Citrus grandiflora, etc.瘿螨科, 跗线螨科, etc.
同时， 通式 （I) 化合物对许多有益的昆虫和螨虫、 哺乳动物、 鱼、 鸟具有低毒性， 而 且没有植物毒性。  At the same time, the compounds of formula (I) are less toxic to many beneficial insects and aphids, mammals, fish, birds, and are not phytotoxic.
由于其积极的特性， 上述化合物可有利地用于保护农业和园艺业重要的作物、家畜和种 畜， 以及人类常去的环境免于有害虫、 螨的伤害。  Due to their positive properties, the above compounds are advantageously used to protect crops, livestock and stocks important in agriculture and horticulture, as well as the environment in which humans are often exposed to pests and mites.
为获得理想效果， 化合物的用量因各种因素而改变， 例如所用化合物、 预保护的作物、 有害生物的类型、 感染程度、 气候条件、 施药方法、 采用的剂型。  To achieve the desired effect, the amount of the compound varies depending on various factors such as the compound used, the pre-protected crop, the type of the pest, the degree of infection, the climatic conditions, the method of application, and the dosage form employed.
每公顷 10克一 5公斤的化合物剂量能提供充分的防治。  A dose of 10 grams to 5 kilograms of compound per hectare provides adequate control.
为了实际应用于农业， 使用含一种或多种通式 （I) 化合物的组合物通常是有益的。 因此， 本发明的另外一种技术方案还包括一种杀虫杀螨组合物， 含有作为活性组分的通 式 （I) 化合物和农业上可接受的载体， 组合物中活性组分的重量百分含量为 0.5-90%。  For practical application in agriculture, it is generally advantageous to use a composition comprising one or more compounds of formula (I). Therefore, another technical solution of the present invention further comprises an insecticidal and acaricidal composition comprising as an active ingredient a compound of the formula (I) and an agriculturally acceptable carrier, the weight of the active ingredient in the composition The content of the fraction is 0.5-90%.
组合物的使用形式可以是干粉、 可湿性粉剂、 乳油、 微乳剂、 糊剂、 颗粒剂、 溶液、 悬 浮剂等： 组合物类型的选择取决于具体的应用。  The composition may be used in the form of a dry powder, a wettable powder, an emulsifiable concentrate, a microemulsion, a paste, a granule, a solution, a suspending agent, etc.: The choice of the type of composition depends on the particular application.
组合物是以已知方式制备的， 例如任选在表面活性剂的存在下， 通过用溶剂介质和 /或 固体稀释剂稀释或溶解活性物质。  The composition is prepared in a known manner, for example by diluting or dissolving the active substance with a solvent medium and/or a solid diluent, optionally in the presence of a surfactant.
可用的固体稀释剂或载体是例如： 二氧化硅、 高岭土、膨润土、滑石、硅藻土、 白云石、 碳酸钙、 氧化镁、 白垩、 粘土、 合成硅酸盐、 硅镁土、 海泡石。  Useful solid diluents or carriers are, for example, silica, kaolin, bentonite, talc, diatomaceous earth, dolomite, calcium carbonate, magnesium oxide, chalk, clay, synthetic silicate, attapulgite, sepiolite.
除水以外，可用的液体稀释剂是例如芳族有机溶剂 (二甲苯或垸基苯的混合物、氯苯等)， 石蜡 (石油熘分)， 醇类 (甲醇、 丙醇、 丁醇、 辛醇、 甘油)， 酯类 (乙酸乙酯、 乙酸异丁酯等)， 酮类 (环己酮、 丙酮、 苯乙酮、 异佛尔酮、 乙基戊基酮等)， 酰胺类 (Ν,Ν-二甲基甲酰胺、 Ν- 甲基吡咯垸酮等)。  In addition to water, useful liquid diluents are, for example, aromatic organic solvents (mixtures of xylene or mercaptobenzene, chlorobenzene, etc.), paraffin (petroleum), alcohols (methanol, propanol, butanol, octanol) , glycerol), esters (ethyl acetate, isobutyl acetate, etc.), ketones (cyclohexanone, acetone, acetophenone, isophorone, ethyl amyl ketone, etc.), amides (Ν, Ν - dimethylformamide, hydrazine-methylpyrrolidone, etc.).
可用的表面活性剂是垸基磺酸盐、 垸基芳基磺酸盐、 聚氧乙烯垸基酚、 山梨醇的聚氧乙 烯酯、 木质素磺酸盐等的钠、 钙、 三乙基胺或三乙醇胺盐。  Useful surfactants are sodium, calcium, triethylamine, such as mercaptosulfonate, mercaptoarylsulfonate, polyoxyethylene nonylphenol, polyoxyethylene ester of sorbitol, lignosulfonate, and the like. Or triethanolamine salt.
组合物还可含特殊的添加剂用于特定的目的， 例如粘合剂如***胶、 聚乙烯醇、 聚乙 烯吡咯垸酮等。  The composition may also contain special additives for specific purposes such as binders such as gum arabic, polyvinyl alcohol, polyvinylpyrrolidone and the like.
上述组合物中活性成分的浓度可根据活性成分、其使用目的、环境条件和采用的制剂类 型而在宽范围内改变。 通常， 活性成分的浓度范围是 1-90%， 优选 5-50%。  The concentration of the active ingredient in the above composition may vary widely depending on the active ingredient, its intended use, environmental conditions, and the type of preparation employed. Generally, the concentration of the active ingredient ranges from 1 to 90%, preferably from 5 to 50%.
如果需要， 可以向组合物中添加能与通式 （I) 化合物兼容的其他活性成分， 例如其他 杀螨剂 /杀虫剂、 杀真菌剂、 植物生长调节剂、 抗生素、 除草剂、 肥料。  If desired, other active ingredients compatible with the compounds of formula (I) may be added to the compositions, such as other acaricides/insecticides, fungicides, plant growth regulators, antibiotics, herbicides, fertilizers.
几种剂型的配制方法举例如下：  Examples of preparation methods for several dosage forms are as follows:
悬浮剂的配制： 常用配方中活性组分含量为 5%-35%。 以水为介质， 将原药、 分散剂、 助悬剂和抗冻剂等加入砂磨机中， 进行研磨， 制成悬浮剂。  Preparation of suspending agent: The active ingredient content in the commonly used formula is 5%-35%. The water, the main drug, the dispersing agent, the suspending agent and the antifreezing agent are added to a sand mill and ground to prepare a suspension.
水乳剂的配制： 将原药、 溶剂和乳化剂加在一起， 使溶解成均匀油相。 将水、 抗冻剂等 混合一起， 成为均一水相。 在高速搅拌下， 将水相加入到油相或将油相加入到水相， 形成分 散性良好的水乳剂。 本发明的水乳剂活性组分含量一般为 5%-15%。 为制备浓乳剂， 本发明 的化合物可溶解于一种或数种混合溶剂， 再加入乳化剂来增强化合物在水中的分散效果。  Preparation of water emulsion: The original drug, solvent and emulsifier are added together to dissolve into a uniform oil phase. Water, antifreeze, and the like are mixed together to form a uniform aqueous phase. The aqueous phase is added to the oil phase or the oil phase is added to the aqueous phase under high-speed agitation to form a water-dispersible water emulsion. The aqueous emulsion active ingredient of the present invention is generally present in an amount of from 5% to 15%. To prepare a concentrated emulsion, the compound of the present invention can be dissolved in one or several mixed solvents, and an emulsifier is added to enhance the dispersion of the compound in water.
可湿性粉剂的配制： 按配方要求， 将原药、 各种表面活性剂及固体稀释剂等充分混合， 经超细粉碎机粉碎后， 即得到预定含量 (例如 10%-40%)的可湿性粉剂产品。 为制备适于喷洒 用的可湿性粉剂， 本发明的化合物可以和研细的固体粉末如粘土、 无机硅酸盐、碳酸盐以及 润湿剂、 粘合剂和 /或分散剂组成混合物。 Preparation of wettable powder: According to the formulation requirements, the original drug, various surfactants and solid diluents are thoroughly mixed and pulverized by an ultrafine pulverizer to obtain a wettable property of a predetermined content (for example, 10% to 40%). Powder products. To prepare a wettable powder suitable for spraying, the compounds of the present invention can be combined with finely divided solid powders such as clays, inorganic silicates, carbonates, and A mixture of wetting agents, binders and/or dispersing agents.
水分散性粒剂的配制：将原药和粉状固体稀释剂、润湿展着剂及粘合剂等进行混合粉碎， 再加水捏合后， 加入装有 10至 100目筛网的造粒机中进行造粒， 然后再经干燥、 筛分 (按筛 网范围)。 也可将原药、 分散剂、 崩解剂和润湿剂及固体稀释剂加入砂磨机中， 以水为介质 研磨， 制成悬浮剂， 然后进行喷雾干燥造粒， 通常配制含量为 20%— 30%颗粒状产品。 具体实施方式  Preparation of water-dispersible granules: mixing and pulverizing the original drug with powdered solid diluent, wetting spreader and binder, adding water and kneading, adding granulator with 10 to 100 mesh screen Granulation is carried out, followed by drying and sieving (by sieve range). The original drug, dispersing agent, disintegrating agent and wetting agent and solid diluent may also be added to a sand mill, ground with water as a suspending agent, and then spray-dried and granulated, usually in a content of 20%. — 30% granulated product. Detailed ways
以下具体实施例用来进一步说明本发明， 但本发明绝非仅限于这些例子。  The following specific examples are intended to further illustrate the invention, but the invention is in no way limited to these examples.
合成实施例  Synthesis example
实施例 1 : 2-甲基 -5-氰基 -6-(4-氯苯基) -烟酰氯的制备  Example 1 Preparation of 2-methyl-5-cyano-6-(4-chlorophenyl)-nicotinoyl chloride
1)2-甲基 -5-氰基 -6-羟基-烟酸乙酯的制备
Figure imgf000045_0001
1) Preparation of 2-methyl-5-cyano-6-hydroxy-nicotinic acid ethyl ester
Figure imgf000045_0001
将 100.0 g(0.54 mol) 2-乙氧亚甲基乙酰乙酸乙酯和 45.2 g(0.54 mol)氰基乙酰胺加入装有 150 mL乙醇的三口瓶中， 再向其中加入 36.5 g(0.54 mol)乙醇钠， 室温反应 5 h， TLC监测反 应完毕后， 减压除去溶剂， 将残余物倒入水中， 用 20%盐酸调 pH至 2， 有大量固体析出， 抽滤， 滤饼用水洗涤， 空气干燥得白色固体 50.8 g， 收率： 45.9%。  100.0 g (0.54 mol) of ethyl 2-ethoxymethylene acetoacetate and 45.2 g (0.54 mol) of cyanoacetamide were added to a three-necked flask containing 150 mL of ethanol, and 36.5 g (0.54 mol) was added thereto. Sodium ethoxide, reacted at room temperature for 5 h. After the reaction was completed by TLC, the solvent was removed under reduced pressure. The residue was poured into water and adjusted to pH 2 with 20% hydrochloric acid. A large amount of solid was precipitated, filtered, and the filter cake was washed with water and air dried. A white solid was obtained in 50.8 g, yield: 45.9%.
2)2-甲基 -5-氰基 -6-氯- 乙酯
Figure imgf000045_0002
2) 2-methyl-5-cyano-6-chloro-ethyl ester
Figure imgf000045_0002
将 50.8 g(0.25 mol) 2-甲基 -5-氰基 -6-羟基-烟酸乙酯放入 1000 mL单口烧瓶中， 向其中加 入 200 mL草酰氯， 升温至回流， 反应 8 h， TLC监测反应完毕后， 减压除去溶剂， 将残余 物倒入水中，有固体析出，抽滤，滤饼用水洗涤，空气干燥得土黄色固体 23.7 g,收率： 42.8% 50.8 g (0.25 mol) of 2-methyl-5-cyano-6-hydroxy-nicotinic acid ethyl ester was placed in a 1000 mL single-necked flask, 200 mL of oxalyl chloride was added thereto, and the temperature was raised to reflux for 8 h, TLC After the completion of the reaction, the solvent was removed under reduced pressure, and the residue was poured into water, and solid was precipitated, filtered, filtered, washed with water, and dried in air to give a solid solid 23.7 g, yield: 42.8%
3) 2-甲 -5-氰基 -6-(4-氯苯基) -烟酸乙酯的制备 3) Preparation of 2-methyl-5-cyano-6-(4-chlorophenyl)-nicotinic acid ethyl ester
Figure imgf000045_0003
Figure imgf000045_0003
将 20.0 g(0.089 mol) 2-甲基 -5-氰基 -6-氯-烟酸乙酯放入 500 mL单口烧瓶中， 向其中加入 80 mL甲苯， 再向其中加入 12.3 g(0.089 mol)碳酸钾， 再称取 13.9 g(0.089 mol)对氯苯硼酸放 入其中， 加入催化量的四三苯基膦钯， 升温至回流， 反应 4 h， TLC监测反应完毕后， 冷却 至室温， 抽滤， 滤饼用 100 mL甲苯洗涤 3次， 滤液减压脱溶得到棕色固体 18.3 g， 收率： 68.3%。  20.0 g (0.089 mol) of 2-methyl-5-cyano-6-chloro-nicotinic acid ethyl ester was placed in a 500 mL single-necked flask, 80 mL of toluene was added thereto, and 12.3 g (0.089 mol) was added thereto. Potassium carbonate, weighed 13.9 g (0.089 mol) of p-chlorophenylboronic acid into it, added a catalytic amount of tetrakistriphenylphosphine palladium, heated to reflux, reaction for 4 h, after TLC monitoring reaction, cooled to room temperature, pumping After filtration, the cake was washed three times with 100 mL of toluene, and the filtrate was evaporated to dryness to give a brown solid, 18.3 g, yield: 68.3%.
4) 2-甲基 -5-氰基 -6- 4-氯苯基) -烟酸的制备  4) Preparation of 2-methyl-5-cyano-6- 4-chlorophenyl)-nicotinic acid
Figure imgf000045_0004
Figure imgf000045_0004
将 10.0 g(0.033 mol) 2-甲基 -5-氰基 -6-(4-氯苯基)-烟酸乙酯放入 250 mL的三口瓶中， 向 其中加入 80 mL的甲醇， 使其溶解， 再将配好的 2.7 g(0.066 mol)氢氧化钠 80 mL水溶液滴 入其中， 室温反应 3 h， TLC监测反应完毕后， 减压除去甲醇， 将剩余物倒入水中， 用浓盐 酸调 pH至 2~3， 有大量白色固体析出， 抽滤， 空气干燥得到白色固体 8.0 g， 收率： 88%。 Put 10.0 g (0.033 mol) of 2-methyl-5-cyano-6-(4-chlorophenyl)-nicotinic acid ethyl ester into a 250 mL three-necked flask. 80 mL of methanol was added to dissolve it, and then a solution of 2.7 g (0.066 mol) of sodium hydroxide in 80 mL was added dropwise thereto, and reacted at room temperature for 3 h. After TLC was monitored, the methanol was removed under reduced pressure. The product was poured into water, and the pH was adjusted to 2 to 3 with concentrated hydrochloric acid. A large white solid was precipitated, suction filtered, and air dried to give a white solid 8.0 g, yield: 88%.
5) 2-甲基 -5-氰基 -6- -氯苯基) -烟酰氯的制备  5) Preparation of 2-methyl-5-cyano-6-chlorophenyl)-nicotinyl chloride
Figure imgf000046_0001
Figure imgf000046_0001
将 6.0g(0.022mol) 2-甲基 -5-氰基 -6-(4-氯苯基) -烟酸放入装有尾气吸收装置的 250 mL的 三口瓶中， 向其中加入 100 mL的氯化亚砜， 逐渐升温至回流， 反应 4 h， 至反应液澄清并无 气体放出， 停止反应， 减压除去氯化亚砜， 得到棕色油状物 5.1 g， 收率 80.0%。  6.0 g (0.022 mol) of 2-methyl-5-cyano-6-(4-chlorophenyl)-nicotinic acid was placed in a 250 mL three-necked flask equipped with a tail gas absorption device, and 100 mL was added thereto. The thionyl chloride was gradually warmed to reflux, and the reaction was carried out for 4 h until the reaction mixture was clarified, and no gas evolved. The reaction was stopped, and the thionyl chloride was removed under reduced pressure to give a brown oil (5.1 g, yield: 80.0%).
实施例 2: 中间体 2-苯基 -4-甲基 -5-嘧啶甲酰氯的制备  Example 2: Preparation of intermediate 2-phenyl-4-methyl-5-pyrimidinecarbonyl chloride
1) 2-苯基 -4-甲
Figure imgf000046_0002
1) 2-phenyl-4-methyl
Figure imgf000046_0002
将 18.6 g(0.1 mol) 2-乙氧亚甲基乙酰乙酸乙酯和 15.6 g(0.54 mol)苯脒加入到装有 200 mL 乙醇溶液的三口瓶中， 向其中加入 6.8 g(0.1 mol)乙醇钠， 室温反应 5h， TLC监测反应完毕 后， 减压除去溶剂， 将残余物倒入水中， 用 20%盐酸调 pH至 2， 有大量固体析出， 抽滤， 滤饼用水洗涤， 空气干燥得白色固体 15.6 g， 收率： 64.5%。  18.6 g (0.1 mol) of ethyl 2-ethoxymethyleneacetoacetate and 15.6 g (0.54 mol) of phenylhydrazine were added to a three-necked flask containing 200 mL of ethanol solution, and 6.8 g (0.1 mol) of ethanol was added thereto. Sodium, reacted at room temperature for 5 h, after TLC monitoring reaction was completed, the solvent was removed under reduced pressure, the residue was poured into water, pH was adjusted to 2 with 20% hydrochloric acid, and a large amount of solid was precipitated, suction filtered, and the filter cake was washed with water and dried in air. The solid was 15.6 g, yield: 64.5%.
2) 2-苯基 -4-甲基 -5-  2) 2-Phenyl-4-methyl-5-
Figure imgf000046_0003
Figure imgf000046_0003
将 10.0 g(0.041 mol) 中间体 2-苯基 -4-甲基 -5-羧酸乙酯嘧啶放入 250 mL的三口瓶中， 向 其中加入 80 mL的甲醇， 使其溶解， 再将配好的 3.3 g(0.082 mol)氢氧化钠 80 mL水溶液滴 入其中， 室温反应 3 h， TLC监测反应完毕后， 减压除去甲醇， 将剩余物倒入水中， 用浓盐 酸调 pH至 2~3， 有大量白色固体析出， 抽滤， 空气干燥得到白色固体 6.5 g， 收率： 73.6%。  10.0 g (0.041 mol) of the intermediate 2-phenyl-4-methyl-5-carboxylic acid ethyl pyrimidine was placed in a 250 mL three-necked flask, 80 mL of methanol was added thereto to dissolve it, and then A good 3.3 g (0.082 mol) sodium hydroxide 80 mL aqueous solution was added dropwise thereto, and reacted at room temperature for 3 h. After the TLC monitoring reaction was completed, the methanol was removed under reduced pressure, and the residue was poured into water, and the pH was adjusted to 2 to 3 with concentrated hydrochloric acid. , a large amount of white solid precipitated, suction filtration, air drying to obtain a white solid 6.5 g, yield: 73.6%.
3) 2-苯基 -4-甲基 -5- 甲酰氯的制备  3) Preparation of 2-phenyl-4-methyl-5-formyl chloride
Figure imgf000046_0004
Figure imgf000046_0004
将 5.0g(0.023mol) 2-苯基 -4-甲基 -5-羧基嘧啶放入装有尾气吸收装置的 250 mL的三口瓶 中， 向其中加入 100 mL的氯化亚砜， 逐渐升温至回流， 反应 4 h， 至反应液澄清并无气体放 出， 停止反应， 减压除去氯化亚砜， 得到棕色油状物 4.1 g， 收率 75.5%。  5.0 g (0.023 mol) of 2-phenyl-4-methyl-5-carboxypyrimidine was placed in a 250 mL three-necked flask equipped with an exhaust gas absorption device, 100 mL of thionyl chloride was added thereto, and the temperature was gradually raised to After refluxing, the reaction was carried out for 4 h, until the reaction mixture was clarified, and no gas evolved. The reaction was stopped, and the thionyl chloride was removed under reduced pressure to give a brown oil (4.1 g, yield: 75.5%).
实施例 3 : 1-(3-氯吡啶 -2-基)哌嗪盐酸盐的制备
Figure imgf000047_0001
Example 3: Preparation of 1-(3-chloropyridin-2-yl)piperazine hydrochloride
Figure imgf000047_0001
将 N-Boc-哌嗪 5.0 g(0.027 mol)加入装有 40 mLN,N-二甲基甲酰胺的 150 mL反应瓶中， 再向其中加入碳酸钾 3.7 g(0.027 mol),升温至 40°C，搅拌下向其中滴加 2,3-二氯吡啶 (市售 )4.0 g(0.027 mol) 的 Ν,Ν-二甲基甲酰胺溶液， 15 min加完， 保持 80°C反应 4 h。 TLC监测反应完 毕后， 将反应液倒入水中， 有白色固体析出， 过滤， 得白色固体 5.5g， 收率： 68.8%。
Figure imgf000047_0002
5.0 g (0.027 mol) of N-Boc-piperazine was added to a 150 mL reaction flask containing 40 mL of N,N-dimethylformamide, and then 3.7 g (0.027 mol) of potassium carbonate was added thereto, and the temperature was raised to 40°. C, 2 g of 2,3-dichloropyridine (commercially available) 4.0 g (0.027 mol) of hydrazine, hydrazine-dimethylformamide solution was added dropwise thereto under stirring, and the reaction was continued for 15 min, and the reaction was maintained at 80 ° C for 4 h. After the completion of the reaction by TLC, the reaction mixture was poured into water, and a white solid was precipitated and filtered to give a white solid, 5.5 g, yield: 68.8%.
Figure imgf000047_0002
将 5.0 g(0.017 mol) 4-(3-氯吡啶 -2-基)哌嗪 -1-碳酸叔丁酯放入 250 mL单口瓶中， 向其中 加入 50 mL四氢呋喃， 再向其中加入 3.4 g(0.034 mol)浓盐酸， 室温反应 4 h。 TLC监测反应 完毕后， 减压除去溶剂， 得白色固体 2.8 g， 收率： 71.0%。  5.0 g (0.017 mol) of 4-(3-chloropyridin-2-yl)piperazine-1-carbonate tert-butyl ester was placed in a 250 mL single-mouth bottle, 50 mL of tetrahydrofuran was added thereto, and 3.4 g was added thereto ( 0.034 mol) concentrated hydrochloric acid, reacted at room temperature for 4 h. After the reaction was monitored by TLC, the solvent was evaporated under reduced pressure to give white crystals (yield: 278 g).
实施例 4: 化合物 5510的制备  Example 4: Preparation of Compound 5510
Figure imgf000047_0003
取 0.5 g(2.1 mmol) 1-(3-氯吡啶 -2-基)哌嗪盐酸盐、三乙胺 0.42 g(4.2 mmol)于 50 mL反应 瓶中，加入 15 mL二氯甲垸，搅拌下加入 0.62 g(2.1 mol) 2-甲基 -5-氰基 -6-(4-氯苯基) -烟酰氯， 室温搅拌反应 1 h。 TLC监测反应完毕后，过滤，滤液减压脱溶，残余物柱层析得产品 0.55 g, 收率： 57.0%。
Figure imgf000047_0003
Take 0.5 g (2.1 mmol) of 1-(3-chloropyridin-2-yl)piperazine hydrochloride, triethylamine 0.42 g (4.2 mmol) in a 50 mL reaction flask, add 15 mL of dichloromethane, and stir. 0.62 g (2.1 mol) of 2-methyl-5-cyano-6-(4-chlorophenyl)-nicotinoyl chloride was added thereto, and the mixture was stirred at room temperature for 1 h. After the completion of the reaction by TLC, the mixture was filtered, and the filtrate was evaporated under reduced pressure, and the residue was subjected to column chromatography to give the product 0.55 g, yield: 57.0%.
实施例 5: 化合物 9134的制备  Example 5: Preparation of Compound 9134
Figure imgf000047_0004
取 0.5 g(1.6 mmol) 1-(2,6-二氯 -4硝基苯基)哌嗪盐酸盐、三乙胺 0.16g(1.6 mmol)于 50 mL 反应瓶中， 加入 15 mL二氯甲垸， 搅拌下加入 0.47 g(1.6 mol) 2-(4-氯苯基)-5-氯甲基-6-甲基- 烟腈， 室温搅拌反应 l h。 TLC监测反应完毕后， 过滤， 滤液减压脱溶， 残余物柱层析得产 品 0.32 g， 收率： 37.7%。
Figure imgf000047_0004
Take 0.5 g (1.6 mmol) of 1-(2,6-dichloro-4-nitrophenyl)piperazine hydrochloride, triethylamine 0.16 g (1.6 mmol) in a 50 mL reaction flask, and add 15 mL of dichloro Formazan, 0.47 g (1.6 mol) of 2-(4-chlorophenyl)-5-chloromethyl-6-methyl-nicotinonitrile was added with stirring, and the reaction was stirred at room temperature for 1 h. After the TLC monitoring reaction was completed, the mixture was filtered, and the filtrate was evaporated to dryness, and the residue was subjected to column chromatography to give the product 0.32 g, yield: 37.7%.
Figure imgf000047_0005
Figure imgf000047_0005
取 0.5 g(2.0 mmol) 1-(4-氯-苄基)哌嗪盐酸盐、 三乙胺 0.20 g(2.0 mmol)于 50 mL反应瓶 中， 加入 15 mL二氯甲垸， 搅拌下加入 0.59 g(2.0 mol) 2-(4-氯苯基 )-5-氯甲基 -6-甲基-烟腈， 室温搅拌反应 1 h。 TLC监测反应完毕后，过滤，滤液减压脱溶，残余物柱层析得产品 0.35 g, 收率： 37.2%。 Take 0.5 g (2.0 mmol) of 1-(4-chloro-benzyl)piperazine hydrochloride, triethylamine 0.20 g (2.0 mmol) in a 50 mL reaction flask, add 15 mL of dichloromethane, and add with stirring. 0.59 g (2.0 mol) 2-(4-chlorophenyl)-5-chloromethyl-6-methyl-nicotinonitrile was stirred at room temperature for 1 h. After the TLC monitoring reaction was completed, the mixture was filtered, and the filtrate was decomposed under reduced pressure, and the residue was subjected to column chromatography to obtain a product of 0.35 g. Yield: 37.2%.
Figure imgf000048_0001
Figure imgf000048_0001
取 0.5 g(2.8 mmol) 1-苄基哌嗪、三乙胺 0.28 g(2.8 mmol)于 50 mL反应瓶中，加入 15 mL 二氯甲垸，搅拌下加入 0.83g(2.8 mol) 2-(4-氯苯基 )-5-氯甲基 -6-甲基-烟腈，室温搅拌反应 1 h。 TLC监测反应完毕后， 过滤， 滤液减压脱溶， 残余物柱层析得产品 0.41 g， 收率： 33.5%。 通式 (I)的其他化合物可以用本发明提供的制备方法制得。  Take 0.5 g (2.8 mmol) of 1-benzylpiperazine and triethylamine 0.28 g (2.8 mmol) in a 50 mL reaction flask, add 15 mL of dichloromethane, and add 0.83 g (2.8 mol) of 2-(2) with stirring. 4-Chlorophenyl)-5-chloromethyl-6-methyl-nicotinonitrile was stirred at room temperature for 1 h. After the TLC monitoring reaction was completed, the mixture was filtered, and the filtrate was evaporated to dryness, and the residue was subjected to column chromatography to give the product 0.41 g, yield: 33.5%. Other compounds of the formula (I) can be obtained by the preparation methods provided by the present invention.
部分化合物熔点和核磁数据 (1HNMR, 300MHz, 内标 TMS， 溶剂 CDC13)如下: The melting point and nuclear magnetic data of some compounds (1H NMR, 300MHz, internal standard TMS, solvent CDC1 3 ) are as follows:
编号 物性和核磁数据  No. Physical and nuclear magnetic data
黄色固体； 130-131 °C ; δ 8.22-8.21 (m, 1H), 8.11 (d, J = 15.6 Hz, 1H), 8.08— 7.86 (m, 2H).Yellow solid; 130-131 °C ; δ 8.22-8.21 (m, 1H), 8.11 (d, J = 15.6 Hz, 1H), 8.08- 7.86 (m, 2H).
4869 7.66-7.65 (m,lH), 7.60 - 7.40 (m, 2H), 6.95-6.91 (m,lH), 4.20 - 3.82 (m, 2H), 3.67 - 3.23 4869 7.66-7.65 (m,lH), 7.60 - 7.40 (m, 2H), 6.95-6.91 (m,lH), 4.20 - 3.82 (m, 2H), 3.67 - 3.23
(m, 6H).  (m, 6H).
黄色固体； 152- 153 °C； δ 8.22 - 8.09 (m, 2H), 8.05 - 7.96 (m, 2H), 7.65 (d, J = 2.4 Hz, 1H): Yellow solid; 152- 153 °C; δ 8.22 - 8.09 (m, 2H), 8.05 - 7.96 (m, 2H), 7.65 (d, J = 2.4 Hz, 1H) :
4891 4891
7.56 (d, J = 8.7 Hz, 2H), 4.02-3.95 (m, 2H), 3.54 - 3.25 (m, 6H).  7.56 (d, J = 8.7 Hz, 2H), 4.02-3.95 (m, 2H), 3.54 - 3.25 (m, 6H).
白色固体； 169- 170 °C； 5 8.13 (s, 1H), 8.08 - 7.89 (m, 2H), 7.76 - 7.65 (m, 1H), 7.63 - 7.46 White solid; 169-170 °C; 5 8.13 (s, 1H), 8.08 - 7.89 (m, 2H), 7.76 - 7.65 (m, 1H), 7.63 - 7.46
4922 4922
(m, 2H), 4.17 - 3.80 (m, 2H), 3.52-3.36 (m, 6H).  (m, 2H), 4.17 - 3.80 (m, 2H), 3.52-3.36 (m, 6H).
白色固体； 158- 159°C； δ 8.43 (s, 1H), 8.14 (s, 1H), 8.07 - 7.94 (m, 2H), 7.83 (s, 1H), 7.67 - White solid; 158-159°C; δ 8.43 (s, 1H), 8.14 (s, 1H), 8.07 - 7.94 (m, 2H), 7.83 (s, 1H), 7.67 -
4931 4931
7.40 (m, 2H), 4.1-3.89 (m,2H), 3.70 - 3.34 (m, 6H).  7.40 (m, 2H), 4.1-3.89 (m, 2H), 3.70 - 3.34 (m, 6H).
白色固体； 145- 147°C； δ 8.49 - 8.03 (m, 4H), 7.85 (d, J = 8.1Hz, 2H), 7.66- 7.63(m, 1H), 7.12 White solid; 145-147°C; δ 8.49 - 8.03 (m, 4H), 7.85 (d, J = 8.1Hz, 2H), 7.66- 7.63(m, 1H), 7.12
5035 5035
- 6.75 (m, 1H), 4.09-3.94 (m, 2H), 3.78 - 3.06 (m, 6H).  - 6.75 (m, 1H), 4.09-3.94 (m, 2H), 3.78 - 3.06 (m, 6H).
白色固体； 157- 158°C； δ 8.50 (d, J = 4.8 Hz, 1H), 8.29 - 8.08 (m, 3H), 7.93 (d, J = 7.8 Hz, White solid; 157-158°C; δ 8.50 (d, J = 4.8 Hz, 1H), 8.29 - 8.08 (m, 3H), 7.93 (d, J = 7.8 Hz,
5039 5039
1H), 7.85 (d, J = 8.1 Hz, 2H), 7.15-7.13 (m,lH), 4.12 - 3.87 (m, 2H), 3.46-3.32 (m,6H).  1H), 7.85 (d, J = 8.1 Hz, 2H), 7.15-7.13 (m, lH), 4.12 - 3.87 (m, 2H), 3.46-3.32 (m, 6H).
白色固体； 160- 161 °C； δ 8.43 (s, 1H), 8.17 (d, J = 8.4 Hz, 3H), 7.86 (d, J = 8.1 Hz, 2H), 7.71 White solid; 160-161 °C; δ 8.43 (s, 1H), 8.17 (d, J = 8.4 Hz, 3H), 7.86 (d, J = 8.1 Hz, 2H), 7.71
5041 (d, J = 6.9 Hz, 1H), 6.70 (d, J = 9.0 Hz, 1H), 4.03 (s, 1H), 3.87-3.71 (m,5H), 3.40 (t, J = 5.1 Hz, 2H). 5041 (d, J = 6.9 Hz, 1H), 6.70 (d, J = 9.0 Hz, 1H), 4.03 (s, 1H), 3.87-3.71 (m, 5H), 3.40 (t, J = 5.1 Hz, 2H ).
白色固体； 159- 160 °C； δ 8.52 - 8.32 (m, 1H), 8.31 - 8.02 (m, 3H), 7.85 (d, J = 8.1 Hz, 3H), White solid; 159-160 °C; δ 8.52 - 8.32 (m, 1H), 8.31 - 8.02 (m, 3H), 7.85 (d, J = 8.1 Hz, 3H),
5053 5053
6.92-6.89 (m,lH), 4.10 (s, 1H), 3.95 - 3.79 (m, 2H), 3.70-3.60 (m,3H), 3.48-3.46 (m, 2H).  6.92-6.89 (m,lH), 4.10 (s, 1H), 3.95 - 3.79 (m, 2H), 3.70-3.60 (m, 3H), 3.48-3.46 (m, 2H).
白色固体； 253- 254°C； δ 8.32 (d, J = 4.8 Hz, 1H), 8.17 (d, J = 8.1 Hz, 3H), 7.86 (d, J = 8.4 White solid; 253-254 ° C; δ 8.32 (d, J = 4.8 Hz, 1H), 8.17 (d, J = 8.1 Hz, 3H), 7.86 (d, J = 8.4
5054 5054
Hz, 2H), 6.87 (d, J = 5.1 Hz, 2H), 4.04 (s, 1H), 3.92 - 3.56 (m, 5H), 3.41 (t, J = 5.1 Hz, 2H). 黄色固体； 147- 148 °C； δ 8.34 - 8.04 (m, 4H), 7.85 (d, J = 8.4 Hz, 2H), 7.66 (d, J = 2.3 Hz: Hz, 2H), 6.87 (d, J = 5.1 Hz, 2H), 4.04 (s, 1H), 3.92 - 3.56 (m, 5H), 3.41 (t, J = 5.1 Hz, 2H). Yellow solid; 147- 148 °C; δ 8.34 - 8.04 (m, 4H), 7.85 (d, J = 8.4 Hz, 2H), 7.66 (d, J = 2.3 Hz :
5057 5057
1H), 4.14 - 3.84 (m, 2H), 3.47-3. ll(m, 6H).  1H), 4.14 - 3.84 (m, 2H), 3.47-3. ll(m, 6H).
黄色固体； 164- 165°C ; 5 8.16 (d, J = 10.8Hz, 3H), 7.85 (d, J = 8.2 Hz, 2H), 7.72 (s, 1H), 4.17 Yellow solid; 164-165 ° C; 5 8.16 (d, J = 10.8 Hz, 3H), 7.85 (d, J = 8.2 Hz, 2H), 7.72 (s, 1H), 4.17
5088 5088
- 3.80 (m, 2H), 3.53-3.37 (m, 6H).  - 3.80 (m, 2H), 3.53-3.37 (m, 6H).
白色固体; 164- 165°C ;S 8.44 (d, J = 1.2 Hz, 1H), 8.30 - 8.03 (m, 3H), 7.87- 7.83(m,3H), 4.21 White solid; 164-165 ° C; S 8.44 (d, J = 1.2 Hz, 1H), 8.30 - 8.03 (m, 3H), 7.87- 7.83 (m, 3H), 4.21
5097 5097
- 4.00 (m, 1H), 4.00 - 3.83 (m, 1H), 3.73 - 3.52 (m, 2H), 3.58-3.46 (m, 4H).  - 4.00 (m, 1H), 4.00 - 3.83 (m, 1H), 3.73 - 3.52 (m, 2H), 3.58-3.46 (m, 4H).
棕色液体； δ 8.41 (s, 1H), 8.29 - 8.06 (m, 3H), 7.86 (d, J = 8.4 Hz, 2H), 4.39 (q, J = 7.2 Hz, Brown liquid; δ 8.41 (s, 1H), 8.29 - 8.06 (m, 3H), 7.86 (d, J = 8.4 Hz, 2H), 4.39 (q, J = 7.2 Hz,
5112 5112
2H), 4.19-3.87 (m, 6H), 3.49 (t, J = 5.1 Hz, 2H), 1.39 (t, J = 7.2 Hz, 3H).  2H), 4.19-3.87 (m, 6H), 3.49 (t, J = 5.1 Hz, 2H), 1.39 (t, J = 7.2 Hz, 3H).
褐色液体； δ 8.21-8.19 (m, 1H), 8.00 - 7.86 (m, 3H), 7.66-7.63 (m, 1H), 7.51 (d, J = 8.4 Hz Brown liquid; δ 8.21-8.19 (m, 1H), 8.00 - 7.86 (m, 3H), 7.66-7.63 (m, 1H), 7.51 (d, J = 8.4 Hz
5510 5510
2H), 6.95-6.91 (m,lH), 4.01 (s, 2H), 3.48 (d, J = 4.5 Hz, 4H), 3.34 (s, 2H), 2.70 (s, 3H)  2H), 6.95-6.91 (m, lH), 4.01 (s, 2H), 3.48 (d, J = 4.5 Hz, 4H), 3.34 (s, 2H), 2.70 (s, 3H)
5552 黄色液体； δ 8.16 (d, J = 2.1 Hz, 1H), 7.91 (d, J = 8.1 Hz, 3H), 7.66 (d, J = 2.1 Hz, 1H), 7.52 (d, J = 8.7 Hz, 2H), 4.00 (s, 2H), 3.39 (d, J = 45.0 Hz, 6H), 2.69 (s, 3H). 5552 yellow liquid; δ 8.16 (d, J = 2.1 Hz, 1H), 7.91 (d, J = 8.1 Hz, 3H), 7.66 (d, J = 2.1 Hz, 1H), 7.52 (d, J = 8.7 Hz, 2H), 4.00 (s, 2H), 3.39 (d, J = 45.0 Hz, 6H), 2.69 (s, 3H).
黄色固体； 170-171 °C； δ 8.43 (s, IH), 8.10 - 7.88 (m, 3H), 7.83 (s, IH), 7.52 (d, J = 8.7 Hz, Yellow solid; 170-171 °C; δ 8.43 (s, IH), 8.10 - 7.88 (m, 3H), 7.83 (s, IH), 7.52 (d, J = 8.7 Hz,
5573 5573
2H), 4.01 (s, 2H), 3.52-3.48 (m, 6H), 2.70 (s, 3H).  2H), 4.01 (s, 2H), 3.52-3.48 (m, 6H), 2.70 (s, 3H).
黄色液体； δ 7.91 (d, J = 8.1 Hz, 3H), 7.72 (s, IH), 7.52 (d, J = 8.4 Hz, 2H), 3.99 (s, 2H), Yellow liquid; δ 7.91 (d, J = 8.1 Hz, 3H), 7.72 (s, IH), 7.52 (d, J = 8.4 Hz, 2H), 3.99 (s, 2H),
5594 5594
3.50-3.46 (m, 7H), 2.69 (s, 3H).  3.50-3.46 (m, 7H), 2.69 (s, 3H).
白色液体； δ 8.28 - 8.05 (m, 3H), 7.84 (d, 2H), 7.64 (dd, 2H), 7.04 (s, IH), 6.99 - 6.82 (m, White liquid; δ 8.28 - 8.05 (m, 3H), 7.84 (d, 2H), 7.64 (dd, 2H), 7.04 (s, IH), 6.99 - 6.82 (m,
5663 5663
IH), 4.12 (d, 2H), 4.01 (s, 2H), 3.49 (d, 2H), 3.36 (d, 2H).  IH), 4.12 (d, 2H), 4.01 (s, 2H), 3.49 (d, 2H), 3.36 (d, 2H).
浅黄色固体； δ 8.31 (dd, IH), 8.25 - 7.99 (m, 4H), 7.97 - 7.43 (m, 5H), 7.26 (s, IH), 6.81 Light yellow solid; δ 8.31 (dd, IH), 8.25 - 7.99 (m, 4H), 7.97 - 7.43 (m, 5H), 7.26 (s, IH), 6.81
5664 5664
(dd, 2H), 3.91 (d, 2H), 4.08 - 3.40 (m, 4H), 3.30 -3.19 (m, 2H)  (dd, 2H), 3.91 (d, 2H), 4.08 - 3.40 (m, 4H), 3.30 -3.19 (m, 2H)
浅黄色固体； δ 8.41 (dd, IH), 8.20 - 8.06 (m, 2H), 8.20 - 8.09 (m, 2H), 7.91 - 7.75 (m, 2H), Light yellow solid; δ 8.41 (dd, IH), 8.20 - 8.06 (m, 2H), 8.20 - 8.09 (m, 2H), 7.91 - 7.75 (m, 2H),
5684 5684
7.05 (s, IH), 6.69 (t, IH), 3.82 (d, 2H), 3.69 (m, 2H), 3.56 (dd, 4H).  7.05 (s, IH), 6.69 (t, IH), 3.82 (d, 2H), 3.69 (m, 2H), 3.56 (dd, 4H).
浅黄色固体； δ 8.49 - 8.10 (m, 3H), 8.10 - 7.25 (m, 5H), 6.80 (dd, 4H), 6.46 (s, IH), 4.12 - Light yellow solid; δ 8.49 - 8.10 (m, 3H), 8.10 - 7.25 (m, 5H), 6.80 (dd, 4H), 6.46 (s, IH), 4.12 -
5685 5685
3.79 (m, 2H), 1 3.71 - 3.41 (m, 4H), 3.36 - 2.49 (m, 2H),  3.79 (m, 2H), 1 3.71 - 3.41 (m, 4H), 3.36 - 2.49 (m, 2H),
白色液体； δ 8.15 - 8.16 (m, 3H), 7.84 (d, 2H), 7.65 (d, 2H), 6.86 (t, IH), 4.00 (s, 4H), 3.40 White liquid; δ 8.15 - 8.16 (m, 3H), 7.84 (d, 2H), 7.65 (d, 2H), 6.86 (t, IH), 4.00 (s, 4H), 3.40
5705 5705
(d, 4H),  (d, 4H),
浅黄色固体； δ 8.25 - 8.09 (m, IH), 8.07 (d, 2H), 8.05 - 7.67 (m, 5H), 7.67 - 7.35 (m, 4H), Light yellow solid; δ 8.25 - 8.09 (m, IH), 8.07 (d, 2H), 8.05 - 7.67 (m, 5H), 7.67 - 7.35 (m, 4H),
5706 5706
3.93 (d, 2H), 3.77 - 3.41 (m, 4H), , 3.20 (d, 2H),  3.93 (d, 2H), 3.77 - 3.41 (m, 4H), , 3.20 (d, 2H),
浅黄色固体； δ 8.34 (s, IH), 8.25 - 8.01 (m, 2H), 7.95 - 7.70 (m, 5H), 7.70 - 7.67 (m, 2H), Light yellow solid; δ 8.34 (s, IH), 8.25 - 8.01 (m, 2H), 7.95 - 7.70 (m, 5H), 7.70 - 7.67 (m, 2H),
5790 5790
7.70 - 7.26 (m, 2H), 6.51 (d, IH), 4.04 (dt, 4H), 3.69 (d, 2H), 3.09 (d, 2H).  7.70 - 7.26 (m, 2H), 6.51 (d, IH), 4.04 (dt, 4H), 3.69 (d, 2H), 3.09 (d, 2H).
浅黄色固体 δ 8.43 (s, IH), 8.14 (d, 2H), 7.84 (d, 2H), 7.70 (dd, IH), 6.86 (t, IH), 6.69 (s, Light yellow solid δ 8.43 (s, IH), 8.14 (d, 2H), 7.84 (d, 2H), 7.70 (dd, IH), 6.86 (t, IH), 6.69 (s,
5789 5789
IH), 3.96 (s, 2H), 3.82 - 3.40 (m,4H), 3.40 - 3.23 (m, 2H).  IH), 3.96 (s, 2H), 3.82 - 3.40 (m, 4H), 3.40 - 3.23 (m, 2H).
黄色固体； 127-128 °C ; 5 8.91 (s, IH), δ 8.54- 8.51 (m, 2H), δ 8.21- 8.19(m, IH), δ 7.65-7.62Yellow solid; 127-128 °C ; 5 8.91 (s, IH), δ 8.54- 8.51 (m, 2H), δ 8.21- 8.19 (m, IH), δ 7.65-7.62
5951 (m, IH), δ 7.58-7.56 (m, 3H), δ 6.94-6.90 (m, IH), δ 4.02 (d, J = 5.7Hz, 2H), δ 3.48-3.45 (m, 4H), δ 3.33(d, J = 5.4 Hz, 2H). 5951 (m, IH), δ 7.58-7.56 (m, 3H), δ 6.94-6.90 (m, IH), δ 4.02 (d, J = 5.7 Hz, 2H), δ 3.48-3.45 (m, 4H), δ 3.33 (d, J = 5.4 Hz, 2H).
棕色液体； δ 8.91 (s, IH), δ 8.54-8.51 (m, 2H), 58.14 (d, J = 2.4Hz, IH), 57.64 (d, J = 2.1Hz, Brown liquid; δ 8.91 (s, IH), δ 8.54-8.51 (m, 2H), 58.14 (d, J = 2.4Hz, IH), 57.64 (d, J = 2.1Hz,
5999 5999
IH), δ 7.58-7.52 (m, 3H), δ 4.02- 3.99(m, 2H), δ 3.46-3.44 (m, 4H), δ 3.32-3.29 (m, 2H). 灰色固体； 113- 114°C； δ 8.20-8.18 (m, IH), 7.96 (d, J = 8.7 Hz, 2H), 7.71 - 7.50 (m, 3H), IH), δ 7.58-7.52 (m, 3H), δ 4.02- 3.99 (m, 2H), δ 3.46-3.44 (m, 4H), δ 3.32-3.29 (m, 2H). Gray solid; 113- 114° C; δ 8.20-8.18 (m, IH), 7.96 (d, J = 8.7 Hz, 2H), 7.71 - 7.50 (m, 3H),
7128 7.44 (d, J = 8.7 Hz, 2H), 6.92-6.88 (m, IH), 4.10 - 3.94 (m, 2H), 3.46 (d, J = 4.8Hz, 4H), 3.30 (d, J = 5.1 Hz, 2H), 2.63 (s, 3H). 7128 7.44 (d, J = 8.7 Hz, 2H), 6.92-6.88 (m, IH), 4.10 - 3.94 (m, 2H), 3.46 (d, J = 4.8Hz, 4H), 3.30 (d, J = 5.1 Hz, 2H), 2.63 (s, 3H).
棕色液体； δ 8.20-8.19 (m,lH), 7.91 (d, J = 8.1 Hz, IH), 7.72 - 7.49 (m, 5H), 7.35 (d, J = 7.8 Brown liquid; δ 8.20-8.19 (m,lH), 7.91 (d, J = 8.1 Hz, IH), 7.72 - 7.49 (m, 5H), 7.35 (d, J = 7.8
7152 Hz, IH), 6.95 - 6.83 (m, IH), 4.01 (s, 2H), 3.42 (d, J = 20.4 Hz, 4H), 3.32 (d, J = 5.4 Hz, 2H), 2.57 (s, 3H). 7152 Hz, IH), 6.95 - 6.83 (m, IH), 4.01 (s, 2H), 3.42 (d, J = 20.4 Hz, 4H), 3.32 (d, J = 5.4 Hz, 2H), 2.57 (s, 3H).
褐色液体； δ 8.36 - 8.12 (m, 3H), 8.01 (d, J = 8.7 Hz, 2H), 7.56 (d, J = 8.7Hz, 2H), 4.02 (d, J Brown liquid; δ 8.36 - 8.12 (m, 3H), 8.01 (d, J = 8.7 Hz, 2H), 7.56 (d, J = 8.7Hz, 2H), 4.02 (d, J
8455 8455
= 4.2 Hz, 2H), 3.45 (d, J = 4.8 Hz, 4H), 3.31 (d, J = 3.9 Hz, 2H).  = 4.2 Hz, 2H), 3.45 (d, J = 4.8 Hz, 4H), 3.31 (d, J = 3.9 Hz, 2H).
黄色固体； 240-241 °C； 5 8.16 (s, IH), 8.11 - 7.94 (m, 2H), 7.69 - 7.44 (m, 2H), 4.13- 4.02(m, Yellow solid; 240-241 °C; 5 8.16 (s, IH), 8.11 - 7.94 (m, 2H), 7.69 - 7.44 (m, 2H), 4.13- 4.02 (m,
8508 8508
2H), 3.71 - 3.36 (m, 6H).  2H), 3.71 - 3.36 (m, 6H).
褐色液体； δ 8.32 - 8.11 (m, 4H), 7.85 (d, J = 8.4 Hz, 2H), 4.02 (d, J = 4.5 Hz, 2H), 3.46 (d, J Brown liquid; δ 8.32 - 8.11 (m, 4H), 7.85 (d, J = 8.4 Hz, 2H), 4.02 (d, J = 4.5 Hz, 2H), 3.46 (d, J
8716 8716
= 5.1 Hz, 4H), 3.31 (s, 2H).  = 5.1 Hz, 4H), 3.31 (s, 2H).
黄色固体； 150- 151 °C； δ 8.33 - 8.06 (m, 3H), 7.86 (d, J = 8.1 Hz, 2H), 4.25 - 3.92 (m, 2H), Yellow solid; 150- 151 °C; δ 8.33 - 8.06 (m, 3H), 7.86 (d, J = 8.1 Hz, 2H), 4.25 - 3.92 (m, 2H),
8769 8769
3.76 - 3.41 (m, 6H).  3.76 - 3.41 (m, 6H).
褐色液体； δ 8.20 (s, IH), 7.91 (d, J = 6.9 Hz, 2H), 7.52 (d, J = 8.4 Hz, 2H), 4.00 (s, 2H), Brown liquid; δ 8.20 (s, IH), 7.91 (d, J = 6.9 Hz, 2H), 7.52 (d, J = 8.4 Hz, 2H), 4.00 (s, 2H),
9134 9134
3.58 - 3.21 (m, 6H), 2.71 (s, 3H).  3.58 - 3.21 (m, 6H), 2.71 (s, 3H).
黄色固体； 222-223 °C； δ 8.02 - 7.87 (m, 3H), 7.53 (d, J = 8.7 Hz, 2H), 4.07 (s, 2H), 3.67 - Yellow solid; 222-223 °C; δ 8.02 - 7.87 (m, 3H), 7.53 (d, J = 8.7 Hz, 2H), 4.07 (s, 2H), 3.67 -
9155 9155
3.39 (m, 6H), 2.71 (s, 3H). 黄色固体； 221- 222°C ; 5 7.93 (d, J = 8.1 Hz, 1H), 7.80 - 7.49 (m, 4H), 7.37 (d, J = 7.8 Hz,3.39 (m, 6H), 2.71 (s, 3H). Yellow solid; 221- 222 ° C; 5 7.93 (d, J = 8.1 Hz, 1H), 7.80 - 7.49 (m, 4H), 7.37 (d, J = 7.8 Hz,
9597 9597
1H), 4.10 (s, 2H), 3.67 - 3.36 (m, 6H), 2.58 (s, 3H).  1H), 4.10 (s, 2H), 3.67 - 3.36 (m, 6H), 2.58 (s, 3H).
黄色固体； 190- 192 °C； δ 7.98 (d, J = 8.7 Hz, 2H), 7.62 (s, 2H), 7.47 (t, J = 5.7 Hz, 2H), 4.09 Yellow solid; 190- 192 °C; δ 7.98 (d, J = 8.7 Hz, 2H), 7.62 (s, 2H), 7.47 (t, J = 5.7 Hz, 2H), 4.09
9621 9621
(s, 2H), 3.69 - 3.33 (m, 6H), 2.65 (s, 3H).  (s, 2H), 3.69 - 3.33 (m, 6H), 2.65 (s, 3H).
黄色固体； 190- 191 °C ; δ 8.30 (s, 1H), 8.20 (d, J = 7.8 Hz, 1H), 7.77 - 7.54 (m, 4H), 4.12 (d, Yellow solid; 190- 191 °C; δ 8.30 (s, 1H), 8.20 (d, J = 7.8 Hz, 1H), 7.77 - 7.54 (m, 4H), 4.12 (d,
9645 9645
J = 7.2 Hz, 2H), 3.68 - 3.32 (m, 6H), 2.66 (s, 3H).  J = 7.2 Hz, 2H), 3.68 - 3.32 (m, 6H), 2.66 (s, 3H).
白色固体； 174-175 °C ; δ 8.32 - 7.98 (m, 3H), 7.84 (d, J = 8.1Hz, 2H), 7.56 - 7.34 (m, 2H), 9724 I 7.24 (tt, J = 7.4, 5.2 Hz, 2H), 3.85 (s, 2H), 3.69 (s, 2H), 3.29 (t, J = 5.1 Hz, 2H), 2.73 - 2.37 (m, 4H).  White solid; 174-175 ° C; δ 8.32 - 7.98 (m, 3H), 7.84 (d, J = 8.1 Hz, 2H), 7.56 - 7.34 (m, 2H), 9724 I 7.24 (tt, J = 7.4, 5.2 Hz, 2H), 3.85 (s, 2H), 3.69 (s, 2H), 3.29 (t, J = 5.1 Hz, 2H), 2.73 - 2.37 (m, 4H).
白色固体； 180- 181 °C ; δ 8.23 - 8.07 (m, 3H), 7.84 (d, J = 8.4 Hz, 2H), 7.69 (d, J = 7.8 Hz, White solid; 180-181 °C; δ 8.23 - 8.07 (m, 3H), 7.84 (d, J = 8.4 Hz, 2H), 7.69 (d, J = 7.8 Hz,
9756 1H), 7.64 - 7.45 (m, 2H), 7.40 (t, J = 7.5 Hz, 1H), 3.80 (d, J = 27.6 Hz, 4H), 3.30 (s, 2H), 2.81 - 2.37 (m, 4H). 9756 1H), 7.64 - 7.45 (m, 2H), 7.40 (t, J = 7.5 Hz, 1H), 3.80 (d, J = 27.6 Hz, 4H), 3.30 (s, 2H), 2.81 - 2.37 (m, 4H).
土黄色固体； 189-190 °C； δ 8.08 (s, 1H), 8.03 - 7.89 (m, 2H), 7.60 - 7.47 (m, 2H), 7.32-7.25 Earthy yellow solid; 189-190 °C; δ 8.08 (s, 1H), 8.03 - 7.89 (m, 2H), 7.60 - 7.47 (m, 2H), 7.32-7.25
9779 9779
(m,4H), 3.82 (s, 2H), 3.52 (s, 2H), 3.27 (s, 2H), 2.54 (s, 2H), 2.39 (s, 2H).  (m,4H), 3.82 (s, 2H), 3.52 (s, 2H), 3.27 (s, 2H), 2.54 (s, 2H), 2.39 (s, 2H).
浅黄色固体； 169-170°C ; δ 8.15-8.13 (m, 3H), 7.85-7.82 (m, 2H), 7.32 - 7.25 (m, 4H), 3.83Light yellow solid; 169-170°C ; δ 8.15-8.13 (m, 3H), 7.85-7.82 (m, 2H), 7.32 - 7.25 (m, 4H), 3.83
9788 9788
(s, 2H), 3.47 (s, 2H), 3.29- 3.26 (m, 2H), 2.55(s, 2H), 2.40 (m, 2H).  (s, 2H), 3.47 (s, 2H), 3.29- 3.26 (m, 2H), 2.55(s, 2H), 2.40 (m, 2H).
土黄色固体； 173- 174 °C； δ 8.08 (s, 1H), 8.04 - 7.90 (m, 2H), 7.65 - 7.47 (m, 2H), 7.45 - Earthy yellow solid; 173- 174 °C; δ 8.08 (s, 1H), 8.04 - 7.90 (m, 2H), 7.65 - 7.47 (m, 2H), 7.45 -
7.26 (m, 5H), 3.83 (t, J = 4.8 Hz, 2H), 3.56 (s, 2H), 3.26 (t, J = 5.0 Hz, 2H), 2.65 - 2.50 (m,7.26 (m, 5H), 3.83 (t, J = 4.8 Hz, 2H), 3.56 (s, 2H), 3.26 (t, J = 5.0 Hz, 2H), 2.65 - 2.50 (m,
2H), 2.47 - 2.30 (m, 2H). 2H), 2.47 - 2.30 (m, 2H).
土黄色固体; 191-192 °C;S 8.12 (d, J = 7.2 Hz, 3H), 7.82 (d, J = 8.4 Hz, 2H), 7.28 (d, J = 13.2 Earthy yellow solid; 191-192 °C; S 8.12 (d, J = 7.2 Hz, 3H), 7.82 (d, J = 8.4 Hz, 2H), 7.28 (d, J = 13.2
9820 9820
Hz, 5H), 3.82 (s, 2H), 3.55 (s, 2H), 3.27 (s, 2H), 2.62 - 2.34 (m, 4H).  Hz, 5H), 3.82 (s, 2H), 3.55 (s, 2H), 3.27 (s, 2H), 2.62 - 2.34 (m, 4H).
土黄色固体； 202-203 °C； δ 8.09 (s, 1H), 7.99 (d, J = 8.4 Hz, 2H), 7.55 (d, J = 8.6 Hz, 2H), 9843 I 7.35 (d, J = 8.1 Hz, 2H), 7.26 (d, J = 3.5 Hz, 2H), 3.83 (s, 2H), 3.53 (s, 2H), 3.27 (s, 2H), 2.56 (d, J = 4.8 Hz, 2H), 2.43 (s, 2H), 1.29 (s, 9H).  Earthy yellow solid; 202-203 °C; δ 8.09 (s, 1H), 7.99 (d, J = 8.4 Hz, 2H), 7.55 (d, J = 8.6 Hz, 2H), 9843 I 7.35 (d, J = 8.1 Hz, 2H), 7.26 (d, J = 3.5 Hz, 2H), 3.83 (s, 2H), 3.53 (s, 2H), 3.27 (s, 2H), 2.56 (d, J = 4.8 Hz, 2H) , 2.43 (s, 2H), 1.29 (s, 9H).
棕色液体； δ 8.14 (t, J = 7.2 Hz, 3H), 7.84 (d, J = 8.1 Hz, 2H), 7.36 (d, J = 8.1 Hz, 2H), 7.28 9852 I - 7.19 (m, 2H), 3.84 (s, 2H), 3.54 (s, 2H), 3.28 (s, 2H), 2.58 (s, 2H), 2.45 (s, 2H), 1.42 - 1.22 (m, 9H).  Brown liquid; δ 8.14 (t, J = 7.2 Hz, 3H), 7.84 (d, J = 8.1 Hz, 2H), 7.36 (d, J = 8.1 Hz, 2H), 7.28 9852 I - 7.19 (m, 2H) , 3.84 (s, 2H), 3.54 (s, 2H), 3.28 (s, 2H), 2.58 (s, 2H), 2.45 (s, 2H), 1.42 - 1.22 (m, 9H).
褐色液体； δ 7.90- 7.85(m, 3H), 7.51 (d, J = 8.4 Hz, 2H), 7.40 - 7.25 (m, 4H), 3.84 (s, 2H), Brown liquid; δ 7.90- 7.85(m, 3H), 7.51 (d, J = 8.4 Hz, 2H), 7.40 - 7.25 (m, 4H), 3.84 (s, 2H),
9891 9891
3.52 (s, 2H), 3.36 - 3.21 (m, 2H), 2.66 (s, 3H), 2.55 (s, 2H), 2.39 (d, J = 4.8 Hz, 2H).  3.52 (s, 2H), 3.36 - 3.21 (m, 2H), 2.66 (s, 3H), 2.55 (s, 2H), 2.39 (d, J = 4.8 Hz, 2H).
土黄色固体； 184-185 °C； δ 7.99 - 7.80 (m, 3H), 7.62 - 7.45 (m, 2H), 7.40 - 7.26 (m, 5H), 9912 I 3.86 (s, 2H), 3.56 (s, 2H), 3.39 - 3.23 (m, 2H), 2.65(s, 3H), 2.58 (d, J = 4.8 Hz, 2H),  Earthy yellow solid; 184-185 °C; δ 7.99 - 7.80 (m, 3H), 7.62 - 7.45 (m, 2H), 7.40 - 7.26 (m, 5H), 9912 I 3.86 (s, 2H), 3.56 (s , 2H), 3.39 - 3.23 (m, 2H), 2.65(s, 3H), 2.58 (d, J = 4.8 Hz, 2H),
2.43-2.40 (m, 2H).  2.43-2.40 (m, 2H).
棕色液体； δ 7.89-7.86 (m, 3H), 7.51 (d, J = 8.7 Hz, 2H), 7.37 (d, J = 8.1 Hz, 2H), 7.28 (d, J 9933 I = 6.9 Hz, 2H), 4.31 (t, J = 6.6 Hz, 2H), 3.88 (s, 2H), 3.61 (s, 2H), 3.36 (s, 2H), 2.65 (s, 3H), 2.48 (s, 2H), 1.40 (s, 9H).  Brown liquid; δ 7.89-7.86 (m, 3H), 7.51 (d, J = 8.7 Hz, 2H), 7.37 (d, J = 8.1 Hz, 2H), 7.28 (d, J 9933 I = 6.9 Hz, 2H) , 4.31 (t, J = 6.6 Hz, 2H), 3.88 (s, 2H), 3.61 (s, 2H), 3.36 (s, 2H), 2.65 (s, 3H), 2.48 (s, 2H), 1.40 ( s, 9H).
白色固体； 236-237 °C ; δ 8.19-8.09 (m, 3H), 7.94 - 7.46 (m, 5H), 7.35 (t, J = 8.1 Hz, 1H),White solid; 236-237 °C ; δ 8.19-8.09 (m, 3H), 7.94 - 7.46 (m, 5H), 7.35 (t, J = 8.1 Hz, 1H),
10042 10042
4.36 - 3.91 (m, 2H), 3.91 - 3.48 (m, 3H), 3.43 - 3.29 (m, 2H), 3.19 (s, 1H).  4.36 - 3.91 (m, 2H), 3.91 - 3.48 (m, 3H), 3.43 - 3.29 (m, 2H), 3.19 (s, 1H).
浅黄色固体； δ 8.43 (s, 1H)， 8.12 (d， 2H), 7.84 (m， 3H)， 7.04 (s， 1H)， 6.86 (s， 1H)， 3.90 - 3.22 Light yellow solid; δ 8.43 (s, 1H), 8.12 (d, 2H), 7.84 (m, 3H), 7.04 (s, 1H), 6.86 (s, 1H), 3.90 - 3.22
13414 (m, 4H)， 3.50 (d， 2H), 3.50 (d， 2H). 13414 (m, 4H), 3.50 (d, 2H), 3.50 (d, 2H).
浅黄色固体； δ 8.14 (dd, 1H)， 7.89 (s， 1H)， 7.63 (dt, 2H), 7.35 (t, 1H)， 7.02 (s， 1H)， 6.68 (t, 1H). Light yellow solid; δ 8.14 (dd, 1H), 7.89 (s, 1H), 7.63 (dt, 2H), 7.35 (t, 1H), 7.02 (s, 1H), 6.68 (t, 1H).
13456 13456
3.71 (d， 2H), 3.37 (dd, 4H), 3.20 - 3.11 (m, 2H).  3.71 (d, 2H), 3.37 (dd, 4H), 3.20 - 3.11 (m, 2H).
浅黄色固体； δ 8.43 (s, 1H), 8.15 - 8.11 (m， 1H)， 8.00 (d， 1H)， 7.86 (d， 1H)， 7.77— 7.50 (m， H). Light yellow solid; δ 8.43 (s, 1H), 8.15 - 8.11 (m, 1H), 8.00 (d, 1H), 7.86 (d, 1H), 7.77-7.50 (m, H).
13435 13435
7.35 (t, 1H)， 6.84 (t, 1H)， 3.94 (d， 2H), 3.63 - 3.29 (m, 6H).  7.35 (t, 1H), 6.84 (t, 1H), 3.94 (d, 2H), 3.63 - 3.29 (m, 6H).
13477 浅黄色固体， δ 8.19— 8.06 (m， 2H), 7.89 (s， 1H)， 7.70 - 7.55 (m， 3H)， 7.43 (dd, 1H)， 6.85 (t, 1H). 3.71 (d， 2H), 3.45 - 3.08 (m， 4H)， 3.08 - 2.93 (m,2H). 13477 pale yellow solid, δ 8.19 - 8.06 (m, 2H), 7.89 (s, 1H), 7.70 - 7.55 (m, 3H), 7.43 (dd, 1H), 6.85 (t, 1H). 3.71 (d, 2H), 3.45 - 3.08 (m, 4H), 3.08 - 2.93 (m, 2H).
浅黄色固体； δ 8.32 (d, 3H), 8.14 (d, J = 7.0 Hz, 10H), 7.84 (d， J = 8.2 Hz, 7H)， 7.04 (s， 1H)， Light yellow solid; δ 8.32 (d, 3H), 8.14 (d, J = 7.0 Hz, 10H), 7.84 (d, J = 8.2 Hz, 7H), 7.04 (s, 1H),
13498 13498
6.86 (t, 1H)， 4.46 - 3.96 (m， 4H)， 3.85 (d， 2H), 3.65 (d， 2H).  6.86 (t, 1H), 4.46 - 3.96 (m, 4H), 3.85 (d, 2H), 3.65 (d, 2H).
浅黄色固体； δ 8.49 (s, 1H)， 8.09 (s， 1H)， 7.96 - 7.81 (m， 1H)， 7.66 - 7.43 (m， 1H)， 7.34 (t, 2H), Light yellow solid; δ 8.49 (s, 1H), 8.09 (s, 1H), 7.96 - 7.81 (m, 1H), 7.66 - 7.43 (m, 1H), 7.34 (t, 2H),
13540 13540
7.14 - 6.92 (m, 1H)， 6.86 (t, 1H)， 3.98 - 3.31 (m, 4H)， 3.31 - 3.30 (m, 2H), 3.23 (d， 2H).  7.14 - 6.92 (m, 1H), 6.86 (t, 1H), 3.98 - 3.31 (m, 4H), 3.31 - 3.30 (m, 2H), 3.23 (d, 2H).
浅黄色固体； δ 8.54 - 8.33 (m， 1H)， 8.10 (s， 1H)， 7.93 - 7.74 (m， 1H)， 7.67 (t, J = 1H)， 7.53 (dd， Light yellow solid; δ 8.54 - 8.33 (m, 1H), 8.10 (s, 1H), 7.93 - 7.74 (m, 1H), 7.67 (t, J = 1H), 7.53 (dd,
13561 13561
2H), 7.02 (s，lH)， 6.88 (dt, 1H)， 4.09 (d， 2H), 3.48 (dd， 4H)， 3.16 (d， 2H).  2H), 7.02 (s,lH), 6.88 (dt, 1H), 4.09 (d, 2H), 3.48 (dd, 4H), 3.16 (d, 2H).
浅黄色固体； δ 8.31 (dd, 1 Hz, 1H)， 8.10 (s, 1H)， 7.90 (s, 1H)， 7.61 (t, 1 H)， 7.34 (dd， 2H), 7.01 Light yellow solid; δ 8.31 (dd, 1 Hz, 1H), 8.10 (s, 1H), 7.90 (s, 1H), 7.61 (t, 1 H), 7.34 (dd, 2H), 7.01
13582 13582
(s, 1H)， 6.86 (dd, 1H)， 3.90 (d， 2H), 3.70 (d， 2H), 3.42 (dd, 4H).  (s, 1H), 6.86 (dd, 1H), 3.90 (d, 2H), 3.70 (d, 2H), 3.42 (dd, 4H).
浅黄色固体； δ 8.21 (dd, lH)，8.10 (s， 1H)， 7.83 (t, 2H), 7.75 - 7.51 (m， 2H), 7.49 (d， 1H), 7.01 - Light yellow solid; δ 8.21 (dd, lH), 8.10 (s, 1H), 7.83 (t, 2H), 7.75 - 7.51 (m, 2H), 7.49 (d, 1H), 7.01 -
13603 13603
6.82 (m, 1H)， 6.79 (t, 1H)， 4.01 (s， 2H), 3.86 - 3.17 (m, 6H).  6.82 (m, 1H), 6.79 (t, 1H), 4.01 (s, 2H), 3.86 - 3.17 (m, 6H).
浅黄色固体； δ 8.33 - 8.07 (m， 2H), 7.93 - 7.79 (m， 2H), 7.79 - 7.56 (m， 2H), 7.04 (s， 1H)， 6.87 Light yellow solid; δ 8.33 - 8.07 (m, 2H), 7.93 - 7.79 (m, 2H), 7.79 - 7.56 (m, 2H), 7.04 (s, 1H), 6.87
13645 13645
(t, 1H)， 3.99 (d， 2H), 3.40 (d， 6H)  (t, 1H), 3.99 (d, 2H), 3.40 (d, 6H)
浅黄色固体； δ 8.41 (s, 1H)， 8.32 - 8.12 (m， 2H), 7.95 - 7.76 (m， 2H), 7.76 - 7.47 (m， 2H), 7.05 Light yellow solid; δ 8.41 (s, 1H), 8.32 - 8.12 (m, 2H), 7.95 - 7.76 (m, 2H), 7.76 - 7.47 (m, 2H), 7.05
13624 (s, 1H)， 6.87 (t, 1H)， 4.00 (d, J = 38.1 Hz, 12H), 3.82 - 2.74 (m， 4H)， 3.61 - 3.02 (m， 2H), 3.68 - 2.11 (m, 2H) 13624 (s, 1H), 6.87 (t, 1H), 4.00 (d, J = 38.1 Hz, 12H), 3.82 - 2.74 (m, 4H), 3.61 - 3.02 (m, 2H), 3.68 - 2.11 (m, 2H)
浅黄色固体； δ 8.41 (s, 1H)， 8.32 - 8.12 (m， 2H), 7.95 - 7.76 (m， 2H), 7.76 (s，lH)， 7.05 (s， 1H)， Light yellow solid; δ 8.41 (s, 1H), 8.32 - 8.12 (m, 2H), 7.95 - 7.76 (m, 2H), 7.76 (s, lH), 7.05 (s, 1H),
13645 6.87 (t, 1H)， 4.00 (d, J = 38.1 Hz, 12H), 3.82 - 2.74 (m, 4H)， 3.61 - 3.02 (m, 2H), 3.68 - 2.11 (m, 2H) 13645 6.87 (t, 1H), 4.00 (d, J = 38.1 Hz, 12H), 3.82 - 2.74 (m, 4H), 3.61 - 3.02 (m, 2H), 3.68 - 2.11 (m, 2H)
浅黄色固体； δ 8.41 (s, 1H)， 8.32 - 8.12 (m， 3H)， 7.95 (s， 1H)， 7.76 (s，lH)， 7.05 (s， 1H)， 6.87 (t, Light yellow solid; δ 8.41 (s, 1H), 8.32 - 8.12 (m, 3H), 7.95 (s, 1H), 7.76 (s, lH), 7.05 (s, 1H), 6.87 (t,
13666 13666
1H)， 4.00 (d, J = 38.1 Hz, 12H), 3.82 - 2.74 (m， 4H)， 3.61 - 3.02 (m, 2H), 3.68 - 2.11 (m， 2H) 浅黄色固体 ,δ 8.21 (s， 1H)， 7.83 (s， 1H)， 7.75 - 7.51 (m， 5H)， 7.49 (s， 1H)， 7.01 - 6.82 (m， 4H)， 1H), 4.00 (d, J = 38.1 Hz, 12H), 3.82 - 2.74 (m, 4H), 3.61 - 3.02 (m, 2H), 3.68 - 2.11 (m, 2H) light yellow solid, δ 8.21 (s, 1H), 7.83 (s, 1H), 7.75 - 7.51 (m, 5H), 7.49 (s, 1H), 7.01 - 6.82 (m, 4H),
13688 13688
4.01 (s， 2H), 3.86 - 3.17 (m, 6H).  4.01 (s, 2H), 3.86 - 3.17 (m, 6H).
浅黄色固体； δ 8.21 (s， 1H)， 7.83 (s， 1H)， 7.75 - 7.51 (m， 5H)， 7.49 (s， 1H)， 7.01 - 6.82 (m， 4H)， Light yellow solid; δ 8.21 (s, 1H), 7.83 (s, 1H), 7.75 - 7.51 (m, 5H), 7.49 (s, 1H), 7.01 - 6.82 (m, 4H),
13709 13709
4.01 (s， 2H), 3.82 - 2.74 (m， 4H)， 3.61 - 3.02 (m， 2H).  4.01 (s, 2H), 3.82 - 2.74 (m, 4H), 3.61 - 3.02 (m, 2H).
浅黄色固体； δ 8.21 (s， 1H)， 7.83 (s， 1H)， 7.75 - 7.51 (m， 5H)， 7.49 (d， 2H), 7.01 - 6.82 (m， 4H)， Light yellow solid; δ 8.21 (s, 1H), 7.83 (s, 1H), 7.75 - 7.51 (m, 5H), 7.49 (d, 2H), 7.01 - 6.82 (m, 4H),
13730 13730
4.01 (s， 2H), 3.82 - 2.74 (m， 4H)， 3.61 - 3.02 (m， 2H).  4.01 (s, 2H), 3.82 - 2.74 (m, 4H), 3.61 - 3.02 (m, 2H).
浅黄色固体； δ 8.23 (s， 1H)， 7.89 (s， 1H)， 7.79 - 7.55 (m， 5H)， 7.49 (d， 2H), 7.02 - 6.80 (m， 4H)， Light yellow solid; δ 8.23 (s, 1H), 7.89 (s, 1H), 7.79 - 7.55 (m, 5H), 7.49 (d, 2H), 7.02 - 6.80 (m, 4H),
13761 13761
4.01 (s， 2H), 3.80 - 2.75 (m， 4H)， 3.69 - 3.82 (m， 2H). 制剂实施例 (各组分加入量均为重量百分含量， 活性化合物折百后计量加入） 实施例 8: 30%可湿性粉剂  4.01 (s, 2H), 3.80 - 2.75 (m, 4H), 3.69 - 3.82 (m, 2H). Formulation examples (all components are added in weight percent, and the active compound is metered in.) Example 8: 30% wettable powder
化合物 4891 30%  Compound 4891 30%
十二垸基硫酸钠 2%  Sodium decyl sulfate 2%
木质素磺酸钠 3%  Sodium lignosulfonate 3%
萘磺酸甲醛缩合物 5%  Naphthalenesulfonic acid formaldehyde condensate 5%
轻质碳酸钙 补足至 100%  Light calcium carbonate to 100%
将化合物 4891及其他组分充分混合， 经超细粉碎机粉碎后， 即得到 30%的可湿性粉剂 实施例 9: 40%浓悬浮剂  Compound 4891 and other components were thoroughly mixed and pulverized by an ultrafine pulverizer to obtain 30% wettable powder. Example 9: 40% concentrated suspending agent
化合物 5035 40%  Compound 5035 40%
乙二醇 10%  Ethylene glycol 10%
壬基苯酚聚乙二醇醚 6% 木质素磺酸钠 10% Nonylphenol polyglycol ether 6% Sodium lignosulfonate 10%
羧甲基纤维素 1%  Carboxymethyl cellulose 1%
37%甲醛水溶液 0.2%  37% formaldehyde solution 0.2%
75%硅油水乳液 0.8%  75% silicone oil emulsion 0.8%
水 补足至 100%  Water to 100%
将化合物 5035及其他组分充分混合， 由此得到的浓悬浮剂， 用水稀释所得悬浮剂可得 到任何所需浓度的稀释液。  The compound 5035 and the other components are thoroughly mixed, and the resulting suspension concentrate is diluted with water to obtain a desired concentration of the diluent.
实施例 10: 60%水分散性粒剂  Example 10: 60% water dispersible granules
化合物 5057 60%  Compound 5057 60%
萘磺酸钠甲醛缩合物 12%  Sodium naphthalene sulfonate formaldehyde condensate 12%
N-甲基- N-油酰基-牛磺酸钠 8%  N-methyl-N-oleoyl-taurate sodium 8%
聚乙烯吡咯垸酮 2%  Polyvinylpyrrolidone 2%
羧甲基纤维素 2%  Carboxymethyl cellulose 2%
高岭土 补足至 100%  Kaolin is made up to 100%
加水捏合后， 加入 10-100目筛网的造粒机中进
Figure imgf000052_0001
生物活性测定实施例 After adding water and kneading, add into the granulator of 10-100 mesh screen.
Figure imgf000052_0001
Biological activity assay example
用本发明化合物进行了杀虫杀螨活性测定试验。 测定的方法及测试结果如下： 实施例 11 : 杀虫活性测定  The insecticidal and acaricidal activity assay was carried out using the compound of the present invention. The method of determination and the test results are as follows: Example 11: Determination of insecticidal activity
取 2.5 mL丙酮 /甲醇 (1 : 1)的混合溶剂加入到盛有 3 mg待测化合物 (纯度以 100%计)的称 量瓶中， 搅拌使其充分溶解， 加入 2.5 mL含有 2%。吐温 80的静置自来水， 搅拌均匀后得到 600 mg/L的待测化合物溶液 5 mL。 供试靶标为： 粘虫、 小菜蛾、 桃蚜。 采用 Airbrush喷雾 法对试虫进行喷雾处理， 其中粘虫、 小菜蛾处理后 3天调查试虫的死亡率； 桃蚜在喷雾处理 2天内调查试虫的死亡率。  A mixed solvent of 2.5 mL of acetone/methanol (1:1) was added to a weighing flask containing 3 mg of the test compound (100% purity), and the mixture was thoroughly dissolved by stirring, and 2.5 mL was added to contain 2%. The Tween 80 was allowed to stand in tap water, and after stirring, a solution of 600 mg/L of the test compound was obtained in 5 mL. The test targets were: armyworm, diamondback moth, peach aphid. The test insects were sprayed by Airbrush spray method, in which the mortality of the test insects was investigated 3 days after the treatment of the armyworm and the diamondback moth; the mortality of the test insects was investigated within 2 days of the spray treatment.
部分测试结果如下：  Some test results are as follows:
药液浓度为 600 mg/L时， 化合物 9155等对小菜蛾的致死率为 100%。  When the concentration of the drug solution was 600 mg/L, the lethal rate of compound 9155 against Plutella xylostella was 100%.
药液浓度为 600 mg/L时， 9155等对粘虫的致死率大于 70%。  When the concentration of the drug solution is 600 mg/L, the lethal rate of 9155 and other insects is more than 70%.
药液浓度为 600 mg/L时， 化合物 5573、 5769、 13775、 13796、 13826等对桃蚜的致死 率为 100% ; 5705、 5789、 13456、 13435、 13477、 13645、 13871、 14128等对桃蚜的致死率 大于 70%。  When the concentration of the drug solution is 600 mg/L, the lethal rate of compounds 5573, 5769, 13775, 13796, 13826 and so on is 100%; 5705, 5789, 13456, 13435, 13477, 13645, 13871, 14128, etc. The mortality rate is greater than 70%.
实例 12: 对朱砂叶螨成螨室内毒力测定：  Example 12: Determination of virulence in the cinnabar
待测化合物称量后用丙酮制成母液，按试验设计用含有 0.1%吐温 80的静置自来水稀释系 列浓度。 取两片真叶菜豆苗， 接种朱砂叶螨成螨并调查基数后， 用手持喷雾器喷雾处理， 每 处理 3次重复， 处理后置于标准观察室， 72小时后调查存活螨数， 计算死亡率。  After the compound to be tested was weighed, the mother liquor was made of acetone, and the concentration of the series was diluted according to the experimental design with static tap water containing 0.1% Tween 80. Two leaves of true leafy bean seedlings were inoculated, and the cinnabar was inoculated into a sputum and the base was investigated. The mixture was sprayed with a hand-held sprayer, and each treatment was repeated three times. After treatment, it was placed in a standard observation room. After 72 hours, the survival number was counted and the mortality was calculated.
部分测试结果如下：  Some test results are as follows:
药液浓度为 100 mg/L时， 化合物 4891、 5035、 5041、 5053、 5057、 5097、 5552、 5573、 5594、 5663、 5664、 5684、 5685、 5693、 5705、 5706、 5768、 5789、 5790、 13414、 13435、 13456、 13477、 13624等对朱砂叶螨的致死率为 100%， 4869对朱砂叶螨的致死率为 95%， 5510对朱砂叶螨的致死率为 97%。  When the concentration of the chemical solution is 100 mg/L, the compounds 4891, 5035, 5041, 5053, 5057, 5097, 5552, 5573, 5594, 5663, 5664, 5684, 5685, 5693, 5705, 5706, 5768, 5789, 5790, 13414 The lethal rate of 13435, 13456, 13477, 13624 and other cinnabar mites was 100%, the lethal rate of 4869 to cinnabarinus was 95%, and the lethal rate of 5510 to cinnabarinus was 97%.
药液浓度为 10 mg/L时， 化合物 4891、 5035、 5053、 5057、 5706、 5552、 5663、 5664、 5684、 5685 、 5705、 5789、 13414、 13624等对朱砂叶螨的致死率为 100%， 5573对朱砂叶 螨的致死率为 98%， 化合物 5041对朱砂叶螨的致死率为 95%。 进行了部分化合物与对照药剂及中间体的活性对比试验， 测试结果见表 288。 When the concentration of the chemical solution is 10 mg/L, the mortality rate of the compounds 4891, 5035, 5053, 5057, 5706, 5552, 5663, 5664, 5684, 5685, 5705, 5789, 13414, 13624, etc. on the cinnabar leafhopper is 100%. 5573 pairs of cinnabar leaves The mortality rate of cockroach was 98%, and the lethal rate of compound 5041 to cinnabarinus was 95%. The activity comparison test of some compounds with the control agents and intermediates was carried out, and the test results are shown in Table 288.
表 288 对朱砂叶螨的致死率  Table 288 Lethality rate of Tetranychus cinnafolia
Figure imgf000053_0001
KC19 0 0 0
Figure imgf000053_0001
KC19 0 0 0
KC20 44 11 3  KC20 44 11 3
KC21 38 14 11  KC21 38 14 11
KC22 0 0 0  KC22 0 0 0
KC23 3 2 0  KC23 3 2 0
KC24 38 11 4  KC24 38 11 4
KC25 25 10 0 对照化合物 KCl至 KC25均为发明人自制， 其中 KC1、 KC3、 KC4、 KC5、 KC7、 KC8、 KC10、 KC17、KC18及 KC19与 US2013072497中的部分化合物类似， KC15是 CN102015627 中报道的化合物， KC20、 KC21、 KC22是 CN101381342中报道的化合物。  KC25 25 10 0 The control compounds KCl to KC25 were all made by the inventors, among which KC1, KC3, KC4, KC5, KC7, KC8, KC10, KC17, KC18 and KC19 are similar to some compounds in US2013072497, and KC15 is a compound reported in CN102015627. KC20, KC21, and KC22 are compounds reported in CN101381342.
Figure imgf000054_0001
Figure imgf000054_0001
Figure imgf000055_0001
Figure imgf000055_0001
08Ζ而 SIOZ OAV 08Ζ and SIOZ OAV

Claims

权 利 要 种芳基吡 (嘧)啶 Rights to arylpyrimidines
Figure imgf000056_0001
Figure imgf000056_0001
式中： In the formula:
！^选自氢、 卤素、 CN、 N02、 巯基、 -C12垸基、 卤代 CrC12垸基、 12垸氧基、 卤 代 12垸氧基、 氰基 12垸氧基、 12垸硫基、 ¾代 12垸硫基、 -C12垸氧基 Ci-Ci2 ¾υ¾ \ ί Ci-Ci2 C1-C12 ¾υ¾ Ci-Cn ¾¾¾¾¾ C1-C12 ¾υ¾ \ ί Ci-Cn ¾¾¾¾¾ -C12垸基、 卤代 -C12垸基氨基、 哌啶基、 四氢吡咯基、 N-甲基哌嗪基、 吗啉基、 C2-C12 烯基、 卤代 C2-C12烯基、 ¾ 12烯氧基、 卤代 ¾ 12烯氧基、 C2-C12炔基、 卤代 C2-C12炔基、 ¾ 12炔氧基、 卤代 ¾ 12炔氧基、 12垸基亚磺酰基、 -C12垸基磺酰基、 C3-C12环垸 基、 ¾代 12垸基亚磺酰基、 ¾代 d-C12垸基磺酰基、 d-C12垸氧基羰基、 ¾代 d-C12 垸基羰基、 12垸基羰基氧基、 12垸基羰基氨基、 d-C12垸基磺酰基氧基、 12垸 氧基 12垸氧基、 d-C12垸氧基羰基 C C12垸基、 C C12垸氧基羰基氨基、 C C12垸氧基 羰基 ^ ^垸氧基、 CHO、 C02H、 C02Na、 C02NH4、 NR7R8、 C(=0)NR7R8、 OC(=0)NR7R8、 C(=S)NR7R8、 S02NR7R8或 R6; m选自 0至 5的整数； 当 m大于 1时， 可相同或不同； ! ^ is selected from hydrogen, halogen, CN, N0 2 , mercapto group, -C 12 alkyl group, halogenated C r C 12 alkyl group, 12 alkyloxy group, halogenated 12 alkyloxy group, cyano group 12 alkyloxy group, 12 alkyl group Sulfide group, ¾ generation 12 alkylthio group, -C 12 alkoxy group Ci-Ci2 ¾υ¾ \ ί Ci-Ci2 C1-C12 ¾υ¾ Ci-Cn ¾¾¾¾¾ C1-C12 ¾υ¾ \ ί Ci-Cn ¾¾¾¾¾ -C 12 alkyl group, halo Substituted -C 12 alkyl amino, piperidinyl, tetrahydropyrrolyl, N-methylpiperazinyl, morpholinyl, C 2 -C 12 alkenyl, halogenated C 2 -C 12 alkenyl, ¾ 12 alkenyl Oxygen group, halogenated ¾12 alkenyloxy group, C 2 -C 12 alkynyl group, halogenated C 2 -C 12 alkynyl group, ¾ 12 alkynyloxy group, halogenated ¾ 12 alkynyloxy group, 12 alkylsulfinyl group, -C 12 alkylsulfonyl group, C 3 -C 12 cycloalkyl group, ¾ generation 12 alkylsulfinyl group, ¾ generation dC 12 alkylsulfonyl group, dC 12 alkyloxycarbonyl group, ¾ generation dC 12 alkylcarbonyl group, 12 alkylcarbonyloxy, 12 alkylcarbonylamino, dC 12 alkylsulfonyloxy , 12 alkyloxy 12 alkyloxy, dC 12 alkoxycarbonyl CC 12 alkyl, CC 12 alkyloxycarbonylamino, CC 12Alkoxycarbonyl ^ ^Alkyloxy, CHO, C0 2 H, C0 2 Na, C0 2 NH 4 , NR 7 R 8 , C(=0)NR 7 R 8 , OC(=0)NR 7 R 8 , C(=S)NR 7 R 8 , S0 2 NR 7 R 8 or R 6; m is selected from an integer from 0 to 5; when m is greater than 1, it can be the same or different;
R2选自氢、 卤素、 氰基 d-C12垸基、 d-C12垸基、 卤代 C C12垸基、 12垸氧基、 卤 代 12垸氧基、 氰基 12垸氧基、 12垸硫基、 ¾代 12垸硫基、 d-C12垸氧基 Ci-Ci2 ¾υ¾ \ ί Ci-Ci2 C1-C12 ¾υ¾ Ci-Cn ¾¾¾¾¾ C1-C12 ¾υ¾ \ ί Ci-Cn ¾¾¾¾¾ C C12垸基、 12垸基亚磺酰基、 d-C12垸基磺酰基、 C3-C6环垸基或 R6; R 2 is selected from hydrogen, halogen, cyano dC 12 alkyl, dC 12 alkyl, halogenated CC 12 alkyl, 12 alkoxy, halogenated 12 alkyloxy, cyano 12 alkyloxy, 12 alkylthio , ¾ generation 12 alkylthio group, dC 12 alkoxy group Ci-Ci2 ¾υ¾ \ ί Ci-Ci2 C1-C12 ¾υ¾ Ci-Cn ¾¾¾¾¾ C1-C12 ¾υ¾ \ ί Ci-Cn ¾¾¾¾¾ CC 12 alkyl group, 12 alkyl sulfenic group Acyl group, dC 12 alkylsulfonyl group, C 3 -C 6 cycloalkyl group or R 6;
Ra、 Rb、 Rc、 Rd、 Re Rf、 Rg和 Rh各自独立的表示氢原子、 C C4垸基、 卤代 C C4垸 基、 卤代 C C4垸氧基或 d-C4垸氧羰基； ！^与 Rh—起或者 Rc与 Rf—起可以结合形成饱和 的五元环、 六元环或者七元环； R a , R b , R c , R d , R e R f , R g and R h each independently represent a hydrogen atom, CC 4 alkyl group, halogenated CC 4 alkyl group, halogenated CC 4 alkyloxy group or dC 4 alkyloxycarbonyl; ! ^ together with R h or R c and R f can be combined to form a saturated five-membered ring, a six-membered ring or a seven-membered ring;
Xi选自 N或 CR3; Xi is selected from N or CR 3;
R3选自氢、 CN、 N02、 CONHNH2、 C(=0)NR7R8、 C(=S)NR7R8、 d-C12垸氧基羰基、 R 3 is selected from hydrogen, CN, N0 2 , CONHNH 2 , C(=0)NR 7 R 8 , C(=S)NR 7 R 8 , dC 12 alkyloxycarbonyl,
C(=0)N=CR7R8、 C02NR7R8、 C02N=CR7R8、 CONHN=CR7NR7R8或 C(=0)NR7N=CR7R8; C(=0)N=CR 7 R 8 , C0 2 NR 7 R 8 , C0 2 N=CR 7 R 8 , CONHN=CR 7 NR 7 R 8 or C(=0)NR 7 N=CR 7 R 8 ;
X2选自 (CR7R8)k、 CO(CR7R8)p、（CR7R8)pCO、 SOq(CR7R8)p或 (CR7R8)pSOq; X 2 is selected from (CR 7 R 8 ) k , CO (CR 7 R 8 ) p , (CR 7 R 8 ) p CO, SOq (CR 7 R 8 ) p or (CR 7 R 8 ) pSOq;
k选自 1、 2或 3; p选自 0、 1、 2或 3; q选自 0、 1或 2; k is selected from 1, 2 or 3; p is selected from 0, 1, 2 or 3; q is selected from 0, 1 or 2;
选自氢、 NH2、 CrC12垸基、 -C12卤代垸基、 12垸氧基、 d-C12卤代垸氧基、 苯基或杂芳基， 所述的苯基或杂芳基环上还可以含有 1-3个下述取代基团： F、 Cl、 Br、 I、 CN、 N02、 CH3、 C(CH3)3、 OCH3、 C02CH3、 C02CH2CH3、 S02CH3、 OCH2CF3、 CF3或 OCF3; Selected from hydrogen, NH 2 , C r C 12 alkyl, -C 12 haloalkyl, 12 alkyloxy, dC 12 haloalkyloxy, phenyl or heteroaryl, the phenyl or heteroaryl The base ring may also contain 1-3 of the following substituent groups: F, Cl, Br, I, CN, N0 2 , CH 3 , C(CH 3 ) 3 , OCH 3 , C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 , OCH 2 CF 3 , CF 3 or OCF 3;
Y 选自 -CO-、 -SO2-、 -(CR7R8)t-、 -CH=CHCHR7-、 - (CR7R8)tCO-、 -CH=CHCO-、 -S(CR7R8)tCO-、 -N(CR7R8)tCO-、 -0(CR7R8)tCO-、 -S(CR7R8)tS02-、 -N(CR7R8)tS02-、 -0(CR7R8)tS02-、 -CONR7CO-、 -S02NR7C(=S) -、 -S02NR7C(=0)-、 -CONR7C(=S) -、 -NR7CO (CR7R8)t -、 -CO(CR7R8)r -NR7CO-或 -NR7C(=S)-; t选自 0、 1或 2; x选自 0或 1; Y is selected from -CO-, -SO2-, -(CR 7 R 8 ) t -, -CH=CHCHR 7 -, - (CR 7 R 8 ) t CO-, -CH=CHCO-, -S(CR 7 R 8 ) t CO-, -N(CR 7 R 8 ) t CO-, -0(CR 7 R 8 ) t CO-, -S(CR 7 R 8 ) t S0 2 -, -N(CR 7 R 8 ) t S0 2 -, -0(CR 7 R 8 ) t S0 2 -, -CONR 7 CO-, -S0 2 NR 7 C(=S) -, -S0 2 NR 7 C(=0)-, -CONR 7 C(=S) -, -NR 7 CO (CR 7 R 8 ) t -, -CO(CR 7 R 8 )r -NR 7 CO- or -NR 7 C(=S)-; choose t from 0, 1 or 2; x is selected from 0 or 1;
Q选自被 n个各自独立的 取代的苯基或杂芳基； Q is selected from phenyl or heteroaryl substituted by n independently substituted phenyl or heteroaryl;
R5选自卤素、 CN、 N02、 -C12垸基、 卤代 -C12垸基、 C3-C12环垸基、 12垸氧基、 卤代 12垸氧基、 12垸硫基、卤代 12垸硫基、 C2-C12烯基、卤代 C2-C12録基、 C2-C12 炔基、 卤代 C2-C12炔基、 ¾ 12烯氧基、 卤代 ¾ 12烯氧基、 ¾ 12炔氧基、 卤代 ¾ 12炔 氧基、 12垸基亚磺酰基、 ¾代 12垸基亚磺酰基、 -C12垸基磺酰基、 ¾代 12垸 基磺酰基、 -C12垸基羰基、 ¾代 d-C12垸基羰基、 12垸基羰基氧基、 12垸基羰基 氨基、 -C12垸基磺酰基氧基、 d-C12垸氧基羰基、 CrC12垸氧基 12垸氧基、 12垸 氧基羰基 -C12垸基、 d-C12垸氧基羰基氨基、 -C12垸氧基羰基 12垸氧基、 COR8、 C02R7、 CONR7R8、 NR7R8、 NR7COR8、 NR7COR8、 NR8C02R7、 SOqR8、 S02NR7R8、 芳基、 杂芳基、 芳胺基、 芳垸基氧基、 芳氧基或杂芳胺基， 所述的芳基、 杂芳基、 芳胺基、 芳垸基 氧基、芳氧基或杂芳胺基环上的氢还可以进一步被 1-4个下述基团所取代： 卤素、 CN、 N02、 d-C12垸基、 -C12卤代垸基、 d-C12卤代垸氧基、 d-C12垸氧基、 -C12垸氧基羰基或 -C12 垸基磺酰基； R 5 is selected from halogen, CN, N0 2 , -C 12 alkyl group, halogenated -C 12 alkyl group, C 3 -C 12 cycloalkyl group, 12 alkyloxy group, halogenated 12 alkyloxy group, 12 alkylthio group , Halogenated C 2 -C 12 alkylthio group, C 2 -C 12 alkenyl group, Halogenated C 2 -C 12 alkyl group, C 2 -C 12 alkynyl group, Halogenated C 2 -C 12 alkynyl group, ¾ 12 alkenyloxy group, Halogenated ¾ 12 alkenyloxy, ¾ 12 alkynoxy, halogenated ¾ 12 alkyne Oxygen, 12 alkylsulfinyl, -C 12 alkylsulfonyl, -C 12 alkylsulfonyl, -C 12 alkylcarbonyl, -C 12 alkylcarbonyl, 12 alkylcarbonyloxy, 12 alkylcarbonylamino, -C 12 alkylsulfonyloxy, dC 12 alkyloxycarbonyl, C r C 12 alkyloxy 12 alkyloxy, 12 alkyloxycarbonyl -C 12 Alkyl, dC 12 alkoxycarbonylamino, -C 12 alkyloxycarbonyl 12 alkyloxy, COR 8 , C0 2 R 7 , CONR 7 R 8 , NR 7 R 8 , NR 7 COR 8 , NR 7 COR 8 , NR 8 C0 2 R 7 , SOqR 8 , S0 2 NR 7 R 8 , aryl group, heteroaryl group, arylamine group, arylalkyloxy group, aryloxy group or heteroarylamino group, the aryl group, The hydrogen on the heteroaryl, arylamine, arylalkyloxy, aryloxy or heteroarylamino ring can be further substituted by 1 to 4 of the following groups: halogen, CN, N0 2 , dC 12 Alkyl group, -C 12 haloalkyl group, dC 12 haloalkyloxy group, dC 12 alkyloxy group, -C 12 alkyloxycarbonyl group or -C 12 alkylsulfonyl group;
n选自 0至 5的整数； 当 n大于 1时， R5可相同或不同； n is selected from an integer from 0 to 5; when n is greater than 1, R 5 can be the same or different;
R6选自未取代的或被 1-5个独立选自以下基团进一步取代的苯基、苯甲酰基、苯氧基羰 基、 苯基胺基羰基、 苯基 -C6垸基、 萘基、 萘基 d-C6垸基、 杂芳基、 杂芳基羰基、 杂芳 基氧基羰基、 杂芳基胺基羰基或杂芳基 CrC6垸基： 卤素、 硝基、 氰基、 巯基、 -C12垸基、 卤代 d-C12垸基、 C3-C12环垸基、 12垸氧基、 卤代 12垸氧基、 12垸硫基、 卤代 12垸硫基、 C2-C12烯基、 卤代 C2-C12烯基、 C2-C12炔基、 卤代 C2-C12炔基、 C2-C12烯氧 基、 卤代 C2-C12烯氧基、 C2-C12炔氧基、 卤代 C2-C12炔氧基、 -C12垸基亚磺酰基、 卤代 12垸基亚磺酰基、 d-C12垸基磺酰基、 ¾代 d-C12垸基磺酰基、 C C12垸基羰基、 卤代 C C12垸基羰基、 12垸基羰基氧基、 12垸基羰基氨基、 d-C12垸基磺酰基氧基、 d-C12 垸氧基羰基、 C C12垸氧基 12垸氧基、 d-C12垸氧基羰基 C C12垸基、 12垸氧基羰 基氨基、 C C12垸氧基羰基 12垸氧基、 CHO、C02H、C02Na、C02NH4、NR7R8、C(=0)NR7R8、 OC(=0)NR7R8、 C(=S)NR7R8或 S02NR7R8; R 6 is selected from phenyl, benzoyl, phenoxycarbonyl, phenylaminocarbonyl, phenyl-C 6 alkyl, naphthyl that is unsubstituted or further substituted by 1 to 5 groups independently selected from the following groups , naphthyl dC 6 alkyl, heteroaryl, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroarylaminocarbonyl or heteroaryl C r C 6 alkyl: halogen, nitro, cyano, mercapto , -C 12 alkyl, halogenated dC 12 alkyl, C 3 -C 12 cycloalkyl, 12 alkyloxy, halogenated 12 alkoxy, 12 alkylthio, halogenated 1 2 alkyl, C 2 -C 12 alkenyl, halogenated C 2 -C 12 alkenyl, C 2 -C 12 alkynyl, halogenated C 2 -C 12 alkynyl, C 2 -C 12 alkenyloxy, halogenated C 2 -C 12 Alkenyloxy, C 2 -C 12 alkynyloxy, halogenated C 2 -C 12 alkynyloxy, -C 12 alkylsulfinyl, halogenated 1 2 alkylsulfinyl, dC 12 alkylsulfonyl, ¾ generation dC 12 alkylsulfonyl, CC 12 alkylcarbonyl, halogenated CC 12 alkylcarbonyl, 12 alkylcarbonyloxy, 12 alkylcarbonylamino, dC 12 alkylsulfonyloxy, dC 12 alkyloxy Carbonyl, CC 12 alkoxycarbonyl 12 alkyloxy, dC 12 alkyloxycarbonyl CC 12 alkyl, 12 alkyloxycarbonylamino, CC 12 alkyloxycarbonyl 12 alkyloxy, CHO, C0 2 H, C0 2 Na , C0 2 NH 4 , NR 7 R 8 , C(=0)NR 7 R 8 , OC(=0)NR 7 R 8 , C(=S)NR 7 R 8 or S0 2 NR 7 R 8 ;
R7、 R8可相同或不同， 分别选自氢、 氰基、 SCN、 甲酰基、 C C12垸基、 卤代 C C12 垸基、 12垸氧基、 ¾代^ 12垸氧基、 12垸硫基、 ¾代 12焼硫基、 d-C12垸基 羰基、 d-C12垸氧基羰基、 d-C12垸氧基羰基 d-C12垸基、 d-C12垸基亚磺酰基、 12垸 基磺酰基、 氰基 d-C12垸基、 羟基 d-C12垸基、 C3-C12环垸基或 C C12垸基氨基。 R 7 and R 8 may be the same or different, and are respectively selected from hydrogen, cyano group, SCN, formyl group, CC alkyl group, halogenated CC alkyl group, alkyloxy group, substituted alkyloxy group, and alkyl group. Thio group, ¾-generation 12- alkylthio group, dC 12 -alkylcarbonyl group, dC 12 -alkyloxycarbonyl group, dC 12 -alkyloxycarbonyl group, dC 12 -alkyl group, dC 12- alkylsulfinyl group, 12 -alkylsulfonyl group, cyano group dC 12 alkyl, hydroxyl dC 12 alkyl, C 3 -C 12 cycloalkyl or CC 12 alkyl amino.
2、 根据权利要求 1所述的化合物， 其特征在于： 通式 (I)中 2. The compound according to claim 1, characterized in that: in general formula (I)
选自氢、 卤素、 CN、 N02、 巯基、 d-C8垸基、 卤代 d-C8垸基、 C C8垸氧基、 卤 代 d-C8垸氧基、 氰基 d-C8垸氧基、 C C8焼硫基、 ¾代 8垸硫基、 C C8垸氧基 C C8 垸基、 ¾代 -0¾垸氧基 C C8垸基、 d-C8垸硫基 C C8垸基、 ^代 C C8焼硫基 C C8垸 基、 卤代 C C8垸基氨基、 哌啶基、 四氢吡咯基、 N-甲基哌嗪基、 吗啉基、 C2-C8烯基、 卤 代 C2-C8烯基、 C2-C8烯氧基、 卤代 C2-C8烯氧基、 C2-C8炔基、 卤代 C2-C8炔基、 C2-C8炔氧 基、 卤代 C2-C8炔氧基、 d-C8垸基亚磺酰基、 d-C8垸基磺酰基、 C3-C8环垸基、 卤代 d-C8 垸基亚磺酰基、 ¾代 CrC8垸基磺酰基、 -C8垸氧基羰基、 ¾代 -C8垸基羰基、 8垸 基羰基氧基、 CrC8垸基羰基氨基、 -C8垸基磺酰基氧基、 -C8垸氧基 8垸氧基、 d-C8 垸氧基羰基 d-C8垸基、 -C8垸氧基羰基氨基、 -C8垸氧基羰基 -C8垸氧基、 CHO、C02H、 C02Na、 C02NH4、 NR7R8、 C(=0)NR7R8、 OC(=0)NR7R8、 C(=S)NR7R8、 S02NR7R8或 R6; m选自 0至 5的整数； 当 m大于 1时， ！^可相同或不同； Selected from hydrogen, halogen, CN, N0 2 , mercapto group, dC 8 alkyl group, halogenated dC 8 alkyl group, CC 8 alkyloxy group, halogenated dC 8 alkyloxy group, cyano group dC 8 alkyloxy group, CC 8 alkyl group Sulfide group, ¾ alkylthio group, CC 8 alkyloxy CC 8 alkyl group, ¾ generation-CO alkyloxy CC 8 alkyl group, dC 8 alkylthio group CC 8 alkyl group, 2 generation CC 8 alkylthio group CC 8 alkyl, halogenated CC 8 alkyl amino, piperidinyl, tetrahydropyrrolyl, N-methylpiperazinyl, morpholinyl, C 2 -C 8 alkenyl, halogenated C 2 -C 8 alkenyl , C 2 -C 8 alkenyloxy, halogenated C 2 -C 8 alkenyloxy, C 2 -C 8 alkynyl, halogenated C 2 -C 8 alkynyl, C 2 -C 8 alkynyloxy, halogenated C 2 -C 8 alkynyloxy, dC 8 alkylsulfinyl, dC 8 alkylsulfonyl, C 3 -C 8 cycloalkyl, halogenated dC 8 alkylsulfinyl, ¾ generation C r C 8 alkyl -C 8 alkylcarbonyloxy group, -C 8 alkylcarbonyloxy group , -C 8 alkylcarbonyloxy group, -C 8 alkylcarbonyloxy group, -C 8 alkylcarbonyloxy group, -C 8 alkylcarbonyloxy group Alkyloxy 8alkyloxy , dC 8alkyloxycarbonyldC 8alkyl, -C 8alkyloxycarbonylamino , -C 8alkyloxycarbonyl -C 8alkyloxy , CHO, C0 2 H, C0 2 Na, C0 2 NH 4 , NR 7 R 8 , C(=0)NR 7 R 8 , OC(=0)NR 7 R 8 , C(=S)NR 7 R 8 , S0 2 NR 7 R 8 or R 6 ; m is selected from an integer from 0 to 5; when m is greater than 1, ! ^can be the same or different;
R2选自氢、 卤素、 氰基 CrC8垸基、 -C8垸基、 卤代 -C8垸基、 -C8垸氧基、 卤代 8垸氧基、 氰基 8垸氧基、 8垸硫基、 ¾代 8垸硫基、 -C8垸氧基 8垸 基、 ^代^-^垸氧基 -C8垸基、 CrC8垸硫基 -C8垸基、 ¾代 8垸硫基 -C8垸基、 8垸基亚磺酰基、 -C8垸基磺酰基、 ¾- 环垸基或 R6; R 2 is selected from hydrogen, halogen, cyano C r C 8 alkyl, -C 8 alkyl, halogenated -C 8 alkyl, -C 8 alkyloxy, halogenated 8 alkyloxy, cyano 8 alkoxy base, 8 alkylthio group, ¾ generation 8 alkylthio group, -C 8 alkyloxy 8 alkyl group, ^ generation ^-^ alkyloxy-C 8 alkyl group, C r C 8 alkylthio group -C 8 alkyl group , ¾ generation 8 alkylthio-C 8 alkyl, 8 alkylsulfinyl, -C 8 alkylsulfonyl, ¾-cycloalkyl or R 6;
Ra、 Rb、 Rc、 Rd、 Re Rf、 Rg和 Rh各自独立的表示氢原子、 CrC4垸基、 卤代 CrC4垸 基、 卤代 CrC4垸氧基或 -C4垸氧羰基； 与 一起或者 Rc与 Rf—起可以结合形成饱和 的五元环、 六元环或者七元环； Xi选自 N或 CR3; R a , R b , R c , R d , R e R f , R g and R h each independently represent a hydrogen atom, C r C 4 alkyl group, halogenated C r C 4 alkyl group, halogenated C r C 4 alkyloxy or -C 4 alkyloxycarbonyl; together or R c and R f can be combined to form a saturated five-membered ring, six-membered ring or seven-membered ring; Xi is selected from N or CR 3;
R3选自氢、 CN、 N02、 CONHNH2、 C(=0)NR7R8、 C(=S)NR7R8、 -C12垸氧基羰基、 C(=0)N=CR7R8、 C02NR7R8、 C02N=CR7R8、 CONHN=CR7NR7R8或 C(=0)NR7N=CR7R8; R 3 is selected from hydrogen, CN, N0 2 , CONHNH 2 , C(=0)NR 7 R 8 , C(=S)NR 7 R 8 , -C 12 alkoxycarbonyl, C(=0)N=CR 7 R 8 , C0 2 NR 7 R 8 , C0 2 N=CR 7 R 8 , CONHN=CR 7 NR 7 R 8 or C(=0)NR 7 N=CR 7 R 8 ;
X2选自 (CR7R8)k、 CO(CR7R8)p、 （CR7R8)pCO、 SOq(CR7R8)p或 (CR7R8)pSOq; X 2 is selected from (CR 7 R 8 ) k , CO (CR 7 R 8 ) p , (CR 7 R 8 ) p CO, SOq (CR 7 R 8 ) p or (CR 7 R 8 ) pSOq;
k选自 1、 2或 3; p选自 0、 1、 2或 3; q选自 0、 1或 2; k is selected from 1, 2 or 3; p is selected from 0, 1, 2 or 3; q is selected from 0, 1 or 2;
R4选自氢、 NH2、 -C8垸基、 CrC8卤代垸基、 CrC8垸氧基、 -C8卤代垸氧基、 苯基 或杂芳基， 所述的苯基或杂芳基环上还可以含有 1-3个下述取代基团： F、 Cl、 Br、 I、 CN、 N02、 CH3、 C(CH3)3、 OCH3、 C02CH3、 C02CH2CH3、 S02CH3、 OCH2CF3、 CF3或 OCF3; R4 is selected from hydrogen, NH 2 , -C 8 alkyl, C r C 8 haloalkyl, C r C 8 alkyloxy, -C 8 haloalkyloxy, phenyl or heteroaryl, as described The phenyl or heteroaryl ring may also contain 1-3 of the following substituent groups: F, Cl, Br, I, CN, N0 2 , CH 3 , C(CH 3 ) 3 , OCH 3 , C0 2 CH 3. C0 2 CH 2 CH 3 , S0 2 CH 3 , OCH 2 CF 3 , CF 3 or OCF 3;
Y 选自 -CO-、 -S02-、 -(CR7R8)t-、 -CH=CHCHR7-、 - (CR7R8)tCO-、 -CH=CHCO-、 -S(CR7R8)tCO-、 -N(CR7R8)tCO-、 -0(CR7R8)tCO-、 -S(CR7R8)tS02-、 -N(CR7R8)tS02-、 -0(CR7R8)tS02-、 -CONR7CO-、 -S02NR7C(=S) -、 -S02NR7C(=0)-、 -CONR7C(=S) -、 -NR7CO (CR7R8)t -、 -CO(CR7R8)t -、 -NR7CO-或 -NR7C(=S)-; t分别选自 0、 1或 2; x选自 0或 1; Y is selected from -CO-, -S0 2 -, -(CR 7 R 8 ) t -, -CH=CHCHR 7 -, - (CR 7 R 8 ) t CO-, -CH=CHCO-, -S(CR 7 R 8 ) t CO-, -N(CR 7 R 8 ) t CO-, -0(CR 7 R 8 ) t CO-, -S(CR 7 R 8 ) t S0 2 -, -N(CR 7 R 8 ) t S0 2 -, -0(CR 7 R 8 ) t S0 2 -, -CONR 7 CO-, -S0 2 NR 7 C(=S) -, -S0 2 NR 7 C(=0)- , -CONR 7 C(=S) -, -NR 7 CO (CR 7 R 8 ) t -, -CO(CR 7 R 8 ) t -, -NR 7 CO- or -NR 7 C(=S)- ; t is selected from 0, 1 or 2 respectively; x is selected from 0 or 1;
Q选自被 n个各自独立的 取代的苯基或杂芳基； Q is selected from phenyl or heteroaryl substituted by n independently substituted phenyl or heteroaryl;
R5选自卤素、 CN、 N02、 -C8垸基、 卤代 -C8垸基、 ¾- 环垸基、 -C8垸氧基、 卤代 CrC8垸氧基、 -C8垸硫基、 卤代 -C8垸硫基、 C2-C8烯基、 卤代 C2-C8烯基、 C2-C8 炔基、 卤代 C2-C8炔基、 ¾- 烯氧基、 卤代 C2-Q^ 氧基、 ¾ 8炔氧基、 卤代 C2-C8炔氧 基、 d-C8垸基亚磺酰基、 ¾代 d-C8垸基亚磺酰基、 C C8垸基磺酰基、 ¾代 d-C8垸基磺 酰基、 d-C8垸基羰基、 ¾代 d-C8垸基羰基、 C C8垸基羰基氧基、 C C8垸基羰基氨基、 d-C8垸基磺酰基氧基、 d-C8垸氧基羰基、 d-C8垸氧基 C C8垸氧基、 C C8垸氧基羰基 C C8 垸基、 d-C8垸氧基羰基氨基、 C C8垸氧基羰基 C C8垸氧基、 COR8、 C02R7、 CONR7R8、 NR7R8、 NR8COR7、 NR7COR8、 NR8C02R7、 SOqR8、 S02NR7R8、 芳基、 杂芳基、 芳胺基、 芳垸基氧基、 芳氧基或杂芳胺基， 所述的芳基、 杂芳基、 芳胺基、 芳垸基氧基、 芳氧基或杂 芳胺基环上的氢还可以进一步被 1-4个下述基团所取代： 卤素、 CN、 N02、 d-C8垸基、 d-C8 卤代垸基、 d-C8¾代垸氧基、 C C8垸氧基、 C C8垸氧基羰基或 C C8垸基磺酰基； R 5 is selected from halogen, CN, N0 2 , -C 8 alkyl, halo-C 8 alkyl, ¾-cycloalkyl, -C 8 alkyloxy, halogenated C r C 8 alkoxy, -C 8 alkylthio group, halogenated-C 8 alkylthio group, C 2 -C 8 alkenyl group, halogenated C 2 -C 8 alkenyl group, C 2 -C 8 alkynyl group, halogenated C 2 -C 8 alkynyl group, ¾-alkenyloxy, halogenated C 2 -Q^ oxygen, ¾ 8 alkynyloxy, halogenated C 2 -C 8 alkynyloxy, dC 8 alkylsulfinyl, ¾ dC 8 alkylsulfinyl , CC 8 alkylsulfonyl, ¾ dC 8 alkylsulfonyl, dC 8 alkylcarbonyl, ¾ dC 8 alkylcarbonyl, CC 8 alkylcarbonyloxy, CC 8 alkylcarbonylamino, dC 8 alkyl Sulfonyloxy, dC 8 alkoxycarbonyl, dC 8 alkyloxyCC 8 alkyloxy, CC 8 alkyloxycarbonyl CC 8 alkyl, dC 8 alkyloxycarbonylamino, CC 8 alkyloxycarbonylCC 8 Alkoxy, COR 8 , C0 2 R 7 , CONR 7 R 8 , NR 7 R 8 , NR 8 COR 7 , NR 7 COR 8 , NR 8 C0 2 R 7 , SOqR 8 , S0 2 NR 7 R 8 , aromatic group, heteroaryl group, arylamine group, arylalkyloxy group, aryloxy group or heteroarylamino group, the aryl group, heteroaryl group, arylamine group, arylalkyloxy group, aryloxy group or heteroarylamine group The hydrogen on the arylamine ring can be further substituted by 1-4 of the following groups: halogen, CN, N0 2 , dC 8 alkyl group, dC 8 haloalkyl group, dC 8 ¾ alkyloxy group, CC 8 alkyloxy, CC 8 alkyloxycarbonyl or CC 8 alkylsulfonyl;
n选自 0至 5的整数； 当 n大于 1时， R5可相同或不同； n is selected from an integer from 0 to 5; when n is greater than 1, R 5 can be the same or different;
R6选自未取代的或被 1-5个独立选自以下基团进一步取代的苯基、苯甲酰基、苯氧基羰 基、 苯基胺基羰基、 苯基 C C6垸基、 萘基、 萘基 d-C6垸基、 杂芳基、 杂芳基羰基、 杂芳 基氧基羰基、 杂芳基胺基羰基或杂芳基 d-C6垸基： 卤素、 硝基、 氰基、 巯基、 d-C8垸基、 卤代 d-C8垸基、 C3-C8环垸基、 C C8垸氧基、 ¾代 -0¾垸氧基、 C C8垸硫基、 ^代 C C8 垸硫基、 C2-C8烯基、 卤代 C2-C8烯基、 C2-C8炔基、 卤代 C2-C8炔基、 C2-C8烯氧基、 卤代 C2-C8烯氧基、 C2-C8炔氧基、 卤代 C2-C8炔氧基、 d-C8垸基亚磺酰基、 卤代 d-C8垸基亚磺 酰基、 d-C8垸基磺酰基、 ¾代 d-C8垸基磺酰基、 C C8垸基羰基、 ¾代 C C8垸基羰基、 8垸基羰基氧基、 8垸基羰基氨基、 -C8垸基磺酰基氧基、 d-C8垸氧基羰基、 d-C8 垸氧基 8垸氧基、 -C8垸氧基羰基 -C8垸基、 -C8垸氧基羰基氨基、 8垸氧基羰 基 -^垸氧基、 CHO、 C02H、 C02Na、 C02NH4、 NR7R8、 C(=0)NR7R8、 OC(=0)NR7R8、 C(=S)NR7R8或 S02NR7R8; R 6 is selected from phenyl, benzoyl, phenoxycarbonyl, phenylaminocarbonyl, phenyl CC alkyl, naphthyl, which is unsubstituted or further substituted by 1 to 5 groups independently selected from the following groups. Naphthyl dC 6 alkyl, heteroaryl, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroarylaminocarbonyl or heteroaryl dC 6 alkyl: halogen, nitro, cyano, mercapto, dC 8 Alkyl group, halogenated C alkyl group, C 3 -C cycloalkyl group, CC alkyloxy group, substituted-C alkyloxy group, CC alkylthio group, substituted CC alkylthio group, C 2 - C 8 alkenyl, halogenated C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, halogenated C 2 -C 8 alkynyl, C 2 -C 8 alkenyloxy, halogenated C 2 -C 8 alkene Oxygen, C 2 -C 8 alkynyloxy, halogenated C 2 -C 8 alkynyloxy, dC 8 alkylsulfinyl, halogenated dC 8 alkylsulfinyl, dC 8 alkylsulfonyl, ¾ generation dC 8 alkylsulfonyl, CC 8 alkylcarbonyl, ¾ generation CC 8 alkylcarbonyl, 8 alkylcarbonyloxy, 8 alkylcarbonylamino, -C 8 alkylsulfonyloxy, dC 8 alkyloxycarbonyl , dC 8 alkoxycarbonyl-C 8 alkyloxy, -C 8 alkoxycarbonyl-C 8 alkyl, -C 8 alkyloxycarbonylamino, 8 alkyloxycarbonyl-^ alkyloxy, CHO, C0 2 H, C0 2 Na, C0 2 NH 4 , NR 7 R 8 , C(=0)NR 7 R 8 , OC(=0)NR 7 R 8 , C(=S)NR 7 R 8 or S0 2 NR 7 R 8 ;
R7、 R8可相同或不同， 分别选自氢、 氰基、 SCN、 甲酰基、 -C8垸基、 卤代 -C8垸 基、 8垸氧基、 ^代^-^垸氧基、 8垸硫基、 ¾代 8垸硫基、 d-C8垸基羰基、 -C8垸氧基羰基、 - 垸氧基羰基 -C8垸基、 - 垸基亚磺酰基、 -C8垸基磺酰基、 氰基 CrC8垸基、 羟基 -C8垸基、 ¾- 环垸基或 -C8垸基氨基。 R 7 and R 8 may be the same or different, and are respectively selected from hydrogen, cyano group, SCN, formyl group, -C 8 alkyl group, halogenated -C 8 alkyl group, 8 alkyloxy group, and hydroxyl-C alkyloxy group. , 8 alkylthio group, ¾ generation 8 alkylthio group, dC 8 alkylcarbonyl group, -C 8 alkyloxycarbonyl group, - alkyloxycarbonyl group -C 8 alkyl group, - alkylsulfinyl group, -C 8 alkyl group Sulfonyl group, cyano C r C 8 alkyl group, hydroxyl - C 8 alkyl group, ¾ - cycloalkyl group or - C 8 alkyl amino group.
3、 根据权利要求 2所述的化合物， 其特征在于： 通式 (I)中 3. The compound according to claim 2, characterized in that: in general formula (I)
！^选自氢、 卤素、 CN、 N02、 巯基、 CrC4垸基、 卤代 -C4垸基、 -C4垸氧基、 卤 代 d-C4垸氧基、 氰基 -C4垸氧基、 -C4焼硫基、 卤代 -C4垸硫基、 -C4垸氧基 -C4 \ ί Ci-C4 Ci-C4 ¾υ¾ Ci-C4 ¾¾¾¾¾ Ci-C4¾¾¾ \ ί Ci-C4 ¾¾¾¾¾ Ci-C4 i 基、 卤代 CrC4垸基氨基、 哌啶基、 四氢吡咯基、 N-甲基哌嗪基、 吗啉基、 C2-C4烯基、 卤 代 C2-C4烯基、 C2-C4烯氧基、 卤代 C2-C4烯氧基、 C2-C4炔基、 卤代 C2-C4炔基、 C2-C4炔氧 基、 卤代 C2-C4炔氧基、 CrC4垸基亚磺酰基、 CrC4垸基磺酰基、 C3-C6环垸基、 卤代 -C4 垸基亚磺酰基、 代 CrC4垸基磺酰基、 -C4垸氧基羰基、 代 -C4垸基羰基、 -C4垸 基羰基氧基、 d-C4垸基羰基氨基、 -C4垸基磺酰基氧基、 -C4垸氧基 -C4垸氧基、 C C4 垸氧基羰基 CrC4垸基、 -C4垸氧基羰基氨基、 -C4垸氧基羰基 -C4垸氧基、 CHO、C02H、 C02Na、 C02NH4、 NR7R8、 C(=0)NR7R8、 OC(=0)NR7R8、 C(=S)NR7R8、 S02NR7R8或 R6; m选自 0至 5的整数； 当 m大于 1时， ！^可相同或不同； ! ^Selected from hydrogen, halogen, CN, N0 2 , mercapto group, C r C 4 alkyl group, halogenated-C 4 alkyl group, -C 4 alkyloxy group, halogenated C 4 alkyloxy group, cyano group - C 4 alkyl group Oxygen group, -C 4 alkylthio group, halo-C 4 alkylthio group, -C 4 alkoxy group -C 4 \ί Ci-C 4 Ci-C 4 ¾υ¾ Ci-C 4 ¾¾¾¾¾ Ci-C 4 ¾¾¾ \ ί Ci-C 4 ¾¾¾¾¾ Ci-C 4 i base, halogenated C r C 4 alkyl amino group, piperidinyl group, tetrahydropyrrolyl group, N-methylpiperazinyl group, morpholinyl group, C 2 -C 4 alkenyl group, halogenated C 2 -C 4 alkenyl group , C 2 -C 4 alkenyloxy, halogenated C 2 -C 4 alkenyloxy, C 2 -C 4 alkynyl, halogenated C 2 -C 4 alkynyl, C 2 -C 4 alkynyloxy, halogenated C 2 -C 4 alkynyloxy, C r C 4 alkylsulfinyl, C r C 4 alkylsulfinyl, C 3 -C 6 cycloalkyl, halo-C 4 alkylsulfinyl, substitution C r C 4 alkylsulfonyl, -C 4 alkyloxycarbonyl, -C 4 alkylcarbonyl, -C 4 alkylcarbonyloxy, dC 4 alkylcarbonylamino, -C 4 alkylsulfonyloxy, -C 4 alkyloxy-C 4 alkyloxy, CC 4 alkyloxycarbonyl C r C 4 alkyl, -C 4 alkyloxycarbonylamino, -C 4 alkyloxycarbonyl -C 4 alkyloxy, CHO , C0 2 H, C0 2 Na, C0 2 NH 4 , NR 7 R 8 , C(=0)NR 7 R 8 , OC(=0)NR 7 R 8 , C(=S)NR 7 R 8 , S0 2 NR 7 R 8 or R 6 ; m is selected from an integer from 0 to 5; when m is greater than 1, ! ^can be the same or different;
R2选自氢、 卤素、 CN、 N02、 CONH2、 氰基 CrC4垸基、 -C4垸基、 卤代 CrC4垸基、 -C4垸氧基、 卤代 -C4垸氧基、 氰基 CrC4垸氧基、 CrC4垸硫基、 卤代 -C4垸硫基、 Ci-C4 Ci-C4 ¾υ¾ \ ί Ci-C4¾¾¾,¾ Ci-C4¾¾¾ Ci-C4¾¾¾¾¾ Ci-C4¾¾¾ Ci-C4 垸硫基 d-C4垸基、 -C4垸基亚磺酰基、 -C4垸基磺酰基、 C3-C6环垸基或 R6; R 2 is selected from hydrogen, halogen, CN, N0 2 , CONH 2 , cyano C r C 4 alkyl, -C 4 alkyl, halogenated C r C 4 alkyl, -C 4 alkyloxy, halogenated - C 4 alkyloxy, cyano C r C 4 alkoxy, C r C 4 alkylthio, halo-C 4 alkylthio, Ci-C 4 Ci-C 4 ¾υ¾ \ ί Ci-C 4 ¾¾¾, ¾ Ci-C 4 ¾¾¾ Ci-C 4 ¾¾¾¾¾ Ci-C 4 ¾¾¾ Ci-C 4 alkylthioyldC 4 alkyl, -C 4 alkylsulfinyl, -C 4 alkylsulfonyl, C 3 -C 6 cycloalkyl or R 6;
Ra、 Rb、 Rc、 Rd、 Re Rf、 Rg和 Rh各自独立的表示氢原子、 CrC4垸基、 卤代 CrC4垸 基、 卤代 CrC4垸氧基或 -C4垸氧羰基； 与 一起或者 Rc与 Rf—起可以结合形成饱和 的五元环、 六元环或者七元环； R a , R b , R c , R d , R e R f , R g and R h each independently represent a hydrogen atom, C r C 4 alkyl group, halogenated C r C 4 alkyl group, halogenated C r C 4 alkyloxy group or -C 4 alkyloxycarbonyl group; together or R c and R f can be combined to form a saturated five-membered ring, six-membered ring or seven-membered ring;
Xi选自 N或 CR3; Xi is selected from N or CR 3;
R3选自氢、 CN、 N02、 CONHNH2、 C(=0)NR7R8、 C(=S)NR7R8、 d-C12垸氧基羰基、 C(=0)N=CR7R8、 C02NR7R8、 C02N=CR7R8、 CONHN=CR7NR7R8或 C(=0)NR7N=CR7R8; R 3 is selected from hydrogen, CN, N0 2 , CONHNH 2 , C(=0)NR 7 R 8 , C(=S)NR 7 R 8 , dC 12 alkoxycarbonyl, C(=0)N=CR 7 R 8 , C0 2 NR 7 R 8 , C0 2 N=CR 7 R 8 , CONHN=CR 7 NR 7 R 8 or C(=0)NR 7 N=CR 7 R 8 ;
X2选自 (CR7R8)k、 CO(CR7R8)p、 （CR7R8)pCO、 SOq(CR7R8)p或 (CR7R8)pSOq; X 2 is selected from (CR 7 R 8 ) k , CO (CR 7 R 8 ) p , (CR 7 R 8 ) p CO, SOq (CR 7 R 8 ) p or (CR 7 R 8 ) pSOq;
k选自 1、 2或 3; p选自 0、 1、 2或 3; q选自 0、 1或 2; k is selected from 1, 2 or 3; p is selected from 0, 1, 2 or 3; q is selected from 0, 1 or 2;
选自氢、 NH2、 C C4垸基、 d-C4卤代垸基、 d-C4垸氧基、 d-C4卤代垸氧基、 苯基 或杂芳基， 所述的苯基或杂芳基环上还可以含有 1-3个下述取代基团： F、 Cl、 Br、 I、 CN、 N02、 CH3、 C(CH3)3、 OCH3、 C02CH3、 C02CH2CH3、 S02CH3、 OCH2CF3、 CF3或 OCF3; Selected from hydrogen, NH 2 , CC 4 alkyl, dC 4 haloalkyl, dC 4 alkyloxy, dC 4 haloalkyloxy, phenyl or heteroaryl, the phenyl or heteroaryl ring may also contain 1-3 of the following substituent groups: F, Cl, Br, I, CN, N0 2 , CH 3 , C(CH 3 ) 3 , OCH 3 , C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 , OCH 2 CF 3 , CF 3 or OCF 3;
Y 选自 -CO-、 -S02-、 -(CR7R8)t-、 -CH=CHCHR7-、 - (CR7R8)tCO-、 -CH=CHCO-、 -S(CR7R8)tCO-、 -N(CR7R8)tCO-、 -0(CR7R8)tCO-、 -S(CR7R8)tS02-、 -N(CR7R8)tS02-、 -0(CR7R8)tS02-、 -CONR7CO-、 -S02NR7C(=S) -、 -S02NR7C(=0)-、 -CONR7C(=S) -、 -NR7CO (CR7R8)t -、 -CO(CR7R8)t-、 -NR7CO-或 -NR7C(=S)-; t分别选自 0、 1或 2; x选自 0或 1; Y is selected from -CO-, -S0 2 -, -(CR 7 R 8 ) t -, -CH=CHCHR 7 -, - (CR 7 R 8 ) t CO-, -CH=CHCO-, -S(CR 7 R 8 ) t CO-, -N(CR 7 R 8 ) t CO-, -0(CR 7 R 8 ) t CO-, -S(CR 7 R 8 ) t S0 2 -, -N(CR 7 R 8 ) t S0 2 -, -0(CR 7 R 8 ) t S0 2 -, -CONR 7 CO-, -S0 2 NR 7 C(=S) -, -S0 2 NR 7 C(=0)- , -CONR 7 C(=S) -, -NR 7 CO (CR 7 R 8 ) t -, -CO(CR 7 R 8 ) t -, -NR 7 CO- or -NR 7 C(=S)- ; t is selected from 0, 1 or 2 respectively; x is selected from 0 or 1;
Q选自被 n个各自独立的 R5取代的苯基或杂芳基； Q is selected from phenyl or heteroaryl substituted by n independently R 5 ;
R5选自卤素、 CN、 N02、 C C4垸基、 卤代 C C4垸基、 C3-C6环垸基、 C C4垸氧基、 卤代 C C4垸氧基、 d-C4垸硫基、 卤代 C C4垸硫基、 C2-C4烯基、 卤代 C2-C4烯基、 C2-C4 炔基、 卤代 C2-C4炔基、 C2-C4烯氧基、 卤代 C2-C4烯氧基、 C2-C4炔氧基、 卤代 C2-C4炔氧 基、 CrC4垸基亚磺酰基、 卤代 C C4垸基亚磺酰基、 C C4垸基磺酰基、 卤代 C C4垸基磺 酰基、 -C4垸基羰基、 ¾代 -C4垸基羰基、 CrC4垸基羰基氧基、 -C4垸基羰基氨基、 -C4垸基磺酰基氧基、 CrC4垸氧基羰基、 -C4垸氧基 -C4垸氧基、 CrC4垸氧基羰基 -C4 垸基、 -C4垸氧基羰基氨基、 CrC4垸氧基羰基 -C4垸氧基、 COR8、 C02R7、 CONR7R8、 NR7R8、 NR8COR7、 NR7COR8、 NR8C02R7、 SOqR8、 S02NR7R8、 芳基、 杂芳基、 芳胺基、 芳垸基氧基、 芳氧基或杂芳胺基， 所述的芳基、 杂芳基、 芳胺基、 芳垸基氧基、 芳氧基或杂 芳胺基环上的氢还可以进一步被 1-4个下述基团所取代： 卤素、 CN、 N02、 CrC4垸基、 C C4 卤代垸基、 -C4卤代垸氧基、 CrC4垸氧基、 CrC4垸氧基羰基或 -C4垸基磺酰基； R 5 is selected from halogen, CN, N0 2 , CC 4 alkyl, halogenated CC 4 alkyl, C 3 -C 6 cycloalkyl, CC 4 alkyloxy, halogenated CC 4 alkyloxy, dC 4 alkyl sulfide base, halogenated C 4 alkylthio group, C 2 -C 4 alkenyl group, halogenated C 2 -C 4 alkenyl group, C 2 -C 4 alkynyl group, halogenated C 2 -C 4 alkynyl group, C 2 -C 4 alkenyloxy, halogenated C 2 -C 4 alkenyloxy, C 2 -C 4 alkynyloxy, halogenated C 2 -C 4 alkynyloxy, CrC 4 alkylsulfinyl, halogenated CC 4 alkyl Sulfinyl, CC 4 alkylsulfonyl, halogenated CC 4 alkylsulfonyl, -C 4 alkylcarbonyl, ¾ -C 4 alkylcarbonyl, C r C 4 alkylcarbonyloxy, -C 4 alkyl Carbonylamino group, -C 4 alkylsulfonyloxy group, C r C 4 alkyloxycarbonyl group, - C 4 alkyloxy carbonyl group - C 4 alkyloxy group, C r C 4 alkyloxycarbonyl group - C 4 alkyl group, -C 4 alkoxycarbonylamino, C r C 4 alkyloxycarbonyl -C 4 alkoxy, COR 8 , C0 2 R 7 , CONR 7 R 8 , NR 7 R 8 , NR 8 COR 7 , NR 7 COR 8. NR 8 C0 2 R 7 , SOqR 8 , S0 2 NR 7 R 8 , aryl group, heteroaryl group, arylamine group, arylalkyloxy group, aryloxy group or heteroarylamino group, the aryl group The hydrogen on the , heteroaryl, arylamine, arylalkyloxy, aryloxy or heteroarylamino ring can be further substituted by 1-4 of the following groups: halogen, CN, N0 2 , C r C 4 alkyl, CC 4 haloalkyl, -C 4 haloalkyloxy, C r C 4 alkyloxy, C r C 4 alkyloxycarbonyl or -C 4 alkylsulfonyl;
n选自 0至 5的整数； 当 n大于 1时， R5可相同或不同； n is selected from an integer from 0 to 5; when n is greater than 1, R 5 can be the same or different;
R6选自未取代的或被 1-5个独立选自以下基团进一步取代的苯基、苯甲酰基、苯氧基羰 基、 苯基胺基羰基、 苯基 -C6垸基、 萘基、 萘基 d-C6垸基、 杂芳基、 杂芳基羰基、 杂芳 基氧基羰基、 杂芳基胺基羰基或杂芳基 CrC6垸基： 卤素、 硝基、 氰基、 巯基、 d-C4垸基、 卤代 d-C4垸基、 C3-C6环垸基、 -C4垸氧基、 ¾代 1 4垸氧基、 -C4垸硫基、 ¾代 1 4 垸硫基、 C2-C4烯基、 卤代 C2-C4烯基、 C2-C4炔基、 卤代 C2-C4炔基、 C2-C4烯氧基、 卤代 C2-C4烯氧基、 C2-C4炔氧基、 卤代 C2-C4炔氧基、 -C4垸基亚磺酰基、 卤代 d-C4垸基亚磺 酰基、 -C4垸基磺酰基、 代 CrC4垸基磺酰基、 CrC4垸基羰基、 代 CrC4垸基羰基、 -C4垸基羰基氧基、 -C4垸基羰基氨基、 -C4垸基磺酰基氧基、 CrC4垸氧基羰基、 C C4 垸氧基 d-C4垸氧基、 -C4垸氧基羰基 -C4垸基、 -C4垸氧基羰基氨基、 -C4垸氧基羰 基^ 垸氧基、 CHO、 C02H、 C02Na、 C02NH4、 NR7R8、 C(=0)NR7R8、 OC(=0)NR7R8、 C(=S)NR7R8或 S02NR7R8; R 6 is selected from phenyl, benzoyl, phenoxycarbonyl, phenylaminocarbonyl, phenyl-C 6 alkyl, naphthyl that is unsubstituted or further substituted by 1 to 5 groups independently selected from the following groups , naphthyl dC 6 alkyl, heteroaryl, heteroarylcarbonyl, heteroaryloxycarbonyl, heteroarylaminocarbonyl or heteroaryl C r C 6 alkyl: halogen, nitro, cyano, mercapto , dC 4 alkyl group, halogenated dC 4 alkyl group, C 3 -C 6 cycloalkyl group, -C 4 alkyloxy group, ¾ alkyloxy group, -C 4 alkylthio group, ¾ substituted 1 4 Alkylthio, C 2 -C 4 alkenyl, halogenated C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, halogenated C 2 -C 4 alkynyl, C 2 -C 4 alkenyloxy, halo Substituted C 2 -C 4 alkenyloxy, C 2 -C 4 alkynyloxy, halogenated C 2 -C 4 alkynyloxy, -C 4 alkylsulfinyl, halogenated C 4 alkylsulfinyl, - C 4 alkylsulfonyl, C r C 4 alkylsulfonyl, C r C 4 alkylcarbonyl, C r C 4 alkylcarbonyl, -C 4 alkylcarbonyloxy, -C 4 alkylcarbonylamino , -C 4 alkylsulfonyloxy, C r C 4 alkyloxycarbonyl, CC 4 alkoxydC 4 alkyloxy, -C 4 alkyloxycarbonyl -C 4 alkyl, -C 4 alkyloxy Carbonylamino, -C 4 alkoxycarbonyl^ alkyloxy, CHO, C0 2 H, C0 2 Na, C0 2 NH 4 , NR 7 R 8 , C(=0)NR 7 R 8 , OC(=0) NR 7 R 8 , C(=S)NR 7 R 8 or S0 2 NR 7 R 8 ;
R7、 R8可相同或不同， 分别选自氢、 氰基、 SCN、 甲酰基、 CrC4垸基、 卤代 -C4垸 基、 -C4垸氧基、 ^代^ 垸氧基、 -C4垸硫基、 ¾代 4垸硫基、 CrC4垸基羰基、 -C4垸氧基羰基、 -C4垸氧基羰基 -C4垸基、 -C4垸基亚磺酰基、 -C4垸基磺酰基、 氰基 CrC4垸基、 羟基 -C4垸基、 C3-C6环垸基或 -C4垸基氨基。 R 7 and R 8 may be the same or different, and are respectively selected from hydrogen, cyano, SCN, formyl, C r C 4 alkyl, halo-C 4 alkyl, -C 4 alkyloxy, and substituted alkoxy. base, -C 4 alkylthio group, ¾ generation 4 alkylthio group, C r C 4 alkylcarbonyl group, -C 4 alkyloxycarbonyl group, -C 4 alkyloxycarbonyl group -C 4 alkyl group, -C 4 alkyl group Sulfinyl, -C 4 alkylsulfonyl, cyano C r C 4 alkyl, hydroxyl -C 4 alkyl, C 3 -C 6 cycloalkyl or -C 4 alkyl amino.
4、 根据权利要求 3所述的化合物， 其特征在于： 通式 (I)中 4. The compound according to claim 3, characterized in that: in general formula (I)
！^选自氢、 卤素、 CN、 N02、 CrC4垸基、 卤代 CrC4垸基、 CrC4垸氧基、 卤代 -C4 #ΐ¾ Ci-C4 Ci-C4 ¾¾¾,¾ Ci-C4 ¾¾¾ \ ί Ci-C4 Ci-C4 C3-C6 环垸基或 R6; m选自 0至 5的整数； 当 m大于 1时， ！^可相同或不同； ! ^ is selected from hydrogen, halogen, CN, NO 2 , C r C 4 alkyl group, halogenated C r C 4 alkyl group, C r C 4 alkoxy group, halogenated -C 4 #ΐ¾ Ci-C 4 Ci-C 4 ¾¾¾,¾ Ci-C 4 ¾¾¾ \ί Ci-C 4 Ci-C 4 C 3 -C 6 cycloalkyl or R 6; m is selected from an integer from 0 to 5; when m is greater than 1, ! ^can be the same or different;
R2选自氢、 卤素、 CN、 CrC4垸基、 卤代 -C4垸基、 CrC4垸氧基、 卤代 CrC4垸氧基、 氰基 d-C4垸氧基、 C C4垸氧基 C C4垸基、 ^代 C C4垸氧基 C C4垸基、 C3-C6环垸基或 R6; 一 R 2 is selected from hydrogen, halogen, CN, C r C 4 alkyl group, halo-C 4 alkyl group, C r C 4 alkoxy group, halo C r C 4 alkoxy group, cyano dC 4 alkyl oxygen group. , CC 4 alkyloxy CC 4 alkyl, ^ generation CC 4 alkoxy CC 4 alkyl, C 3 -C 6 cycloalkyl or R 6 ;
Ra、 Rb、 Rc、 Rd、 Re Rf、 Rg和 Rh各自独立的表示氢原子、 C C4垸基、 卤代 C C4垸 基、 卤代 C C4垸氧基或 d-C4垸氧羰基； ！^与 Rh—起或者 Rc与 Rf—起可以结合形成饱和 的五元环、 六元环或者七元环； R a , R b , R c , R d , R e R f , R g and R h each independently represent a hydrogen atom, CC 4 alkyl group, halogenated CC 4 alkyl group, halogenated CC 4 alkyloxy group or dC 4 alkyloxycarbonyl; ! ^ together with R h or R c and R f can be combined to form a saturated five-membered ring, a six-membered ring or a seven-membered ring;
Xi选自 N或 CR3 ; Xi is selected from N or CR 3;
R3选自氢、 CN、 N02、 CONHNH2、 C(=0)NR7R8、 C(=S)NR7R8、 d-C12垸氧基羰基、 C(=0)N=CR7R8、 C02NR7R8、 C02N=CR7R8、 CONHN=CR7NR7R8或 C(=0)NR7N=CR7R8; R 3 is selected from hydrogen, CN, N0 2 , CONHNH 2 , C(=0)NR 7 R 8 , C(=S)NR 7 R 8 , dC 12 alkoxycarbonyl, C(=0)N=CR 7 R 8 , C0 2 NR 7 R 8 , C0 2 N=CR 7 R 8 , CONHN=CR 7 NR 7 R 8 or C(=0)NR 7 N=CR 7 R 8 ;
X2选自 (CR7R8)k、 CO(CR7R8)p、 （CR7R8)pCO、 SOq(CR7R8)p或 (CR7R8)pSOq; X 2 is selected from (CR 7 R 8 ) k , CO (CR 7 R 8 ) p , (CR 7 R 8 ) p CO, SOq (CR 7 R 8 ) p or (CR 7 R 8 ) pSOq;
k选自 1、 2或 3; p选自 0、 1、 2或 3; q选自 0、 1或 2; k is selected from 1, 2 or 3; p is selected from 0, 1, 2 or 3; q is selected from 0, 1 or 2;
选自氢、 NH2、 C C4垸基、 d-C4卤代垸基、 C C4垸氧基、 C C4卤代垸氧基、 未取 代或被 1-3个下述基团进一步取代的苯基、 吡啶基、 噻吩基、 呋喃基、 吡咯基、 咪唑基、 噻 唑基或吡唑基： F、 Cl、 Br、 I、 CN、 N02、 CH3、 C(CH3)3、 OCH3、 C02CH3、 C02CH2CH3、 S02CH3、 OCH2CF3、 CF3或 OCF3 ; Selected from hydrogen, NH 2 , CC 4 alkyl, dC 4 haloalkyl, CC 4 alkyloxy, CC 4 haloalkyloxy, unsubstituted or phenyl further substituted by 1 to 3 of the following groups , pyridyl, thienyl, furyl, pyrrolyl, imidazolyl, thiazolyl or pyrazolyl: F, Cl, Br, I, CN, N0 2 , CH 3 , C(CH 3 ) 3 , OCH 3 , C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 , OCH 2 CF 3 , CF 3 or OCF 3;
Y选自 -CO-、 -S02-、 -CH2-、 -CH=CHCHR7-、 - (CR7R8)tCO-、 -CH=CHCO-、 -S(CR7R8)tCO-、 -N(CR7R8)tCO-、 -0(CR7R8)tCO-、 -S(CR7R8)tS02-、 -N(CR7R8)tS02-、 -0(CR7R8)tS02-、 -CONR7CO-、 -S02NR7C(=S)-、 -S02NR7C(=0)-、 -CONR7C(=S)-、 -NR7CO (CR7R8)t-、 -CO(CR7R8)t- -NR7CO-或 -NR7C(=S)-; t分别选自 0、 1或 2; x选自 0或 1 ; Y is selected from -CO-, -S0 2 -, -CH 2 -, -CH=CHCHR 7 -, - (CR 7 R 8 ) t CO-, -CH=CHCO-, -S(CR 7 R 8 ) t CO-, -N(CR 7 R 8 ) t CO-, -0(CR 7 R 8 ) t CO-, -S(CR 7 R 8 ) t S0 2 -, -N(CR 7 R 8 ) t S0 2 -, -0(CR 7 R 8 ) t S0 2 -, -CONR7CO-, -S0 2 NR 7 C(=S)-, -S0 2 NR 7 C(=0)-, -CONR 7 C(= S)-, -NR 7 CO (CR 7 R 8 ) t -, -CO(CR 7 R 8 ) t - -NR 7 CO- or -NR 7 C(=S)- ; t is selected from 0 and 1 respectively or 2; x is selected from 0 or 1;
Q选自被 n个各自独立的 R5取代的苯基、 吡啶基、 嘧啶基、 哒嗪基、 吡嗪基、 喹啉基、 噻吩基、 苯并噻吩基、 呋喃基、 苯并呋喃基、 吲哚基、 吡咯基、 恶唑基、 咪唑基、 苯并恶唑 基、 苯并噻唑基、 苯并咪唑基、 苯并吡嗪基、 噻唑基、 吡唑基、 ***并嘧啶基、 咪唑并哒嗪 基、 咪唑并吡啶基或哒嗪酮基； Q is selected from phenyl , pyridyl, pyrimidinyl, pyridinyl, pyrazinyl, quinolyl, thienyl, benzothienyl, furyl, benzofuryl, Indolyl, pyrrolyl, oxazolyl, imidazolyl, benzoxazolyl, benzothiazolyl, benzimidazolyl, benzopyrazinyl, thiazolyl, pyrazolyl, triazolopyrimidinyl, imidazole Pyridazinyl, imidazopyridinyl or pyridazinonyl;
R5选自卤素、 CN、 N02、 CrC4垸基、 C3-C6环垸基、 CrC4卤代垸基、 -C4垸氧基、 CrC4卤代垸氧基、 C2-C4烯基、 C2-C4炔基、 C2-C4烯氧基、 C2-C4炔氧基、 COCH3、 COC2H5、 C02CH3、 C02C2H5、 S02CH3或 S02C2H5 ; R 5 is selected from halogen, CN, N0 2 , C r C 4 alkyl group, C 3 -C 6 cycloalkyl group, C r C 4 haloalkyl group, -C 4 alkyloxy group, C r C 4 haloalkyl group. Oxygen group, C 2 -C 4 alkenyl group, C 2 -C 4 alkynyl group, C 2 -C 4 alkenyloxy group, C 2 -C 4 alkynyloxy group, COCH 3 , COC 2 H 5 , C0 2 CH 3 , C0 2 C 2 H 5 , S0 2 CH 3 or S0 2 C 2 H 5 ;
n选自 0至 5的整数； 当 n大于 1时， 可相同或不同； n is selected from an integer from 0 to 5; when n is greater than 1, it can be the same or different;
R6选自苯基、 4-氯苯基、 2,4-二氯苯基、 4-甲基苯基、 4-三氟甲基苯基、 4-甲氧基苯基、 2,6-二氯 -4-三氟甲基苯基、 苄基、 4-氯苄基、 4-叔丁基苄基、 4-三氟甲基苄基、 苯乙基、 2- 吡啶基、 3-氯 -2-吡啶基、 3,5-二氯 -2-吡啶基、 3,5,6-三氯 -2-吡啶基、 5-三氟甲基 -2-吡啶基、 5-甲基 -2-吡啶基、 3-氯 -5-氰基 -2-吡啶基、 3-氯 -5-三氟甲基 -2-吡啶基、 2-吡啶甲基、 2-氯 -5- 吡啶甲基、 3-氯 -5-三氟甲基 -2-吡啶甲基、 2-吡啶乙基、 3-氯 -5-三氟甲基 -2-吡啶乙基、噻唑 -2- 基、 2-氯 -5-噻唑基甲基或 2-嘧啶基； R 6 is selected from phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl, 2,6- Dichloro-4-trifluoromethylphenyl, benzyl, 4-chlorobenzyl, 4-tert-butylbenzyl, 4-trifluoromethylbenzyl, phenethyl, 2- Pyridyl, 3-chloro-2-pyridyl, 3,5-dichloro-2-pyridyl, 3,5,6-trichloro-2-pyridyl, 5-trifluoromethyl-2-pyridyl, 5-methyl-2-pyridyl, 3-chloro-5-cyano-2-pyridyl, 3-chloro-5-trifluoromethyl-2-pyridyl, 2-pyridylmethyl, 2-chloro- 5-pyridylmethyl, 3-chloro-5-trifluoromethyl-2-pyridylmethyl, 2-pyridylethyl, 3-chloro-5-trifluoromethyl-2-pyridylethyl, thiazole-2- base, 2-chloro-5-thiazolylmethyl or 2-pyrimidinyl;
R7、 R8可相同或不同， 分别选自氢、 氰基、 SCN、 甲酰基、 CrC4垸基、 卤代 CrC4垸 基、 -C4垸氧基、 ^代^ 垸氧基、 -C4垸硫基、 ¾代 4垸硫基、 CrC4垸基羰基、 -C4垸氧基羰基、 -C4垸氧基羰基 -C4垸基、 -C4垸基亚磺酰基、 -C4垸基磺酰基、 氰基 CrC4垸基、 羟基 -C4垸基、 C3-C6环垸基或 -C4垸基氨基。 R 7 and R 8 may be the same or different, and are respectively selected from hydrogen, cyano group, SCN, formyl group, C r C 4 alkyl group, halogenated C r C 4 alkyl group, -C 4 alkyloxy group, and ^ substituted alkyl group. Oxygen group, -C 4 alkylthio group, ¾ generation 4 alkylthio group, C r C 4 alkylcarbonyl group, -C 4 alkyloxycarbonyl group, -C 4 alkyloxycarbonyl group -C 4 alkyl group, -C 4 alkyl group sulfinyl group, -C 4 alkylsulfonyl group, cyano C r C 4 alkyl group, hydroxyl -C 4 alkyl group, C 3 -C 6 cycloalkyl group or -C 4 alkyl amino group.
5、 根据权利要求 4所述的化合物， 其特征在于： 通式 (I)中 5. The compound according to claim 4, characterized in that: in general formula (I)
Ri选自氢、 F、 Cl、 Br、 I、 CN、 N02、 CrC4垸基、 卤代 CrC4垸基、 CrC4垸氧基、 卤 代 d-C4垸氧基或¾-0>环垸基； m选自 1至 5的整数； 当 m大于 1时， ！^可相同或不同； R2选自氢、 F、 Cl、 Br、 I、 CN、 CrC4垸基、 卤代 CrC4垸基、 CrC4垸氧基、 卤代 -C4 垸氧基、 C3-C6环垸基或 R6; Ri is selected from hydrogen , F, Cl, Br, I , CN , N02 , CrC4alkyl, halogenated CrC4alkyl , CrC4alkoxy , halogenated C4alkyloxy or ¾-0>Cycloalkyl group; m is selected from an integer from 1 to 5; when m is greater than 1, ! ^ can be the same or different; R 2 is selected from hydrogen, F, Cl, Br, I, CN, C r C 4 alkyl, halogenated C r C 4 alkyl, C r C 4 alkyloxy, halogenated -C 4 alkoxy group, C 3 -C 6 cycloalkyl group or R6;
Ra、 Rb、 Rc、 Rd、 Re Rf、 Rg和 Rh各自独立的表示氢原子、 CrC4垸基、 卤代 CrC4垸 基、 卤代 CrC4垸氧基或 -C4垸氧羰基； 与 一起或者 Rc与 Rf—起可以结合形成饱和 的五元环、 六元环或者七元环； R a , R b , R c , R d , R e R f , R g and R h each independently represent a hydrogen atom, C r C 4 alkyl group, halogenated C r C 4 alkyl group, halogenated C r C 4 alkyloxy group or -C 4 alkyloxycarbonyl group; together or R c and R f can be combined to form a saturated five-membered ring, six-membered ring or seven-membered ring;
Xi选自 N或 CR3 ; Xi is selected from N or CR 3;
R3选自氢、 CN、 N02、 CONH2、 CSNH2、 C02CH3、 CONHCH3、 CONHCN、 C02N=C(CH3)2、 CONHNH2、 CONHN(CH3)2、 CONHN=CHOCH3或 CONHN=CHN(CH3)2; R 3 is selected from hydrogen, CN, N0 2 , CONH 2 , CSNH 2 , C0 2 CH 3 , CONHCH 3 , CONHCN, C0 2 N=C(CH 3 ) 2 , CONHNH 2 , CONHN(CH 3 ) 2 , CONHN= CHOCH 3 or CONHN=CHN(CH 3 ) 2 ;
X2选自 CH2、 CO、 S02、 CH(CH3)、 CH(CN)、 COCH2、 CH2CH2、 CH2CO或 S02CH2; 选自氢、 NH2、 C C4垸基或 C C4卤代垸基； X 2 is selected from CH 2 , CO, SO 2 , CH(CH 3 ), CH(CN), COCH 2 , CH 2 CH 2 , CH 2 CO or SO 2 CH 2; selected from hydrogen, NH 2 , CC 4 alkyl base or CC 4 haloalkyl;
Y选自 -CO-、 -S02-、 -CH2-或 -COCH(CH(CH3)2)-; x选自 0或 1 ; Y is selected from -CO-, -S0 2 -, -CH 2 - or -COCH(CH(CH 3 ) 2 )- ; x is selected from 0 or 1;
Q选自被 n个各自独立的 R5取代的苯基、 吡啶基、 嘧啶基、 噻唑基、 苯并恶唑基、 苯 并吡嗪基或哒嗪酮基； Q is selected from phenyl, pyridyl, pyrimidinyl, thiazolyl, benzoxazolyl, benzopyrazinyl or pyridazinonyl substituted by n independent R 5 ;
R5选自 F、 Cl、 Br、 I、 CN、 N02、 C C4垸基、 卤代 C C4垸基、 C C4垸氧基、 卤代 d-C4垸氧基、 C02CH3、 C02CH2CH3、 S02CH3或 OCH2CF3 ; R 5 is selected from F, Cl, Br, I, CN, N0 2 , CC 4 alkyl, halogenated CC 4 alkyl, CC 4 alkyloxy, halogenated dC 4 alkyloxy, C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 or OCH 2 CF 3 ;
R6选自苯基、 4-氯苯基、 2,4-二氯苯基、 4-甲基苯基、 4-三氟甲基苯基、 4-甲氧基苯基、 2,6-二氯 -4-三氟甲基苯基、 苄基、 4-氯苄基、 4-叔丁基苄基、 4-三氟甲基苄基、 苯乙基、 2- 吡啶基、 3-氯 -2-吡啶基、 3,5-二氯 -2-吡啶基、 3,5,6-三氯 -2-吡啶基、 5-三氟甲基 -2-吡啶基、 5-甲基 -2-吡啶基、 3-氯 -5-氰基 -2-吡啶基、 3-氯 -5-三氟甲基 -2-吡啶基、 2-吡啶甲基、 2-氯 -5- 吡啶甲基、 3-氯 -5-三氟甲基 -2-吡啶甲基、 2-吡啶乙基、 3-氯 -5-三氟甲基 -2-吡啶乙基、噻唑 -2- 基、 2-氯 -5-噻唑基甲基或 2-嘧啶基； R 6 is selected from phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl, 2,6- Dichloro-4-trifluoromethylphenyl, benzyl, 4-chlorobenzyl, 4-tert-butylbenzyl, 4-trifluoromethylbenzyl, phenethyl, 2-pyridyl, 3-chloro -2-pyridyl, 3,5-dichloro-2-pyridyl, 3,5,6-trichloro-2-pyridyl, 5-trifluoromethyl-2-pyridyl, 5-methyl-2 -pyridyl, 3-chloro-5-cyano-2-pyridyl, 3-chloro-5-trifluoromethyl-2-pyridyl, 2-pyridylmethyl, 2-chloro-5-pyridylmethyl, 3-chloro-5-trifluoromethyl-2-pyridylmethyl, 2-pyridylethyl, 3-chloro-5-trifluoromethyl-2-pyridylethyl, thiazol-2-yl, 2-chloro- 5-thiazolylmethyl or 2-pyrimidinyl;
其中， 当 Q选自苯基或苯并吡嗪基时， n选自 1、 2、 3、 4或 5 ; Wherein, when Q is selected from phenyl or benzopyrazinyl, n is selected from 1, 2, 3, 4 or 5;
当 Q选自吡啶或苯并恶唑基时， n选自 1、 2、 3或 4; When Q is selected from pyridine or benzoxazolyl, n is selected from 1, 2, 3 or 4;
当 Q选自嘧啶或哒嗪酮基时， n选自 1、 2或 3 ; When Q is selected from pyrimidine or pyridazinone group, n is selected from 1, 2 or 3;
当 Q选自噻唑基时， n选自 1或 2; When Q is selected from thiazolyl, n is selected from 1 or 2;
当 n大于 1时， R5可相同或不同。 When n is greater than 1, R5 may be the same or different.
6、 根据权利要求 5所述的化合物， 其特征在于： 通式 (I)中 6. The compound according to claim 5, characterized in that: in general formula (I)
选自氢、 F、 Cl、 Br、 I、 CN、 N02、 CrC4垸基、 卤代 CrC4垸基、 CrC4垸氧基或卤 代 CrC4垸氧基； m选自 0至 5的整数； 当 m大于 1时， ！^可相同或不同； Selected from hydrogen , F, Cl, Br , I, CN , N02 , CrC4alkyl, halogenated CrC4alkyl , CrC4alkoxy or halogenated CrC4alkyloxy ; m is selected from an integer from 0 to 5; when m is greater than 1, ! ^can be the same or different;
R2选自氢、 F、 Cl、 Br、 I、 CN、 CrC4垸基、 卤代 CrC4垸基、 CrC4垸氧基、 卤代 -C4 垸氧基 R6; R 2 is selected from hydrogen, F, Cl, Br, I, CN, C r C 4 alkyl group, halogenated C r C 4 alkyl group, C r C 4 alkyloxy group, halogenated -C 4 alkyloxy group R6;
Ra、 Rb、 Rc、 Rd、 Re Rf、 Rg和 Rh各自独立的表示氢原子、 CrC4垸基、 卤代 CrC4垸 基、 卤代 CrC4垸氧基或 -C4垸氧羰基； 与 一起或者 Rc与 Rf—起可以结合形成饱和 的六元环； R a , R b , R c , R d , R e R f , R g and R h each independently represent a hydrogen atom, C r C 4 alkyl group, halogenated C r C 4 alkyl group, halogenated C r C 4 alkyloxy or -C 4 alkyloxycarbonyl; together or R c and R f can be combined to form a saturated six-membered ring;
Xi选自 N或 CR3 ; Xi is selected from N or CR 3;
R3选自氢或 CN; R 3 is selected from hydrogen or CN;
X2选自 CH2或 CO; X2 is selected from CH2 or CO;
选自氢、 CH3或 CF3; Selected from hydrogen, CH 3 or CF 3;
Y选自 -CO-或 -CH2-; x选自 0或 1 ; Y is selected from -CO- or -CH 2 - ; x is selected from 0 or 1;
Q选自被 n个各自独立的 R5取代的苯基、 吡啶基、 嘧啶基或者噻唑基； Q is selected from phenyl, pyridyl, pyrimidinyl or thiazolyl substituted by n independently R 5 ;
R5选自 F、 Cl、 Br、 I、 CN、 N02、 CrC4垸基、 卤代 CrC4垸基、 CrC4垸氧基、 卤代 d-C4垸氧基、 C02CH3、 C02CH2CH3、 S02CH3或 OCH2CF3 ; R5 is selected from F, Cl , Br, I , CN , N02 , CrC4alkyl, halogenated CrC4alkyl , CrC4alkoxy , halogenated C4alkyloxy , C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 or OCH 2 CF 3 ;
R6选自苯基、 4-氯苯基、 2,4-二氯苯基、 4-甲基苯基、 4-三氟甲基苯基、 4-甲氧基苯基、 R 6 is selected from phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl,
2,6-二氯 -4-三氟甲基苯基、 苄基、 4-氯苄基、 4-叔丁基苄基、 4-三氟甲基苄基或苯乙基、 2- 吡啶基、 3-氯 -2-吡啶基、 3,5-二氯 -2-吡啶基、 3,5,6-三氯 -2-吡啶基、 5-三氟甲基 -2-吡啶基、 5-甲基 -2-吡啶基、 3-氯 -5-氰基 -2-吡啶基、 3-氯 -5-三氟甲基 -2-吡啶基、 2-吡啶甲基、 2-氯 -5- 吡啶甲基、 3-氯 -5-三氟甲基 -2-吡啶甲基、 2-吡啶乙基或 3-氯 -5-三氟甲基 -2-吡啶乙基； 2,6-dichloro-4-trifluoromethylphenyl, benzyl, 4-chlorobenzyl, 4-tert-butylbenzyl, 4-trifluoromethylbenzyl or phenethyl, 2-pyridyl , 3-chloro-2-pyridyl, 3,5-dichloro-2-pyridyl, 3,5,6-trichloro-2-pyridyl, 5-trifluoromethyl-2-pyridyl, 5- Methyl-2-pyridyl, 3-chloro-5-cyano-2-pyridyl, 3-chloro-5-trifluoromethyl-2-pyridyl, 2-pyridylmethyl, 2-chloro-5- Pyridylmethyl, 3-chloro-5-trifluoromethyl-2-pyridylmethyl, 2-pyridylethyl or 3-chloro-5-trifluoromethyl-2-pyridylethyl;
其中， 当 Q选自苯基时， n选自 1、 2、 3或 4或 5; Wherein, when Q is selected from phenyl, n is selected from 1, 2, 3 or 4 or 5;
当 Q选自吡啶时， n选自 1、 2或 3或 4; When Q is selected from pyridine, n is selected from 1, 2 or 3 or 4;
当 Q选自嘧啶时， n选自 1、 2或 3; When Q is selected from pyrimidine, n is selected from 1, 2 or 3;
当 Q选自噻唑时， n选自 1或 2; When Q is selected from thiazole, n is selected from 1 or 2;
当 n大于 1时， R5可相同或不同。 When n is greater than 1, R5 may be the same or different.
7、 根据权利要求 6所述的化合物， 其特征在于： 通式 (I)中 7. The compound according to claim 6, characterized in that: in general formula (I)
Ri选自氢、 F、 Cl、 Br、 I、 CN、 N02、 C C4垸基或卤代 C C4垸基 C C4垸氧基或卤代 C C4垸氧基； m选自 0至 5的整数； 当 m大于 1时， 可相同或不同； Ri is selected from hydrogen, F, Cl, Br, I, CN, N0 2 , CC 4 alkyl or halogenated CC 4 alkyl CC 4 alkyloxy or halogenated CC 4 alkyloxy; m is selected from 0 to 5. Integer; when m is greater than 1, it can be the same or different;
R2选自氢、 F、 Cl、 Br、 I、 CN、 C C4垸基、 卤代 C C4垸基或 R6; R 2 is selected from hydrogen, F, Cl, Br, I, CN, CC 4 alkyl, halogenated CC 4 alkyl or R6;
Ra、 Rb、 Rc Rd、 Re、 Rf、 Rg和 各自独立的表示氢原子； R a , R b , Rc R d , R e , R f , R g and each independently represent hydrogen atoms;
Xi选自 CR3 ; Xi is selected from CR 3;
R3选自 CN; R 3 is selected from CN;
X2选自 CH2或 CO; X2 is selected from CH2 or CO;
选自氢； Selected from hydrogen;
Y选自 -CO-或 -CH2-; x选自 0或 1 ; Y is selected from -CO- or -CH 2 - ; x is selected from 0 or 1;
Q选自被 n个各自独立的 R5取代的苯基、 吡啶基、 嘧啶基或者噻唑基； Q is selected from phenyl, pyridyl, pyrimidinyl or thiazolyl substituted by n independently R 5 ;
R5选自 F、 Cl、 Br、 I、 CN、 N02、 C C4垸基或卤代 C C4垸基、 C C4垸氧基、 卤代 d-C4垸氧基、 C02CH3、 C02CH2CH3、 S02CH3或 OCH2CF3 ; R 5 is selected from F, Cl, Br, I, CN, N0 2 , CC 4 alkyl or halogenated CC 4 alkyl, CC 4 alkoxy, halogenated C 4 alkoxy, C0 2 CH 3 , C0 2 CH 2 CH 3 , S0 2 CH 3 or OCH 2 CF 3;
R6选自苯基、 4-氯苯基、 2,4-二氯苯基、 4-甲基苯基、 4-三氟甲基苯基、 4-甲氧基苯基、 2,6-二氯 -4-三氟甲基苯基、 苄基、 4-氯苄基、 4-叔丁基苄基、 4-三氟甲基苄基或苯乙基； 其中， 当 Q选自苯基时， n选自 1、 2、 3、 4或 5; R 6 is selected from phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl, 2,6- Dichloro-4-trifluoromethylphenyl, benzyl, 4-chlorobenzyl, 4-tert-butylbenzyl, 4-trifluoromethylbenzyl or phenethyl; wherein, when Q is selected from phenyl When , n is selected from 1, 2, 3, 4 or 5;
当 Q选自吡啶时， n选自 1或 2、 3或 4; When Q is selected from pyridine, n is selected from 1 or 2, 3 or 4;
当 Q选自嘧啶时， n选自 1或 2或 3; When Q is selected from pyrimidine, n is selected from 1 or 2 or 3;
当 Q选自噻唑时， n选自 1或 2; When Q is selected from thiazole, n is selected from 1 or 2;
当 n大于 1时， R5可相同或不同。 When n is greater than 1, R5 may be the same or different.
8、 根据权利要求 7所述的化合物， 其特征在于： 通式 (I)中 8. The compound according to claim 7, characterized in that: in general formula (I)
！^选自氢、 F、 Cl、 Br、 I、 CN、 N02、 CrC4垸基或卤代 CrC4垸基 CrC4垸氧基或卤代 CrC4垸氧基； m选自 0至 5的整数； 当 m大于 1时， ！^可相同或不同； ! ^ is selected from hydrogen, F, Cl, Br, I, CN, NO 2 , C r C 4 alkyl or halosubstituted C r C 4 alkyl C r C 4 alkyloxy or halosubstituted C r C 4 alkyloxy. ; m is selected from an integer from 0 to 5; when m is greater than 1, ! ^can be the same or different;
R2选自氢、 F、 Cl、 Br、 I、 CN、 CrC4垸基、 卤代 CrC4垸基或 R6; R 2 is selected from hydrogen, F, Cl, Br, I, CN, C r C 4 alkyl, halogenated C r C 4 alkyl or R6;
Ra、 Rb、 Rc Rd、 Re、 Rf、 Rg和 Rh各自独立的表示氢原子； Xi选自 CR3 ; R a , R b , R c R d , R e , R f , R g and R h each independently represent hydrogen atoms; Xi is selected from CR 3;
R3选自 CN; R 3 is selected from CN;
X2选自 CH2或 CO; X2 is selected from CH2 or CO;
选自氢； Selected from hydrogen;
Y选自 -CO-或 -CH2-; x选自 0或 1 ; Y is selected from -CO- or -CH 2 - ; x is selected from 0 or 1;
Q选自被 n个各自独立的 R5取代的苯基、 吡啶基、 嘧啶基或噻唑基； Q is selected from phenyl, pyridyl, pyrimidinyl or thiazolyl substituted by n independently R 5 ;
R5选自 F、 Cl、 Br、 I、 CN、 N02、 CrC4垸基、 卤代 CrC4垸基、 CrC4垸氧基、 卤代 d-C4垸氧基、 S02CH3或 OCH2CF3 ; R5 is selected from F, Cl , Br , I , CN , N02 , CrC4alkyl, halogenated CrC4alkyl, CrC4alkoxy , halogenated C4alkyloxy , S0 2 CH 3 or OCH 2 CF 3 ;
R6选自苯基、 4-氯苯基、 2,4-二氯苯基、 4-甲基苯基、 4-三氟甲基苯基、 4-甲氧基苯基或 2,6-二氯 -4-三氟甲基苯基。 R 6 is selected from phenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 4-methylphenyl, 4-trifluoromethylphenyl, 4-methoxyphenyl or 2,6- Dichloro-4-trifluoromethylphenyl.
其中， 当 Q选自苯基时， n选自 1、 2或 3; Wherein, when Q is selected from phenyl, n is selected from 1, 2 or 3;
当 Q选自吡啶时， n选自 1或 2或 3; When Q is selected from pyridine, n is selected from 1 or 2 or 3;
当 Q选自嘧啶时， n选自 1或 2; When Q is selected from pyrimidine, n is selected from 1 or 2;
当 Q选自噻唑时， n选自 1或 2; When Q is selected from thiazole, n is selected from 1 or 2;
当 n大于 1时， R5可相同或不同。 When n is greater than 1, R5 may be the same or different.
9、 根据权利要求 8所述的化合物， 其特征在于： 通式 (I)中 9. The compound according to claim 8, characterized in that: in general formula (I)
Ri选自氢、 F、 Cl、 Br、 I、 CN、 N02、 C C4垸基或卤代 C C4垸基； m选自 0至 5的 整数； 当 m大于 1时， 可相同或不同； Ri is selected from hydrogen, F, Cl, Br, I, CN, N0 2 , CC 4 alkyl or halogenated CC 4 alkyl; m is selected from an integer from 0 to 5; when m is greater than 1, it can be the same or different;
R2选自氢、 C C4垸基、 卤代 C C4垸基或 R6; R 2 is selected from hydrogen, CC 4 alkyl, halogenated CC 4 alkyl or R6;
Ra、 Rb、 Rc、 Rd、 Re、 Rf、 Rg和 Rh各自独立的表示氢原子； R a , R b , R c , R d , R e , R f , R g and R h each independently represent hydrogen atoms;
Xi选自 CR3 ; Xi is selected from CR 3;
R3选自 CN; R 3 is selected from CN;
X2选自 CO; X 2 is selected from CO;
选自氢； Selected from hydrogen;
Y选自 -CO-或 -CH2-; x选自 0; Y is selected from -CO- or -CH 2 - ; x is selected from 0;
Q选自被 1个 R5取代的吡啶基； Q is selected from pyridyl substituted by 1 R 5 ;
R5选自氢、 F、 Cl、 Br、 I、 CN、 N02、 C C4垸基或卤代 C C4垸基； R 5 is selected from hydrogen, F, Cl, Br, I, CN, N0 2 , CC 4 alkyl or halogenated CC 4 alkyl;
R6选自苯基。 R 6 is selected from phenyl.
10、一种制备如权利要求 1所述的通式 (I)化合物的方法， 由通式 (II)与通式 (III)化合物在 适 10. A method for preparing the compound of general formula (I) as claimed in claim 1, by compound of general formula (II) and general formula (III) at the appropriate
Figure imgf000063_0001
Figure imgf000063_0001
式中： L是离去基团， 选自卤素、 甲磺酰基或对甲苯磺酰基， 其他各基团定义如权利要 求 1所述。 In the formula: L is a leaving group, selected from halogen, methanesulfonyl or p-toluenesulfonyl, and the other groups are defined as described in claim 1.
11、 一种按照权利要求 1-9中任意一项所述的通式 (I)化合物在农业或其他领域中作为杀 虫杀螨剂的用途。 11. The use of a compound of general formula (I) according to any one of claims 1 to 9 as an insecticide and acaricide in agriculture or other fields.
12、 一种杀虫杀螨组合物， 其特征在于： 含有如权利要求 1-9中任意一项所述的通式 (I) 化合物作为活性组分， 组合物中通式 (I)化合物的重量百分含量为 0.1-99%。 12. An insecticidal and acaricidal composition, characterized in that: it contains the compound of general formula (I) as described in any one of claims 1 to 9 as an active component, and the compound of general formula (I) in the composition The weight percentage is 0.1-99%.
13、 一种按照权利要求 12所述的组合物在农业或其他领域中作为杀虫杀螨剂的用途。 13. Use of a composition according to claim 12 as an insecticide and acaricide in agriculture or other fields.
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WO2021215393A1 (en) * 2020-04-22 2021-10-28 日本曹達株式会社 Benzamide compound and pest control agent
WO2022207462A1 (en) 2021-03-30 2022-10-06 Syngenta Crop Protection Ag Pesticidally active cyclic amine compounds
WO2022219146A2 (en) 2021-04-16 2022-10-20 Syngenta Crop Protection Ag Pesticidally active cyclic amine compounds
WO2022239798A1 (en) 2021-05-14 2022-11-17 日本曹達株式会社 (hetero)arylamide compound and pest control agent
KR20240008308A (en) 2021-05-14 2024-01-18 닛뽕소다 가부시키가이샤 (Hetero)arylamide compounds and harmful organism control agents

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