KR960007610A - N-아실-5-플루오로시티딘 유도체의 제조 방법 - Google Patents
N-아실-5-플루오로시티딘 유도체의 제조 방법 Download PDFInfo
- Publication number
- KR960007610A KR960007610A KR1019950026517A KR19950026517A KR960007610A KR 960007610 A KR960007610 A KR 960007610A KR 1019950026517 A KR1019950026517 A KR 1019950026517A KR 19950026517 A KR19950026517 A KR 19950026517A KR 960007610 A KR960007610 A KR 960007610A
- Authority
- KR
- South Korea
- Prior art keywords
- acyl
- formula
- preparing
- fluorocytidine
- aralkyl
- Prior art date
Links
- 125000003342 alkenyl group Chemical group 0.000 claims abstract 3
- 125000000217 alkyl group Chemical group 0.000 claims abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims abstract 3
- 125000003118 aryl group Chemical group 0.000 claims abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 3
- 150000001875 compounds Chemical class 0.000 claims 2
- 150000007529 inorganic bases Chemical class 0.000 claims 1
- 150000007530 organic bases Chemical class 0.000 claims 1
- 239000003960 organic solvent Substances 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/067—Pyrimidine radicals with ribosyl as the saccharide radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biotechnology (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Saccharide Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
하기 일반식(I)의 공지 항종양제인 N4-아실-5'-데옥시-5-플루오로시티딘 유도체는 일반식(Ⅱ)의 신규 중간화합물로부터 제조된다:
상기식에서, R은 알킬, 사이클로알킬, 알케닐, 아르알킬 또는 아릴이다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (2)
- 수성 또는 불활성 유기 용매중에서 하기 일반식(Ⅱ)의 화합물을 유기 또는 무기 염기로 처리함을 포함하는, 하기 일반식(I)의 N4-아실-5'-데옥시-5-플루오로시티딘 유도체의 제조 방법.상기식에서, R은 알킬, 사이클로알킬, 알케닐, 아르알킬 또는 아릴이다.
- 하기 일반식(Ⅱ)의 화합물:상기식에서, R은 알킬, 사이클로알킬, 알케닐, 아르알킬 또는 아릴이다.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/296,842 US5476932A (en) | 1994-08-26 | 1994-08-26 | Process for producing N4-acyl-5'-deoxy-5-fluorocytidine derivatives |
US08/296842 | 1994-08-26 | ||
US08/296,842 | 1994-08-26 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR960007610A true KR960007610A (ko) | 1996-03-22 |
KR100335542B1 KR100335542B1 (ko) | 2002-11-08 |
Family
ID=23143805
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019950026517A KR100335542B1 (ko) | 1994-08-26 | 1995-08-25 | N-아실-5-플루오로시티딘유도체의제조방법 |
Country Status (9)
Country | Link |
---|---|
US (1) | US5476932A (ko) |
EP (1) | EP0698611B1 (ko) |
JP (1) | JP3986574B2 (ko) |
KR (1) | KR100335542B1 (ko) |
CN (1) | CN1053194C (ko) |
AT (1) | ATE185811T1 (ko) |
DE (1) | DE69512851T2 (ko) |
DK (1) | DK0698611T3 (ko) |
ES (1) | ES2138691T3 (ko) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20060042198A (ko) * | 2004-02-26 | 2006-05-12 | 미쓰이 가가쿠 가부시키가이샤 | N4─아실시티딘 유도체의 금속염, 및 이 금속염을 사용하는 n4─아실시티딘 유도체의 제조 방법 |
Families Citing this family (43)
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NZ330360A (en) * | 1997-06-02 | 1999-03-29 | Hoffmann La Roche | 5'-deoxy-cytidine derivatives, their manufacture and use as antitumoral agents |
KR100631754B1 (ko) * | 2000-08-09 | 2006-10-09 | 주식회사 코오롱 | N-알킬옥시카르보닐-5-플루오로사이토신 유도체 및 그의제조방법 |
WO2003097609A1 (en) | 2002-05-15 | 2003-11-27 | Janssen Pharmaceutica N.V. | N-substituted tricyclic 3-aminopyrazoles as pdfg receptor inhibitors |
KR100851272B1 (ko) * | 2003-12-22 | 2008-08-08 | 에프. 호프만-라 로슈 아게 | 플루오로시티딘 유도체에 대한 방법 |
CN100383128C (zh) * | 2004-02-23 | 2008-04-23 | 上海迪赛诺医药发展有限公司 | N4-氧羰基胞嘧啶衍生物及制备方法与应用 |
US20080161251A1 (en) | 2005-01-21 | 2008-07-03 | Astex Therapeutics Limited | Pharmaceutical Compounds |
US10603314B2 (en) | 2005-02-03 | 2020-03-31 | The General Hospital Corporation | Method for treating gefitinib resistant cancer |
EP1868608A2 (en) * | 2005-04-01 | 2007-12-26 | F. Hoffmann-Roche AG | Method for administration of capecitabine |
CN100569790C (zh) * | 2005-07-15 | 2009-12-16 | 上海奥锐特国际贸易有限公司 | 合成n4-酰基-5'-脱氧-5-氟胞苷衍生物的方法 |
AR057854A1 (es) | 2005-11-04 | 2007-12-19 | Wyeth Corp | Combinaciones antineoplasicas con inhibidor de mtor, herceptina y/o hki-272 (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi) anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida |
US20080085310A1 (en) * | 2006-10-06 | 2008-04-10 | Maria Oksana Bachynsky | Capecitabine rapidly disintegrating tablets |
EP2073807A1 (en) | 2006-10-12 | 2009-07-01 | Astex Therapeutics Limited | Pharmaceutical combinations |
US8916552B2 (en) | 2006-10-12 | 2014-12-23 | Astex Therapeutics Limited | Pharmaceutical combinations |
CN100425617C (zh) * | 2006-10-31 | 2008-10-15 | 浙江海正药业股份有限公司 | 一种含氟嘧啶类化合物烷氧羰酰化的方法 |
ITMI20070435A1 (it) | 2007-03-05 | 2008-09-06 | Innovate Biotechnology Srl | 2',3'-di-o-acil-5-fluoronucleosidi |
WO2009022435A1 (ja) * | 2007-08-15 | 2009-02-19 | Japan Absorbent Technology Institute | 吸収体製品およびその製造方法 |
US8022216B2 (en) | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
KR101013312B1 (ko) * | 2007-11-19 | 2011-02-09 | 한미홀딩스 주식회사 | 카페시타빈의 제조방법 및 이에 사용되는 β-아노머가강화된 트리알킬카보네이트 화합물의 제조방법 |
AR064165A1 (es) | 2007-12-06 | 2009-03-18 | Richmond Sa Com Ind Y Financie | Un procedimiento para la preparacion de capecitabina e intermediarios utilizables en dicho procedimiento |
WO2009094847A1 (fr) * | 2007-12-28 | 2009-08-06 | Topharman Shanghai Co., Ltd. | Dérivé hydroxyle de capécitabine, procédés de préparation et d' utilisation de la capécitabine |
WO2009082846A1 (fr) * | 2007-12-28 | 2009-07-09 | Topharman Shanghai Co., Ltd. | Dérivé hydroxyle de la capécitabine, ses procédés de préparation et ses utilisations pour préparer la capécitabine |
CN101469008B (zh) * | 2007-12-29 | 2013-08-07 | 上海特化医药科技有限公司 | 卡培他滨羟基衍生物、其制备方法和用于制备卡培他滨 |
WO2009082844A1 (fr) * | 2007-12-28 | 2009-07-09 | Topharman Shanghai Co., Ltd | Dérivé hydroxyle de la capécitabine, ses procédés de préparation et ses utilisations pour préparer la capécitabine |
US20090209754A1 (en) * | 2008-01-03 | 2009-08-20 | Macdonald Peter Lindsay | Process for the preparation of capecitabine |
HUE028327T2 (en) | 2008-06-06 | 2017-02-28 | Neurmedix Inc | A process for the preparation of 17-alkynyl-7-hydroxy steroids and related compounds |
PT2310011E (pt) | 2008-06-17 | 2013-10-07 | Wyeth Llc | Combinações antineoplásicas contendo hki-272 e vinorelbina |
LT2326329T (lt) | 2008-08-04 | 2017-05-25 | Wyeth Llc | 4-anilin-3-cianochinolinų ir kapecitabino antinavikiniai deriniai |
AU2010234968B2 (en) | 2009-04-06 | 2015-05-14 | Wyeth Llc | Treatment regimen utilizing neratinib for breast cancer |
WO2011067588A1 (en) | 2009-12-04 | 2011-06-09 | Generics [Uk] Limited | Cyclic sulphinyl esters of cytidine |
WO2011104540A1 (en) | 2010-02-24 | 2011-09-01 | Generics [Uk] Limited | One step process for the preparation of capecitabine |
CN102260309B (zh) * | 2010-05-24 | 2014-10-22 | 重庆福安药业(集团)股份有限公司 | 一种高纯度卡培他滨的制备方法 |
KR102090740B1 (ko) | 2011-10-03 | 2020-03-18 | 엠엑스 아쥬바크 에이비 | 암 치료 및 식품 관련 화합물을 포함하는 의학 분야에서 양친매성 또는 소수성 분자를 위한 나노입자, 제조 방법 및 담체로의 용도 |
TWI560195B (en) * | 2012-01-13 | 2016-12-01 | Pharmaessentia Corp | Novel synthesis of 5-deoxy-5'-fluorocytidine compounds |
AR095962A1 (es) | 2013-04-01 | 2015-11-25 | Moreinx Ab | Nanopartículas, compuestas de esterol y saponina de quillaja saponaria molina, proceso para preparación y uso de las mismas como portadores para moléculas anfipáticas o hidrófobas en el campo de la medicina incluyendo tratamiento de cáncer y compuestos relacionados con alimentos |
CN104926901B (zh) * | 2015-06-15 | 2018-04-20 | 广安凯特制药有限公司 | 一种卡培他滨关键中间体的合成方法 |
US11584733B2 (en) | 2017-01-09 | 2023-02-21 | Shuttle Pharmaceuticals, Inc. | Selective histone deacetylase inhibitors for the treatment of human disease |
CA3049435A1 (en) | 2017-01-09 | 2018-07-12 | Scott Grindrod | Selective histone deacetylase inhibitors for the treatment of human disease |
US10435429B2 (en) | 2017-10-03 | 2019-10-08 | Nucorion Pharmaceuticals, Inc. | 5-fluorouridine monophosphate cyclic triester compounds |
US11407723B2 (en) | 2018-01-09 | 2022-08-09 | Shuttle Pharmaceuticals, Inc. | Selective histone deacetylase inhibitors for the treatment of human disease |
WO2019143860A1 (en) * | 2018-01-19 | 2019-07-25 | Nucorion Pharmaceuticals, Inc. | 5-fluorouracil compounds |
US11427550B2 (en) | 2018-01-19 | 2022-08-30 | Nucorion Pharmaceuticals, Inc. | 5-fluorouracil compounds |
EP3669890A1 (en) | 2018-12-18 | 2020-06-24 | Croda International PLC | Filamentous nanoparticles having vaccine adjuvant effect |
KR20230004716A (ko) | 2020-04-21 | 2023-01-06 | 리간드 파마슈티칼스 인코포레이티드 | 뉴클레오티드 프로드러그 화합물 |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1982000997A1 (en) * | 1980-09-22 | 1982-04-01 | Johannson R | Carriage assembly with shiftable forks |
CA1327358C (en) * | 1987-11-17 | 1994-03-01 | Morio Fujiu | Fluoro cytidine derivatives |
TW254946B (ko) * | 1992-12-18 | 1995-08-21 | Hoffmann La Roche | |
AU671491B2 (en) * | 1992-12-18 | 1996-08-29 | F. Hoffmann-La Roche Ag | N-oxycarbonyl substituted 5'-deoxy-5-fluorcytidines |
-
1994
- 1994-08-26 US US08/296,842 patent/US5476932A/en not_active Expired - Lifetime
-
1995
- 1995-08-09 DE DE69512851T patent/DE69512851T2/de not_active Expired - Lifetime
- 1995-08-09 ES ES95112521T patent/ES2138691T3/es not_active Expired - Lifetime
- 1995-08-09 DK DK95112521T patent/DK0698611T3/da active
- 1995-08-09 EP EP95112521A patent/EP0698611B1/en not_active Expired - Lifetime
- 1995-08-09 AT AT95112521T patent/ATE185811T1/de active
- 1995-08-21 JP JP21157995A patent/JP3986574B2/ja not_active Expired - Lifetime
- 1995-08-25 CN CN95109396A patent/CN1053194C/zh not_active Expired - Lifetime
- 1995-08-25 KR KR1019950026517A patent/KR100335542B1/ko not_active IP Right Cessation
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20060042198A (ko) * | 2004-02-26 | 2006-05-12 | 미쓰이 가가쿠 가부시키가이샤 | N4─아실시티딘 유도체의 금속염, 및 이 금속염을 사용하는 n4─아실시티딘 유도체의 제조 방법 |
Also Published As
Publication number | Publication date |
---|---|
DE69512851T2 (de) | 2000-05-04 |
CN1053194C (zh) | 2000-06-07 |
ATE185811T1 (de) | 1999-11-15 |
CN1126726A (zh) | 1996-07-17 |
KR100335542B1 (ko) | 2002-11-08 |
DE69512851D1 (de) | 1999-11-25 |
US5476932A (en) | 1995-12-19 |
JPH0859687A (ja) | 1996-03-05 |
ES2138691T3 (es) | 2000-01-16 |
JP3986574B2 (ja) | 2007-10-03 |
DK0698611T3 (da) | 2000-03-27 |
EP0698611A1 (en) | 1996-02-28 |
EP0698611B1 (en) | 1999-10-20 |
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