JP5628427B2 - ロスバスタチンカルシウム中間物の調製方法 - Google Patents
ロスバスタチンカルシウム中間物の調製方法 Download PDFInfo
- Publication number
- JP5628427B2 JP5628427B2 JP2013522078A JP2013522078A JP5628427B2 JP 5628427 B2 JP5628427 B2 JP 5628427B2 JP 2013522078 A JP2013522078 A JP 2013522078A JP 2013522078 A JP2013522078 A JP 2013522078A JP 5628427 B2 JP5628427 B2 JP 5628427B2
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- JP
- Japan
- Prior art keywords
- borohydride
- potassium
- cooh
- lithium
- zinc
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
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- 0 CCCC(C1*)=NC(N(C)*)=NC1c(cc1)ccc1F Chemical compound CCCC(C1*)=NC(N(C)*)=NC1c(cc1)ccc1F 0.000 description 2
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Description
(1)式IIに示すエステル類化合物を金属化合物の存在する条件の下で加水分解して、式IIIに示すカルボン酸化合物が得られる。
II
III
RはC1〜C5のアルキル基である。
Claims (4)
- ステップ(1)において、前記金属化合物はLiOH又はその水素化物であることを特徴とする請求項1に記載のロスバスタチンカルシウム中間物の調製方法。
- ホウ水素化物とルイス酸還元システムは、水素化ホウ素カリウムと三フッ化ホウ素ジエチルエーテルシステム、水素化ホウ素ナトリウムと三フッ化ホウ素ジエチルエーテルシステム、水素化ホウ素リチウムと三フッ化ホウ素ジエチルエーテルシステム、水素化ホウ素カリウムとH2SO4システム、水素化ホウ素カリウムとZnCl2システム、水素化ホウ素カリウムとAlCl3システム、水素化ホウ素カリウムとI2システム、水素化ホウ素カリウムとCF3COOHシステム、水素化ホウ素カリウムとHCOOHシステム、水素化ホウ素カリウムとMsOHシステム、水素化ホウ素カリウムとCH3COOHシステム、水素化ホウ素カリウムとNiCl2システム、水素化ホウ素亜鉛とH2SO4システム、水素化ホウ素亜鉛とZnCl2システム、水素化ホウ素亜鉛とAlCl3システム、水素化ホウ素亜鉛とI2システム、水素化ホウ素亜鉛とCF3COOHシステム、水素化ホウ素亜鉛とHCOOHシステム、水素化ホウ素亜鉛とMsOHシステム、水素化ホウ素亜鉛とCH3COOHシステム、水素化ホウ素亜鉛とNiCl2システム、水素化ホウ素ナトリウムとH2SO4システム、水素化ホウ素ナトリウムとZnCl2システム、水素化ホウ素ナトリウムとAlCl3システム、水素化ホウ素ナトリウムとI2システム、水素化ホウ素ナトリウムとCF3COOHシステム、水素化ホウ素ナトリウムとHCOOHシステム、水素化ホウ素ナトリウムとMsOHシステム、水素化ホウ素ナトリウムとCH3COOHシステム、水素化ホウ素ナトリウムとNiCl2システム、水素化ホウ素リチウムとH2SO4システム、水素化ホウ素リチウムとZnCl2システム、水素化ホウ素リチウムとAlCl3システム、水素化ホウ素リチウムとI2システム、水素化ホウ素リチウムとCF3COOHシステム、水素化ホウ素リチウムとHCOOHシステム、水素化ホウ素リチウムとMsOHシステム、水素化ホウ素リチウムとCH3COOHシステム、水素化ホウ素リチウムとNiCl2システムであることを特徴とする請求項1に記載のロスバスタチンカルシウム中間物の調製方法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2010102449638A CN101955463B (zh) | 2010-08-04 | 2010-08-04 | 瑞舒伐他汀钙中间体的制备方法 |
CN201010244963.8 | 2010-08-04 | ||
PCT/CN2011/075757 WO2012016479A1 (zh) | 2010-08-04 | 2011-06-15 | 瑞舒伐他汀钙中间体的制备方法 |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2013532693A JP2013532693A (ja) | 2013-08-19 |
JP5628427B2 true JP5628427B2 (ja) | 2014-11-19 |
Family
ID=43483082
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2013522078A Expired - Fee Related JP5628427B2 (ja) | 2010-08-04 | 2011-06-15 | ロスバスタチンカルシウム中間物の調製方法 |
Country Status (6)
Country | Link |
---|---|
US (1) | US8703944B2 (ja) |
EP (1) | EP2602250B1 (ja) |
JP (1) | JP5628427B2 (ja) |
KR (1) | KR20130027568A (ja) |
CN (1) | CN101955463B (ja) |
WO (1) | WO2012016479A1 (ja) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101955463B (zh) * | 2010-08-04 | 2012-01-04 | 重庆博腾制药科技股份有限公司 | 瑞舒伐他汀钙中间体的制备方法 |
CN102757318B (zh) * | 2011-04-29 | 2015-06-24 | 上海医药工业研究院 | 一种阿利克伦中间体的制备方法 |
CN102351662B (zh) * | 2011-08-17 | 2014-02-05 | 常州市华人化工有限公司 | (s)-(+)-2-甲氧基甲氧基-1-丙醇的制备方法 |
CN102617481A (zh) * | 2012-03-16 | 2012-08-01 | 湖南欧亚生物有限公司 | 一种瑞舒伐他汀钙的制备方法 |
CN103044339A (zh) * | 2012-10-15 | 2013-04-17 | 武汉市江润精细化工有限责任公司 | 瑞舒伐他汀钙中间体的制备方法 |
CN103864697A (zh) * | 2012-12-11 | 2014-06-18 | 润泽制药(苏州)有限公司 | 瑞舒伐中间体主链醇的制备方法 |
CN103319419A (zh) * | 2013-06-18 | 2013-09-25 | 复旦大学 | 一种4-对氟苯基6-异丙基-2-(n-甲基甲磺酰胺基)嘧啶-5-羧酸的制备方法 |
CN103570762B (zh) * | 2013-11-25 | 2015-12-09 | 复旦大学 | ((4-对氟苯基-6-异丙基-2-(n-甲基甲磺酰胺基)-5-吡啶基)甲基)三苯基鏻盐的制备方法 |
CN106632078B (zh) * | 2016-11-11 | 2019-05-07 | 上海雅本化学有限公司 | 一种瑞舒伐他汀钙中间体的精制方法 |
Family Cites Families (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2648897B2 (ja) | 1991-07-01 | 1997-09-03 | 塩野義製薬株式会社 | ピリミジン誘導体 |
AR034772A1 (es) * | 2001-07-13 | 2004-03-17 | Astrazeneca Uk Ltd | Preparacion de los compuestos de aminopirimidina |
EA200401533A1 (ru) * | 2002-05-21 | 2005-06-30 | Ранбакси Лабораторис Лимитед | Способ получения росувастатина |
WO2004103977A2 (en) * | 2003-05-21 | 2004-12-02 | Ciba Specialty Chemicals Holding Inc. | Process for the preparation of pyrimidine derivatives |
HUP0400405A3 (en) * | 2004-02-10 | 2009-03-30 | Sanofi Synthelabo | Pyrimidine derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates |
CN1872841A (zh) * | 2005-06-01 | 2006-12-06 | 信谊药厂 | 瑞舒伐他汀钙及其关键中间体的制备方法 |
CN1958593B (zh) * | 2005-11-03 | 2010-05-05 | 上海医药工业研究院 | 一种用于合成瑞舒伐他汀钙的中间体的制备方法 |
US7659281B2 (en) * | 2006-04-25 | 2010-02-09 | Bristol-Myers Squibb Company | HMG-CoA reductase inhibitors |
WO2008059519A2 (en) * | 2006-09-25 | 2008-05-22 | Glenmark Pharmaceuticals Limited | A process for the preparation of intermediates of rosuvastatin |
CN101190897B (zh) * | 2006-11-30 | 2011-05-11 | 天津天士力集团有限公司 | 一种4-(4-氟苯基)-6-异丙基-2-甲胺基嘧啶-5-甲酸酯的合成方法 |
CN101376647B (zh) * | 2007-08-31 | 2010-12-08 | 中山奕安泰医药科技有限公司 | 一种用于合成瑞舒伐他汀中间体及瑞舒伐他汀的合成方法 |
CN103025727B (zh) * | 2010-07-01 | 2015-09-02 | 柳韩洋行 | HMG-CoA还原酶抑制剂及其中间体的制备方法 |
CN101955463B (zh) * | 2010-08-04 | 2012-01-04 | 重庆博腾制药科技股份有限公司 | 瑞舒伐他汀钙中间体的制备方法 |
-
2010
- 2010-08-04 CN CN2010102449638A patent/CN101955463B/zh active Active
-
2011
- 2011-06-15 EP EP11814062.3A patent/EP2602250B1/en not_active Not-in-force
- 2011-06-15 WO PCT/CN2011/075757 patent/WO2012016479A1/zh active Application Filing
- 2011-06-15 KR KR1020137003414A patent/KR20130027568A/ko not_active Application Discontinuation
- 2011-06-15 JP JP2013522078A patent/JP5628427B2/ja not_active Expired - Fee Related
-
2013
- 2013-02-03 US US13/757,846 patent/US8703944B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
EP2602250A4 (en) | 2014-02-26 |
CN101955463A (zh) | 2011-01-26 |
EP2602250B1 (en) | 2016-03-23 |
US8703944B2 (en) | 2014-04-22 |
CN101955463B (zh) | 2012-01-04 |
EP2602250A1 (en) | 2013-06-12 |
JP2013532693A (ja) | 2013-08-19 |
KR20130027568A (ko) | 2013-03-15 |
WO2012016479A1 (zh) | 2012-02-09 |
US20130143908A1 (en) | 2013-06-06 |
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