发明公开
- 专利标题: Racemization and Enantiomer Separation of Clopidogrel
- 专利标题(中): 消旋和氯吡格雷的Ennatiomertrennung
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申请号: EP09171852.8申请日: 2002-11-22
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公开(公告)号: EP2168969A3公开(公告)日: 2011-02-09
- 发明人: Merli, Valeriano , Daverio, Paola , Bianchi, Stefano
- 申请人: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
- 申请人地址: 5 Basel Street, P.O. Box 3190 49131 Petah Tiqva IL
- 专利权人: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
- 当前专利权人: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
- 当前专利权人地址: 5 Basel Street, P.O. Box 3190 49131 Petah Tiqva IL
- 代理机构: Russell, Tim
- 优先权: US400738P 20020802
- 主分类号: C07D495/04
- IPC分类号: C07D495/04 ; A61K31/4365 ; A61P9/00
摘要:
Processes for separation of enantiomers of clopidogrel, and converting one enantiomer of clopidogrel to another enantiomer of clopidogrel are provided. The enantiomers are separated by crystallizing the (S) enantiomer as camphor sulfonate salt from a hydrocarbon, or a mixture of a hydrocarbon and a co-solvent, preferably DMF:toluene. The (R) enantiomer is then racemized and recycled by reaction with a catalytic amount of a base, preferably with t-butoxide.
公开/授权文献
- EP2168969A2 Racemization and Enantiomer Separation of Clopidogrel 公开/授权日:2010-03-31
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