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公开(公告)号:EP1809638B1
公开(公告)日:2010-02-17
申请号:EP04806740.9
申请日:2004-11-01
申请人: Hetero Drugs Limited
发明人: PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, K., Hetero Drugs Limited (R & D) , RAJI REDDY, R., Hetero Drugs Limited (R & D) , MURALIDHARA REDDY, D., Hetero Drugs Limited R & D , MURALI, Nagabelli, Hetero Drugs Limited
IPC分类号: C07D501/04 , C07D501/22
CPC分类号: C07D501/22 , C07F7/188
摘要: The present invention relates to a process for preparing a key intermediate of cefprozil and use of this intermediate in the preparation of cefprozil thereby avoiding impurity-causing self-acylation. [R-(Z)]-[4-hydroxy-α-[(3-methoxy-l-methyl-3-oxo-1-propenyl)amino]] benzeneacetic acid, mono potassium salt is reacted with ethyl chloroformate to obtain mixed anhydride which is then silylated with N,O-bis(trimethylsilyl)acetamide. The silylated compound obtained is reacted with [7-trimethylsilylamino-3-(Z/E-propen-1-yl)-3-cephem-4-carboxylic acid]trimethylsilyl ester and deprotected with aqueous hydrochloric acid to give cefprozil.
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公开(公告)号:EP1809638A1
公开(公告)日:2007-07-25
申请号:EP04806740.9
申请日:2004-11-01
申请人: Hetero Drugs Limited
发明人: PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, K., Hetero Drugs Limited (R & D) , RAJI REDDY, R., Hetero Drugs Limited (R & D) , MURALIDHARA REDDY, D., Hetero Drugs Limited R & D , MURALI, Nagabelli, Hetero Drugs Limited
IPC分类号: C07D501/04 , C07D501/22
CPC分类号: C07D501/22 , C07F7/188
摘要: The present invention relates to a process for preparing a key intermediate of cefprozil and use of this intermediate in the preparation of cefprozil thereby avoiding impurity-causing self-acylation. [R-(Z)]-[4-hydroxy-α-[(3-methoxy-l-methyl-3-oxo-1-propenyl)amino]] benzeneacetic acid, mono potassium salt is reacted with ethyl chloroformate to obtain mixed anhydride which is then silylated with N,O-bis(trimethylsilyl)acetamide. The silylated compound obtained is reacted with [7-trimethylsilylamino-3-(Z/E-propen-1-yl)-3-cephem-4-carboxylic acid]trimethylsilyl ester and deprotected with aqueous hydrochloric acid to give cefprozil.
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