发明授权
US06903211B2 Process for the preparation of 3-propenyl cephalosporin DMF solvate
失效
3-丙烯基头孢菌素DMF溶剂化物的制备方法
- 专利标题: Process for the preparation of 3-propenyl cephalosporin DMF solvate
- 专利标题(中): 3-丙烯基头孢菌素DMF溶剂化物的制备方法
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申请号: US10315010申请日: 2002-12-10
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公开(公告)号: US06903211B2公开(公告)日: 2005-06-07
- 发明人: Pandurang Balwant Deshpande , Bhausaheb Pandharinath Khadangale , Kumar Gurusamy , Ramesh Athmaram Konda
- 申请人: Pandurang Balwant Deshpande , Bhausaheb Pandharinath Khadangale , Kumar Gurusamy , Ramesh Athmaram Konda
- 申请人地址: IN Chennai
- 专利权人: Orchid Chemicals & Pharmaceuticals Limited
- 当前专利权人: Orchid Chemicals & Pharmaceuticals Limited
- 当前专利权人地址: IN Chennai
- 代理机构: Oliff & Berridge, PLC
- 优先权: IN800/MAS/2002 20021030
- 主分类号: C07D501/00
- IPC分类号: C07D501/00 ; C07D501/04 ; C07D501/12 ; C07D510/22
摘要:
The present invention relates to an improved process for the preparation of cefprozil DMF solvate of formula (I), which is useful for the preparation of cefprozil, comprising: i) reacting a compound of formula (VIII) with acetaldehyde to produce a compound of formula (IX), ii) deesterifying the carboxy protecting group of the compound of formula (IX) using an acid to yield a compound of formula (X), iii) converting the compound of formula (X) to a compound of formula (XI), iv) neutralizing the compound of formula (XI) followed by enzymatic hydrolysis to produce an APCA of formula (V), v) silylating the APCA using a mixture of trimethylsilylchloride and hexamethyldisilazane to produce silylated APCA of formula (XII), and vi) condensing the silylated APCA with a mixed anhydride to produce the DMF solvate compound of formula (I).
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