公开(公告)号：US06903211B2

公开(公告)日：2005-06-07

申请号：US10315010

申请日：2002-12-10

申请人： Pandurang Balwant Deshpande ,  Bhausaheb Pandharinath Khadangale ,  Kumar Gurusamy ,  Ramesh Athmaram Konda

发明人： Pandurang Balwant Deshpande ,  Bhausaheb Pandharinath Khadangale ,  Kumar Gurusamy ,  Ramesh Athmaram Konda

IPC分类号： C07D501/00 ,  C07D501/04 ,  C07D501/12 ,  C07D510/22

CPC分类号： C07D501/00 ,  Y02P20/55

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).

摘要翻译： 本发明涉及用于制备式（I）的头孢丙呋胺溶剂化物的改进方法，其可用于制备头孢丙烯，其包括：i）使式（Ⅷ）化合物与乙醛反应以制备式 （Ⅸ）化合物，ⅱ）使用酸去除式（Ⅸ）化合物的羧基保护基，得到式（Ⅹ）化合物，ⅲ）将式（Ⅹ）化合物转化为式（Ⅺ）化合物， iv）中和式（XI）化合物，然后进行酶水解以产生式（V）的APCA，v）使用三甲基甲硅烷基氯和六甲基二硅氮烷的混合物使APCA甲硅烷基化以制备式（XII）的甲硅烷基化APCA，和vi） 用混合酸酐缩合甲硅烷基化APCA以制备式（I）的DMF溶剂合物。