Novel Process For Preparation of Cefprozil Intermediate
    44.
    发明申请
    Novel Process For Preparation of Cefprozil Intermediate 审中-公开
    头孢司他中间体的制备新方法

    公开(公告)号:US20080281093A1

    公开(公告)日:2008-11-13

    申请号:US10595544

    申请日:2004-11-01

    IPC分类号: C07D501/04 C07F7/02

    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-1-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.

    摘要翻译: 本发明涉及一种制备头孢司定的关键中间体的方法,并且在制备头孢丙烯时使用该中间体,从而避免杂质自身酰化。 [R-(Z)] - [4-羟基-α-[(3-甲氧基-1-甲基-3-氧代-1-丙烯基)氨基]]苯乙酸,单钾盐与氯甲酸乙酯反应,得到混合 酸酐,然后用N,O-双(三甲基甲硅烷基)乙酰胺进行甲硅烷基化。 所得甲硅烷基化的化合物与[7-三甲基甲硅烷基氨基-3-(Z / E-丙烯-1-基)-3-头孢烯-4-羧酸]三甲基甲硅烷基酯反应,并用盐酸水溶液脱保护,得到头孢丙烯。