头孢丙烯合成过程中杂质乙氧羰基头孢丙烯的控制  

Synthesis of Cefprozil and Control of Process Impurity Ethoxycarbonylcefprozil

作　　者：李庆 韩贵良 徐俊强 范玉珍 Li Qing;Han Guiliang;Xu Junqiang;Fan Yuzhen(Guangzhou Baiyunshan Pharmaceutical Holdings Co.,Ltd.,Baiyunshan Chemical Pharmaceutical Factory,Guangzhou 510515,China)

机构地区：[1]广州白云山医药集团股份有限公司白云山化学制药厂

出　　处：《广东化工》2019年第9期71-72,共2页Guangdong Chemical Industry

基　　金：广州市珠江科技新星专项资助(201710010121)

摘　　要：以7-氨基-3-((Z/E-丙烯)-1-基)-3-头孢烯-4-羧酸(7-APRA)和D-对羟基苯甘氨酸邓钾盐为起始原料,经混酐、成盐及缩合反应后,得到头孢丙烯N,N-二甲基甲酰胺溶剂化物,之后用水将DMF置换,得到头孢丙烯一水合物。在混合酸酐制备过程中,加入甲酸,可以减少杂质乙氧羰基头孢丙烯的产生,提高产品质量。Cefprozil dimethyl formamide solvate was prepared with silylated 7-APRA and dipotassium 7-hydroxynaphthalene-1,3-disulphonate(Dane Salt) as starting materials.Then,it reacted with water and produced cefprozil monohydrate.During the mixed anhydride,a process impurity ethoxycarbonylcefprozil,formed in the synthesis of cefprozil was controlled with addition of a catalytic amount of formic acid.

关 键 词：头孢丙烯 乙氧羰基头孢丙烯 7-APRA D-对羟基苯甘氨酸邓钾盐 甲酸 

分 类 号：O65[理学—分析化学]