盐酸头孢匹伏卡品酯的合成  

Study on Synthesis Process of Cefcapene Pivoxil Hydrochloride

作　　者：陈言德[1] 赵桂林[1] 金荣庆[1] 孟霆[1] 李冬梅[1] 张海波[1] 王志贤[1] 

机构地区：[1]江苏(泰州)新药研究院,扬子江药业集团有限公司,江苏泰州225321

出　　处：《化工中间体》2009年第10期35-38,共4页

摘　　要：;本文主要选择BOC头孢卡品作为起始原料,经过成钠盐、酯化、脱保护、成盐酸盐、转晶最终得产品盐酸匹伏头孢卡品酯一水合物,并对酯化反应和脱保护的条件如反应投料比、时间、温度等进行了重点考察与研究。酯化反应的最佳条件为n(POMI)/n(中间体Ⅱ)=1.2;0℃,反应3h。三氟乙酸脱保护反应的最佳条件为:n(TFA)/n(中间体Ⅲ)=3;0℃反应3h。现五步反应总收率可达50%以上,成品批量100克以上。The synthesis technology of Cefcapene Pivoxil Hydrochloride was investigated in this paper. It was prepared by BOC Cefcapene ,which was treated with sodium bicarbonate, Iodomethyl Pivalate, trifluoroacetic acid and hydrochloric acid. Esterification and deprotection conditions such as reagent molar ratio , reaction temperature and time were the focus of the study and research. The optimization condition of esterification is reagent molar ratio, n （POMI）/n （intermediate Ⅱ =1.2; reaction temperature 0℃; and time 3h , The optimization condition of deprotection is reagent molar ratio, n（TFA）/n（intermediate Ⅲ）=3; reaction temperature 0℃; and time 3h , the total yield is up to 50%, product volume was more than 100 grams.

关 键 词：卡品酯 合成 抗生素 酯化反应 脱保护 

分 类 号：TQ465.9[化学工程—制药化工]