盐酸头孢甲肟的合成  

Synthesis of Cefmenoxime Hydrochloride

作　　者：白国义[1] 李新娟[1] 彭洪伟[1] 贾春伟[1] 王海龙[1] 

机构地区：[1]河北大学化学与环境科学学院河北省化学生物重点实验室,河北保定071002

出　　处：《精细化工》2009年第1期51-53,93,共4页Fine Chemicals

基　　金：河北省自然科学基金资助项目(B2007000156)~~

摘　　要：以7-氨基头孢烷酸(7-ACA)为原料,通过两条路线对第三代头孢菌素——盐酸头孢甲肟的合成进行了系统考察。实验证明,7-ACA先在C-3位与5-巯基-1-甲基-1H-四氮唑(MMT)反应生成3-(1-甲基-1H-四氮唑-5-基)硫甲基-7-氨基头孢霉烷酸(7-ACT),再在C-7位和MAEM反应合成头孢甲肟的路线(摩尔收率为86%)优于先进行7-ACA的C-7位改造再进行C-3位改造的合成路线(摩尔收率为69%)。溶剂对反应的摩尔收率有较大影响,以二氯甲烷为溶剂时的反应效果最佳;同时证明超声能够显著缩短反应时间。The third generation cephalosporin of cefmenoxime hydrochloride was synthesized by two routes using 7-ACA as the raw material. The route, in which 7-ACT was synthesized firstly from the reaction of 5-mereapto-1-methyltetrazole（MMT） and 7-ACA in C3-position of 7-ACA and then reacted with MAEM in C7-position to produce eefmenoxime （ the yield was 86% ） , was proved to be superior to the route that the C7-position of 7-ACA was transformed before the C3-position （ the yield was 69% ）. It was found that solvent has remarkable effect on the yield and dichloromethane can give the best result. Moreover, it was proved that ultrasound can significantly shorten the reaction time.

关 键 词：头孢甲肟 盐酸头孢甲肟 7-ACA 超声 

分 类 号：R978.1[医药卫生—药品]