盐酸头孢甲肟的合成

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。

Synthesis of Cefmenoxime Hydrochloride

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-mercapto-1-methyltetrazole(MMT) and 7-ACA in C3-position of 7-ACA and then reacted with MAEM in C7-position to produce cefmenoxime(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.