盐酸头孢吡肟合成方法的改进

An improvement of the synthetic method for cefepime hydrochloride

依据自行设计的合成路线对盐酸头孢吡肟进行合成方法研究,力求通过研究解决现有文献方法的不足,为研制适合我国国情的盐酸头孢吡肟的生产工艺奠定基础。本文报道的盐酸头孢吡肟的合成方法,是以3-氯甲基型新型活性头孢菌素中间体ACLE为起始原料,合成盐酸头孢吡肟总收率约26%。工艺操作简单,条件温和,可获得优良的产品质量,适合于规模化生产。

A novel method for conversion of ACLE （7-amino-3-chloromethyl-2-cephem-2-carboxylic acid p-methoxybenzylester hydrochloride） to cefepime hydrochloride via inner salt as intermediate was presented. Cefepime hydrochloride was prepared in overall yields of 26% from ACLE（1） with good quality. The materials were easy to obtain, this method was simple and could be scale-up to industrial production.