7-氨基-3-乙烯基头孢烷酸的合成研究进展

Progress in Synthesis of 7-Amino-3-Vinyl-4-Cephalosporanic Acid

7-氨基-3-乙烯基头孢烷酸(7-AVCA)是合成头孢类药物——头孢克肟和头孢地尼的关键中间体。对7-AVCA的不同合成方法进行了总结,指出以7-苯乙酰氨基-3-氯甲基-4-头孢烷酸对甲氧基苄酯(GCLE)为原料的合成路线中由于酶解法具有对环境友好、反应条件温和等诸多优点,有逐步取代化学法的趋势。

7-amino-3-vinyl-4-cephalosporanic acid （7-AVCA） is the key intermediate for the synthesis of cephalosporins-cefixime and cefdinir. Different methods for the synthesis of the 7-AVCA are summarized. The chemical method will be replaced stage by stage by the enzymolysis method among the synthesis routes of using 7-phenylacetamide-3-chloromethyl-3-cepham-4-carboxylic acid p-methoxybenzyl ester（GCLE） as the starting material because the enzymolysis method possesses advantages of the environmental friendliness and reaction mildness, etc.