头孢尼西钠的合成

Synthesis of Cefonicid sodium

7-ACA经六甲基二硅烷保护羧基和氨基,用三甲基硅碘烷进行取代反应,与1-磺酸甲基-5-巯基四唑钠盐反应,脱保护基制得(6R,7R)-7-氨基-3-[[(1-磺酸甲基-1H-四唑-5-基)硫基]甲基]头孢霉烷酸,再与二氯乙酰扁桃酰氯缩合制得头孢尼西酸,成盐得到头孢尼西钠,总收率62%(以7-ACA计)。

Cefonicid sodium was synthesized from 7-ACA by protection with hexamethyldisilazane, substitution with trimethylsilyliodide, reaction with 1-sulfomethyltetrazole-5-thiol sodium salt and then deprotection to give （6R,7R） -7-amino-3- E E （1- （sulfomethyl-1H-tetrazol-5-yl） thio] methyl] -3-cephalosporanic acid, which was subjected to condensation with dichloroacetylmandeloyl chloride with an overall yield of 62 % （based on 7-ACA）.