头孢美唑钠合成工艺的改进

The Improvement of Synthetic Process for Cefmetazole Sodium

以7-MAC为起始原料,在氯甲酸乙酯和三乙胺的作用下和氰甲巯基乙酸钾缩合得化合物1;化合物1在三氯化铝和苯甲醚作用下脱去羧基保护,经多次转相、结晶得头孢美唑酸;头孢美唑酸和碳酸氢钠成盐、冻干得头孢美唑钠。改进后的头孢美唑钠合成路线不使用五氯化磷、DMAC、吡啶,操作简单,原料价格便宜,质量提高,对环境污染小,是一种适合工业化生产的合成方法。

Using 7-Mac as starting material,compound 1 was obtained by the condensation with potassium cyanothioglycolate under the reaction of ethyl chloroformate and triethylamine.Compound 1 was decarboxylate protected under the reaction of aluminum trichloride and anisole,and cefmetazole acid was obtained by multiple phase conversion and crystallization.Cefmetazole sodium was obtained by salification and lyophilization of cefmetazole acid and sodium bicarbonate.The improved synthesis route does not use phosphorus pentachloride、DMAC and pyridine,with simple operation,cheap raw materials,quality improvement and little environmental pollution,and is a suitable synthesis method for industrial production.