头孢洛林酯合成工艺改进  

The Improvement of Synthetic Process for Ceftaroline Fosamil

作　　者：孔瑜 蒋宪龙 焦翠玲 刘彩锋 Kong Yu;Jiang Xianlong;Jiao Cuiling;Liu Caifeng(Xinfa Pharma Ltd.,Dongying 262500,China)

机构地区：[1]新发药业有限公司,山东东营262500

出　　处：《山东化工》2024年第15期85-87,91,共4页Shandong Chemical Industry

摘　　要：以GHYH为起始物料,GHYH与苯磺酰氯制备磺酸酯,与PTT发生取代反应;甲基苯磺酸甲酯作为甲基化试剂,用甲酚和固定化青霉素酶分别脱掉羧基和氨基保护基,然后与ATDE-Cl反应,在醋酸和水的混合溶液中重结晶得到头孢洛林酯;这种合成方法比较适用于工业化生产,甲酰氯在改进后的合成路线中不使用,操作简单,不产生含磷废水,产生较少杂质,原料便宜,质量提高,对环境的污染也较小。Using GHYH as starting material,sulfonate was obtained under the reation of GHYH and benzenesulfonyl chloride.A substitution reaction occurs with PTT.Methyl toluenesulfonate as the methylation reagent,cresol and immobilized penioillin acylase were used to remove the carboxyl and amino protecting groups.Rereacted with ATDE-Cl and recrystallized in a mixture of acetic acid and water to obtain Ceftaroline fosamil.The improved synthesis route does not use methanesulfonyl chloride,simple operation,phosphorus free wastewater,less impurities,cheap raw materials,quality improvement and little environmental pollution,and is a suitable synthisis method for industrial prodution.

关 键 词：GHYH 抗生素 头孢洛林酯 苯磺酰氯 青霉素酰化酶 

分 类 号：TQ465[化学工程—制药化工]