头孢妥仑匹酯的合成  

Synthesis of Cefditoren Pivoxil

作　　者：戴伟中[1] 谢斌[1] 范钢[2] 盛力[2] 陈钢[2] 

机构地区：[1]浙江医药股份有限公司昌海生物分公司,浙江绍兴312000 [2]浙江医药股份有限公司新昌制药厂,浙江新昌312500

出　　处：《中国医药工业杂志》2015年第8期803-805,共3页Chinese Journal of Pharmaceuticals

摘　　要：7-ACA经三甲基硅基取代、碘代、Wittig反应、脱保护,一锅法制得关键中间体7-ATCA,再经酰化、成钠盐和酯化得头孢妥仑匹酯,总收率为35%。7-ATCA及头孢妥仑匹酯经1H NMR和MS确证结构。该方法反应步骤少、操作简便、原料易得,较适合工业化生产。The key intermediate 7-ATCA was synthesized by one-pot via silylation, idol substitution, Wittig reaction and deprotection from the staring material 7-ACA. Then cefditoren pivoxil was obtained from 7-ATCA via acylation, salt formation and esterification with an overall yield of 35 %. The structures of 7-ATCA and cefditoren pivoxil were confirmed by 1H NMR and MS. In comparison of reported procedure, the improved route has the advantages of low cost, simple operation, short steps, and it was suitable for industrial production.

关 键 词：头孢妥仑匹酯 抗生素 7-ACA 合成 

分 类 号：R978.1[医药卫生—药品]