替米沙坦的合成工艺优化  

Optimization for the synthesis process of telmisartan

作　　者：李兵 刘广勇 吴祥林 李秀文 陈玉梅 吴羡[2] Li Bing;Liu Guangyong;Wu Xianglin;Li Xiuwen;Chen Yumei;Wu Xian(Xuzhou Kedah Fine Chemicals Co.Ltd.,Xuzhou 221011,China;School of Chemical Engineering,Xuzhou College of Industrial Technology,Xuzhou 221140,China)

机构地区：[1]徐州开达精细化工有限公司,江苏徐州221011 [2]徐州工业职业技术学院化学工程学院,江苏徐州221140

出　　处：《现代盐化工》2020年第6期12-15,共4页Modern Salt and Chemical Industry

摘　　要：通过实验对替米沙坦(TMST)原料药的合成工艺路线进行优化,确定以3-甲基-4-氨基苯甲酸为起始原料,经酯化、酰化、硝化、还原、环合反应得到2-正丙基-4-甲基-6-羧基苯并咪唑;在多聚磷酸的作用下,与N-甲基邻苯二胺缩合,产物再与4’-溴甲基联苯-2-羧酸甲酯缩合,水解得到替米沙坦,总收率约为36%。The synthesis process of telmisartan was optimized by experiments,and 3-methyl-4-aminobenzoic acid was used as the starting material,and 2-n-propyl-4-methyl-6-carboxybenzimidazole was obtained by esterification,acylation,nitration,reduction and cyclization.The product was condensed with N-methyl-o-phenylenediamine under the action of polyphosphate,and then condensed with 4’-bromomethyl-biphenyl-2-carboxylate and hydrolyzed to telmisartan.The total yield of telmisartan was about 36%.

关 键 词：替米沙坦 合成 晶体结构 

分 类 号：TQ460.6[化学工程—制药化工]