文献类型：期刊文献

中文题名：降血压药物替米沙坦的合成

英文题名：Synthesis of the antihypertensive drug telmisartan

作者：肖时俊[1];杨雪艳[1];吴范宏[2];王飞[1]

机构：[1]华东理工大学化学与分子工程学院,上海200237;[2]上海应用技术学院,上海200235

年份：2010

卷号：19

期号：18

起止页码：1726

中文期刊名：中国新药杂志

外文期刊名：Chinese Journal of New Drugs

收录：CSTPCD;;Scopus;北大核心:【北大核心2008】；CSCD:【CSCD_E2011_2012】；

语种：中文

中文关键词：降血压药;替米沙坦;合成

外文关键词：antihypertensive drug ; telmisartan ; synthesis

摘要：目的:合成替米沙坦,并对其工艺进行改进。方法: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、水解得2-正丙基-4-甲基-6-羧基苯并咪唑,在多聚磷酸作用下与N-甲基邻苯二胺缩合后的产物,再与2-氰基-4-溴甲基联苯反应,水解后即得替米沙坦。结果和结论:目标产物的成本降低,反应条件温和,适合于工业化生产。
Objective： To synthesize telmisartan, and then optimize its process. Methods： Using 3-meth- yl-4-aminobenzonic acid as the starting material, 2-n-propyl-4-methyl-6-carboxy benzimidazole was synthesized via esterification, acylation, nitration, reduction, cyclization and hydrolysis. This compound was condensed with N- methyl-o-phenylenediamine in polyphosphoric acid, and the product then reacted with 2-cyano-4＇-bromomethylbi- phenyl to produce telmisartan after hydrolysis. Results and Conclusion： The target compound is obtained under mild reaction condition with lower cost, which is suitable for large-scale production.