文献类型：期刊文献

英文题名：Highly Efficient and Practical Synthesis of the Key Intermediate of Telmisartan

作者：Zhao, Jianhong[1];Xiong, Yicheng[1];Yang, Wu-Lin[1];Yang, Fan[1];Jin, Yu[1]

机构：[1]East China Univ Sci & Technol, Engn Res Ctr Pharmaceut Proc Chem, Minist Educ, Sch Pharm, Shanghai 200237, Peoples R China

年份：2021

卷号：25

期号：4

起止页码：1022

外文期刊名：ORGANIC PROCESS RESEARCH & DEVELOPMENT

收录：;EI(收录号：20211510199416);WOS:【SCI-EXPANDED(收录号:WOS:000641295300032)，CCR-EXPANDED(收录号:WOS:000641295300032)】；

基金：This work was supported by the Jiangsu Zhongbang Pharmaceutical Co. Ltd.

语种：英文

外文关键词：Telmisartan; practical synthesis; 1,7 '-dimethyl-2 '-propyl-2,5 '-bi(1H-benzimidazole); Duff reaction; benzimidazole

摘要：We reported herein an efficient and practical method to access 1,7'-dimethyl-2'- propyl-2,5'-bi(1H-benzimidazole) 1, a key intermediate for the synthesis of telmisartan. The synthetic route was based on readily available o-methylaniline as the starting material, and the target product 1 was prepared through a six-step process, including amidation, formylation, cyclization, hydrolysis, amidine, and oxidation. The overall yield for the preparation of 1 was 51.5% on the 100 g scale, with a purity of 99.91%. The salient features of this method include economic and easily available starting materials, operational simplicity, and environmentally friendly, which is suitable for the industrial production.