替米沙坦合成工艺研究进展  

Research Progress on Synthesis of Telmisartan

作　　者：李维思[1] 黄双 曹亚运 LI Wei-si;HUANG Shuang;CAO Ya-yun(Jiangsu Zhongbang Pharmaceutical Co.,Ltd.,Jiangsu Nanjing 211300;Nanjing Red Sun Pharmaceutical Research Institute Co.,Ltd.,Jiangsu Nanjing 211300,China)

机构地区：[1]江苏中邦制药有限公司,江苏南京211300 [2]南京红太阳医药研究院有限公司,江苏南京211300

出　　处：《广州化工》2022年第18期32-36,43,共6页GuangZhou Chemical Industry

摘　　要：替米沙坦作为一种特异性血管紧张素Ⅱ受体拮抗剂,在降压药市场占有一席之地。本文总结了替米沙坦原料药的主要合成工艺,并对每种路线的工艺情况进行了描述和评价。以不同的起始物料作为分类依据对其关键中间体主链双咪唑的合成工艺研究进行了概述,同时对另外一个重要中间体侧链氰基联苯的合成工艺做了回顾,以期为该产品的工艺研究、中间体的技术改进、杂质谱的研究提供思路。Telmisartan,as a specific angiotensin II receptor antagonist,has a place in the antihypertensive drug market.The main synthesis process of telmisartan API was summarized,and the process conditions of each route was described and evaluated.Based on different starting materials as the classification basis,the synthesis process of its key intermediate main chain bisimidazole was summarized,and the synthesis process of another important intermediate,side chain cyanobiphenyl,was also reviewed,in order to provide ideas for the process research of this product,the technical improvement of intermediates,and the research of impurity spectrum.

关 键 词：替米沙坦 合成工艺 中间体 

分 类 号：R914.4[医药卫生—药物化学]