| 替米沙坦的合成工艺改进 |
| |
| 引用本文： | 常选妞,李伟,何新蕾,张慧勇.替米沙坦的合成工艺改进[J].精细化工,2006,23(7):661-663. |
| |
| 作者姓名： | 常选妞 李伟 何新蕾 张慧勇 |
| |
| 作者单位： | 河南师范大学,化学与环境科学学院,河南,新乡,453007 |
| |
| 摘 要： | 以3-甲基-4-硝基苯甲酸(Ⅰ)为起始原料,经多步反应合成了替米沙坦(Ⅸ)。3-甲基-4-硝基苯甲酸经酯化、还原、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(Ⅶ),在多聚磷酸的作用下Ⅶ与N-甲基邻苯二胺缩合,生成的产物(Ⅷ)再与4′-溴甲基联苯-2-羧酸甲酯缩合、水解得替米沙坦Ⅸ。其总收率从1993年文献3]的20.9%提高到30%。该产品已在河南天方药业股份有限公司中试。
|
| 关 键 词： | 替米沙坦 血管紧张素Ⅱ受体拮抗剂 |
| 文章编号： | 1003-5214（2006）07-0661-03 |
| 收稿时间： | 2005-10-11 |
| 修稿时间： | 2005-10-112006-02-13 |
An Improved Synthetic Method of Telmisartan |
| |
| CHANG Xuan-niu,LI Wei,HE Xin-lei,ZHANG Hui-yong.An Improved Synthetic Method of Telmisartan[J].Fine Chemicals,2006,23(7):661-663. |
| |
| Authors: | CHANG Xuan-niu LI Wei HE Xin-lei ZHANG Hui-yong |
| |
| Affiliation: | College of Chemistry and Environmental Science,Henan Normal University,Xinxiang 453007 ,Henan, China |
| |
| Abstract: | Telmisartan was synthesized through multistep reactions with 3-methyl-4-nitrobenzoic acid as starting material.3-Methyl-4-nitrobenzoic acid via esterification,reduction,butyrylation,nitration,reduction and cyclization gave 2-n-propyl-4-methyl-6-carboxybenzimidazole,which condensed with N-methyl-o-phenylenediamine in the presence of polyphosphoric acid and followed by condensation with 4′-bromomethyl-biphenyl-2-carboxylic acid methyl ester and hydrolysis to give Telmisartan.The overall yield was improved from 20.9% to 30%.It has been produced in Henan Tianfang Phamaceutical Co.Ltd. |
| |
| Keywords: | Telmisartan angiotensin Ⅱ receptor antagonist |
| 本文献已被 CNKI 维普 万方数据 等数据库收录！ |
|
