武汉工程大学学报2012，Vol.34Issue(12)：1-3,7,4.DOI:10.3969/j.issn.1674-2869.2012.12.001
波生坦的合成
On synthesis of bosentan
杨艺虹 1尹迪 1张珩1
作者信息
- 1. 武汉工程大学绿色化工过程教育部重点实验室,湖北武汉430074
- 折叠
摘要
Abstract
Bosentan is an orally active dual endothelin (ET) receptor antagonist, can improve exercise capacity and survival in patients with pulmonary arterial hypertension. With 5-(2-methoxy-phenyl)-2-(pyrimidin-2-yl)-tetrahydropyr-imidin- 4, 6-dione as starting material, bosentan (1) was prepared by chlorination, sulfonylation and etherification,. The structures of target molecule and intermediates were confirmed by IR、1H-NMR and MS . Using single factor analysis and the uniform design, the optimal reaction conditions of each reaction were obtained. The total yield was up to 71. 5%. The chlorination reaction of this process gets rid of deacid reagent and uses less phosphorus oxychloride; phase transfer catalyst in sulfonylation reaction shortens reaction time and increases reaction yield; etherification reaction introduces hydroxyethoxy group only in one step, decreasing reaction steps. Therefore the process is concise, environmental friendly and economically.关键词
抗肺动脉高压药物/波生坦/合成Key words
pulmonary arterial hypertension drug/bosentan/synthesis分类
化学化工引用本文复制引用
杨艺虹,尹迪,张珩..波生坦的合成[J].武汉工程大学学报,2012,34(12):1-3,7,4.
