两种合成抗高血压药物方法的比较  

Compared Two Methods for Synthesising of Anti-hypertensive Drugs

作　　者：王宏飞[1] 杨晴来[1] 郑晓晖[1] 

机构地区：[1]西北大学生命科学学院,陕西西安710069

出　　处：《青岛科技大学学报（自然科学版）》2011年第2期142-144,共3页Journal of Qingdao University of Science and Technology:Natural Science Edition

基　　金：国家自然科学基金项目(20875074/b0501)

摘　　要：分别采用羧酸经酰卤化后与4-氨基-2-哌嗪基-6,7-二氧基喹唑反应的方法和羧酸酯化后与哌嗪缩合再与2-氯4-氨-基6,7-二氧基喹唑反应的方法制得多沙唑嗪、特拉唑嗪、哌唑嗪3种抗血压药物。在两种方法下产物的产率分别为71.1%,80.1%,74.2%和80.0%,85.5%,82.3%。产物结构经红外光谱(IR)、核磁氢谱(1H NMR)确证。结果表明,后一种方法对环境污染小,且目标化合物总收率较高,适用于目标化合物的合成。By adopting the carboxylic acid which was acylated react with 2-chlorin-4-amino-6,7-dimethoxy quinazoline,and after the carboxylic acid being esterified,condensatied with piperazine,and then reacting with 2-chlorin-4-amino-6,7-dimethoxy quinazoline,the products of Doxazosin,Terazosin and Prazosin were produced.The yield under two methods respectively were 71.1%,80.1%,74.2% and 80.0%,85.5%,82.3%.The structure of products was verified by NMR Spectroscopy（1H NMR）,Infrared spectroscopy（IR）.The results show that the latter approach to environmental pollution was mild,and higher overall yield for target compounds.It was appropriate for the synthesis for target compounds.

关 键 词：多沙唑嗪 特拉唑嗪 哌唑嗪 

分 类 号：TQ460.6[化学工程—制药化工]