PDF全文下载：2011020142
王宏飞， 杨晴来， 郑晓晖*
（ 西北大学 生命科学学院，陕西 西安 710069）
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。
关键词: 多沙唑嗪； 特拉唑嗪； 哌唑嗪
中图分类号: TQ 460.6 文献标志码： A
Compared Two Methods for Synthesising of Anti-hypertensive Drugs
WANG Hong-fei,YANG Qing-lai, ZHENG Xiao-hui
(College of Life Sciences, Northwest University, Xi’an 710069, China)
Abstract: 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.
Key words: doxazosin; terazosin; prazosin
收稿日期：2010-10-09
基金项目： 国家自然科学基金项目(20875074/b0501).
作者简介：王宏飞（1984—）,男，硕士研究生. *通信联系人.
