用4-氨基-2-氯-6,7.二甲氧基喹唑啉与无水哌嗪反应制得4-氨基-2-哌嗪基-6,7-二甲氧基喹唑啉(2)。另用2-氯-4,6-二甲氧基-1,3,5.三嗪(3)和4.甲基吗啉(4)反应后加入相应的羧酸,制得的中间体7再与2反应分别制得多沙唑嗪(1a)、特拉唑嗪(1b)和哌唑嗪(1c),总收率分别为82.3%、88.0%和86.4%(以3计)。
The target products, doxazosin(la), terazosin(lb) and prazosin(lc), were synthesized from 2-chloro-4,6-dimethoxy-l,3,5-triazine (3) by reaction with 4-methylmorpholine (4) and then reaction with 2,3-dihydrobenzo[1,4]dioxine-2-carboxylic acid(6a), tetrahydrofuran-2-carboxylic acid(6b) or furan-2-carboxylic acid (6c), respectively, followed by acylation with 4-amino-2-piperazinyl-6,7-dimethoxyquinazoline (2) with overall yields of 82.3 %, 88.0 % and 86.4 %, respectively.