盐酸阿夫唑嗪的改进合成方法  

An Improved Synthesis Method of Alfuzosin Hydrochloride

作　　者：陈霰[1] 张奇[1] 李英[1] 史大昕[1] 李加荣[1] 

机构地区：[1]北京理工大学化工与环境学院,北京100081

出　　处：《精细化工》2011年第7期710-713,共4页Fine Chemicals

摘　　要：2-氨基-4,5-二甲氧基苯甲腈与DMF缩合得到6,7-二甲氧基-1H,3H-喹唑啉-2,4-二酮(Ⅱ),Ⅱ经过氯化、胺化、缩合和酸化得到目标产物盐酸阿夫唑嗪(Ⅰ),总产率38.5%。探讨了催化剂、反应温度和反应时间对中间体Ⅱ收率的影响。化合物的结构经IR、1HNMR和ESI-MS等进行了表征。An improved synthesis method of alfuzosin hydrochloride（Ⅰ） was reported.Ⅰ was obtained in an overall yield of 38.5% in 5 steps with 2-amino-4,5-dimethoxybenzonitrile as a starting material.The method involved the cyclocondensation of 2-amino-4,5-dimethoxybenzonitrile with DMF to get 6,7-dimethoxy-1H,3H-quinazoline-2,4-dione（Ⅱ）,and subsequent chloridization,amination and condensation.The optimum conditions for the preparation of Ⅱ were investigated.The target products were characterized by means of IR,1HNMR and ESI-MS.

关 键 词：环缩合 氯化锌 盐酸阿夫唑嗪 6 7-二甲氧基-1H 3H-喹唑啉-2 4-二酮 医药原料 

分 类 号：TQ253.23[化学工程—有机化工] O625.6[理学—有机化学]