| 盐酸阿夫唑嗪的改进合成方法 |
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| 引用本文： | 陈霰,张奇,李英,史大昕,李加荣. 盐酸阿夫唑嗪的改进合成方法[J]. 精细化工, 2011, 28(7): 710-713 |
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| 作者姓名： | 陈霰 张奇 李英 史大昕 李加荣 |
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| 作者单位： | 北京理工大学化工与环境学院,北京,100081 |
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| 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。
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| 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 |
| 收稿时间： | 2011-01-17 |
| 修稿时间： | 2011-05-09 |
A Modified Synthesis of Alfuzosin Hydrochloride |
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| CHEN Xian,ZHANG Qi,LI Ying,SHI Da-xin and LI Jia-rong. A Modified Synthesis of Alfuzosin Hydrochloride[J]. Fine Chemicals, 2011, 28(7): 710-713 |
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| Authors: | CHEN Xian ZHANG Qi LI Ying SHI Da-xin LI Jia-rong |
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| Affiliation: | School of Chemical Engineering and Environment, Beijing Institute of Technology,School of Chemical Engineering and Environment, Beijing Institute of Technology,School of Chemical Engineering and Environment, Beijing Institute of Technology,School of Chemical Engineering and Environment, Beijing Institute of Technology,School of Chemical Engineering and Environment, Beijing Institute of Technology |
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| Abstract: | 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. |
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| Keywords: | cyclocondensation zinc chloride alfuzosin hydrochloride 6,7-dimethoxy-1H,3H-quinazoline-2,4-dione drug materials |
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