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固体酸催化合成3,4-二氢嘧啶二酮类药物中间体
引用本文:裴蕾,宋静茹,郭英.固体酸催化合成3,4-二氢嘧啶二酮类药物中间体[J].东北林业大学学报,2009,37(2).
作者姓名:裴蕾  宋静茹  郭英
作者单位:哈尔滨理工大学,哈尔滨,150040
摘    要:选取价廉、易得且对环境无污染的4种固体酸为催化剂,以苯甲醛、乙酰乙酸乙酯与脲进行环化缩合,一步合成了6-甲基-4-苯基-5-乙氧羰基-3,4-二氢嘧啶-2(1 H)-酮.考查了反应时间、催化剂用量、反应物的摩尔比对反应产率的影响.通过正交试验,找出不同催化剂条件下的最佳工艺条件.与传统合成方法相比,在固体酸的催化下,反应时间大大缩短,产率可达87.8%,而且催化剂易溶于水,对环境无污染,因而后处理更为简单.

关 键 词:Biginelli反应  3  4-二氢嘧啶-2(1H)-酮  固体酸

Synthesis of 3,4-dihydropyrimidin-2(1H)-one Catalyzed by Solid Acid
Pei Lei,Song Jingru,Guo Ying.Synthesis of 3,4-dihydropyrimidin-2(1H)-one Catalyzed by Solid Acid[J].Journal of Northeast Forestry University,2009,37(2).
Authors:Pei Lei  Song Jingru  Guo Ying
Institution:Pei Lei,Song Jingru,Guo Ying(College of Chemistry , Circumstance Engineering,Harbin University of Science , Technology,Harbin 150040,P.R.China)
Abstract:The 5-ethoxycarbonyl-4-phenyl-3,4-dihydropyrimidin-2(1H)-one was synthesized by one-step cyclocondensation of aldehyde,ethyl acetoacetate and urea using four kinds of solid acids as catalysts which are cheap but harmless to environment.Effects of reaction time,mole fraction of the catalysts,and mole ratio of the reactants on the yield of the product were studied.Then the optimized synthetic conditions were respectively determined under different catalysts by the experiments.Compared with the traditional syn...
Keywords:Biginelli reaction  3  4-dihydropyrimidin-2(1H)-one  Solid acid  
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