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有机化学
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有机化学 ›› 2008, Vol. 28 ›› Issue (2): 325-329. 上一篇    下一篇

研究简报

一步合成1,3,4-三芳基取代3,4,5,6-四氢嘧啶-2(1H)-酮衍生物

薛娜a,b，陈也伟a，吕秀阳b，胡永洲*,a   

  1. (a浙江大学药学院药物化学研究室 杭州 310058)
    (b浙江大学材料与化学工程学院制药工程所 杭州 310027)
  • 收稿日期:2007-05-09 修回日期:2007-07-30 发布日期:2008-02-01
  • 通讯作者: 胡永洲

One-Step Synthesis of 1,3,4,-Triaryl-substituted-3,4,5,6-tetrahydropyrimidin-2(1H)-one Derivatives

XUE Naa,b,CHEN Ye-Weia,LU Xiu-Yangb,HU Yong-Zhou*,a   

  1. (a Department of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang Univer-sity,
    Zijingang Campus, Hangzhou 310058)
    (b Department of Chemical and Biochemical Engineering, College of Material Sciences and Chemical Engineering,
    Zhejiang University, Hangzhou 310027)
  • Received:2007-05-09 Revised:2007-07-30 Published:2008-02-01
  • Contact: HU Yong-Zhou

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以芳基异氰酸酯(1)和β-芳胺基苯丙酮(2)为原料, 甲苯为溶剂, 在回流条件下一步有效地合成了1,3,4-三芳基取代3,4,5,6-四氢嘧啶-2(1H)-酮类化合物3, 并研究了反应条件对产率的影响. 结果表明, 该法具有操作简单、原料易得、反应收率高(79～96%)等优点.

关键词: 环合反应, 芳基异氰酸酯, β-芳胺基苯丙酮, 3,4,5,6-四氢嘧啶-2(1H)-酮

A novel and convenient one-step method for the synthesis of 1,3,4,-Triaryl-substituted- 3,4,5,6-tetrahydropyrimidin-2(1H)-ones (3) was developed by cyclization of aromatic isocyanates (1) with 3-arylamino-1-phenylpropan-1-ones (2) under refluxing of toluene. Effects of reaction conditions on the converting ratio and yield were investigated. The method offered several advantages including simple experimental procedure, easily available starting materials and excellent yields (79%～96%).

Key words: aromatic isocyanate, cyclization, 3-arylamino-1-phenylpropan-1-one, 3,4,5,6-tetrahydro- pyrimidin-2(1H)-one