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

Chin. J. Org. Chem. ›› 2008, Vol. 28 ›› Issue (2): 325-329. Previous Articles Next Articles

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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

(^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 Na^a,b,CHEN Ye-Wei^a,LU Xiu-Yang^b,HU Yong-Zhou*^,a

(^aDepartment of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang Univer-sity,
Zijingang Campus, Hangzhou 310058)
(^bDepartment 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

Abstract

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

Cite this article

XUE Na,b,CHEN Ye-Wei^a,LU Xiu-Yang^b,HU Yong-Zhou*^,a. One-Step Synthesis of 1,3,4,-Triaryl-substituted-3,4,5,6-tetrahydropyrimidin-2(1H)-one Derivatives[J]. Chin. J. Org. Chem., 2008, 28(2): 325-329.

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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

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

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