An efficient synthesis of 4-alkyl-2(1H)-quinazolinones and 4-alkyl-2-chloroquinazolines from 1-(2-alkynylphenyl)ureas

被引：19

作者：

Wang, Honggen ^{[1
]}

Liu, Lanying ^{[1
]}

Wang, Yong ^{[1
]}

Peng, Changlan ^{[1
]}

Zhang, Jiancun ^{[1
]}

Zhu, Qiang ^{[1
]}

机构：

[1] Chinese Acad Sci, State Key Lab Resp Dis, Guangzhou Inst Biomed & Hlth, Guangzhou 510663, Guangdong, Peoples R China

来源：

TETRAHEDRON LETTERS | 2009年 / 50卷 / 49期

基金：

美国国家科学基金会;

关键词：

QUINAZOLINES; CHEMISTRY;

D O I：

10.1016/j.tetlet.2009.09.130

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

An efficient synthesis of 4-alkyl-2(1H)-quinazolinones has been achieved by cyclization of 1-(2-alkynylphenyl)ureas (2 R-2 = alkyl) in dichloroethane catalyzed by TfOH. In the case of aryl substitution (2 R-2 = aryl), a mixture of quinazolinone tautomers is obtained in dichloroethane with TFA as co-solvent. Chlorination of the resulting mixture affords 4-alkyl-2-chloro-quinazolines as sole products. (C) 2009 Elsevier Ltd. All rights reserved.

引用

收藏

页码：6841 / 6843

页数：3

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