Efficient synthesis of imidazoles from aldehydes and 1,2-diketones using microwave irradiation

被引：440

作者：

Wolkenberg, SE ^{[1
]}

Wisnoski, DD ^{[1
]}

Leister, WH ^{[1
]}

Wang, Y ^{[1
]}

Zhao, ZJ ^{[1
]}

Lindsley, CW ^{[1
]}

机构：

[1] Merck Sharp & Dohme Ltd, Res Labs, Dept Med Chem, Technol Enabled Synth Grp, W Point, PA 19486 USA

来源：

ORGANIC LETTERS | 2004年 / 6卷 / 09期

关键词：

D O I：

10.1021/ol049682b

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A simple, high-yielding synthesis of 2,4,5-trisubstituted imidazoles from 1,2-diketones and aldehydes in the presence of NH4OAc is described. Under microwave irradiation, alkyl-, aryl-, and heteroaryl-substituted imidazoles are formed in yields ranging from 80 to 99%. Short syntheses of lepidiline B and trifenagrel illustrate the utility of this approach.

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页码：1453 / 1456

页数：4

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