An optimized process for formation of 2,4-disubstituted imidazoles from condensation of amidines and α-haloketones

被引：44

作者：

Li, B ^{[1
]}

Chiu, CKF ^{[1
]}

Hank, RF ^{[1
]}

Murry, J ^{[1
]}

Roth, J ^{[1
]}

Tobiassen, H ^{[1
]}

机构：

[1] Pfizer Inc, Global Res & Dev, Groton Labs, Groton, CT 06340 USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2002年 / 6卷 / 05期

关键词：

D O I：

10.1021/op025552b

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

The preparation of 2,4-disubstituted imidazoles from the condensation of alpha-haloketones with amidines is described. The optimal reaction protocol is to add the alpha-bromoketone solution to the amidine in aqueous tetrahydrofuran in the presence of potassium bicarbonate under vigorous reflux. Imidazole was isolated in 83-91% yield with >95% purity without column chromatography.

引用

页码：682 / 683

页数：2

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