Conversion of sterically hindered diacylated 1,2-phenylenediamines into 2-substituted benzimidazoles

被引：38

作者：

Charton, J

Girault-Mizzi, S

Sergheraert, C

机构：

[1] Univ Lille 2, Inst Biol, CNRS, UMR 8525, F-59021 Lille, France

[2] Inst Pasteur, F-59019 Lille, France

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2005年 / 53卷 / 05期

关键词：

benzimidazole; cyclization; mechanism;

D O I：

10.1248/cpb.53.492

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

A series of bulky 2-substituted benzimidazoles was designed in order to find new leads for several biological targets. Formation by eye lode hydration from their monoacylated counterparts was shown to be strongly dependent upon the nature of the acyl group. In the case of a dicyclohexylmethyl group, cyclization was only observed in a p-toluenesulfonic acid/toluene mixture from the symmetrical diacylated precursor. Analysis of the mechanism was begun starting from mixed diacylated derivatives.

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收藏

页码：492 / 497

页数：6

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