A solid phase traceless synthesis of benzimidazoles with three combinatorial steps

被引：64

作者：

Smith, JM ^{[1
]}

Krchnák, V ^{[1
]}

机构：

[1] SIDDCO, Tucson, AZ 85747 USA

来源：

TETRAHEDRON LETTERS | 1999年 / 40卷 / 43期

关键词：

D O I：

10.1016/S0040-4039(99)01560-9

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A three combinatorial step solid-phase traceless synthesis of benzimidazoles is reported. The aldehyde resin was reductively alkylated by amines, the resin bound secondary amines were reacted with o-fluoronitrobenzenes, and the resulting o-nitroanilines were reduced by tin chloride. The primary aniline was acylated by acid chlorides. Exposure to acetic acid at elevated temperature cleaved and cyclized the acylated o-phenylenediamines to benzimidazoles. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.

引用

页码：7633 / 7636

页数：4

共 16 条

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