A solid-phase synthetic route to substituted 7-azabenzimidazoles suitable for combinatorial library synthesis

被引：18

作者：

Farrant, E ^{[1
]}

Rahman, SS ^{[1
]}

机构：

[1] SmithKline Beecham Pharmaceut, Combinatorial & Chem Technol, Harlow CM1 5AW, Essex, England

来源：

TETRAHEDRON LETTERS | 2000年 / 41卷 / 28期

关键词：

solid-phase synthesis; combinatorial chemistry;

D O I：

10.1016/S0040-4039(00)00859-5

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A novel route for the solid-phase synthesis of 1,2,5-substituted 7-azabenzimidazole derivatives has been developed. Primary amines are attached to an aldehyde resin then coupled to 6-chloro-5-nitro-nicotinyl chloride. Subsequent alkylation with amines, reduction of the nitro group and cyclisation with aldehydes gives 1,2,5-substituted 7-azabenzimidazole derivatives. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：5383 / 5386

页数：4

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