Solid phase synthesis of benzimidazoles

被引：81

作者：

Phillips, GB

Wei, GP

机构：

[1] Berlex Biosciences, Richmond, CA 94804, San Pablo Avenue

来源：

TETRAHEDRON LETTERS | 1996年 / 37卷 / 28期

关键词：

D O I：

10.1016/0040-4039(96)01002-7

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

An efficient solid phase synthesis of benzimidazoles is described. Polymer bound o-fluoronitroaromatic compound 2 was treated with an amine to give o-nitroaniline derivative 3, Reduction of 3 with NaBH4-Cu(acac)(2) followed by cyclization with an aryl imidate and cleavage with TFA gave 5. A library of benzimidazoles has been prepared in three steps in 70-95 % crude yield and 70-98 % purity. Final purified yield ranged from 54-93 %. Extension of this synthesis to the split/pool method is also reported. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：4887 / 4890

页数：4

共 17 条

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