Solid-phase synthesis of substituted 2-aminomethylbenzimidazoles

被引：50

作者：

Kilburn, JP ^{[1
]}

Lau, J

Jones, RCF

机构：

[1] Novo Nordisk AS, DK-2760 Maaleov, Denmark

[2] Open Univ, Dept Chem, Milton Keynes MK7 6AA, Bucks, England

来源：

TETRAHEDRON LETTERS | 2000年 / 41卷 / 28期

关键词：

solid-phase synthesis; benzimidazole; combinatorial chemistry;

D O I：

10.1016/S0040-4039(00)00871-6

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Resin-bound 4-fluoro-3-nitrobenzoic acid is converted by reaction with a range of amines and reduction, to substituted 1,2-diaminobenzenes, whose reaction with activated amino acids followed by acid-catalyzed cyclisation gave resin-bound benzimidazoles; Fmoc-deprotection, acylation and TFA-mediated cleavage gave substituted 2-aminomethylbenzimidazoles via a new solid support strategy. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：5419 / 5421

页数：3

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[Anonymous], ANGEW CHEM INT EDIT, DOI DOI 10.1002/ANIE.199622881

[2]

Blettner CG, 1999, SYNLETT, P307

[3]

DORWALD FZ, 2000, ORGANIC SYNTHESIS SO

[4] Organic chemistry on solid supports [J].