High-throughput combinatorial synthesis of substituted benzimidazolones

被引：32
|
作者：
Pan, PC [1 ]
Sun, CM [1 ]
机构：
[1] Natl Dong Hwa Univ, Dept Chem, Shoufeng 974, Hualien, Taiwan
来源：
TETRAHEDRON LETTERS | 1999年 / 40卷 / 35期
关键词：
D O I：
10.1016/S0040-4039(99)01276-9
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
An efficient liquid-phase synthesis of substituted benzimidazolones 7 is described. Resin bound o-fluoronitrobenzene 1 is reacted with various primary amines to afford o-nitroaniline derivatives 2. Subsequent reduction of the aromatic nitro group followed by cyclization gives a PEG bound benzimidazole-2-one 4. N-Alkylation of this resin bound scaffold 4 with several electrophiles gives the resulting library in excellent yield and purity after cleavage. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：6443 / 6446
页数：4
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