Synthesis of tetrasubstituted thiophenes on solid-support using the Gewald reaction

被引：72

作者：

Castanedo, GM ^{[1
]}

Sutherlin, DP ^{[1
]}

机构：

[1] Genentech Inc, Dept Bioorgan Chem, S San Francisco, CA 94080 USA

来源：

TETRAHEDRON LETTERS | 2001年 / 42卷 / 41期

关键词：

D O I：

10.1016/S0040-4039(01)01470-8

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The Gewald reaction was performed on solid support. This reaction combines a ketone or aldehyde, an activated nitrile, and sulfur in the presence of a suitable amine base to make tri- and tetrasubstituted thiophenes. After optimizing conditions for maximum yield and purity, the scope of the reaction was investigated. Finally, this method is highlighted in the synthesis of two biologically relevant compounds. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：7181 / 7184

页数：4

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