A new and efficient multicomponent solid-phase synthesis of 2-acylaminomethylthiazoles

被引：29
|
作者：
Henkel, B
Sax, M
Dömling, A
机构：
[1] Morphochem AG, D-81379 Munich, Germany
[2] Univ Munster, Inst Med & Pharmazeut Chem, D-48149 Munster, Germany
来源：
TETRAHEDRON LETTERS | 2003年 / 44卷 / 18期
关键词：
D O I：
10.1016/S0040-4039(03)00662-2
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A new multicomponent reaction (MCR) for the preparation of 2-substituted thiazole libraries using Rink amide resin is described. Thiazoles are assembled in a one-pot MCR of a thiocarboxylic acid, aldehyde, 3-(N,N-dimethylamino)-2-isocyanoacrylate with a resin-bound primary amine. Aliphatic and aromatic thiocarboxylic acids as well as aliphatic and (hetero-) aromatic aldehydes work in the reaction. Cleavage of the product yields the substituted thiazoles in reasonable to good purity. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：3679 / 3682
页数：4
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