Efficient one-pot preparation of 5-substituted-2-amino-1,3,4-oxadiazoles using resin-bound reagents

被引：128

作者：

Coppo, FT ^{[1
]}

Evans, KA ^{[1
]}

Graybill, TL ^{[1
]}

Burton, G ^{[1
]}

机构：

[1] GlaxoSmithKline Pharmaceut, Discovery Res, Collegeville, PA 19426 USA

来源：

TETRAHEDRON LETTERS | 2004年 / 45卷 / 16期

关键词：

oxadiazole; 2-amino-1,3,4-oxadiazole; 1,3,4-oxadiazole; carbodiimide; acylhydrazine; acylthiosemicarbazide; parallel synthesis; solid-supported reagents;

D O I：

10.1016/j.tetlet.2004.02.119

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A robust one-pot solution-phase synthesis of 2-amino-1,3,4-oxadiazoles directly from acylhydrazines and isothiocyanates is described. Commercially-available polymer-supported reagents help facilitate both cyclization and purification. This convenient method benefits from its broad applicability, ease and safety of reagent handling, simple product isolation, and the ability to perform multiple reactions in parallel fashion without need for purification. The details and scope of this reaction strategy are presented herein. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：3257 / 3260

页数：4

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