Solid-phase synthesis of N,N′-substituted acylguanidines

被引：21

作者：

Dodd, DS ^{[1
]}

Zhao, Y ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Early Discovery Chem, Princeton, NJ 08543 USA

来源：

TETRAHEDRON LETTERS | 2001年 / 42卷 / 07期

关键词：

D O I：

10.1016/S0040-4039(00)02265-6

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

An efficient method for the solid-phase synthesis of N,N'-substituted acylguanidines is presented. The key-step involves the N-acylation of resin immobilized S-methylisothiourea with a variety of carboxylic acids using PyAOP as the coupling agent. The resulting resin bound N-acyl-derivatives are reacted with a host of amines and the N-acyl,N'-alkyl(aryl)guanidines liberated from the resin upon exposure to TFA. (C) 2001 Published by Elsevier Science Ltd.

引用

页码：1259 / 1262

页数：4

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