A new catalytic cross-coupling approach for the synthesis of protected aryl and heteroaryl amidines

被引：87

作者：

Kusturin, CL

Liebeskind, LS

Neumann, WL

机构：

[1] Pharmacia Corp, St Louis, MO USA

[2] Emory Univ, Dept Chem, Atlanta, GA 30322 USA

来源：

ORGANIC LETTERS | 2002年 / 4卷 / 06期

关键词：

D O I：

10.1021/ol025547s

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

[GRAPHICS] A new method for the synthesis of protected benzamidines is described. The commercially available 1,3-bis(tert-butoxycarbonyl)-2-methyl-2-thiopseudourea guanidylation reagent, after SEM-protection, functions as an amidine-forming cross-coupling partner under Liebeskind-Srogl conditions. In the presence of copper(I) thiophenecarboxylate (CuTC), the palladium-catalyzed cross-coupling of the SEM-protected thiopseudourea reagent with boronic acids affords fully protected benzamidines in good to excellent yield (40-91%).

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收藏

页码：983 / 985

页数：3

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