Hydroxylamine as an ammonia equivalent in microwave-enhanced aminocarbonylations

被引：72

作者：

Wu, XY ^{[1
]}

Wannberg, J ^{[1
]}

Larhed, M ^{[1
]}

机构：

[1] Uppsala Univ, Dept Med Chem, SE-75123 Uppsala, Sweden

来源：

TETRAHEDRON | 2006年 / 62卷 / 19期

关键词：

carbonylation; microwave; palladium catalysis; inhibitors;

D O I：

10.1016/j.tet.2005.11.093

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A novel palladium-catalyzed and Mo(CO)(6) promoted aminocarbonylation protocol was developed for rapid generation of primary aromatic amides from aryl bromides and iodides. Employing controlled microwave heating, hydroxylamine was first reduced in situ to ammonia, which thereafter reacted with carbon monoxide and the aryl halide substrate, delivering the benzamide product in less than 20 min. Based on this in Situ carbonylation, a facile preparation of a novel HIV-1 protease inhibitor was achieved. (c) 2006 Elsevier Ltd. All rights reserved.

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页码：4665 / 4670

页数：6

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