Mild Palladium-Catalyzed Cyanation of (Hetero)aryl Halides and Triflates in Aqueous Media

被引：119

作者：

Cohen, Daniel T. ^{[1
]}

Buchwald, Stephen L. ^{[1
]}

机构：

[1] MIT, Dept Chem, Cambridge, MA 02139 USA

来源：

ORGANIC LETTERS | 2015年 / 17卷 / 02期

基金：

美国国家卫生研究院;

关键词：

REVERSE-TRANSCRIPTASE INHIBITORS; ARYL HALIDES; NITRILE; CYANIDE; CONVENIENT; HALOARENES; BROMIDES;

D O I：

10.1021/ol5032359

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A mild, efficient, and low-temperature palladium-catalyzed cyanation of (hetero)aryl halides and triflates is reported. Previous palladium-catalyzed cyanations of (hetero)aryl halides have required higher temperatures to achieve good catalytic activity. This current reaction allows the cyanation of a general scope of (hetero)aryl halides and triflates at 25 mol % catalyst loadings with temperatures ranging from rt to 40 degrees C. This mild method was applied to the synthesis of lersivirine, a reverse transcriptase inhibitor.

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页码：202 / 205

页数：4

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