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

被引:116
作者
Cohen, Daniel T. [1 ]
Buchwald, Stephen L. [1 ]
机构
[1] MIT, Dept Chem, Cambridge, MA 02139 USA
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.
引用
收藏
页码:202 / 205
页数:4
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