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Gold(I)-Catalyzed Selective Hydroarylation of Indoles with Haloalkynes

Cunbo Wei, Jiawen Wu, Lizhu Zhang, Zhonghua Xia

2022Organic Letters15 citationsDOI

Abstract

A highly regio- and stereoselective synthesis of a Z-alkenyl indole via the gold-catalyzed addition of an indole to a haloalkyne was developed. In the presence of gold catalyst SIPrAuCl and cocatalyst NaBARF, a broad range of indoles react with haloalkynes to afford Z-alkenyl indoles with high selectivity at room temperature. Computational studies suggest that the hydroarylation reaction takes place via a concerted C2 addition pathway of the indole to the activated haloalkyne.

Topics & Concepts

Indole testChemistryStereoselectivityCatalysisSelectivityCombinatorial chemistryStereochemistryOrganic chemistryCatalytic Alkyne ReactionsCatalytic C–H Functionalization MethodsAsymmetric Hydrogenation and Catalysis
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