Copper-Catalyzed anti-Markovnikov Hydroindolation of Terminal Alkynes: Regioselective Synthesis of Bis(indolyl)alkanes

J Org Chem. 2016 Dec 2;81(23):11664-11670. doi: 10.1021/acs.joc.6b02058. Epub 2016 Nov 10.

Abstract

An efficient copper-catalyzed intermolecular hydroindolation reaction of terminal aryl alkynes to expeditiously synthesize bis(indolyl)alkanes in moderate to high yields is described. The double nucleophilic addition of two molecules of indole to one molecule of alkyne occurs in a tandem manner through an anti-Markovnikov pathway. Various arenes and alkynes allow for this transformation. Preliminary mechanistic study sheds light on the observed regioselectivity involving a Cu-vinylidene complex, and 3-styryl-1H-indole as probable intermediates.

Publication types

  • Research Support, Non-U.S. Gov't