Catalytic α-Arylation of Imines Leading to N-Unprotected Indoles and Azaindoles

ACS Catal. 2016 May 6;6(5):2930-2938. doi: 10.1021/acscatal.6b00040. Epub 2016 Mar 30.

Abstract

A palladium N-heterocyclic carbene catalyzed methodology for the synthesis of substituted, N-unprotected indoles and azaindoles is reported. The protocol permits access to various, highly substituted members of these classes of compounds. Although two possible reaction pathways (deprotonative and Heck-like) can be proposed, control experiments, supported by computational studies, point toward a deprotonative mechanism being operative.