Palladium-Catalyzed Arylation/Heteroarylation of Indoles: Access to 2,3-Functionalized Indolines

Abstract

A palladium-catalyzed diastereoselective dearomatization of N-(2-bromobenzoyl)indoles by an arylation/heteroarylation sequence is reported. Diverse functionalized indolines are accessed in good to excellent yields and selectivity. Studies conducted on the effects of copper in the reaction revealed that, along with improving conversions, the additive inhibits epimerization of the product.