Synthesis of indolines via palladium-catalyzed [4 + 1] annulation of (2-aminophenyl)methanols with sulfoxonium ylides

Abstract

A facile strategy for the synthesis of valuable indolines has been developed, involving a palladium(II)/Brønsted acid co-catalyzed annulation of readily available (2-aminophenyl)methanols and sulfoxonium ylides. This protocol allows for the direct utilization of the OH group as a leaving group, tolerates alkyl and aryl groups on the N atom of the aniline moiety, operates under mild reaction conditions, and exhibits good efficiency.