Palladium/<scp>Xu‐Phos</scp> Catalyzed Enantioselective Tandem Heck/Cacchi Reaction of Unactivated Alkenes

Abstract

Main observation and conclusion A highly enantioselective palladium‐catalyzed intermolecular tandem Heck/Cacchi reaction of unactivated alkenes with ortho ‐ethynylanilines was developed, which provides a powerful route to access a broad range of enantioenriched 2,3‐dihydrobenzofuran‐ or indoline‐substituted indoles bearing all‐carbon quaternary stereocenter of interest in pharmaceutical research. Its salient features include inherent atom‐ and step‐economy, high functional group tolerance, mild conditions, broad structural diversity together with excellent enantioselectivities.