Enantioselective Pd-Catalyzed Tandem Aza-Heck/Carbene Insertion for the Construction of Quaternary Stereocenter Isoindolinones

-tosylhydrazones has been developed. This protocol provides an efficient and practical strategy for the synthesis of alkenyl-substituted isoindolinones bearing quaternary stereocenter in high yields and with excellent enantioselectivities under mild conditions. Key to the success of this transformation is the use of a sterically demanding chiral phosphoramidite ligand, which enables outstanding chemo- and enantioselectivity. In addition, the reaction exhibits broad substrate scope, excellent functional-group tolerance, and versatile synthetic utility through diverse downstream transformations.