Facile ligand-free Pd-catalyzed tandem C–C/C–N coupling reaction: a novel access to highly diverse tetrazole tag isoindoline derivatives

Abstract

A novel and robust route for the synthesis of diversely substituted isoindoline skeletons through a ligand-free Pd-catalyzed cascade consisting of isocyanide insertion into Ugi-tetrazole has been developed. The tetrazole precursor is prepared in one step by the Ugi-four component reaction. The reaction proceeds smoothly under mild conditions with high efficiency. This chemistry is simple, economical, and is believed to be the key step during the synthesis of significant pharmaceuticals.