Diversity-driven and facile 1,3-dipolar cycloaddition to access dispirooxindole-imidazolidine scaffolds

Abstract

A diversity-driven three-component 1,3-dipolar cycloaddition of isatins, amino acids and isatin-derived ketimines was developed to facilely assemble dispirooxindole-imidazolidine skeletons bearing vicinal quaternary carbon centers. This protocol features additive-free, minimal solvent usage (0.1 mL DMSO/0.2 mmol scale), wide substrate scope (34 examples), mild reaction conditions (room temperature) and high chemical yield (up to 99%).