Stereoselective Access to Spiro-isoindolinone Scaffolds via Catalytic Asymmetric aza-Piancatelli Rearrangement

A chiral Brønsted acid catalyzed asymmetric aza-Piancatelli rearrangement of 3-furyl-3-hydroxyisoindolinones with anilines has been developed, enabling the divergent construction of chiral spiro-cyclopentenone-isoindolinones in high yields with excellent diastereo- and enantioselectivities even under a low catalyst loading of 0.5 mol%.