Regio- and Enantioselective <i>N</i>‑Heterocyclic\nCarbene-Catalyzed Annulation of Aminoindoles Initiated by Friedel–Crafts\nAlkylation

Chiral indoles annulated\non the benzene ring are unique and significant\nin natural and medicinal compounds. However, accessing these enantioenriched\nmolecules has often been overlooked. The present study introduces\nan organocatalytic protocol to access these compounds efficiently,\ndemonstrated by substrate scope, functional group tolerance, and using\nonly 1 mol % of a chiral conjugated acid catalyst. Additionally, the\nstudy explores regioselectivity, gram-scale reactions, and follow-up\ntransformations, underscoring the method’s potential.