Direct Asymmetric Dearomatization of 2-Naphthols by Scandium-Catalyzed Electrophilic Amination†

Catalytic asymmetric aminative dearomatization of 1-substituted 2-naphthols was successfully implemented with electrophilic azodicarboxylates under the catalysis of chiral ScIII/pybox complexes. This intermolecular reaction represents a hitherto unknown enantioselective CN bond-forming process through direct dearomatization of phenolic compounds to generate chiral nitrogen-containing quaternary carbon stereocenters.