Intermolecular Enantioselective Dearomatization Reaction of β‐Naphthol Using meso ‐Aziridine: A Bifunctional In Situ Generated Magnesium Catalyst

A direct, facile, and highly diastereo‐ and enantioselective dearomatization reaction of β‐naphthol derivatives with aziridines has been developed for the first time. A newly designed Box–OH ligand was employed for an in situ generated magnesium catalyst and proved to be efficient. The corresponding dearomatization product was transformed into a polycyclic scaffold and polyhydroxylated compound. 1 H NMR studies revealed the activation mode of the dearomatization process of β‐naphthols, and a clear positive nonlinear effect was observed in the reaction, and provides insight into the coordination environment around the Mg II center and the possible active species.