Functionalization of 2‐Naphthols via Asymmetric Formal Hydrogenative Coupling

ABSTRACT A ruthenium‐catalyzed formal hydrogenative coupling for the functionalization of naphthols has been developed, γ ‐naphthol‐substituted chiral alcohols were obtained with excellent enantioselectivities (27 examples, up to >99% ee). The products could serve as synthons for the preparation of chiral oxygen‐containing heterocycles. Mechanistic studies indicate that the transformation proceeds through a base‐promoted conjugate addition to generate a ketone intermediate, which subsequently undergoes asymmetric hydrogenation.