Hydrogenative Dearomatization of Pyridine and an Asymmetric Aza-Friedel-Crafts Alkylation Sequence

Highly efficient synthesis of enantiomerically enriched substituted piperidines has been realized via chiral phosphoric acid catalyzed cascade hydrogenative dearomatization of substituted pyridines and aza‐Friedel‐Crafts reaction in good to excellent yields and enantioselectivity. The highly efficient synthesis of enantiomerically enriched substituted piperidines in good to excellent yields and enantioselectivity has been realized by using the title reaction, which is catalyzed by the chiral phosphoric acid (CPA) (R)‐1.