Methyl piperidine-4-carboxylate is a reactant for C-2 arylation of piperidines through directed transition metal-catalyzed sp3 C-H activation. It is used as a reactant for synthesis of antitubercular agents, aminopyrazine inhibitors, orally available naphthyridine protein kinase D inhibitors and a scalable catalyst from asymmetric hydrogenation of sterically demanding aryl enamide.