Vicinal difunctionalization of dehydropiperidines using α-chloro-β-sulfonyl eneformamides

The synthesis of α,β-difunctionalized dehydropiperidines has been accomplished using α-halo-β-sulfonyl eneformamides. This outcome is achieved through sequential regioselective Cβ-alkylative desulfonation and Cα-palladium-catalyzed cross-coupling. In most cases, high yields of the vicinally functionalized eneformamides are obtained.