Direct, Catalytic α-Alkylation of -Heterocycles by Hydroaminoalkylation: Substrate Effects for Regiodivergent Product Formation.

Saturated -heterocycles are prevalent in pharmaceutical and agrochemical industries, yet remain challenging to catalytically alkylate. Most strategies for C-H activation of these challenging substrates use protected amines or high loadings of precious metal catalysts. We report an early transition-metal system for the broad, robust, and direct alkylation of unprotected amine heterocycles with simple alkenes.