Selective Mono- and Diamination of Ketones in a Combined Copper–Organocatalyst System

Herein, we report a simple and mild protocol for the chemoselective mono- and diamination of ketone using pyrazole as the amine source in a combined copper-organocatalyst system. Various substrates are compatible, providing the corresponding products in moderate to good yields. This strategy gives an efficient and convenient solution for the synthesis of α-pyrazole and α,α-dipyrazole ketone derivatives. The control experiment demonstrates that in situ generated hydrazone is a key intermediate in the transformation.