Direct C-H bond functionalization of sp3 carbons via transition-metal catalysis has received a great attention in recent years. Notably, this process does not require the prefunctionalization of the sp3 C-H bonds and the use of stoichiometric amounts of organometallic reagents, and thus is economically and ecologically favorable compared with the traditional approaches. Within this reaction class, copper-catalyzed process is of current research interest, and significant progress has been achieved in recent years. In our efforts to develop novel transition-metal-catalyzed processes, herein, we describe the highly diastereoselective intramolecular dehydrogenative cyclization of N,N-disubstituted hydrazones and direct functionalization of sp3 carbons by the copper-catalyzed sp3 C-H bond activation processes. The reaction protocols utilized O2 as the oxidant, and showed great functional group tolerance.

Copper-catalyzed direct functionalization of sp3 carbons

248th National Meeting (2014)

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