Copper-Promoted Aerobic Oxidative [3+2] Cycloaddition Reactions of N,N-Disubstituted Hydrazines with Alkynoates: Access to Substituted Pyrazoles

A copper-promoted aerobic oxidative [3+2] cycloaddition reaction for the synthesis of various substituted pyrazoles from N,N-disubstituted hydrazines with alkynoates in the presence of bases is developed. This work involves a direct C(sp3)-H functionalization and the formation of new C-C/C-N bonds. In this strategy, inexpensive and easily available Cu2O serves as the promoter and air acts as the green oxidant. The reaction exhibits the advantages of high atom and step economy, high regioselectivity, and easy operation.