Photoinduced Copper‐Catalyzed 1,2‐Alkyl Azolation of 1,3‐Enynes with NHPI Esters and Azoles

Comprehensive Summary

1,3‐Enynes are very fundamental and important building blocks in organic synthesis. The transformations of 1,3‐enynes into a wide variety of valuable chemicals have been extensively studied in recent years. In these transformations, most of the research efforts have focused on the formation of C–C bonds. However, the construction of C‐heteroatom bonds was less explored. Herein, we reported a photoinduced copper‐catalyzed 1,2‐alkyl azolation of 1,3‐enynes with tertiary and benzylic NHPI esters and azoles. Diverse and valuable propargyl azoles were obtained from the readily available starting materials. Moreover, the broad azole scopes, including pyrazoles, indazoles and triazoles, the redox neutral conditions and the good late‐stage transformations of propargyl azole derivatives endow this method with significant advantages in practical utility. The mechanism experiments indicated that the reaction involves a radical process.