Photoinduced Amination of Inert C(sp³)-H Bonds with Diazirines for Access to Diaziridines

The direct functionalization of inert C(sp³)-H bonds is extremely attractive for constructing high-added-value molecules in synthetic chemistry. Herein, a metal-free and operationally simple method for the convenient synthesis of diaziridines is developed and affords moderate to good yields under mild reaction conditions. Various C-H precursors, including simple alkanes, free alcohols, esters, ethers, halides, nitriles, and heterocycles, were successfully utilized. Moreover, the synthesis of medicinally relevant heterocycles further highlights the synthetic potential of this strategy.