Amination/Triazolation of Benzylic/Allylic C(sp ³ )-H with <i>N</i> -Sulfonyl-1,2,3-triazoles in Air

The direct α-C-H amination of alkenes and toluene represents the most straightforward and economically viable method for the construction of biologically active allylic amines. Herein, we report a practical and operationally simple approach for α-C(sp³)-H amination/triazolation of alkenes and toluene with <i>N</i>-sulfonyl-1,2,3-triazoles to construct allylic azoles via intermolecular oxidative C(sp³)-H/N-H cross-coupling. The reaction was completed in air within 1-2 h, giving a nearly quantitative conversion in up to 99% isolated yield with a broad substrate scope via an in situ-generated inner salt process.