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This process demonstrates efficient c-H amination in alkenes, indicating practical synthesis of allylic amines via an in situ reaction.
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 N-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.
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Deng et al. (2025) studied this question.
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