Hydrogen atom transfer (HAT)-mediated strategy has emerged as a straightforward and powerful approach for oxidative C–H bond functionalization. However, despite remarkable progress in this field, the enantioselective allylic and propargylic C–H aminations remain a challenge. In this study, we developed highly enantioselective allylic and propargylic C–H aminations by combining a visible light-activated HAT process with copper catalysis. Using this method, a wide range of alkenes and alkynes can be converted into high-value chiral allylic and propargylic amines with high enantio-, regio-, and E/Z-selectivity. These enantio-enriched amines serve as versatile building blocks in organic synthesis and hold significant potential for applications in the synthesis of pharmaceuticals, natural products and other bioactive molecules.
