Alkene Oxyamination: One-Pot Synthesis of Unprotected N–H Amino γ-Lactones

-activated hydroxylamines (9 examples). The utility of the transformation is further demonstrated through the late-stage functionalization of active pharmaceutical ingredients (3 examples). This operationally simple, one-pot process proceeds via sequential intermolecular, stereospecific olefin aziridination followed by intramolecular aziridine ring-opening.