Synthesis of 2,2-difunctionalized 2H-azirines via I₂-mediated annulation of enamines

Various 2,2-difunctionalized 2H-azirines were synthesized via I-2-mediated annulation reactions of readily accessible enamines in the presence of nitrogen or non-nitrogen nucleophiles. The features of the present synthesis process also include no use of transition metals, simple operation, mild reaction conditions, a broad substrate scope, and gram-scale synthesis.