CuI‐Mediated α‐Ketoacylation of Sulfoximines under Solvent‐Free Conditions

The first preparation of α‐ketoacyl sulfoximines under solvent‐free conditions using aryl ethanones and NH ‐sulfoximines has been discovered and a series of desired 2‐oxo‐2‐arylacetyl sulfoximines were successfully synthesized in good to excellent yields (up to 93 %). The unprecedented protocol requires no extra solvents, bases, or additives and demonstrates outstanding compatibility with assorted functional groups (up to 27 examples). A plausible double catalytic cycle mechanism involving elemental iodine and copper is proposed; in‐situ generated aryl‐α‐iodo‐ethanone and a sulfoximine‐liganded‐Cu II intermediate play important roles in C(sp 3 )–N coupling. The postulated mechanism is inspired by key experimental investigations detailed here.