KINUGASA REACTION AS A CRUCIAL STEP IN THE SYNTHESIS OF β-LACTAMS: A GATEWAY TO ONE OF THE MOST SIGNIFICANT HETEROCYCLES IN COMBATING CONTEMPORARY DISEASES

<jats:p>β-Lactams are indispensable heterocycles in medicinal chemistry, extending beyond antibiotics to diverse therapeutic and synthetic applications. The Kinugasa reaction, a copper-mediated coupling of nitrones and terminal alkynes, provides a direct and versatile route to β-lactams but has long remained underexploited. This review summarizes the evolution of the Kinugasa reaction, highlighting key mechanistic insights, advances in diastereo- and enantioselective variants, intramolecular and cascade processes, and applications under click-like and green conditions. Recent developments demonstrate its effectiveness in constructing complex and highly functionalized β-lactam frameworks relevant to drug discovery. Overall, the Kinugasa reaction has emerged as a valuable contemporary strategy for β-lactam synthesis with significant potential for future medicinal and heterocyclic chemistry applications.</jats:p>