Palladium-Catalyzed Unactivated C(sp3)–H Bond Activation and Intramolecular Amination of Carboxamides: A New Approach to β‑Lactams

An efficient method to synthesize the β-lactams with high regioselectivity via Pd-catalyzed C­(sp3)–H bond activation and intramolecular amination of simple and readily available aminoquinoline carboxamides was demonstrated. C6F5I plays a significant role in the formation of the C–N bond of the four-membered ring β-lactams. High yield along with wide substrate scope and functional group tolerance makes this reaction applicable to build natural-product-derived β-lactams. This method has been applied to the efficient synthesis of the β-lactamase inhibitor MK-8712.