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  • Title: Palladium-catalyzed unactivated C(sp3)-H bond activation and intramolecular amination of carboxamides: a new approach to β-lactams.
    Author: Sun WW, Cao P, Mei RQ, Li Y, Ma YL, Wu B.
    Journal: Org Lett; 2014 Jan 17; 16(2):480-3. PubMed ID: 24341538.
    Abstract:
    An efficient method to synthesize the β-lactams with high regioselectivity via Pd-catalyzed C(sp(3))-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.
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