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Since the discovery of penicillin nearly a century ago, βlactam antibiotics have continued to capture the attention of the synthetic and medicinal chemistry communities. In particular, the α-amino-β-lactam motif is present in both penicillin and cephalosporin. It is also a versatile chiral building block in organic synthesis. Consequently, the preparation of α-amino-β-lactams has been the topic of extensive research efforts, and many stereoselective approaches toward these compounds have been developed. The asymmetric methods used include the Staudinger ketene–imine [2+ 2] cycloaddition, Kinugasa alkyne–nitrone cycloaddition, and Gilman–Speeter ester enolate–imine condensation.[1] The seminal work of Daugulis and co-workers on the palladium-catalyzed arylation of secondary C (sp3) ÀH bonds with an 8-aminoquinoline-derived N, N-bidentate directing group [2] has inspired several research groups to use …