Building Better Beta-Lactams

Beta-lactams are a cornerstone functional group of countless antibiotics including penicillin and cephalosporins. Their ring strain and reactivity are both the blessing that engenders them with antibiotic activity, and the curse that hinders their synthesis. Classically, chemists have used a relatively limited set of disconnections: olefin + isocyanate cycloaddition, C-H insertion with a diazoamide, cyclization of beta amino acids, and the Kinugasa reaction (Name reaction!). Huang and Ding (USTC, Hefei, CN) add a new tool to the mix, combining olefins, imines, and carbon monoxide with Pd to build a sizable library of beta lactams in a single step. Summary Link to the work