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A general strategy for the synthesis of α-trifluoromethyl- and α-perfluoroalkyl-β-lactams via palladium-catalyzed carbonylation
Authors:Yang Li  Cai-Lin Zhang  Wei-Heng Huang  Ning Sun  Meng Hao  Helfried Neumann  Matthias Beller
Institution:Xi''an Key Laboratory of Textile Chemical Engineering Auxiliaries, School of Environmental and Chemical Engineering, Xi''an Polytechnic University, No. 19 Jinhua South Road, 710048 Xi''an China.; Leibniz-Institut für Katalyse e.V., RostockAlbert-Einstein-Straße 29a, 18059 Rostock Germany,
Abstract:β-Lactam compounds play a key role in medicinal chemistry, specifically as the most important class of antibiotics. Here, we report a novel one-step approach for the synthesis of α-(trifluoromethyl)-β-lactams and related products from fluorinated olefins, anilines and CO. Utilization of an advanced palladium catalyst system with the Ruphos ligand allows for selective cycloaminocarbonylations to give diverse fluorinated β-lactams in high yields.

β-Lactam compounds play a key role in medicinal chemistry, specifically as the most important class of antibiotics.
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