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Direct Palladium‐Catalyzed β‐Arylation of Lactams
Authors:Ming Chen  Feipeng Liu  ProfDr Guangbin Dong
Institution:1. Department of Chemistry, University of Chicago, Chicago, USA;2. Department of Applied Chemistry, China Agricultural University, Beijing, China
Abstract:A direct and catalytic method is reported here for β‐arylation of N‐protected lactams with simple aryl iodides. The transformation is enabled by merging soft enolization of lactams, palladium‐catalyzed desaturation, Ar?X bond activation, and aryl conjugate addition. The reaction is operated under mild reaction conditions, is scalable, and is chemoselective. Application of this method to concise syntheses of pharmaceutically relevant compounds is demonstrated.
Keywords:C−  H activation  heterocylces  lactams  palladium  reaction mechanisms
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