Enantioselective Desymmetrization of Cyclobutanones Enabled by Synergistic Palladium/Enamine Catalysis

: The enantioselective intramolecular α-arylation of cyclobutanones has been established by combining palladium and enamine catalyst systems. Two different enantioselective control strategies have been developed for cyclobutanone substrates bearing O- or N-tethered aryl bromides. Further synthetic applications are also reported.