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A Facile Pathway to Enantiomerically Enriched 3-Hydroxy-2-Oxindoles: Asymmetric Intramolecular Arylation of α-Keto Amides Catalyzed by a Palladium–DifluorPhos Complex


  • Financial support was provided by Grant-in-Aid for Young Scientists (S) from the JSPS. L.Y. thanks the JSPS for research fellowships.


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Less metal wastes: The first catalytic, enantioselective intramolecular aryl-transfer reaction of aryl triflates to ketones has been developed (see scheme; R1=R2=aromatic and aliphatic). This method features overall practicality, including substrate stability and accessibility (protecting-group free) plus no need for the use of stoichiometric amounts of metals.