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Amine-Directed Palladium-Catalyzed C?H Halogenation of Phenylalanine Derivatives
Authors:Dr Alexia Ville  Dr Julien Annibaletto  Dr Sébastien Coufourier  Prof Christophe Hoarau  Dr Rodolphe Tamion  Dr Guillaume Journot  Dr Cédric Schneider  Dr Jean-François Brière
Institution:1. Normandie Université, UNIROUEN, INSA Rouen, CNRS, COBRA, 76000 Rouen, France;2. Normandie Université, UNIROUEN, INSA Rouen, CNRS, COBRA, 76000 Rouen, France

These authors contributed equally to this work.;3. Industrial Research Centre-Oril Industrie, CS 60125, 76210 Bolbec, France

Abstract:An efficient primary-amine-directed, palladium-catalyzed C?H halogenation (X=I, Br, Cl) of phenylalanine derivatives is reported on a range of quaternary amino acid (AA) derivatives thanks to suitable conditions employing trifluoroacetic acid as additive. The extension of this original native functionality-directed ortho-selective halogenation was even demonstrated with the more challenging native phenylalanine as tertiary AA.
Keywords:amino acids  CH functionalization  halogenation  homogenous catalysis  palladium
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