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Metal‐Catalyzed Derivatization of Cα‐Tetrasubstituted Amino Acids and Their Use in the Synthesis of Cyclic Peptides
Authors:Andreas Grauer  Andreas Späth  Dawei Ma Prof?Dr  Burkhard König Prof?Dr
Institution:1. Institut für Organische Chemie, Universit?t Regensburg, 93040 Regensburg (Germany), Fax: (+49)?941‐943‐1717;2. State Key Laboratory of Bioorganic & Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Shanghai 200032 (China)
Abstract:Making circles with N and O : Cyclic tripeptides containing an unnatural Cα‐tetrasubstituted THF amino acid are prepared by copper(I) and palladium(0)‐catalyzed N‐ and O‐arylation reactions. The reactions give access to side chain‐modified derivatives of the unnatural amino acid and macrocyclic peptidomimetics.
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Keywords:amino acids  cyclization  homogeneous catalysis  peptides  peptidomimetics
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