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A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Nickel-Photocatalytic Deoxygenative Arylation toward β-Methyl-Branched α-Amino Acids
Berjan Stouwie1, Anna R Emmerich1, Thomas Weyhermüller2
1Max-Planck-Institute for Chemical Energy Conversion, Department for Electrosynthesis, Stiftstr. 34-36, 45470 Mülheim an der Ruhr, Germany.
Abstract:
β-Methyl-branched α-amino acids are important motifs in peptide therapeutics. However, only few methods on their synthesis have been reported to date. Herein we report an efficient, one-step synthesis of these β-Me-branched α-amino acids through the deoxygenative arylation of threonine, yielding a diverse scope of noncanonical α-amino acids with good functional group tolerance. Our method could also be extended to the deoxygenative arylation of 3-hydroxyproline, giving access to various therapeutically relevant arylated amino acids.
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