Oxidative Functionalization of Peptide Side Chains Enabled by <i>N</i>-Chlorination of Amides

DOI

Bibliographic Information

Other Title
  • アミドの<i>N</i>-クロロ化を経由するペプチド側鎖の酸化的官能基化

Abstract

Peptides containing unusual motifs such as abnormal amino acids and macrocyclic substructures have recently attracted much attention as a new modality in middle molecule drug discovery. Therefore, it is highly important to realize the methodology of chemical synthesis for a wide variety of such unusual peptide derivatives, and particularly, the direct modification of already-constructed peptide chains would enable the rapid supply of derivatives based on the parent peptide compound already on hand. However, most of the previous methods require reactive functional groups on the peptide side chains and the applicable substrates are limited in exchange for high site specificity of the transformation. In this account, we describe “an N-chloropeptide strategy” which enables the direct transformation for a wide variety of peptides regardless of their amino acid residues by utilizing amides of peptide main chains as a reactive point.

Journal

  • MEDCHEM NEWS

    MEDCHEM NEWS 34 (2), 93-96, 2024-05-01

    The Pharmaceutical Society of Japan

Details 詳細情報について

  • CRID
    1390581468909753472
  • DOI
    10.14894/medchem.34.2_93
  • ISSN
    24328626
    24328618
  • Text Lang
    ja
  • Data Source
    • JaLC
  • Abstract License Flag
    Disallowed

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