Introducing substituents on backbone amide nitrogens of peptides is an attractive strategy to improve the pharmacological properties of peptides. Here, we describe a solid-phase synthetic method for peptides with various substituents on backbone amide nitrogens. The method utilizes the procedures for introducing substituents on resin, which facilitates introducing diverse functional groups on backbone amide nitrogens.

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Solid-Phase Synthesis of Peptides with Methyl and Larger Substituents on Backbone Amide Nitrogens via On-Resin Incorporation of the Substituents

  • Jumpei Morimoto,
  • Marin Yokomine,
  • Takaya Yamazaki,
  • Shinsuke Sando

摘要

Introducing substituents on backbone amide nitrogens of peptides is an attractive strategy to improve the pharmacological properties of peptides. Here, we describe a solid-phase synthetic method for peptides with various substituents on backbone amide nitrogens. The method utilizes the procedures for introducing substituents on resin, which facilitates introducing diverse functional groups on backbone amide nitrogens.