Construction of Cyclophane-Braced Peptide Macrocycles via Palladium-Catalyzed Picolinamide-Directed Intramolecular C(sp2)-H Arylation

Org Lett. 2020 Sep 4;22(17):6879-6883. doi: 10.1021/acs.orglett.0c02422. Epub 2020 Aug 19.

Abstract

A versatile method for the construction of C(sp2)-linked cyclophane peptide macrocycles via Pd-catalyzed picolinamide-directed intramolecular arylation of aryl and alkenyl C-H bonds of amino acid side chains with aryl iodides is developed. This method provides simple and efficient access to a variety of cyclophane-braced structures from readily accessible linear peptide precursors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acids / chemistry*
  • Catalysis
  • Iodides / chemistry
  • Molecular Structure
  • Palladium / chemistry*
  • Peptides / chemistry
  • Picolinic Acids / chemical synthesis*
  • Picolinic Acids / chemistry*

Substances

  • Amino Acids
  • Iodides
  • Peptides
  • Picolinic Acids
  • Palladium
  • picolinamide