Palladium-Catalyzed Aminocarbonylation in Solid-Phase Peptide Synthesis: A Method for Capping, Cyclization, and Isotope Labeling

Org Lett. 2017 Jun 2;19(11):2873-2876. doi: 10.1021/acs.orglett.7b01068. Epub 2017 May 12.

Abstract

A new synthetic approach for introducing N-capping groups onto peptides attached to a solid support, combining aminocarbonylation under mild conditions using a palladacycle precatalyst and solid-phase peptide synthesis, is reported. The use of a silacarboxylic acid as an in situ CO-releasing molecule allowed the reaction to be performed in a single vial. The method also enables versatile substitution of side chains, side-chain-to-side-chain cyclizations, and selective [13C] acyl labeling of modified peptides.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Cyclization
  • Isotope Labeling
  • Molecular Structure
  • Palladium / chemistry*
  • Peptides
  • Solid-Phase Synthesis Techniques

Substances

  • Peptides
  • Palladium