Highly stereoselective modifications of peptides via Pd-catalyzed allylic alkylation of internal peptide amide enolates

Org Biomol Chem. 2012 Oct 3;10(41):8268-75. doi: 10.1039/c2ob26351c.

Abstract

Pd-catalyzed allylations are excellent tools for stereoselective peptide modifications, showing several advantages compared to normal alkylations. Reactions of internal peptide amide enolates with Pd-allyl complexes proceed not only with high yields of up to 86%, they show also high regio- and diastereoselectivities (88-99%), giving rise to the trans-configured products. Therefore, this protocol is a powerful synthetic tool for the synthesis of natural product and drug molecules.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Allyl Compounds / chemistry*
  • Amides / chemistry*
  • Catalysis
  • Cyclization
  • Molecular Structure
  • Palladium / chemistry*
  • Peptides / chemical synthesis
  • Peptides / chemistry*
  • Stereoisomerism

Substances

  • Allyl Compounds
  • Amides
  • Peptides
  • Palladium