Amino acid bromides: their N-protection and use in the synthesis of peptides with extremely difficult sequences

J Org Chem. 2002 Sep 6;67(18):6372-5. doi: 10.1021/jo020280w.

Abstract

N(alpha)-Protected alpha-amino acid bromides were easily generated in situ with 1-bromo-N,N-2-trimethyl-1-propenylamine from the corresponding amino acids under very mild conditions. o-Nbs and the azido moieties proved to be compatible with these overactivated halides and were successfully applied in difficult peptide bond formations. N-Deprotection methods and the total step-by-step solution synthesis of a peptide containing up to seven consecutive L-(alphaMe)Valine residues are also reported. The assembly of this homopeptide was achieved in a short time and in very high yields by the azido/bromide system in a single repetitive operation.

MeSH terms

  • Amino Acids / chemistry*
  • Bromides / chemistry*
  • Catalysis
  • Chromatography, High Pressure Liquid
  • Combinatorial Chemistry Techniques*
  • Hydrocarbons, Brominated / chemistry
  • Molecular Structure
  • Peptides / chemical synthesis*
  • Spectroscopy, Fourier Transform Infrared
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • 1-bromo-N,N-2-trimethyl-1-propenylamine
  • Amino Acids
  • Bromides
  • Hydrocarbons, Brominated
  • Peptides