Fmoc solid-phase synthesis of peptide thioesters using an intramolecularn,S-acyl shift

Org Lett. 2005 Jun 23;7(13):2647-50. doi: 10.1021/ol050776a.

Abstract

[reaction: see text] We describe the Fmoc solid-phase synthesis of peptide thioesters based on the alkylation of the safety-catch sulfonamide linker with a protected 2-mercaptoethanol derivative. The thioester is generated on the solid phase after the peptide chain assembly as a consequence of an intramolecular N,S-acyl shift. Depending on the stability of the spacer separating the sulfonamide linker from the resin toward TFA, treatment of the peptidyl resin with TFA led to a soluble or supported deprotected thioester.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Amino Acids / chemistry*
  • Combinatorial Chemistry Techniques*
  • Esters
  • Molecular Sequence Data
  • Peptides / chemical synthesis*
  • Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization

Substances

  • Amino Acids
  • Esters
  • Peptides