N-Difluoromethyl-triazole as a constrained scaffold in peptidomimetics

Chem Commun (Camb). 2017 May 2;53(36):5024-5027. doi: 10.1039/c7cc01298e.

Abstract

The N-difluoromethyl triazolo-β-aza-ε-amino acid present in the core of peptides led to constrained conformations due to CH-F and NH-F interactions. Pseudotetrapeptides were obtained in excellent yields directly by click chemistry between azidodifluoroacetamides and alkynes, both linked to an amino acid. This work demonstrates that the N-difluoromethyltriazole scaffold can induce extended structures to β-strand mimics.

MeSH terms

  • Click Chemistry
  • Hydrocarbons, Fluorinated / chemistry*
  • Molecular Structure
  • Peptidomimetics / chemistry*
  • Triazoles / chemistry*

Substances

  • Hydrocarbons, Fluorinated
  • Peptidomimetics
  • Triazoles