Hetero-Diels-Alder click reaction of dithioesters for a catalyst-free indirect 18F-radiolabelling of peptides

Chem Commun (Camb). 2022 Oct 4;58(79):11151-11154. doi: 10.1039/d2cc04148k.

Abstract

The HDA reaction of dithioesters was developed as a new click-reaction compatible with the indirect 18F-labelling of peptides. It involves dithioester-peptides and a radiofluorinated diene as a novel prosthetic group. The method was applied to a PSMA-ligand for the in vivo detection of LNCap tumors in xenografted mice.

MeSH terms

  • Animals
  • Catalysis
  • Cycloaddition Reaction
  • Ligands
  • Mice
  • Peptides*

Substances

  • Ligands
  • Peptides