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

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.