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

Timothé Maujean,Patrice Marchand,Patrick Wagner,Stéphanie Riché,Frédéric Boisson,Nicolas Girard,Dominique Bonnet,Mihaela Gulea

Chemical Communications（2022）

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摘要

The HDA reaction of dithioesters was developed as a new click-reaction compatible with the indirect F-18-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.

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