One-Step Synthesis of [18F]Fluoro-4-(vinylsulfonyl)benzene: A Thiol Reactive Synthon for Selective Radiofluorination of Peptides

Radiolabeled peptide-based molecular imaging probes exploit the advantages of large biologics and small molecules, providing both exquisite selectivity and favorable pharmacokinetic properties. Here, we report an operationally simple and broadly applicable approach for the F-18-fluorination of unprotected peptides via a new radiosynthon, [F-18]fluoro-4-(vinylsulfonyl)benzene. This reagent demonstrates excellent chemoselectivity at the cysteine residue and rapid F-18-labeling of a diverse scope of peptides to generate stable thioether constructs.