Rapid 18F-labeling via Pd-catalyzed S-arylation in aqueous medium

We report radiolabeling of thiol-containing substrates via Pd-catalyzed S-arylation with 2-[F-18]fluoro-5-iodopyridine, which is readily accessible using the minimalist radiofluorination method. The practicality of the procedure was confirmed by preparation of a novel PSMA-specific PET-tracer as well as labeling of glutathione, A beta oligomer-binding RD2 peptide, bovine serum albumin and PSMA I&S.

Automated summary

This study reports the radiolabeling of thiol-containing substrates through Pd-catalyzed S-arylation using 2-[F-18]fluoro-5-iodopyridine, which is easily accessible through a minimalist radiofluorination method. The practicality of this method was confirmed through the preparation of a novel PSMA-specific PET-tracer and the labeling of various compounds.