A practical route for synthesizing a PET ligand containing [18F]fluorobenzene using reaction of diphenyliodonium salt with [18F]F−

The aim of this study was to develop a practical route for preparing a fluorine-18 ([18F]) labelled ligand ([18F]1) containing [18F]fluorobenzene ring by employing the reaction of diphenyliodonium salt with [18F]F−. Diphenyliodonium tosylate (2) was synthesized from tributylphenylstannyl compound (6) with [hydroxy(tosyloxy)iodo]benzene (7). Using this method, [18F]DAA1106 ([18F]3a), a positron emission tomography ligand for imaging peripheral-type benzodiazepine receptor, was prepared.