[¹⁸F]Tosyl fluoride as a versatile [¹⁸F]fluoride source for the preparation of ¹⁸F-labeled radiopharmaceuticals

Positron emission tomography (PET) is an in vivo imaging technology that utilizes positron-emitting radioisotope-labeled compounds as PET radiotracers that are commonly used in clinic and in various research areas, including oncology, cardiology, and neurology. Fluorine-18 is the most widely used PET-radionuclide and commonly produced by proton bombardment of ¹⁸O-enriched water in a cyclotron. The [¹⁸F]fluoride thus obtained generally requires processing by azeotropic drying in order to completely remove H₂O before it can be used for nucleophilic radiofluorination. In general, the drying step is important in facilitating the radiofluorination reactions and the preparation of ¹⁸F-labeled PET radiotracers. In this communication, we have demonstrated the feasibility of using [¹⁸F]tosyl fluoride ([¹⁸F]TsF) as a versatile [¹⁸F]fluoride source for radiofluorination to bypass the azeotropic drying step, and we have developed a continuous flow solid-phase radiosynthesis strategy to generate [¹⁸F]TsF in a form that is excellent for radiofluorination. [¹⁸F]TsF shows high reactivity in radiofluorination and provides the features suitable for preparing PET radiotracers on a small scale and exploring novel radiolabeling technologies. Thus, using [¹⁸F]TsF as a [¹⁸F]fluoride source is a promising strategy that facilitates radiofluorination and provides a convenient and efficient solution for the preparation of ¹⁸F-labeled radiopharmaceuticals that is well matched to the emerging trends in PET imaging technologies.