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

Zhou, Dong; Chu, Wenhua; Xu, Jinbin; Schwarz, Sally; Katzenellenbogen, John A.

doi:10.1038/s41598-023-30200-2

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

Journal Article · Wed Feb 22 23:00:00 EST 2023 · Scientific Reports

DOI:https://doi.org/10.1038/s41598-023-30200-2· OSTI ID:1958336

Zhou, Dong; Chu, Wenhua; Xu, Jinbin; Schwarz, Sally; Katzenellenbogen, John A.

Abstract

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 ¹⁸ O-enriched water in a cyclotron. The [ ¹⁸ F]fluoride thus obtained generally requires processing by azeotropic drying in order to completely remove H ₂ O before it can be used for nucleophilic radiofluorination. In general, the drying step is important in facilitating the radiofluorination reactions and the preparation of ¹⁸ F-labeled PET radiotracers. In this communication, we have demonstrated the feasibility of using [ ¹⁸ F]tosyl fluoride ([ ¹⁸ F]TsF) as a versatile [ ¹⁸ F]fluoride source for radiofluorination to bypass the azeotropic drying step, and we have developed a continuous flow solid-phase radiosynthesis strategy to generate [ ¹⁸ F]TsF in a form that is excellent for radiofluorination. [ ¹⁸ F]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 [ ¹⁸ F]TsF as a [ ¹⁸ F]fluoride source is a promising strategy that facilitates radiofluorination and provides a convenient and efficient solution for the preparation of ¹⁸ F-labeled radiopharmaceuticals that is well matched to the emerging trends in PET imaging technologies.

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Sponsoring Organization:: USDOE

Grant/Contract Number:: SC0008432

OSTI ID:: 1958336

Alternate ID(s):: OSTI ID: 2419802

Journal Information:: Scientific Reports, Journal Name: Scientific Reports Journal Issue: 1 Vol. 13; ISSN 2045-2322

Publisher:: Nature Publishing GroupCopyright Statement

Country of Publication:: United Kingdom

Language:: English

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