Fluorine-18: Radiochemistry and Target-Specific PET Molecular Probes Design

Yunze Wang; Qingyu Lin; Hongcheng Shi; Dengfeng Cheng

doi:10.3389/fchem.2022.884517

Fluorine-18: Radiochemistry and Target-Specific PET Molecular Probes Design

Front Chem. 2022 Jun 29:10:884517. doi: 10.3389/fchem.2022.884517. eCollection 2022.

Authors

Yunze Wang^{1

2

3}, Qingyu Lin^{1

2

3}, Hongcheng Shi^{1

2

3}, Dengfeng Cheng^{1

2

3}

Affiliations

¹ Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai, China.
² Institute of Nuclear Medicine, Fudan University, Shanghai, China.
³ Shanghai Institute of Medical Imaging, Shanghai, China.

Abstract

The positron emission tomography (PET) molecular imaging technology has gained universal value as a critical tool for assessing biological and biochemical processes in living subjects. The favorable chemical, physical, and nuclear characteristics of fluorine-18 (97% β⁺ decay, 109.8 min half-life, 635 keV positron energy) make it an attractive nuclide for labeling and molecular imaging. It stands that 2-[¹⁸F]fluoro-2-deoxy-D-glucose ([¹⁸F]FDG) is the most popular PET tracer. Besides that, a significantly abundant proportion of PET probes in clinical use or under development contain a fluorine or fluoroalkyl substituent group. For the reasons given above, ¹⁸F-labeled radiotracer design has become a hot topic in radiochemistry and radiopharmaceutics. Over the past decades, we have witnessed a rapid growth in ¹⁸F-labeling methods owing to the development of new reagents and catalysts. This review aims to provide an overview of strategies in radiosynthesis of [¹⁸F]fluorine-containing moieties with nucleophilic [¹⁸F]fluorides since 2015.

Keywords: 18 F-radiolabeling; PET imaging; PET radiotracers; fluorination; fluoroalkylation.

Publication types

Review