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

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% beta(+) decay, 109.8 min half-life, 635 keV positron energy) make it an attractive nuclide for labeling and molecular imaging. It stands that 2-[F-18]fluoro-2-deoxy-D-glucose ([F-18]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, F-18-labeled radiotracer design has become a hot topic in radiochemistry and radiopharmaceutics. Over the past decades, we have witnessed a rapid growth in F-18-labeling methods owing to the development of new reagents and catalysts. This review aims to provide an overview of strategies in radiosynthesis of [F-18]fluorine-containing moieties with nucleophilic [F-18]fluorides since 2015.

Automated summary

Positron emission tomography (PET) molecular imaging technology is a critical tool for evaluating biological and biochemical processes. Fluorine-18 has favorable characteristics for labeling and molecular imaging, making it significant in radiochemistry and radiopharmaceutics. The development of new reagents and catalysts has led to rapid growth in F-18 labeling methods over the past decades.