Fluorine-18 Radiochemistry, Labeling Strategies and Synthetic Routes

Fluorine-18 is the most frequently used radioisotope in positron emission tomography (PET) radiopharmaceuticals in both clinical and preclinical research. Its physical and nuclear characteristics (97% beta(+) decay, 109.7 min half-life, 635 keV positron energy), along with high specific activity and ease of large scale production, make it an attractive nuclide for radiochemical labeling and molecular imaging. Versatile chemistry including nucleophilic and electrophilic substitutions allows direct or indirect introduction of F-18 into molecules of interest. The significant increase in F-18 radiotracers for PET imaging accentuates the need for simple and efficient F-18-labeling procedures. In this review, we will describe the current radiosynthesis routes and strategies for F-18 labeling of small molecules and biomolecules.