Fluorine‐18 Radiochemistry for PET Imaging Applications—Fundamentals and Recent Advances

Abstract

Positron emission tomography (PET) is a major molecular imaging modality with prominent roles in biomedical research, medical diagnosis, and drug development. Underpinning the widespread utility of PET is extensive radiochemistry research on the development of PET radiotracers and efficient methods for their labeling in optimal molecular positions. Fluorine‐18 has gained importance for labeling PET radiotracers because of (i) favorable decay characteristics, including a half‐life of 109.8 min and a high rate of decay by relatively low energy positron emission (β + , 97%), (ii) an established capacity to produce this radioisotope in very high activity and molar activity from modern biomedical cyclotrons, and (iii) versatile radiochemistry that enables late‐stage incorporation of this radionuclide into radiotracers that range in size from small drug‐like molecules through to macromolecules. In this chapter, we survey this rapidly evolving area of fluorine‐18 radiochemistry with regard to its fundamentals and key advances in meeting the major challenges in PET radiotracer development.