Radiosyntheses using Fluorine-18: the Art and Science of Late Stage Fluorination
2014
Positron (β + ) emission tomography (PET) is a powerful, noninvasive tool for the in vivo, three-dimensional imaging
of physiological structures and biochemical pathways. The continued growth of PET imaging relies on a corresponding
increase in access to radiopharmaceuticals (biologically active molecules labeled with short-lived radionuclides
such as fluorine-18). This unique need to incorporate the short-lived fluorine-18 atom (t 1/2 = 109.77 min) as late in the
synthetic pathway as possible has made development of methodologies that enable rapid and efficient late stage fluorination
an area of research within its own right. In this review we describe strategies for radiolabeling with fluorine-18, including
classical fluorine-18 radiochemistry and emerging techniques for late stage fluorination reactions, as well as labeling
technologies such as microfluidics and solid-phase radiochemistry. The utility of fluorine-18 labeled radiopharmaceuticals
is showcased through recent applications of PET imaging in the healthcare, personalized medicine and drug discovery
settings.
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