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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Radiosyntheses using Fluorine-18: The Art and Science of Late Stage Fluorination

Author(s): Erin L. Cole, Megan N. Stewart, Ryan Littich, Raphael Hoareau and Peter J. H. Scott

Volume 14, Issue 7, 2014

Page: [875 - 900] Pages: 26

DOI: 10.2174/1568026614666140202205035

Price: $65


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 (t1/2 = 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.

Keywords: Fluorine-18, radiochemistry, radiopharmaceutical synthesis, PET imaging, positron emission tomography.

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