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

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

Volume: 14 Issue: 7

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Cole L. Erin, Stewart N. Megan, Littich Ryan, Hoareau Raphael and Scott J. H. Peter, Radiosyntheses using Fluorine-18: The Art and Science of Late Stage Fluorination, Current Topics in Medicinal Chemistry 2014; 14 (7) . https://dx.doi.org/10.2174/1568026614666140202205035