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Current Radiopharmaceuticals


ISSN (Print): 1874-4710
ISSN (Online): 1874-4729

Fluorine-18 Chemistry for PET: A Concise Introduction

Author(s): Samuel Banister, Dirk Roeda, Frederic Dolle and Michael Kassiou

Volume 3, Issue 2, 2010

Page: [68 - 80] Pages: 13

DOI: 10.2174/1874471011003020068

Price: $65


Fluorine-18 is the most important radionuclide used in positron emission tomography (PET) today, largely due to its attractive physical and nuclear characteristics. Agents such as the clinical oncology tracer 2-[18F]fluoro-2-deoxy-D-glucose ([18F]FDG), the most widely used PET-radiopharmaceutical, are driving an increasing interest in the chemistry of radiopharmaceuticals utilizing fluorine-18. This review outlines the methods for production of fluorine-18, and the development of agents for performing radiofluorination reactions. With a few exceptions, radiofluorinations can be classified as either electrophilic or nucleophilic. The electrophilic reactions mainly use molecular [18F]fluorine of moderately low specific radioactivity, or reagents prepared from it, and include additions to alkenes, reactions with carbanions and especially fluorodehydrogenation and fluorodemetallation. The nucleophilic reactions usually involve no-carrier-added (high-specific- radioactivity) [18F]fluoride as its K[18F]F-K222 complex and include SN2-type substitutions in the aliphatic series and SNAr-type substitutions in the aromatic and heteroaromatic series. Key examples from each class of radiofluorination reaction will be described, highlighting the potential of this radioisotope in the design and preparation of fluorine-18- labeled probes for PET imaging.

Keywords: Fluorine-18, radionuclide, positron emission tomography (PET), radiofluorination reactions, radioisotope, PET imaging

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