Fluorine-18 radiolabeling strategies-advantages and disadvantages of currently applied labeling methods
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Fluorine-18 radiolabeling strategies-advantages and disadvantages of currently applied labeling methods. / Edem, Patricia E.; Steen, E. Johanna L.; Kjær, Andreas; Herth, Matthias M.
Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates. Elsevier, 2019. p. 29-103.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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TY - CHAP
T1 - Fluorine-18 radiolabeling strategies-advantages and disadvantages of currently applied labeling methods
AU - Edem, Patricia E.
AU - Steen, E. Johanna L.
AU - Kjær, Andreas
AU - Herth, Matthias M.
PY - 2019
Y1 - 2019
N2 - The use of fluorine-18 (18F) has had an important impact in medicine since its discovery. Fluorine-18 is the most commonly used isotope in positron emission tomography (PET), which is a noninvasive and sensitive radionuclide-based molecular imaging technology. PET can be used for diagnosis, staging, therapy planning, treatment control, and drug development. Fluorine-18 has ideal nuclear properties for PET, resulting in high resolution, accessibility, and marketability. Furthermore, its nuclear properties result in a low patient radiation burden. From a chemical point of view, fluorine-18 is rather difficult to work with. The fluoride-18 anion possesses limited nucleophilicity. Thus, its chemical applicability is restricted. On the other hand, fluorine-18 gas leads to products with low molar activity (Am), and only a few biological applications can be imaged with low Am. This chapter will provide a broad overview of fluorine-18 chemistry, an in-depth description of challenges, and possible solutions for producing 18F-bioactive molecules and highlight the clinical applicability of the described synthetic strategies. Finally, the chapter will conclude with a critical analysis of the field and provide some considerations moving forward.
AB - The use of fluorine-18 (18F) has had an important impact in medicine since its discovery. Fluorine-18 is the most commonly used isotope in positron emission tomography (PET), which is a noninvasive and sensitive radionuclide-based molecular imaging technology. PET can be used for diagnosis, staging, therapy planning, treatment control, and drug development. Fluorine-18 has ideal nuclear properties for PET, resulting in high resolution, accessibility, and marketability. Furthermore, its nuclear properties result in a low patient radiation burden. From a chemical point of view, fluorine-18 is rather difficult to work with. The fluoride-18 anion possesses limited nucleophilicity. Thus, its chemical applicability is restricted. On the other hand, fluorine-18 gas leads to products with low molar activity (Am), and only a few biological applications can be imaged with low Am. This chapter will provide a broad overview of fluorine-18 chemistry, an in-depth description of challenges, and possible solutions for producing 18F-bioactive molecules and highlight the clinical applicability of the described synthetic strategies. Finally, the chapter will conclude with a critical analysis of the field and provide some considerations moving forward.
KW - 18F-labeled radiopharmaceuticals
KW - Fluorine-18
KW - Low molar activity
KW - Positron emission tomography (PET)
KW - Prostate specific membrane antigen
KW - Radiofluorination
UR - http://www.scopus.com/inward/record.url?scp=85066450801&partnerID=8YFLogxK
U2 - 10.1016/B978-0-12-812958-6.00002-1
DO - 10.1016/B978-0-12-812958-6.00002-1
M3 - Book chapter
AN - SCOPUS:85066450801
SN - 9780128130391
SP - 29
EP - 103
BT - Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates
PB - Elsevier
ER -
ID: 242364560