Advances in [<sup>18</sup>F]Trifluoromethylation Chemistry for PET Imaging

Positron emission tomography (PET) is a preclinical and clinical imaging technique extensively used to study and visualize biological and physiological processes in vivo. Fluorine-18 (<sup>18</sup>F) is the most frequently used positron emitter for PET imaging due to its convenient 109.8...

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Autores principales:	Felix Francis, Frank Wuest
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	fluorine-18 trifluoromethylation chemistry positron emission tomography (PET) Organic chemistry QD241-441
Acceso en línea:	https://doaj.org/article/f0a8376c22c242359255f7d6adc03421
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spelling	oai:doaj.org-article:f0a8376c22c242359255f7d6adc034212021-11-11T18:28:55ZAdvances in [<sup>18</sup>F]Trifluoromethylation Chemistry for PET Imaging10.3390/molecules262164781420-3049https://doaj.org/article/f0a8376c22c242359255f7d6adc034212021-10-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/21/6478https://doaj.org/toc/1420-3049Positron emission tomography (PET) is a preclinical and clinical imaging technique extensively used to study and visualize biological and physiological processes in vivo. Fluorine-18 (<sup>18</sup>F) is the most frequently used positron emitter for PET imaging due to its convenient 109.8 min half-life, high yield production on small biomedical cyclotrons, and well-established radiofluorination chemistry. The presence of fluorine atoms in many drugs opens new possibilities for developing radioligands labelled with fluorine-18. The trifluoromethyl group (CF<sub>3</sub>) represents a versatile structural motif in medicinal and pharmaceutical chemistry to design and synthesize drug molecules with favourable pharmacological properties. This fact also makes CF<sub>3</sub> groups an exciting synthesis target from a PET tracer discovery perspective. Early attempts to synthesize [<sup>18</sup>F]CF<sub>3</sub>-containing radiotracers were mainly hampered by low radiochemical yields and additional challenges such as low radiochemical purity and molar activity. However, recent innovations in [<sup>18</sup>F]trifluoromethylation chemistry have significantly expanded the chemical toolbox to synthesize fluorine-18-labelled radiotracers. This review presents the development of significant [<sup>18</sup>F]trifluoromethylation chemistry strategies to apply [<sup>18</sup>F]CF<sub>3</sub>-containing radiotracers in preclinical and clinical PET imaging studies. The continuous growth of PET as a crucial functional imaging technique in biomedical and clinical research and the increasing number of CF<sub>3</sub>-containing drugs will be the primary drivers for developing novel [<sup>18</sup>F]trifluoromethylation chemistry strategies in the future.Felix FrancisFrank WuestMDPI AGarticlefluorine-18trifluoromethylation chemistrypositron emission tomography (PET)Organic chemistryQD241-441ENMolecules, Vol 26, Iss 6478, p 6478 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	fluorine-18 trifluoromethylation chemistry positron emission tomography (PET) Organic chemistry QD241-441
spellingShingle	fluorine-18 trifluoromethylation chemistry positron emission tomography (PET) Organic chemistry QD241-441 Felix Francis Frank Wuest Advances in [<sup>18</sup>F]Trifluoromethylation Chemistry for PET Imaging
description	Positron emission tomography (PET) is a preclinical and clinical imaging technique extensively used to study and visualize biological and physiological processes in vivo. Fluorine-18 (<sup>18</sup>F) is the most frequently used positron emitter for PET imaging due to its convenient 109.8 min half-life, high yield production on small biomedical cyclotrons, and well-established radiofluorination chemistry. The presence of fluorine atoms in many drugs opens new possibilities for developing radioligands labelled with fluorine-18. The trifluoromethyl group (CF<sub>3</sub>) represents a versatile structural motif in medicinal and pharmaceutical chemistry to design and synthesize drug molecules with favourable pharmacological properties. This fact also makes CF<sub>3</sub> groups an exciting synthesis target from a PET tracer discovery perspective. Early attempts to synthesize [<sup>18</sup>F]CF<sub>3</sub>-containing radiotracers were mainly hampered by low radiochemical yields and additional challenges such as low radiochemical purity and molar activity. However, recent innovations in [<sup>18</sup>F]trifluoromethylation chemistry have significantly expanded the chemical toolbox to synthesize fluorine-18-labelled radiotracers. This review presents the development of significant [<sup>18</sup>F]trifluoromethylation chemistry strategies to apply [<sup>18</sup>F]CF<sub>3</sub>-containing radiotracers in preclinical and clinical PET imaging studies. The continuous growth of PET as a crucial functional imaging technique in biomedical and clinical research and the increasing number of CF<sub>3</sub>-containing drugs will be the primary drivers for developing novel [<sup>18</sup>F]trifluoromethylation chemistry strategies in the future.
format	article
author	Felix Francis Frank Wuest
author_facet	Felix Francis Frank Wuest
author_sort	Felix Francis
title	Advances in [<sup>18</sup>F]Trifluoromethylation Chemistry for PET Imaging
title_short	Advances in [<sup>18</sup>F]Trifluoromethylation Chemistry for PET Imaging
title_full	Advances in [<sup>18</sup>F]Trifluoromethylation Chemistry for PET Imaging
title_fullStr	Advances in [<sup>18</sup>F]Trifluoromethylation Chemistry for PET Imaging
title_full_unstemmed	Advances in [<sup>18</sup>F]Trifluoromethylation Chemistry for PET Imaging
title_sort	advances in [<sup>18</sup>f]trifluoromethylation chemistry for pet imaging
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/f0a8376c22c242359255f7d6adc03421
work_keys_str_mv	AT felixfrancis advancesinsup18supftrifluoromethylationchemistryforpetimaging AT frankwuest advancesinsup18supftrifluoromethylationchemistryforpetimaging
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Advances in [<sup>18</sup>F]Trifluoromethylation Chemistry for PET Imaging

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