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: | , |
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| Formato: | article |
| Lenguaje: | EN |
| Publicado: |
MDPI AG
2021
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| Materias: | |
| Acceso en línea: | https://doaj.org/article/f0a8376c22c242359255f7d6adc03421 |
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| Sumario: | 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. |
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