Abstract
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 (18F) 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 (CF3) represents a versatile structural motif in medicinal and pharmaceutical chemistry to design and synthesize drug molecules with favourable pharmacological properties. This fact also makes CF3 groups an exciting synthesis target from a PET tracer discovery perspective. Early attempts to synthesize [18F]CF3-containing radiotracers were mainly hampered by low radiochemical yields and additional challenges such as low radiochemical purity and molar activity. However, recent innovations in [18F]trifluoromethylation chemistry have significantly expanded the chemical toolbox to synthesize fluorine-18-labelled radiotracers. This review presents the development of significant [18F]trifluoromethylation chemistry strategies to apply [18F]CF3-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 CF3-containing drugs will be the primary drivers for developing novel [18F]trifluoromethylation chemistry strategies in the future.
Highlights
Trifluoromethyl (CF3) groups are important functional groups in pharmaceutical and medicinal chemistry as excellent bioisosteres of methyl groups
We present recent results of significant [18F]trifluoromethylation chemistry strategies for using [18F]CF3-containing radiotracers in preclinical and clinical positron emission tomography (PET) imaging studies
The continuous growth of PET as a functional imaging technique in biomedical and clinical research and the increasing number of CF3-containing drug compounds are the primary drivers for developing novel [18F]trifluoromethylation chemistry strategies
Summary
Trifluoromethyl (CF3) groups are important functional groups in pharmaceutical and medicinal chemistry as excellent bioisosteres of methyl groups. The continuous growth of PET as a functional imaging technique in biomedical and clinical research and the increasing number of CF3-containing drug compounds are the primary drivers for developing novel [18F]trifluoromethylation chemistry strategies. The continuous growth of PET as a functional imaging technique in biomedical and clinical research and the increasing number of CF3‐containing drug compounds ar3eofth25e primary drivers for developing novel [18F]trifluoromethylation chemistry strategies. The overall strategy of radiofluorination of α-diflurobromo ester to generate the radiolabelled ester and a further reduction of the ester to corresponding alcohol was similar to that of Johnstrom et al The higher molar activity radiofluorination route disclosed by Gomez and co-workers was adapted to this synthesis, where DBU is used as an additive to facilitate the radiofluorination (Scheme 2)
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