Alcohol-Supported Cu-Mediated 18F-Fluorination of Iodonium Salts under “Minimalist” Conditions
2019 | journal article. A publication with affiliation to the University of Göttingen.
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Alcohol-Supported Cu-Mediated 18F-Fluorination of Iodonium Salts under “Minimalist” Conditions
Orlovskaya, V. V.; Modemann, D. J.; Kuznetsova, O. F.; Fedorova, O. S.; Urusova, E. A.; Kolks, N. & Neumaier, B. et al. (2019)
Molecules, 24(17) pp. 3197. DOI: https://doi.org/10.3390/molecules24173197
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- Authors
- Orlovskaya, Victoriya V.; Modemann, Daniel J.; Kuznetsova, Olga F.; Fedorova, Olga S.; Urusova, Elizaveta A.; Kolks, Niklas; Neumaier, Bernd; Krasikova, Raisa N.; Zlatopolskiy, Boris D.
- Abstract
- In the era of personalized precision medicine, positron emission tomography (PET) and related hybrid methods like PET/CT and PET/MRI gain recognition as indispensable tools of clinical diagnostics. A broader implementation of these imaging modalities in clinical routine is closely dependent on the increased availability of established and emerging PET-tracers, which in turn could be accessible by the development of simple, reliable, and efficient radiolabeling procedures. A further requirement is a cGMP production of imaging probes in automated synthesis modules. Herein, a novel protocol for the efficient preparation of 18F-labeled aromatics via Cu-mediated radiofluorination of (aryl)(mesityl)iodonium salts without the need of evaporation steps is described. Labeled aromatics were prepared in high radiochemical yields simply by heating of iodonium [18F]fluorides with the Cu-mediator in methanolic DMF. The iodonium [18F]fluorides were prepared by direct elution of 18F− from an anion exchange resin with solutions of the corresponding precursors in MeOH/DMF. The practicality of the novel method was confirmed by the racemization-free production of radiolabeled fluorophenylalanines, including hitherto unknown 3-[18F]FPhe, in 22–69% isolated radiochemical yields as well as its direct implementation into a remote-controlled synthesis unit.
- Issue Date
- 2019
- Publisher
- MDPI
- Journal
- Molecules
- eISSN
- 1420-3049
- Language
- English