Orlovskaya, Victoriya V., Modemann, Daniel J., Kuznetsova, Olga F., Fedorova, Olga S. ORCID: 0000-0002-9122-9622, Urusova, Elizaveta A., Kolks, Niklas
ORCID: 0000-0001-8532-0684, Neumaier, Bernd
ORCID: 0000-0001-5425-3116, Krasikova, Raisa N. and Zlatopolskiy, Boris D.
(2019).
Alcohol-Supported Cu-Mediated F-18-Fluorination of Iodonium Salts under Minimalist Conditions.
Molecules, 24 (17).
BASEL:
MDPI.
ISSN 1420-3049
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 F-18-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 [F-18]fluorides with the Cu-mediator in methanolic DMF. The iodonium [F-18]fluorides were prepared by direct elution of F-18(-) 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-[F-18]FPhe, in 22-69% isolated radiochemical yields as well as its direct implementation into a remote-controlled synthesis unit.
Item Type: | Journal Article | ||||||||||||||||||||||||||||||||||||||||
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URN: | urn:nbn:de:hbz:38-142310 | ||||||||||||||||||||||||||||||||||||||||
DOI: | 10.3390/molecules24173197 | ||||||||||||||||||||||||||||||||||||||||
Journal or Publication Title: | Molecules | ||||||||||||||||||||||||||||||||||||||||
Volume: | 24 | ||||||||||||||||||||||||||||||||||||||||
Number: | 17 | ||||||||||||||||||||||||||||||||||||||||
Date: | 2019 | ||||||||||||||||||||||||||||||||||||||||
Publisher: | MDPI | ||||||||||||||||||||||||||||||||||||||||
Place of Publication: | BASEL | ||||||||||||||||||||||||||||||||||||||||
ISSN: | 1420-3049 | ||||||||||||||||||||||||||||||||||||||||
Language: | English | ||||||||||||||||||||||||||||||||||||||||
Faculty: | Unspecified | ||||||||||||||||||||||||||||||||||||||||
Divisions: | Unspecified | ||||||||||||||||||||||||||||||||||||||||
Subjects: | no entry | ||||||||||||||||||||||||||||||||||||||||
Uncontrolled Keywords: |
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Refereed: | Yes | ||||||||||||||||||||||||||||||||||||||||
URI: | http://kups.ub.uni-koeln.de/id/eprint/14231 |
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