%0 Journal Article
%A Orlovskaya, Victoriya V.
%A Modemann, Daniel
%A Kutnetsova, Olga F.
%A Fedorova, Olga S.
%A Urusova, Elizaveta
%A Kolks, Niklas
%A Neumaier, Bernd
%A Krasikova, Raisa N.
%A Zlatopolskiy, Boris
%T Alcohol-Supported Cu-Mediated 18F-Fluorination of Iodonium Salts under “Minimalist” Conditions
%J Molecules
%V 24
%N 17
%@ 1420-3049
%C Basel
%I MDPI
%M FZJ-2019-04521
%P 3197
%D 2019
%X 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.
%F PUB:(DE-HGF)16
%9 Journal Article
%$ pmid:31484375
%U <Go to ISI:>//WOS:000488613700177
%R 10.3390/molecules24173197
%U https://juser.fz-juelich.de/record/864918