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000864918 1001_ $$0P:(DE-HGF)0$$aOrlovskaya, Victoriya V.$$b0
000864918 245__ $$aAlcohol-Supported Cu-Mediated 18F-Fluorination of Iodonium Salts under “Minimalist” Conditions
000864918 260__ $$aBasel$$bMDPI$$c2019
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000864918 520__ $$aIn 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.
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000864918 7001_ $$0P:(DE-Juel1)162416$$aModemann, Daniel$$b1
000864918 7001_ $$0P:(DE-HGF)0$$aKutnetsova, Olga F.$$b2
000864918 7001_ $$0P:(DE-HGF)0$$aFedorova, Olga S.$$b3
000864918 7001_ $$0P:(DE-Juel1)176705$$aUrusova, Elizaveta$$b4
000864918 7001_ $$0P:(DE-Juel1)178654$$aKolks, Niklas$$b5
000864918 7001_ $$0P:(DE-Juel1)166419$$aNeumaier, Bernd$$b6$$eCorresponding author
000864918 7001_ $$0P:(DE-HGF)0$$aKrasikova, Raisa N.$$b7
000864918 7001_ $$0P:(DE-Juel1)176188$$aZlatopolskiy, Boris$$b8
000864918 773__ $$0PERI:(DE-600)2008644-1$$a10.3390/molecules24173197$$n17$$p3197$$tMolecules$$v24$$x1420-3049$$y2019
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