TY  - JOUR
AU  - Orlovskaya, Victoriya V.
AU  - Modemann, Daniel
AU  - Kutnetsova, Olga F.
AU  - Fedorova, Olga S.
AU  - Urusova, Elizaveta
AU  - Kolks, Niklas
AU  - Neumaier, Bernd
AU  - Krasikova, Raisa N.
AU  - Zlatopolskiy, Boris
TI  - Alcohol-Supported Cu-Mediated 18F-Fluorination of Iodonium Salts under “Minimalist” Conditions
JO  - Molecules
VL  - 24
IS  - 17
SN  - 1420-3049
CY  - Basel
PB  - MDPI
M1  - FZJ-2019-04521
SP  - 3197
PY  - 2019
AB  - 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.
LB  - PUB:(DE-HGF)16
C6  - pmid:31484375
UR  - <Go to ISI:>//WOS:000488613700177
DO  - DOI:10.3390/molecules24173197
UR  - https://juser.fz-juelich.de/record/864918
ER  -