TY  - JOUR
AU  - Zischler, Johannes
AU  - Kolks, Niklas
AU  - Modemann, Daniel
AU  - Neumaier, Bernd
AU  - Zlatopolskiy, Boris D.
TI  - Alcohol-Enhanced Cu-Mediated Radiofluorination
JO  - Chemistry - a European journal
VL  - 23
IS  - 14
SN  - 0947-6539
CY  - Weinheim
PB  - Wiley-VCH
M1  - FZJ-2017-02164
SP  - 3251 - 3256
PY  - 2017
AB  - The potential of many 18F-labeled (hetero)aromatics for applications in positron emission tomography remains underexplored because convenient procedures for their radiosynthesis are lacking. Consequently, simple methods to prepare radiofluorinated (hetero)arenes are highly sought after. Herein, we report the beneficial effect of primary and secondary alcohols on Cu-mediated 18F-labeling. This observation contradicts the assumption that such alcohols are inappropriate solvents for aromatic fluorination. Therefore, we developed a protocol for rapid radiolabeling of an extraordinarily broad scope of boronic and stannyl substrates under general reaction conditions. Notably, radiofluorinated indoles, phenols, and anilines were synthesized directly from the corresponding unprotected precursors. Furthermore, the novel method enabled the preparation of radiofluorinated tryptophans, [18F]F-DPA, [18F]DAA1106, 6-[18F]FDA, and 6-[18F]FDOPA
LB  - PUB:(DE-HGF)16
UR  - <Go to ISI:>//WOS:000395775700003
C6  - pmid:27943464
DO  - DOI:10.1002/chem.201604633
UR  - https://juser.fz-juelich.de/record/828196
ER  -