TY  - JOUR
AU  - Walter, Nils
AU  - Bertram, Jan
AU  - Drewes, Birte
AU  - Bahutski, Victor
AU  - Timmer, Marco
AU  - Schütz, Markus B.
AU  - Krämer, Felicia
AU  - Neumaier, Felix
AU  - Endepols, Heike
AU  - Neumaier, Bernd
AU  - Zlatopolskiy, Boris D.
TI  - Convenient PET-tracer production via SuFEx 18F-fluorination of nanomolar precursor amounts
JO  - European journal of medicinal chemistry
VL  - 237
SN  - 0223-5234
CY  - Amsterdam [u.a.]
PB  - Elsevier
M1  - FZJ-2022-02092
SP  - 114383
PY  - 2022
AB  - Recently, a protocol for radiolabeling of aryl fluorosulfates (“SuFEx click radiolabeling”) using ultrafast18F/19F isotopic exchange has been reported. Although promising, the original procedure turned out to berather inefficient. However, systematic optimization of the reaction parameters allowed for developmentof a robust method for SuFEx radiolabeling which obviates the need for azeotropic drying, base additionand HPLC purification. The developed protocol enabled efficient 18F-fluorination of low nanomolaramounts of aryl fluorosulfates in highly diluted solution (micromolar concentrations). It was successfullyused to prepare a series of 29 18F-fluorosulfurylated phenols e including modified ezetimibe, atocopheroland etoposide, the two tyrosine derivatives Boc-Tyr([18F]FS)-OMe and H-Tyr([18F]FS)-OMe,the FAP-specific ligand [18F]FS-UAMC1110, and the DPA-714 analog [18F]FS-DPA e in fair to excellentyields. Preliminary evaluation demonstrated sufficient in vivo stability of radiofluorinated electron rich orneutral {Boc-Tyr([18F]FS)-OMe), H-Tyr([18F]FS)-OMe and [18F]FS-DPA} aryl fluorosulfates. Furthermore,[18F]FS-DPA was identified as a promising tracer for visualization of TSPO expression
LB  - PUB:(DE-HGF)16
C6  - pmid:35447431
UR  - <Go to ISI:>//WOS:000793618400001
DO  - DOI:10.1016/j.ejmech.2022.114383
UR  - https://juser.fz-juelich.de/record/907585
ER  -