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 -