%0 Journal Article
%A Walter, Nils
%A Bertram, Jan
%A Drewes, Birte
%A Bahutski, Victor
%A Timmer, Marco
%A Schütz, Markus B.
%A Krämer, Felicia
%A Neumaier, Felix
%A Endepols, Heike
%A Neumaier, Bernd
%A Zlatopolskiy, Boris D.
%T Convenient PET-tracer production via SuFEx 18F-fluorination of nanomolar precursor amounts
%J European journal of medicinal chemistry
%V 237
%@ 0223-5234
%C Amsterdam [u.a.]
%I Elsevier
%M FZJ-2022-02092
%P 114383
%D 2022
%X 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
%F PUB:(DE-HGF)16
%9 Journal Article
%$ pmid:35447431
%U <Go to ISI:>//WOS:000793618400001
%R 10.1016/j.ejmech.2022.114383
%U https://juser.fz-juelich.de/record/907585