Journal Article

FZJ-2022-02092

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Convenient PET-tracer production via SuFEx 18F-fluorination of nanomolar precursor amounts

Walter, N.FZJ* ; Bertram, J.FZJ* ; Drewes, B.FZJ* ; Bahutski, V. ; Timmer, M. ; Schütz, M. B. ; Krämer, F. ; Neumaier, F. (Corresponding author)FZJ* ; Endepols, H.FZJ* ; Neumaier, B. (Corresponding author)FZJ* ; Zlatopolskiy, B. D.

2022
Elsevier Amsterdam [u.a.]

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Please use a persistent id in citations: http://hdl.handle.net/2128/31129  doi:10.1016/j.ejmech.2022.114383

Abstract: 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

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Contributing Institute(s):

1. Nuklearchemie (INM-5)

Research Program(s):

1. 5253 - Neuroimaging (POF4-525) (POF4-525)

Appears in the scientific report 2022

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