This title appears in the Scientific Report :
2022
Please use the identifier:
http://hdl.handle.net/2128/31129 in citations.
Please use the identifier: http://dx.doi.org/10.1016/j.ejmech.2022.114383 in citations.
Convenient PET-tracer production via SuFEx 18F-fluorination of nanomolar precursor amounts
Convenient PET-tracer production via SuFEx 18F-fluorination of nanomolar precursor amounts
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 f...
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Personal Name(s): | Walter, Nils |
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Bertram, Jan / Drewes, Birte / Bahutski, Victor / Timmer, Marco / Schütz, Markus B. / Krämer, Felicia / Neumaier, Felix (Corresponding author) / Endepols, Heike / Neumaier, Bernd (Corresponding author) / Zlatopolskiy, Boris D. | |
Contributing Institute: |
Nuklearchemie; INM-5 |
Published in: | European Journal of Medicinal Chemistry European journal of medicinal chemistry, 237 237 (2022 2022) S. 114383 114383 |
Imprint: |
Amsterdam [u.a.]
Elsevier
2022
2022-07-01 |
PubMed ID: |
35447431 |
DOI: |
10.1016/j.ejmech.2022.114383 |
Document Type: |
Journal Article |
Research Program: |
Neuroimaging |
Link: |
Restricted Published on 2022-04-14. Available in OpenAccess from 2024-04-14. |
Publikationsportal JuSER |
Please use the identifier: http://dx.doi.org/10.1016/j.ejmech.2022.114383 in citations.
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 |