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• W4223927102 startingPage "114383" @default.
• W4223927102 abstract "Recently, a protocol for radiolabeling of aryl fluorosulfates (SuFEx click radiolabeling) using ultrafast 18F/19F isotopic exchange has been reported. Although promising, the original procedure turned out to be rather inefficient. However, systematic optimization of the reaction parameters allowed for development of a robust method for SuFEx radiolabeling which obviates the need for azeotropic drying, base addition and HPLC purification. The developed protocol enabled efficient 18F-fluorination of low nanomolar amounts of aryl fluorosulfates in highly diluted solution (micromolar concentrations). It was successfully used to prepare a series of 29 18F-fluorosulfurylated phenols - including modified ezetimibe, α-tocopherol and 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 - in fair to excellent yields. Preliminary evaluation demonstrated sufficient in vivo stability of radiofluorinated electron rich or neutral {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." @default.
• W4223927102 created "2022-04-19" @default.
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• W4223927102 date "2022-07-01" @default.
• W4223927102 modified "2023-10-14" @default.
• W4223927102 title "Convenient PET-tracer production via SuFEx 18F-fluorination of nanomolar precursor amounts" @default.
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• W4223927102 doi "https://doi.org/10.1016/j.ejmech.2022.114383" @default.
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