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024 7 _ |a 10.1016/j.ejmech.2022.114383
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024 7 _ |a 0223-5234
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041 _ _ |a English
082 _ _ |a 610
100 1 _ |a Walter, Nils
|0 P:(DE-Juel1)180982
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245 _ _ |a Convenient PET-tracer production via SuFEx 18F-fluorination of nanomolar precursor amounts
260 _ _ |a Amsterdam [u.a.]
|c 2022
|b Elsevier
264 _ 1 |3 print
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|b Elsevier BV
|c 2022-07-01
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520 _ _ |a 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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700 1 _ |a Bertram, Jan
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700 1 _ |a Drewes, Birte
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700 1 _ |a Bahutski, Victor
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700 1 _ |a Timmer, Marco
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700 1 _ |a Schütz, Markus B.
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700 1 _ |a Krämer, Felicia
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700 1 _ |a Neumaier, Felix
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700 1 _ |a Endepols, Heike
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700 1 _ |a Neumaier, Bernd
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700 1 _ |a Zlatopolskiy, Boris D.
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773 1 8 |a 10.1016/j.ejmech.2022.114383
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|t European Journal of Medicinal Chemistry
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773 _ _ |a 10.1016/j.ejmech.2022.114383
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856 4 _ |y Published on 2022-04-14. Available in OpenAccess from 2024-04-14.
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LibraryCollectionCLSMajorCLSMinorLanguageAuthor
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