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| 001 | 907585 | ||
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| 024 | 7 | _ | |a 10.1016/j.ejmech.2022.114383 |2 doi |
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| 100 | 1 | _ | |a Walter, Nils |0 P:(DE-Juel1)180982 |b 0 |
| 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 |2 Crossref |b Elsevier BV |c 2022-07-01 |
| 336 | 7 | _ | |a article |2 DRIVER |
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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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| 542 | _ | _ | |i 2022-07-01 |2 Crossref |u https://www.elsevier.com/tdm/userlicense/1.0/ |
| 542 | _ | _ | |i 2022-07-01 |2 Crossref |u https://doi.org/10.15223/policy-017 |
| 542 | _ | _ | |i 2022-07-01 |2 Crossref |u https://doi.org/10.15223/policy-037 |
| 542 | _ | _ | |i 2022-07-01 |2 Crossref |u https://doi.org/10.15223/policy-012 |
| 542 | _ | _ | |i 2022-07-01 |2 Crossref |u https://doi.org/10.15223/policy-029 |
| 542 | _ | _ | |i 2022-07-01 |2 Crossref |u https://doi.org/10.15223/policy-004 |
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| 700 | 1 | _ | |a Bertram, Jan |0 P:(DE-Juel1)191040 |b 1 |
| 700 | 1 | _ | |a Drewes, Birte |0 P:(DE-Juel1)131817 |b 2 |
| 700 | 1 | _ | |a Bahutski, Victor |0 P:(DE-Juel1)172894 |b 3 |
| 700 | 1 | _ | |a Timmer, Marco |0 P:(DE-HGF)0 |b 4 |
| 700 | 1 | _ | |a Schütz, Markus B. |0 0000-0003-3381-2729 |b 5 |
| 700 | 1 | _ | |a Krämer, Felicia |0 P:(DE-Juel1)186984 |b 6 |
| 700 | 1 | _ | |a Neumaier, Felix |0 P:(DE-Juel1)175142 |b 7 |e Corresponding author |
| 700 | 1 | _ | |a Endepols, Heike |0 P:(DE-Juel1)180330 |b 8 |
| 700 | 1 | _ | |a Neumaier, Bernd |0 P:(DE-Juel1)166419 |b 9 |e Corresponding author |
| 700 | 1 | _ | |a Zlatopolskiy, Boris D. |0 P:(DE-Juel1)176188 |b 10 |
| 773 | 1 | 8 | |a 10.1016/j.ejmech.2022.114383 |b Elsevier BV |d 2022-07-01 |p 114383 |3 journal-article |2 Crossref |t European Journal of Medicinal Chemistry |v 237 |y 2022 |x 0223-5234 |
| 773 | _ | _ | |a 10.1016/j.ejmech.2022.114383 |g Vol. 237, p. 114383 - |0 PERI:(DE-600)2005170-0 |p 114383 |t European journal of medicinal chemistry |v 237 |y 2022 |x 0223-5234 |
| 856 | 4 | _ | |y Restricted |u https://juser.fz-juelich.de/record/907585/files/1-s2.0-S0223523422002859-main.pdf |
| 856 | 4 | _ | |y Published on 2022-04-14. Available in OpenAccess from 2024-04-14. |u https://juser.fz-juelich.de/record/907585/files/EJMECH-D-21-03231_R2.pdf |
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