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@ARTICLE{Walter:907585,
      author       = {Walter, Nils and Bertram, Jan and Drewes, Birte and
                      Bahutski, Victor and Timmer, Marco and Schütz, Markus B.
                      and Krämer, Felicia and Neumaier, Felix and Endepols, Heike
                      and Neumaier, Bernd and Zlatopolskiy, Boris D.},
      title        = {{C}onvenient {PET}-tracer production via {S}u{FE}x
                      18{F}-fluorination of nanomolar precursor amounts},
      journal      = {European journal of medicinal chemistry},
      volume       = {237},
      issn         = {0223-5234},
      address      = {Amsterdam [u.a.]},
      publisher    = {Elsevier},
      reportid     = {FZJ-2022-02092},
      pages        = {114383},
      year         = {2022},
      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},
      cin          = {INM-5},
      ddc          = {610},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {5253 - Neuroimaging (POF4-525)},
      pid          = {G:(DE-HGF)POF4-5253},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:35447431},
      UT           = {WOS:000793618400001},
      doi          = {10.1016/j.ejmech.2022.114383},
      url          = {https://juser.fz-juelich.de/record/907585},
}