% IMPORTANT: The following is UTF-8 encoded.  This means that in the presence
% of non-ASCII characters, it will not work with BibTeX 0.99 or older.
% Instead, you should use an up-to-date BibTeX implementation like “bibtex8” or
% “biber”.

@INPROCEEDINGS{Craig:865321,
      author       = {Craig, A. and Kolks, N. and Urusova, E. and Zlatopolskiy,
                      Boris and Neumaier, B.},
      title        = {{T}he {E}fficient {P}reparation of {R}adiolabeled
                      {A}romatic {A}mino {A}cids via {C}u-{M}ediated
                      {R}adiofluorination using {N}i-complexes},
      reportid     = {FZJ-2019-04823},
      year         = {2019},
      abstract     = {Ziel/Aim:The aim of this work was to develop a procedure
                      for the preparation of F-18-labeled aromatic amino acids
                      (AAA) via alcohol-enhanced Cu-mediated radiofluorination
                      using Ni-BPX auxiliaries as easily-removable dual-protecting
                      groups.Methodik/Methods:The Bpin-substituted precursors of
                      radiofluorinated AAA and α-Me-AAA were prepared by
                      alkylation of (S)-Ni-BPB-Gly and (S)-Ni-BPA-(RS)-Ala with
                      the corresponding Bpin-substituted benzyl bromides.
                      Radiolabeling was carried out according to the protocol for
                      alcohol-enhanced1 Cu-mediated radiofluorination as follows:
                      F-18-F- was loaded onto a QMA-cartridge which was
                      subsequently washed with MeOH; F-18-F- was eluted with
                      Et4NHCO3 to a solution of Cu(py)4(OTf)2 and precursor in
                      DMF/nBuOH (2:1), and the reaction mixture was stirred under
                      air at 110 °C for 10 min. Evaporation of the DMA/nBuOH was
                      followed by deprotection using 12 M HCl at 110 °C for 15
                      min. The acidic solution was evaporated and the tracer was
                      isolated by HPLC.Ergebnisse/Results:Ni complexes containing
                      2 – 4-F-18-FPhe, 2 – 4-aMe-F-18-FPhe, 6-F-18-FMT,
                      aMe-6-F-18-FMT, 4-F-18-FTrp and 2-Me-F-18-FTyr residues were
                      obtained in RCCs of 50 – $95\%.$ The purified tracers were
                      isolated in n.d.c 15 – $25\%$ RCYs in excellent
                      radiochemical and enantiomeric purity. Radiosyntheses of
                      4-F-18-FPhe and 4-F-18-FTrp were implemented to an automated
                      module furnishing tracers in n.d.c RCYs of $25\%$ and
                      $17\%,$ respectively, within 75 – 80
                      min.Schlussfolgerungen/Conclusions:Alcohol-enhanced
                      Cu-mediated radiofluorination of BPin substituted Ni-BPX-AAA
                      complexes is a simple, yet powerful method for the fast
                      production of structurally diverse radiolabeled AAAs and
                      alpha-methyl substituted AAAs. The attractiveness of the
                      procedure is highlighted by the accessibility of
                      radiolabeling precursors, high RCYs and easy implementation
                      to an automated module.Literatur/References:[1] Zichler, J.,
                      Niklas, K., Modemann, D., Neumaier, B., Zlatopolskiy, B.;
                      Chemistry – A European Journal, 2017, 23, 3251 – 3256},
      month         = {Apr},
      date          = {2019-04-03},
      organization  = {57. Jahrestagung der Deutschen
                       Gesellschaft für Nuklearmedizin,
                       Bremen (Germany), 3 Apr 2019 - 6 Apr
                       2019},
      subtyp        = {After Call},
      cin          = {INM-5},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {573 - Neuroimaging (POF3-573)},
      pid          = {G:(DE-HGF)POF3-573},
      typ          = {PUB:(DE-HGF)6},
      doi          = {10.1055/s-0039-1683568},
      url          = {https://juser.fz-juelich.de/record/865321},
}