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@ARTICLE{Zlatopolskiy:877587,
      author       = {Zlatopolskiy, Boris D. and Neumaier, Felix and Rüngeler,
                      Till and Drewes, Birte and Kolks, Niklas and Neumaier,
                      Bernd},
      title        = {{P}reparation of a {F}irst 18{F}-{L}abeled {A}gonist for
                      {M}1 {M}uscarinic {A}cetylcholine {R}eceptors},
      journal      = {Molecules},
      volume       = {25},
      number       = {12},
      issn         = {1420-3049},
      address      = {Basel},
      publisher    = {MDPI},
      reportid     = {FZJ-2020-02309},
      pages        = {2880 -},
      year         = {2020},
      abstract     = {M1 muscarinic acetylcholine receptors (mAChRs) are abundant
                      in postsynaptic nerve terminals of all forebrain regions and
                      have been implicated in the cognitive decline associated
                      with Alzheimer’s disease and other CNS pathologies.
                      Consequently, major efforts have been spent in the
                      development of subtype-selective positron emission
                      tomography (PET) tracers for mAChRs resulting in the
                      development of several 11C-labeled probes. However,
                      protocols for the preparation of 18F-labeled mAChR-ligands
                      have not been published so far. Here, we describe a
                      straightforward procedure for the preparation of an
                      18F-labeled M1 mAChR agonist and its corresponding pinacol
                      boronate radiolabeling precursor and the non-radioactive
                      reference compound. The target compounds were prepared from
                      commercially available aryl fluorides and Boc protected
                      4-aminopiperidine using a convergent reaction protocol. The
                      radiolabeling precursor was prepared by a modification of
                      the Miyaura reaction and labeled via the alcohol-enhanced
                      Cu-mediated radiofluorination. The developed procedure
                      afforded the radiotracer in a non-decay-corrected
                      radiochemical yield of 17 ± $3\%$ (n = 3) and in excellent
                      radiochemical purity $(>99\%)$ on a preparative scale. Taken
                      together, we developed a straightforward protocol for the
                      preparation of an 18F-labeled M1 mAChR agonist that is
                      amenable for automation and thus provides an important step
                      towards the routine production of a 18F-labeled M1 selective
                      PET tracer for experimental and diagnostic applications.},
      cin          = {INM-5},
      ddc          = {540},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {573 - Neuroimaging (POF3-573)},
      pid          = {G:(DE-HGF)POF3-573},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:32585815},
      UT           = {WOS:000550178600001},
      doi          = {10.3390/molecules25122880},
      url          = {https://juser.fz-juelich.de/record/877587},
}