title: Preparation of the metabotropic glutamate receptor 5 (mGluR5) PET tracer [(18)F]FPEB for human use: An automated radiosynthesis and a novel one-pot synthesis of its radiolabeling precursor.
abstract: The radiotracer 3-[(18)F]fluoro-5-(2-pyridinylethynyl)benzonitrile, or [(18)F]FPEB, is a promising PET imaging agent for the metabotropic glutamate subtype 5 receptor (mGluR5). In an effort to develop a routine production method of this radiotracer for use in clinical research we adapted its radiosynthesis to an automated chemistry module. In the meanwhile, we also developed a simplified "one-pot" method for the preparation of the nitrobenzonitrile radiolabeling precursor for [(18)F]FPEB and its reference standard to replace the existing multi-step synthetic approach.
authors.affiliation: PET Center, Department of Diagnostic Radiology, Yale University School of Medicine, New Haven, CT 06520, USA. Electronic address: Keunpoong.Lim@yale.edu.
authors.forename: Keunpoong
authors.initials: K
authors.lastname: Lim
authors.affiliation: PET Center, Department of Diagnostic Radiology, Yale University School of Medicine, New Haven, CT 06520, USA.
authors.forename: David
authors.initials: D
authors.lastname: Labaree
authors.affiliation: PET Center, Department of Diagnostic Radiology, Yale University School of Medicine, New Haven, CT 06520, USA.
authors.forename: Songye
authors.initials: S
authors.lastname: Li
authors.affiliation: PET Center, Department of Diagnostic Radiology, Yale University School of Medicine, New Haven, CT 06520, USA.
authors.forename: Yiyun
authors.initials: Y
authors.lastname: Huang
mesh_terms: D005462:Fluorine Radioisotopes / Q000737:chemistry* / Q000493:pharmacokinetics*; D006801:Humans; D007553:Isotope Labeling / Q000379:methods*; D057054:Molecular Imaging / Q000379:methods; D009570:Nitriles / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography / Q000379:methods*; D011725:Pyridines / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D064529:Receptor, Metabotropic Glutamate 5 / Q000378:metabolism*; D012371:Robotics / Q000379:methods
chemical_list: C527000:3-fluoro-5-((pyridin-3-yl)ethynyl)benzonitrile; D005462:Fluorine Radioisotopes; D009570:Nitriles; D011725:Pyridines; D019275:Radiopharmaceuticals; D064529:Receptor, Metabotropic Glutamate 5
keywords: PET; Radiotracer synthesis; Suzuki coupling; [(18)F]FPEB; mGluR5