title: Carbon-14 radiosynthesis of the benzofuran derivative and β-amyloid plaque neuroimaging positron emission tomography radioligand AZD4694.
abstract: In support of a metabolite study, the β-amyloid plaque neuroimaging positron-emission tomography radioligand AZD4694 was labeled with carbon-14 in 10 radiosynthetic steps starting from radiolabeled carbon dioxide. [(14)C]AZD4694 was labeled in the benzofuran heterocycle with a specific activity of 2.1 GBq/mmol and with a radiochemical purity of >99%. The described synthesis constitutes a general method to carbon-14-labeled substituted benzofurans.
authors.affiliation: AstraZeneca, Research & Development-Isotope Chemistry, Screening and Profiling Global DMPK IM, B212, Södertälje, SE-151 85, Sweden.
authors.forename: Johan
authors.initials: J
authors.lastname: Sandell
mesh_terms: D001572:Benzofurans / Q000138:chemical synthesis*; D002250:Carbon Radioisotopes / Q000737:chemistry; D006845:Hydrocarbons, Fluorinated / Q000138:chemical synthesis*; D049268:Positron-Emission Tomography / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*
chemical_list: C552498:AZD4694; D001572:Benzofurans; D002250:Carbon Radioisotopes; D006845:Hydrocarbons, Fluorinated; D019275:Radiopharmaceuticals
keywords: AZD4694; BOC t-butyloxycarbonyl; PET radioligand; amyloid; benzofuran