title: Automated synthesis of [18F]Florbetaben as Alzheimer's disease imaging agent based on a synthesis module system.
abstract: An automated synthesis procedure of [(18)F]Florbetaben ([(18)F]BAY94-9172), a radiolabeled imaging agent in phase III study for in vivo mapping of fibrillar amyloid β (Aβ) with PET, was developed using the commercial PET-MF-2V-IT-1 synthesizer. The automated radiosynthesis was carried out via a one-step nucleophilic fluorination of methanesulfonic acid 2-[2-(2-{4-[2-(4-methylamino-phenyl)-vinyl]-phenoxy}-ethoxy)-ethoxy]-ethyl ester, as a new precursor, and separation with semi-preparative high performance liquid chromatography (HPLC). The total synthesis time amounted to 50 min with 20-25% yield (uncorrected for decay) and radiochemical purities of more than 95% in all runs. The described automated radiosynthesis allows the production of [(18)F]Florbetaben using a commercial radiosynthesis module and enables clinical trials of this compound.
authors.affiliation: Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-sen University, Guangzhou, China.
authors.forename: Hongliang
authors.initials: H
authors.lastname: Wang
authors.forename: Xinyan
authors.initials: X
authors.lastname: Guo
authors.forename: Shende
authors.initials: S
authors.lastname: Jiang
authors.forename: Ganghua
authors.initials: G
authors.lastname: Tang
mesh_terms: D000544:Alzheimer Disease / Q000000981:diagnostic imaging*; D000814:Aniline Compounds / Q000138:chemical synthesis*; D001331:Automation; D002851:Chromatography, High Pressure Liquid; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D006801:Humans; D011786:Quality Control; D011877:Radionuclide Imaging; D013267:Stilbenes / Q000138:chemical synthesis*
chemical_list: D000814:Aniline Compounds; D005462:Fluorine Radioisotopes; D013267:Stilbenes; C527756:4-(N-methylamino)-4'-(2-(2-(2-fluoroethoxy)ethoxy)ethoxy)stilbene