Automated synthesis of [18F]Florbetaben as Alzheimer's disease imaging agent based on a synthesis module system

An automated synthesis procedure of [18F]Florbetaben ([18F]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 50min 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 [18F]Florbetaben using a commercial radiosynthesis module and enables clinical trials of this compound. ► We radiosynthesized [18F]Florbetaben from a new precursor using a one-step procedure. ► The radiosynthesis of [18F]Florbetaben was performed on a commercial module within 50min. ► The automated radiosynthesis strategy ensured a high radiochemical yield in a shorter time.