Publikationsrepositorium - Helmholtz-Zentrum Dresden-Rossendorf

(–)-[¹⁸F]flubatine is a promising agent for visualization by PET of cerebral α₄β₂ nicotinic acetylcholine receptors (nAChRs), which are implicated in psychiatric and neurodegenerative disorders. Here, we describe a substantially improved two-step radiosynthesis strategy for (–)-[¹⁸F]flubatine, based on the nucleophilic radiofluorination of an enantiomerically pure precursor followed by deprotection of the intermediate. An extensive leaving group/protecting group library of precursors was tested. Application of a trimethylammonium-iodide precursor with a Boc protecting group provided the best results: Labeling efficiencies of 80-95%, RCY of 60±5%, radiochemical purity of >98%, and a specific activity of >350 GBq/µmol. The radiosynthesis is easily transferable to an automated synthesis module.