کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1876020 | 1532122 | 2013 | 9 صفحه PDF | دانلود رایگان |
(−)-[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.
► Two-step radiosynthesis for (−)-[18F]flubatine as α4β2 nAChR imaging agent was developed.
► Numerous leaving and protecting groups for optimal precursor design were tested.
► A NMe3-iodide/Boc-protected precursor provided the best radiochemical parameters.
► The procedure can be easily transferred to an automated synthesis module.
Journal: Applied Radiation and Isotopes - Volume 74, April 2013, Pages 128–136