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• W1899551010 abstract "The aim of this study was to develop a direct fluorination method for the preparation of [18F]-(E)-N-(3-iodoprop-2-enyl)-2β-carbofluoroethoxy-3β-(4′-methyl-phenyl)nortropane ([18F]FE-PE2I (VI). The synthesis procedure relies on the conventional Kryptofix-mediated nucleophilic 18F-substitution of the tosylate group in the precursor, TsOE-PE2I (V). Out of reaction conditions tested, the highest fluorination efficiency was obtained in dimethyl sulfoxide at 140°C. The reaction mixture was purified by semi-preparative HPLC, followed-up by a standard Sep-Pak SPE procedure. On average, 1.0 GBq of [18F]FE-PE2I was produced from 5-min irradiation at 35 μA (dimethyl sulfoxide, 5 min/140°C). Decay-uncorrected yield of the product after HPLC purification and formulation was in the order of 20%. Specific radioactivity of [18F]FE-PE2I at 15 min after EOS was 3.3–5.1 Ci/µmol (n = 3); radiochemical purity was >98% (n = 4). This direct nucleophilic fluorination strategy is well suited for the automation of the entire synthesis of [18F]FE-PE2I in a modern PET synthesizer for human PET application. In addition, the 18F-incorporation rate into TsOE-PE2I was evaluated using radio-thin layer chromatography (TLC) and radio-HPLC. The suggested HPLC method (ACE 5 C18-HL column and acetonitrile/0.1 M NH4CO2 (80:20)) was found to be suitable for evaluation of ‘free’ 18F-fluoride in the reaction mixture; in addition, this method allowed the detection of three radiolabelled by-products that were not discernable with the TLC approach. Therefore, we conclude that the HPLC approach may serve as a good alternative to traditional radio-TLC technique as it provides more detailed information about the fluorination process in the reaction kinetics or optimization studies. Copyright © 2012 John Wiley & Sons, Ltd." @default.
• W1899551010 created "2016-06-24" @default.
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• W1899551010 date "2012-05-14" @default.
• W1899551010 modified "2023-10-03" @default.
• W1899551010 title "An efficient one-step radiosynthesis of [18F]FE-PE2I, a PET radioligand for imaging of dopamine transporters" @default.
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• W1899551010 doi "https://doi.org/10.1002/jlcr.2927" @default.
• W1899551010 hasPublicationYear "2012" @default.
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