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- W2132489587 abstract "LBT-999 (8-((E)-4-fluoro-but-2-enyl)-3β-p-tolyl-8-aza-bicyclo[3.2.1]octane-2β-carboxylic acid methyl ester) is a cocaine derivative belonging to a new generation of highly selective dopamine transporter ligands (KD:9 nM). LBT-999 was labelled with fluorine-18 at its fluoromethylvinyl moiety using the following two-step radiochemical process: (a) No-carrier-added nucleophilic aliphatic radiofluorination from (E)-1, 4-ditosyloxybut-2-ene and the activated K[18F]F-Kryptofix®222 complex in acetonitrile at 70°C for 10 min giving (E)-1-[18F]fluoro-4-tosyloxybut-2-ene, followed by (b) condensation of the latter with 3β-p-tolyl-8-aza-bicyclo[3.2.1]octane-2β-carboxylic acid methyl ester in N,N-dimethylformamide containing potassium iodide for 20 min at 90°C and (c) HPLC purification (SunFire™ C18, eluent H2O/CH3CN/TFA (72:28:0.1 (v/v/v)). Radiochemically pure (> 95%) [18F]LBT-999 (2.03–2.96 GBq, 37–111 GBq/μmol) was obtained in 95–100 min starting from a 44.4 GBq [18F]fluoride ion production batch (4.6–6.7% non-decay-corrected overall yield). Copyright © 2006 John Wiley & Sons, Ltd." @default.
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- W2132489587 date "2006-01-01" @default.
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- W2132489587 title "Radiosynthesis of [18F]LBT-999, a selective radioligand for the visualization of the dopamine transporter with PET" @default.
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- W2132489587 doi "https://doi.org/10.1002/jlcr.1092" @default.
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