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Radiosynthesis of [18F]LBT-999, a selective radioligand for the visualization of the dopamine transporter with PET

✍ Scribed by Frédéric Dollé; Françoise Hinnen; Patrick Emond; Sylvie Mavel; Zoïa Mincheva; Wadad Saba; Marie-Anne Schöllhorn-Peyronneau; Heric Valette; Lucette Garreau; Sylvie Chalon; Christer Halldin; Julie Helfenbein; Joël Legaillard; Jean-Claude Madelmont; Jean-Bernard Deloye; Michel Bottlaender; Denis Guilloteau

Publisher
John Wiley and Sons
Year
2006
Tongue
French
Weight
161 KB
Volume
49
Category
Article
ISSN
0022-2135

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✦ Synopsis

LBT-999 (8-((E)-4-fluoro-but-2-enyl)-3b-p-tolyl-8-aza-bicyclo[3.2.1]octane-2b-carboxylic acid methyl ester) is a cocaine derivative belonging to a new generation of highly selective dopamine transporter ligands (K D :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[ 18 F]F-Kryptofix 1 222 complex in acetonitrile at 708C for 10 min giving (E)-1-[ 18 F]fluoro-4-tosyloxybut-2-ene, followed by (b) condensation of the latter with 3b-p-tolyl-8-aza-bicyclo[3.2.1]octane-2b-carboxylic acid methyl ester in N,N-dimethylformamide containing potassium iodide for 20 min *

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