Journal of labelled compounds and radiopharmaceuticals p. 1141 - 1149 (2003)
Update date:2022-08-05
Topics:
Roeda
Hinnen
Dolle
Benazoline (2-naphthalen-2-yl-4,5-dihydro-1H-imidazole) is a selective high-affinity ligand for the imidazoline 12 receptor. This compound was labelled with carbon-11 (T1/2 = 20.4 min) at the number two carbon atom of its 2-imidazoline ring. Cyclotron-produced [11C]carbon dioxide reacted with 2-naphthylmagnesium bromide to give 2-[carboxyl- 11C] naphthoic acid in 60% radiochemical yield. The latter was heated with a mixture of ethylenediamine and its dihydrochloride at 300°C to give [11C]benazoline in 16% overall yield, relative to [ 11C]carbon dioxide and with a specific radioactivity of 54GBq/ μmol, decay corrected for end of irradiation. The procedure requires about 45 min from end of cyclotron irradiation. This method should be extendable to other imidazolines. Copyright
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