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Radiosynthesis of a 2-substituted 4,5-dihydro-1H-[2-11C] imidazole: the I2 imidazoline receptor ligand [11C] benazoline

✍ Scribed by D. Roeda; F. Hinnen; F. Dollé

Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
105 KB
Volume
46
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Benazoline (2‐naphthalen‐2‐yl‐4,5‐dihydro‐1H‐imidazole) is a selective high‐affinity ligand for the imidazoline I~2~ receptor. This compound was labelled with carbon‐11 (T~1/2~=20.4 min) at the number two carbon atom of its 2‐imidazoline ring. Cyclotron‐produced [^11^C]carbon dioxide reacted with 2‐naphthylmagnesium bromide to give 2‐[carboxyl‐^11^C]naphthoic acid in 60% radiochemical yield. The latter was heated with a mixture of ethylenediamine and its dihydrochloride at 300°C to give [^11^C]benazoline in 16% overall yield, relative to [^11^C]carbon dioxide and with a specific radioactivity of 54 GBq/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 © 2003 John Wiley & Sons, Ltd.

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