F. Vos, G. Slegers
Jul 1, 1994
Citations
0
Influential Citations
7
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
A procedure for the synthesis of 4-(4-[11C]methoxyphenyl) -(5-fluoro-2-hydroxyphenyl)-methylene-aminobutyric acid has been developed. The production entailed a O-methylation of 5-fluoro-2-hydroxy-4′-hydroxybenzophenone with cyclotron produced [11C]iodomethane in the presence of alkali and a subsequent Schiff reaction of 5-fluoro-2-hydroxy-4′-(11C]methoxybenzophenone with γ-aminobutyric acid. 5-Fluoro-2-hydroxy-4′-hydroxybenzophenone was obtained by a demethylation of the 4′-methoxyderivative with boron tribromide. Subsequent purification by HPLC and sterilisation by filtration gave 740 MBq (20 mCi) of an injectable solution. The radiochemical yield (decaycorrected) from [11C]iodomethane achieved 27%. The specific activity was 3.7 GBq/μmol (100 mCi/μmol) at the end of the radiosynthesis (45 min from EOB). The preparations have been demonstrated to be chemically and radiochemically pure by HPLC and TLC.