The synthesis of 4-(4-([11C]methoxyphenyl) -(5-fluoro-2-hydro-xyphenyl)-methylene-aminobutyric acid, as a potential radioli-gand for the gaba receptor in the brain
✍ Scribed by Filip De Vos; Guido Slegers
- Publisher
- John Wiley and Sons
- Year
- 1994
- Tongue
- French
- Weight
- 485 KB
- Volume
- 34
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
A procedure for the synthesis of 4‐(4‐[^11^C]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 [^11^C]iodomethane in the presence of alkali and a subsequent Schiff reaction of 5‐fluoro‐2‐hydroxy‐4′‐(^11^C]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 [^11^C]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.