Reference : No-Carrier-Added Regioselective Preparation of 6-[18f]Fluoro-L-Dopa
Scientific journals : Article
Human health sciences : General & internal medicine
No-Carrier-Added Regioselective Preparation of 6-[18f]Fluoro-L-Dopa
Bozet, Claire [Centre Hospitalier Universitaire de Liège - CHU > > O.R.L. >]
Guillaume, Marcel [> > > >]
Cantineau, R. [> > > >]
Christiaens, Léon mailto [Université de Liège - ULiège > Services généraux (Faculté des sciences) > Relations académiques et scientifiques (Sciences) >]
Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine
[en] This paper describes the preparation of 6-[18F]fluoro-L-dopa by a no-carrier-added method based on the nucleophilic displacement of nitro groups of two commercially available substrates, 3,4-dimethoxy-2-nitrobenzaldehyde (nitroveratraldehyde) and 6-nitropiperonal. Fluorination was conducted in DMSO with fluorine-18 (18F) in the presence of the aminopolyether Kryptofix 222 and potassium carbonate. The condensation of the fluorinated aldehydes with phenyloxazolone and the subsequent hydrolysis with HI/P yield, after purification by HPLC, only the 6-(D, L) isomers. The racemic mixture (50/50) was resolved on an analytical scale chiral column. The method, which requires 100 min (EOB) to complete, produces 6-[18F]fluoro-L-dopa with a decay-corrected radiochemical yield of 10%, an enantiomeric purity greater than 99%, and a specific activity of 1.2 Ci/mumole.

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