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See detailNo-Carrier-Added Regioselective Preparation of 6-[18f]Fluoro-L-Dopa
Bozet, Claire ULg; Guillaume, Marcel; Cantineau, R. et al

in Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine (1990), 31(7), 1247-51

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 ... [more ▼]

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. [less ▲]

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