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No-Carrier-Added Regioselective Preparation of 6-[¹⁸F]Fluoro-L-Dopa

Cyclotron Research Center, Liege University, Liege, Belgium

Correspondence: For reprints contact: Marcel Guillaume, Cyclotron Research Center, Liege University, 4000 Liège, Belgium.

ABSTRACT

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 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 >99%, and a specific activity of 1.2 Ci/µmole.