Efficient preparation of 6-[18F]fluoroveratraldehyde, the precursor of the multi-step synthesis of [18F]FDOPA
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A. Al-Labadi
Summary
As a clinically well established PET tracer, 6-[18F]fluoro-L-dopa is prepared by a multi-step synthesis if [18F]fluoride is to be used for labelling. The [18F] label is introduced in the first step, i.e. 6-[18F]fluoroveratraldehyde is prepared first with yields reported in the literature ranging between 20 and 50%. To obtain higher over-all yields in the synthesis of 6-[18F]fluoro-L-dopa, the 18F incorporation in the first step was optimised by determining the yield dependencies on solvent, concentration of the precursor, temperature and time of the reaction. Thus, the product is formed with a yield of 89 ± 2% (n = 15) when using 20 mg of 6-nitroveratraldehyde in 1 mL DMF at 140 °C within a reaction time of 10 min.
© Oldenbourg Wissenschaftsverlag, München
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