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Synthesis of 6-[18F]fluoropyridoxal and radioactivity distribution in rat at 60 min
Affiliation:1. College of Pharmacy, LanZhou university, Lanzhou 730000, PR China;2. Department of Pharmacy, Lanzhou General Hospital of PLA, Lanzhou 730050, PR China;3. Department of Pharmacy, The TCM University of Gansu Province, Lanzhou 730000, PR China;4. Department of Endocrinology, Lanzhou General Hospital of PLA, Lanzhou 730050, PR China;5. Drug Discovery, Neurim Pharmaceuticals Ltd., Tel-Aviv, Israel
Abstract:6-[18F]Fluoropyridoxal was synthesized by the flourination of a propylamine derivative of pyridoxal (pyridoxal Schiff base) with 18F-labelled acetylhypofluorite. Two different fluorinating agents, 5% F2 in N2 and acetylhypofluorite, were investigated with nonradioactive material. The evaluation of reactions in CH3CN and chloroform showed CH3CN to be the better solvent and CH3COOF to be the better fluorinating reagent. The synthesis gave a radiochemical yield of about 18% (expressed at the end of synthesis) and required 35–40 min to complete. The specific activity of the final radiopharmaceutical at the end of the synthesis was about 25.9 GBq/mmol (700 mCi/mmol).The tissue distribution of 6-fluoropyridoxal in rat at 60 min is also reported. A large concentration in liver and kidney indicates that this radiopharmaceutical could be of special interest in the imaging of liver functions. The concentration in the brain might also allow in vivo PET imaging of the 6-(fluoropyridoxal) uptake if a high efficiency PET scanner is used.
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