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Optimization of Automated Synthesis of 2-[18F]Fluoro-2-deoxy-D-glucose Involving Base Hydrolysis

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Abstract

Synthesis of 2-[18F]fluoro-2-deoxy-D-glucose ([18F]FDG) involving base hydrolysis was optimized. Fluorine-18 was isolated from irradiated water to more than 90% by sorption of [1 8F]fluoride on QMA anion-exchange resin, which was followed by elution with a 96 : 4 (by volume) acetonitrile-water mixture containing Kryptofix 2.2.2 and potassium carbonate (molar ratio 2 : 1). This composition is the best for preparing the complex [K/K2.2.2]+ 18F- used in nucleophilic fluorinations. No additional azeotropic drying is required. Base hydrolysis under optimized conditions (40-45°C), followed by neutralization with HCl, removal of traces of the solvent, and purification of the final product on a combined SCX/Alumina N column, yielded [1 8F]FDG of high radiochemical (>99%) and chemical purity with minimal product loss. With an RB-86 robotic system (Anatech, Sweden), the synthesis time was 38 min. The procedure is used in the Institute of Human Brain, Russian Academy of Sciences for routine synthesis of FDG; the radiochemical yield of the product by the end of synthesis (EOS) is reproducibly high: 63±3% (n = 40).

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Authors and Affiliations

  1. Russian Academy of Sciences, Institute of Human Brain, St. Petersburg, Russia

    N. A. Gomzina, D. A. Vasil'ev & R. N. Krasikova

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  1. N. A. Gomzina
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  2. D. A. Vasil'ev
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  3. R. N. Krasikova
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Gomzina, N.A., Vasil'ev, D.A. & Krasikova, R.N. Optimization of Automated Synthesis of 2-[18F]Fluoro-2-deoxy-D-glucose Involving Base Hydrolysis. Radiochemistry 44, 403–409 (2002). https://doi.org/10.1023/A:1020689314452

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