THE SYNTHESIS OF 2-[F-18]FLUORO-2-DEOXY-D-GLUCOSE USING GLYCALS - A REEXAMINATION

  • 1 January 1984
    • journal article
    • research article
    • Vol. 25 (12), 1327-1334
Abstract
The reaction of [18F]F2 with D-glucal in water proceeds sufficiently mildly at room temperature to present marked regoispecificity. After hydrolysis, analysis by Fourier-transform 19F-NMR showed the product to consist of a mixture of 2-fluoro-2-deoxy-D-glucose (2-FDG) [a radiopharmaceutical] and 2-fluoro-2-deoxy-D-mannose (2-FDM) in a 2:1 ratio, respectively. The presence of the mannose isomer was revealed by extension of the 19F-NMR analyses to other literature methods for 2-FDS synthesis involving the electrophilic fluorinating agent acetyl hypofluorite. Reaction of acetyl [F-18] hypofluorite, prepared by the reaction of [F-18]F2 with solid sodium acetate trihydrate, with the appropriate glycal/solvent combination, followed by hydrolysis, led to production of [18F]2-FDG with a radiochemical purity of 95%.