Synthesis and preliminary evaluation of [18F]2-deoxy-2,2-difluoro-glucose as a potential PET imaging agent

This paper describes the synthesis and preliminary in-vivo study of a new FDG analog, 2-deoxy-2,2-[F-18]difluoro-glucose (DFDG) for use as a potential imaging agent for PET. DFDG was prepared by the reaction of F-18-acetyl hypofluorite on 3,4,6-tri-O-acetyl-2-fluoro-D-glucal followed by acid deprotection to give the final product in 27% decay corrected radiochemical yield. Biodistribution in mice showed rapid uptake in the heart (10% dose/gram) which remained relatively constant out to two hours. The brain uptake at 2 hours was 1.6% dose per gram. There was rapid clearance of activity from the blood after injection. Brain images in a Rhesus monkey showed a similar distribution when compared to FDG but with significantly more uptake in surrounding muscle.