New high-yield synthesis of 18F-labelled 2-deoxy-2-fluoro- D-glucose

Abstract

A new high-yield synthesis for the production of 18F-2-FDG has been developed by reacting 18F-labelled acetyl hypofluorite, prepared by in situ reaction of 18F-molecular fluorine with sodium acetate in glacial acetic acid, and tri-acetyl- D-glucal at room temperature. Molecular fluorine labelled with 18F was produced by a 20Ne(d,α) 18F reaction. 1,3,4,6-tri-O-acetyl-2-deoxy-2-fluoro- D-glucopyranose is extracted with methylene chloride, evaporated to dryness and hydrolyzed, yielding 98% radiochemically pure 18F-2-FDG. Overall radiochemical yield is about 24 ± 3%. The specific activity of the final product at the end of synthesis is about 25.38 GBq/mmol (685 mCi/mmol). The synthesis time is approximately 60 min. The synthesis proves that small medical cyclotrons are able to produce 18F-molecular fluorine at the levels needed for the synthesis of 18F-2-FDG used in functional imaging with positron emission tomography.