Radiopharmaceuticals 4.: 18F-labelling with water target produced 18F. Synthesis and quality control of 18F-3-deoxy-3-fluoro-D-glucose

Using 1,2:5,6-di-O-isopropylidene-3-O-trifluoromethanesulfonyl-α-D-allofuranose as starting material, 18F-3-deoxy-3-fluoro-D-glucose (18F-3-FDG) was prepared by nucleophilic substitution of the trifluoromethanesulfonyl group by 18F-fluoride in an acetamide melt at 150 deg C followed by acidic hydrolysis. 18F was produced via the 16O(3He,p)18F reaction in a water target with high yields up to 500 mCi. After hydrolysis of the intermediate, purification by high pressure liquid chromatography and sterilization, 18F-3-FDG was obtained in a yield of 30+-5% within a total preparation time of less than one half-life of fluorine-18. (author)