Synthesis of18F-2-deoxy-2-fluoro-d-glucose and18F-3-deoxy-3-fluoro-d-glucose with no-carrier-added18F-fluoride

Using a distillation method for the separation of18F-fluoride from aqueous18F-solutions obtained after cyclotron irradiation of a water target by means of the16O(3He, p)18F reaction, the radiohalogen could be generated as a highly reactive species for nucleophilic substitution reactions. Thus, with the starting compounds 1,3,4,6-tetra-O-acetyl-2-O-trifluoromethanesulfonyl-β-D-mannopyranose and 1,2:5,6-di-O-isopropylidene-3-O-trifluoromethanesulfonyl-α-D-allofuranose18F-2-deoxy-2-fluoro-D-glucose (2-18FDG) and18F-3-deoxy-3-fluoro-D-glucose (3-18FDG) could be synthesized with radiochemical yields of 71.6% and 85.9%, respectively. Including purification by HPLC, the total preparation time was 70 min, yielding the glucose derivatives in a no-carrier-added state. Specific activities coold be calculated to be greater than 103 Ci/mmol.