Synthesis of 18-2-deoxy-2-[18F]fluoro-D-glucose and 18-3-deoxy-3-[18F]fluoro-D-glucose with no-carrier-added [18F]fluoride.

Abstract

Using a distn. method for the sepn. of 18F- from aq. 18F solns. obtained after cyclotron irradn. of a water target by means of the 16O(3He, p) 18F reaction, the radiohalogen could be generated as a highly reactive species for nucleophilic substitution reactions. Thus, with the starting compds. 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-allofuranose, [18F]2-deoxy-2-fluoro-D-glucose (2-18FDG) and [18F]3-deoxy-3-fluoro-D-glucose (3-18FDG) could be synthesized with radiochem. yields of 71.6 and 85.9%, resp. Including purifn. by HPLC, the total prepn. time was 70 min, yielding the glucose derivs. in a no-carrier-added state. Specific activities were >103 Ci/mmol. [on SciFinder(R)]