Journal of labelled compounds & radiopharmaceuticals vol:42 issue:2 pages:147-157
2-O-Methanesulfonyl-beta-D-mannose was reacted with kryptofix/K2CO3/[F-18]fluoride in CH3CN/THF (9:1) at 60 degrees C. Unexpectedly, a mixture of 1 alpha- and 1 beta-glucopyranosyl [F-18]fluoride (4 and 5, respectively) was obtained in 50% radiochemical yield (EOB); 2-[F-18]FDG was not detected. Modification of temperature, solvent or pH did riot result in the formation of 2-[F-18]FDG. Uptake of radioactivity in heart and brain of mice was significantly lower for 4 and 5 than for 2-[F-18]FDG, although 5 seems to pass the blood-brain barrier. Uptake in bone was more pronounced for 4 than for 5 and negligible for 2-[F-18]FDG.