Abstract

The effect of potassium carbonate, potassium bicarbonate and potassium fluoride on the base-mediated decomposition of 1,3,4,6- tetra-O- acetyl-2-O- trifluoromethanesulphonyl-β- d - mannopyranose ( I) during the synthesis of 2-deoxy-2- 18F-fluoro- d-glucose (2- 18FDG) was investigated using 19F-NMR. It has been shown that the addition of KF, K 2CO 3 or KHCO 3 to solutions of I in acetonitrile containing 2,2,2-crypt resulted in the elimination of trifluoromethane-sulphonate anion from I presumably by an E2 mechanism. It has also been shown that the substitution of triflate by [ 18F]fluoride is 90% complete in less than a minute when preparation of the dry [ 18F]fluoride and the subsequent nucleophilic fluorination is done using a domestic microwave oven. Using the modified method the average yield of 2- 18FDG after 30 production runs was found to be very reproducible (47 ± 4% at the end of synthesis).

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