Basic hydrolysis of 2-[18F]fluoro-1,3,4,6-tetra-O-acetyl-d-glucose in the preparation of 2-[18F]fluoro-2-deoxy-d-glucose

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Abstract

In contrast to the commonly used acid hydrolysis of 2-[18F]fluoro-1,3,4,6-tetra-O-acetyl-d-glucose to [18F]FDG, basic hydrolysis is a short, high-yield procedure at room temperature. In case of nucleophilic [18F]FDG synthesis the yield of removing the protective groups is quantitative. Using the electrophilic procedure the yield is about 20% higher than in acid hydrolysis. Under optimal conditions (0.3 M NaOH) the reaction is already completed within 1 min. In alkaline solutions the formed [18F]FDG is stable for more than 20 min. Additionally, the formation of 2-deoxy-2-chloro-d-glucose is avoided.

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