Basic hydrolysis of 2-[F-18]fluoro-1,3,4,6-tetra-O-acetyl-D-glucose in the preparation of 2-[F-18]fluoro-2-deoxy-D-glucose
Basic hydrolysis of 2-[F-18]fluoro-1,3,4,6-tetra-O-acetyl-D-glucose in the preparation of 2-[F-18]fluoro-2-deoxy-D-glucose
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DOI：
10.1016/0969-8043(95)00258-8
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发表时间：
1996-01-01
影响因子：
1.6
通讯作者：
Johannsen, B
中科院分区：
文献类型：
--
作者：
Fuchtner, F;Steinbach, J;Johannsen, B
与通常使用的酸解2-[F-18]fluoro-1，3，4，6-tetra-O-acetyl-D-glucose生成[F-18]FDG不同，碱性水解法在室温下是一个短的、高产量的过程。在亲核的[F-18]FDG合成的情况下，去除保护基团的产率是定量的。用亲电法比用酸水解法的产率高约20%。在最佳反应条件下(0.3M氢氧化钠)，反应在1分钟内完成。在碱性溶液中，形成的[F-18]FDG稳定20min以上。此外，还避免了2-脱氧-2-氯-D-葡萄糖的形成。
In contrast to the commonly used acid hydrolysis of 2-[F-18]fluoro-1,3,4,6-tetra-O-acetyl-D-glucose to [F-18]FDG, basic hydrolysis is a short, high-yield procedure at room temperature. In case of nucleophilic [F-18]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 [F-18]FDG is stable for more than 20 min. Additionally, the formation of 2-deoxy-2-chloro-D-glucose is avoided.