影响2-~(18)F-2-脱氧-β-D-葡萄糖合成效率因素再探

Restudy of the Influence Factor on Synthesis Yield of ~(18)F-FDG

  • 摘要: 以单管法合成2-18F-2-脱氧-β-D-葡萄糖(18F-FDG)为例,再一次深入分析了影响合成18F-FDG效率的因素。结果表明:生产18F-的残留水会影响18F-FDG合成效率;反应管内的亲核反应温度偏高会降低中间体的水解程度并使反应管内放射性残留量上升;除乙腈的氮气流也会使最终放射性丢失;而碱水解中间体能大大减少合成时间。通过对合成时间优化和降低体系中水含量、控制气流,18F-FDG的不校正合成效率(EOS)从59.0%提高到69.3%。

     

    Abstract: The influence factors on the yield of ~(18)F-FDG are investigated with "1-pot" system for improving the synthesis yield of ~(18)F-FDG again. The synthesis yield is affected by water which comes from delivered tube. The percent of hydrolyzation and the remain radioactivity on the reactor are affected by the temperature of nucleophilic reaction. The lost activity relates to the flow of N_2 in acetonitrile removed. The synthesis time can be shortened by basic hydrolyzing the mediates. The uncorrected synthesis yield(EOS) can be increased from 59% to 69.3% by optimizing synthesis time, removed remain water in deliver tube and QMA.

     

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