国产模块LOOP环改良法合成11C-蛋氨酸

Synthesis of 11C-methionine on home-made module by the improved LOOP method

    摘要
  • 摘要:
    目的 用国产11C-多功能合成模块经LOOP环法合成放射性药物11C-蛋氨酸(11C-MET), 与C-18柱固相法合成11C-蛋氨酸进行比较。
    方法 对国产模块LOOP环法制备11C-MET的合成工艺进行探讨, 研究碱当量、溶剂效应及前体量等影响因素。
    结果 LOOP环法制备11C-MET优化后的合成条件:前体量2~3 mg溶于NaOH溶液(2 mol/L), 碱当量5.6~11.5 eq, 加入乙醇100 μl, 室温反应。此条件下11C-MET的合成效率为(65.31±4.32)%(n=24, 11C-CH3I未校正效率), 产品的放化纯度>95%, 产量为(6.61±1.38) GBq。
    结论 LOOP环法提高了11C-MET合成效率, LOOP环可以多次重复利用, 降低了生产成本, 提高了合成产量, 实现了稳定、全自动化合成11C-MET, 且产品能满足临床需求。

     

    Abstract:
    Objective The synthesis of radiopharmaceutical 11C-methionine(11C-MET) by LOOP and C-18 on-column method on home-made 11C-multifunction synthesis module was compared. Method The synthesis conditions of 11C-MET with home-made synthesis module by LOOP method was studied, which included the alkali equivalent, solvents and the amount of precursor.
    Results The optimum condition was 2-3 mg of precursor in NaOH solution(2 mol/L), alkali equivalent(5.6-11.5 eq) and ethanol(100 μL), and at room temperature for synthesis of 11C-MET. It could be got with radiochemical yield of (65.31±4.32)%(n=24, end of synthesis of 11C-CH3I). The radiochemical purity of 11C-MET was higher than 95% and the production radioactivity was (6.61±1.38) GBq(n=24).
    Conclusions By the method of LOOP, it showed that the production efficiency was increased, the output was increased and production cost of synthetic was reduced. The synthetic process was reliable and full automatic, and the product synthesized by this process was suitable for clinical use.

     

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