LOOP环改良法全自动化制备11C-胆碱

为研究国产¹¹C-多功能合成模块经LOOP环法合成放射性药物［N-甲基-¹¹C］胆碱(¹¹C-Choline,¹¹C-CH)的合成方法,对碱当量、溶剂效应及前体量等影响因素进行研究,优化LOOP环法合成¹¹C-CH的合成工艺。¹¹C-CH的优化条件：前体量为60~150 uL,无碱无溶剂,室温与¹¹C-CH₃I反应。此条件下¹¹C-CH的合成效率为(72.16±2.96）%(n=19, ¹¹C-CH₃I未校正效率),产品的放化纯度均大于95%,产量为(7.59±1.54) GBq(n=19)。国产¹¹C-多功能合成模块LOOP环法合成¹¹C-CH与C18柱固相法进行比较表明,LOOP环可以多次重复利用,降低生产成本,提高合成效率,实现稳定、全自动化合成¹¹C-CH,产品满足临床需求。

Full Automated Synthesis of 11C-CH by LOOP Method

The synthesis conditions of radiopharmaceutical-［N-methyl-¹¹C］ Choline (¹¹C-Choline, ¹¹C-CH) with home-made 11C multifunction synthesis module by LOOP method were studied, which included the alkali equivalent, solvents and the amount of precursor. The optimum condition was 60-150 uL of precursor in LOOP without alkali equivalent and solvent, and at room temperature for synthesis of ¹¹C-CH. It could be got with radiochemical yield of (72.16±2.96)% (n=19, EOS of ¹¹C-CH₃I). The radiochemical purity of ¹¹C-CH was higher than 95% and the production radioactivity was (7.59±1.54) GBq(n=19). The synthesis of ¹¹C-CH by LOOP and on-column method on home-made ¹¹C-multifunction synthesis module was compared: 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 fully automatic, and the product synthesized by this process was suitable for clinical use.