国产碳-11多功能模块全自动化合成~(11)C-乙酸盐

采用国产碳-11多功能合成模块,研究全自动化合成11 C-乙酸盐的工艺流程。用0.1mL 1.5mol/L的溴化甲基镁在Loop环中与11 C-CO2反应生成中间体乙酰溴化镁,中间体由乙酸水解,再经纯化、洗脱、盐酸酸化,通入氮气除去未反应的11 C-CO2,以磷酸三钠中和后过无菌滤膜得11 C-乙酸盐注射液。总合成时间约为10min,校正放化产率为(58.5±6.7)%,放化纯度大于99%。使用气相色谱仪测得产品中有机溶剂丙酮和乙腈的残留浓度分别为(0.007±0.002)%和(0.005±0.002)%。整个合成过程实现全自动化,操作简单、灵活,合成产率和放化纯度较高,可以满足临床使用需求。

Application of the Domestic C-11 Multifunction Module in the Automated Synthesis of 11C-acetate

The domestic C-11 multifunction module was used to establish a simple, rapid, efficient synthetic technology for the fully automated synthesis of¹¹C-acetate. Methyl magnesium bromide Grignard (0.1 mL of 1.5 mol/L) was used as a precursor to react with the ¹¹C-CO₂ in the Loop ring to produce intermediate acetyl bromide. The intermediate was first hydrolysis by acetic, and then purified, elution, and hydrochloric with acid. Then, the unreacted¹¹C-CO₂ was removed by nitrogen. Finally, the product was neutralized with sodium phosphate and purified with sterile filtration membrane. The total synthesis time was about 10 minutes. The synthesis yield of ¹¹C-acetate was (58.5±6.7)% (decay corrected), and the radiochemical purity was more than 99%. The residual solvents were analyzed by gas chromatography. Analysis results indicated that concentration of the acetonitrile and acetone were (0.007±0.002)% and (0.005±0.002)%, respectively. The whole synthesis process was automatically completed, and the operation was simple and flexible with high synthesis efficiency and radiochemical purity, it was suitable for clinical performance of PET.