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

ZHAO Shu-qiang1;ZHANG Jin-ming2;ZHANG Xiao-jun2;LI Yun-gang2;LIU Jian2   

  1. 1.PET/CT Center, Shan Dong Tumor Hospital, Ji’nan 250117, China;2.Department of Nuclear Medicine, the PLA General Hospital, Beijing 100853, China
  • Online:2016-02-20 Published:2016-03-01

国产碳-11多功能模块全自动化合成11C-乙酸盐

赵书强1;张锦明2;张晓军2;李云刚2;刘健2   

  1. 1.山东省肿瘤医院 PET/CT中心,山东 济南250117;2.解放军总医院 核医学科,北京100853

Abstract:

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 unreacted 11C-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.

Key words: 11C-acetate, multifunction module, automated synthesis

摘要:

采用国产碳-11多功能合成模块,研究全自动化合成11C-乙酸盐的工艺流程。用0.1 mL 1.5 mol/L的溴化甲基镁在Loop环中与11C-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11C-CO2,以磷酸三钠中和后过无菌滤膜得11C-乙酸盐注射液。总合成时间约为10 min,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。

关键词: 11C-乙酸盐, 多功能模块, 自动化合成