11C-乙酸盐自动化合成改进工艺及PET/CT显像

Improved AutomatedSynthesis and Preliminary Animal PET/CT Imaging of 11C-acetate

  • 摘要: 采用国产碳-11胆碱/蛋氨酸自动合成模块,研究简单、快速、自动化合成11C乙酸盐(11C-AC)的工艺流程。11C-CO2与溴化甲基镁(MeMgBr)在改进的Loop环内反应生成中间体乙酰溴化镁加合物,中间体经在柱水解和SEP-PAK小柱纯化后制备11C-AC 注射液。总合成时间约8min,校正放化产率为(40.5±4.6)%,放化纯度大于95%。该改进法适于多种商用全自动化模块自动化生产11C-AC。生产的11C-AC注射液安全、有效,有望用于动物和人体PET显像研究。

     

    Abstract: To study a simple and rapidautomated synthetic technology of 11C-acetate(11C-AC), automatedsynthesis of 11C-ACwas performed by carboxylation of MeMgBr/tetrahydrofuran (THF) on apolyethylene loop with 11C-CO2,followed by hydrolysis and purification on solid-phase extraction cartridgesusing a 11C-Choline/Methioninesynthesizer made in China. A high and reproducible radiochemical yield of above40% (decay corrected) was obtained within the whole synthesis time about 8 minfrom 11C-CO2.The radiochemical purity of 11C-ACwas over 95%. The novel, simple and rapid on-column hydrolysis-purificationprocedure should adaptable to the fully automated synthesis of 11C-AC at several commercialsynthesis module. 11C-ACinjection produced by the automated procedure is safe and effective, and can beused for PET imaging of animals and humans.

     

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