国产氟多功能模块组合碘代甲烷模块合成11C标记放射性药物

Fully Automated Synthesis Carbon-11 Radiopharmaceuticals using Home Made PET-MV-2-F Module Assembled the Methyl Iodide Module

  • 摘要: 将国产11C碘代甲烷模块和氟多功能模块联合使用,合成11C的正电子放射性药物。由11C碘代甲烷模块合成甲基化试剂11CH3-Triflate,将11CH3-Triflate通入到含有前体的氟多功能模块第二反应管中,加热后经半制备HPLC纯化,收集产品后再经固相萃制备可供注射的11C放射性药物。通过以上结合 ,经HPLC纯化,可自动化合成11C-Ralopride(合成效率(38.2±4.5)%,n=10)、11C-PIB(合成效率(68.4±3.2)%,n=12)、11C-DASB(合成效率(52.4±5.5)%,n=4)、11C-PK11195(合成效率(45.6±7.1)%,n=8)。制备药物的放化纯度大于95%。研究表明,将国产11C碘代甲烷模块和氟多功能模块结合使用,可以合成多种11C放射性药物以满足临床的需求。

     

    Abstract: Combined the home made PET-MV-2-IT module with carbon-11 methyl iodide module, it was used for synthesis of carbon-11 radiotracers. Methylation agent 11C-CH3-Triflate was synthesized with methyl iodide module. The11C-CH3-Triflate was bubbled to the second reaction vessels in PET-MV-2-IT module, which the precursors were stored. The productions were purified by semi-HPLC and solid phase extraction (SPE) to get the final radiopharmaceuticals. There are four carbon-11 radiopharmaceuticals were synthesized with the method, which it were 11C-Raclopride,11C-PIB,11C-DASB and 11C-PK11195,and synthesis yields were (38.2±4.5)% (n=10),(68.4±3.2)% (n=12), (52.4±5.5)%(n=4)and (45.6±7.1)% (n=8)respectively. All productions radiochemical purity were over 95%. Assembled the methyl iodide module with PET-MV-2-F, which it had semi-HPLC, we can synthesize most carbon-11 radiopharmaceuticals for clinical used.

     

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