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

doi:10.7538/tws.2014.27.01.0028

摘要/Abstract

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。

关键词: 合成, 氟-19、¹¹C, 自动化合成模块, 放射性药物

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.

Key words: synthesis, fluorine-18, carbon-11, auto-synthesis module, radiopharmaceuticals

张锦明;张晓军;刘键;陈英茂;田嘉禾. 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[J]. 同位素, 2014, 27(1): 28-34.

ZHANG Jin-ming;ZHANG Xiao-jun;LIU Jian;CHEN Ying-mao;TIAN Jia-he. Fully Automated Synthesis Carbon-11 Radiopharmaceuticals using Home Made PET-MV-2-F Module Assembled the Methyl Iodide Module[J]. Journal of Isotopes, 2014, 27(1): 28-34.

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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

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