国产氟多功能模块组合碘代甲烷模块合成^(11)C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

作　　者：张锦明[1] 张晓军[1] 刘键[1] 陈英茂[1] 田嘉禾[1] 

机构地区：[1]中国人民解放军总医院核医学科,北京100853

出　　处：《同位素》2014年第1期28-34,共7页Journal of Isotopes

基　　金：国家自然科学基金(81071170);北京市自然科学基金(7122162)

摘　　要：将国产11 C碘代甲烷模块和氟多功能模块联合使用,合成11 C的正电子放射性药物。由11 C碘代甲烷模块合成甲基化试剂11 CH3-Triflate,将11 CH3-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11 C放射性药物。通过以上结合,经HPLC纯化,可自动化合成11 C-Ralopride(合成效率(38.2±4.5)%,n=10)、11 C-PIB(合成效率(68.4±3.2)%,n=12)、11 C-DASB(合成效率(52.4±5.5)%,n=4)、11 C-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11 C碘代甲烷模块和氟多功能模块结合使用,可以合成多种11 C放射性药物以满足临床的需求。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 nC-CH3- Triflate was synthesized with methyl iodide module. The 11C_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 l lC_Raclopride, 11 C-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 {or clinical used.

关 键 词：合成 氟-19 11C 自动化合成模块 放射性药物 

分 类 号：TL923[核科学技术—核燃料循环与材料]