• 放射性药物与标记化合物专辑 •

基于国产氟多功能合成模块的18F-FMISO自动合成工艺验证

1. 首都医科大学宣武医院，北京100053
• 出版日期:2017-02-20 发布日期:2017-03-06

Technology Verification for Automated Synthesis Process of 18F-FMISO Based on Domestic Fluorine Multifunctional Module

YU Qian;LIU Ting-ting;LIANG Zhi-gang;CHEN Shu-an;PENG Cheng

1. Xuanwu Hospital of the Capital University of Medical Sciences, Beijing 100053, China
• Online:2017-02-20 Published:2017-03-06

Abstract:

1-H-1-(3-［18F］fluoro-2-hydroxypropyl)-2-nitroimidazole(18F-FMISO) is a special tumor hypoxia imaging agent for PET. Its PET/CT imaging has an important guiding significance on planning cancer radiotherapy target volume. 18F-FMISO was synthesized on domestic fluorine multifunctional automated synthesis apparatus. By  using 1-(2′-nitro-1′-imidazolyl)-2-O-tetrahydropyranyl-3-O-toluenesulphonyl-propanediol as the precursor, 18F-FMISO was obtained via two-step reactions, including the nucleophilic fluoration of the precursor and the acidic hydrolysis of the intermediate. To verify the feasibility, reliability and stability of the automated synthesis process, three continuous batches of 18F-FMISO were produced with optimized preparation process. The key parameters in the pilot production and the quality standard of the product were verified. The procedure could be completed within 40 minutes. The radiochemical yield and specific activity were higher than 45% (no decay corrected, n=5) and 3.7×1010 Bq/mmol. The radiochemical purity was more than 95% after three half-life, indicating its good stability. The automated synthesis process of 18F-FMISO is feasible. All the indicators for each batch of 18F-FMISO meet the quality standard and the requirements of clinical PET imaging.