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    细胞凋亡显像剂18F-ML-10前体合成及放射性标记

    Synthesis Precursor of Apoptosis Imaging Agent 18F-ML-10 and Its Radiolabing With 18F

      摘要
    • 摘要: 18F-2-(5-氟-戊基)-2-甲基丙二酸（18F-ML-10）是一个有潜力的细胞凋亡显像剂。以5-溴-1-戊醇为原料，合成了前体：5-甲基磺酰基戊基-2-甲基丙二酸二乙酯，采用国产MF-2V-IT-1模块，经亲核取代及碱水解，合成了18F-ML-10；粗产品经HPLC纯化及固相萃取，得到18F-ML-10注射液。18F-ML-10的合成效率为（25.3±4.7）%（n=16, 不校正），产品的放射化学纯度大于99%，比活度为740 PBq/mol，K2.2.2含量低于10 mg/L，有机溶剂乙腈残留量为（0.015±0.01）%（质量分数），无菌、无热原符合要求，产品满足临床研究需求。

       

      Abstract: 18F-2-(5-fluoro-pentyl)-2-methyl malonic acid(18F-ML-10) is one of the competitive candidate for apoptosis imaging with PET. ML-10 as reference and its OTs derivative (diethyl 2-methyl-2-(5-(tosyloxy)pentyl) malonate) as precursor for labeling with fluorine-18 were prepared. 18F-ML-10 was synthesized via nucleophilic substitution and base hydrolysis. The 18F-ML-10 injection was got by semi-HPLC and solid-extraction-preparation via home MF-2V-IT-1 module. The synthesis yield of 18F-ML-10 is （25.3±4.7）%（n=16, no corrected decay）, and the specific activity is 740 PBq/mol. The radiochemical purity is over 99%. The residuary acetonitrile in the injection is (0.015±0.01)%（w）. The K2.2.2 mass concentration in the injection is low than 10 mg/L. The injection is free of bacteria and pyrogen. It can be used for clinical research.

       

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