Methods: 18F-FEA-Erlotinib was synthesized from 2-18F-fluorine azide ethane (18F-FEA), a radiochemical intermediate, through the "click chemistry" in the PET-MF-2V-IT-I synthesis module and purified by semi-preparative high performance liquid chromatography (HPLC). The stability of 18F-FEA-Erlotinib was performed in phosphate buffer saline (PBS) and fetal bovine serum (FBS). The octanol/water partition coefficient and routine quality control were tested. Results: 18F-FEA-Erlotinib was achieved within 70 min with (54±2)% radiochemical yield (decay corrected), an average specific activity over 200MBq·μmol-1, and over 99% radiochemical purity. The logP of 18F-FEA-Erlotinib was 2.36±0.01. The final injection was free of bacteria and pyrogen, and the K2.2.2 concentration was lower than 10 mg·L-1. Conclusion: 18F-FEA-Erlotinib was easy to be prepared by the "click chemistry" in an automatic synthesis system. 18F-FEA-Erlotinib has a similar lipophilicity to Erlotinib and a high metabolic stability in vitro."/> 表皮生长因子受体显像剂<sup>18</sup>F-FEA-Erlotinib的自动化合成
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核技术  2018, Vol. 41 Issue (1): 010301    DOI: 10.11889/j.0253-3219.2018.hjs.41.010301
核化学、放射化学、放射性药物和核医学 最新目录| 下期目录| 过刊浏览| 高级检索 |
黄顺1,2, 韩彦江2, 胡孔珍2, 王猛2, 孙朋辉2, 吴湖炳2, 王全师2, 赵肃清1, 郑希1
1 广东工业大学 轻工化工学院 广州 510006;
2 南方医科大学附属南方医院 核医学科 广州 510515
Automated synthesis of EGFR imaging tracer 18F-FEA-Erlotinib
HUANG Shun1,2, HAN Yanjiang2, HU Kongzhen2, WANG Meng2, SUN Penghui2, WU Hubing2, WANG Quanshi2, ZHAO Suqing1, ZHENG Xi1
1 School of Chemical Engineering and Light Industry, Guangdong University of Technology,Guangzhou 510006, China;
2 Department of Nuclear Medicine, Nanfang Hospital, Southern Medical University, Guangzhou 510515,China
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