摘要
目的:制备^(18)F-氟赤硝基咪唑(^(18)F-fluoroerythronitroimidazole,^(18)F-FETNIM),并对产品进行质量分析。方法:基于优化后的制备工艺和CFN-MPS-200合成系统,以1-(2’-硝基-1’-咪唑基)-2,3-O-异亚丙基-4-甲苯磺酰基丁烷为前体进行氟化,采用半制备高效液相色谱系统(high performance liquid chromatography,HPLC)对粗产品进行分离纯化。利用带放射性检测器的薄层色谱(thin layer chromatography,TLC)和分析型HPLC对产品进行质量分析。结果:整个合成过程所需时间约为50 min,合成产率为24%~30%(衰减校正后,n=8)。产品为无色透明溶液,p H值在7.0~7.5之间。分析型HPLC结果显示产品放射化学纯度高于97%,与19F-FETNIM标准品保留时间一致。TLC结果显示产品的放射化学纯度超过99%,且在4 h内稳定。结论:本研究所报道的^(18)F-FETNIM制备方法稳定,产率高,合成时间短,所得到的产品无溶剂,有助于^(18)F-FETNIM的临床推广应用。同时本研究也能够为其他^(18)F标记正电子药物的制备提供一些启示和参考。
Objective:To synthesize^(18)F-fluoroerythronitroimidazole(^(18)F-FETNIM),and analyze its quality.Methods:Based on optimized preparation process and CFNMPS-200 synthesis system,1-(2’-nitro-1’-imidazolyl)-2,3-O-isopropylidene-4-tosyloxybutane was used as the precursor for fluorination,and the crude product was separated and purified with semi-preparative high performance liquid chromatography(HPLC).Thin layer chromatography(TLC)and analytical HPLC with radioactivity detector were used for quality analysis of the product.Results:The entire synthesis process took about 50 minutes and the synthesis yield was 24%-30%(decay-corrected,n=8).The product was a colorless and transparent solution with a p H value ranging from 7.0 to 7.5.The analytical HPLC results showed that the radiochemical purity of the product was greater than 97%,and its retention time was consistent with19F-FETNIM,the reference standard.The TLC results showed that the radiochemical purity of product was more than 99%,and it was stable within 4 hours.Conclusion:The preparation method of ^(18)F-FETNIM reported in this study is stable and time-saving with high yield,and the product is solvent-free,and ready for clinical promotion.At the same time,this study also enlightens the preparation of other ^(18)F-labeled tracers.
作者
王潇雄
江骁
申太鹏
姚玉唐
陆皓
陈世容
张歌
李秀丽
谌佳琪
寇莹
肖定琼
赵檬
周星
杨童舒
程祝忠
Wang Xiaoxiong;Jiang Xiao;Shen Taipeng;Yao Yutang;Lu Hao;Chen Shirong;Zhang Ge;Li Xiuli;Shen Jiaqi;Kou Ying;Xiao Dingqiong;Zhao Meng;Zhou Xing;Yang Tongshu;Cheng Zhuzhong(Radiation Oncology Key Laboratory of Sichuan Province,Sichuan Cancer Hospital&Institute,Sichuan Cancer Center,School of Medicine,University of Electronic Science and Technology of China,Chengdu 610041,Sichuan,China;School of Imaging,North Sichuan Medical College,Nanchong 637000,Sichuan,China)
出处
《肿瘤预防与治疗》
2022年第4期347-353,共7页
Journal of Cancer Control And Treatment
基金
四川省科技计划项目(编号:2019YJ0574)
四川省肿瘤医院优秀青年基金(编号:YB2021029)。
