摘要
目的:合成多巴胺转运蛋白显像剂[^(18)F]氟-氮-(3-氟丙基)-2β-甲酯基-3β-(4'-碘苯基)去甲基托烷([^(18)F]氟-FP-CIT),并进行质量控制分析。方法:^(18)F^(-)与氮-(3'-甲基黄酰氧基丙基)-2β-甲酯基-3β-(4'-碘苯基)去甲托烷2β-甲酯基-3β-(4-碘苯基)降托烷发生亲核取代以获得产品。采用高效液相色谱进行分离,再以C_(18)小柱进行纯化,得到成品。结果:不校正产率(EOS)≥15%(n=8),合成时间<60 min,产品的放化纯度>98%。结论:[^(18)F]氟-FP-CIT可以用CFN-MPS200多功能合成模块全自动稳定合成,并有较高的工艺稳定性和产率,避免了工作人员被辐照的风险,产品符合GMP要求,满足临床和动物实验研究。
Objective:Using a fully automatic chemical synthesizer,after nucleophilic substitution,high performance liquid chromatography purification,and solid phase extraction,the dopamine transporter imaging agent[^(18)F]fluoronitrogen-(3-fluoropropyl)-2'-methyl ester group-3'-(4'-iodophenylphenyldomethyltolane([^(18)F]Fluoro-FP-CIT) is obtained,and the quality control analysis is carried out.Methods:^(18)F~-nucleophilic substitution occurs with nitrogen-(3'-methylflavinoyloxypropyl)-2β-methyl ester group-3β-(4'-iodophenyl) norepinephrine 2 β-methyl ester group-3β-(4-iodophenyl)nortropane to obtain the product.It is separated by high performance liquid chromatography,and then purified by C_(18) column to obtain the finished product.Results:The uncorrected yield(EOS) is higher than 15%(n=8),the synthesis time is less than 60 min,and the exothermic purity of the product is higher than 98%.Conclusion:[^(18)F]Fluorine-FP-CIT can be fully automatically and stably synthesized with CFN-MPS200 multifunctional syntheszer,and has high process stability and yield,avoiding the risk of staff being irradiated.The products meet GMP requirements and meet clinical and animal experimental research.
作者
时光
赵阳
崔夫新
刘岩
SHI Guang;ZHAO Yang;CUI Fuxin;LIU Yan(Department of Forensic Science,Jilin Police College,Changchun 130117,China;Beijing Xia Shi Rong Technology Co.,Ltd.,Beijing 100024,China;Beijing Advance Medical Systems Limited Co.,Ltd.,Beijing 100021,China)
出处
《生物化工》
CAS
2024年第4期73-77,87,共6页
Biological Chemical Engineering
基金
2022年度吉林省教育厅科学技术研究项目(JJKH20220928)。
