基于CFN-MPS200模块的[^(18)F]氟-FP-CIT合成与质量分析  

Synthesis and Quality Analysis of [~(18)F] Fluorine-FP-CIT Based on CFN-MPS200 Synthesizer

作　　者：时光[1] 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)

机构地区：[1]吉林警察学院刑事科学技术系,吉林长春130117 [2]北京霞世融科技有限公司,北京100024 [3]北京安迪科电子有限责任公司,北京100021

出　　处：《生物化工》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)。

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.

关 键 词：多巴胺转运蛋白显像 药物成瘾 自动化合成 [^(18)F]氟-FP-CIT 

分 类 号：O644.2[理学—物理化学]