生物化工2024,Vol.10Issue(4) :73-77,87.

基于CFN-MPS200模块的[18F]氟-FP-CIT合成与质量分析

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

时光 赵阳 崔夫新 刘岩
生物化工2024,Vol.10Issue(4) :73-77,87.

基于CFN-MPS200模块的[18F]氟-FP-CIT合成与质量分析

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

时光 1赵阳 2崔夫新 3刘岩3
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作者信息

  • 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
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摘要

目的:合成多巴胺转运蛋白显像剂[18F]氟-氮-(3-氟丙基)-2β-甲酯基-3β-(4'-碘苯基)去甲基托烷([18F]氟-FP-CIT),并进行质量控制分析.方法:18F-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C18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:[18F]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.

Abstract

Objective:Using a fully automatic chemical synthesizer,after nucleophilic substitution,high performance liquid chromatography purification,and solid phase extraction,the dopamine transporter imaging agent[18F]fluoro-nitrogen-(3-fluoropropyl)-2′-methyl ester group-3′-(4′-iodophenylphenyldomethyltolane([18F]Fluoro-FP-CIT)is obtained,and the quality control analysis is carried out.Methods:18F-nucleophilic substitution occurs with nitrogen-(3′-methylflavinoyloxypropyl)-2β-methyl ester group-3β-(4'-iodophenyl)norepinephrine 2 β-methyl ester group-3 β-(4-iodophenyl)nortropane to obtain the product.It is separated by high performance liquid chromatography,and then purified by C18 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:[18F]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/[18F]氟-FP-CIT

Key words

dopamine transporter imaging/drug addiction/automated synthesis/[18F]Fluorine-FP-CIT

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基金项目

2022年度吉林省教育厅科学技术研究项目(JJKH20220928)

出版年

2024
生物化工

生物化工

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参考文献量7
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