A simplified protocol for the automated production of 2-[18F]fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine ([18F]nifene) on an IBA Synthera® module

IF 0.9 4区医学 Q4 BIOCHEMICAL RESEARCH METHODS

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-11-05 DOI:10.1002/jlcr.4071

Mohammed Bhuiyan, Jeffrey Souris, Anna Kucharski, Richard Freifelder, Jogeshwar Mukherjee, Chin-Tu Chen

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引用次数: 0

Abstract

The α4β2 nicotinic acetylcholine receptor (nAChR) ligand 2-[¹⁸F]fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine ([¹⁸F]nifene) has been synthesized in 10% decay-corrected radiochemical yield using the IBA Synthera® platform (IBA Cyclotron Solutions, Louvain-la-Neuve, Belgium) with an integrated fluidic processor (IFP). Boc-nitronifene served as the precursor, and 20% trifluoroacetic acid (TFA) was used to deprotect the Boc-group after radiolabeling. By omitting the solvent extraction step after radiolabeling, the process was simplified to a single step with no manual intervention. [¹⁸F]Nifene was obtained in decay-corrected radiochemical yields of 10 ± 2% (n = 20) and radiochemical purity >99%. Typical specific radioactivities of 2700–4865 mCi/μmole (100–180 GBq/μmol) were measured at the end of synthesis; total synthesis times were about 1 h 40 min.

Abstract Image

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在IBA Synthera®模块上自动生产2-[18F]氟-3-[2-（（S）-3-吡咯烷基）甲氧基]吡啶（[18F]niffee）的简化方案。

α4β2烟碱型乙酰胆碱受体（nAChR）配体2-[18F]氟-3-[2-（（S）-3-吡咯啉基）甲氧基]吡啶（[18F]niffee）已使用IBA Synthera®平台（IBA Cyclotron Solutions，Louvain la Neuve，Belgium）和集成流体处理器（IFP）以10%的衰变校正放射化学产率合成。Boc-硝基硝烟烯作为前体，在放射性标记后使用20%三氟乙酸（TFA）对Boc基团进行脱保护。通过省略放射性标记后的溶剂提取步骤，该过程简化为单一步骤，无需手动干预。[18F]Nifene的衰变校正放射化学产率为10 ± 2%（n = 20）放射化学纯度>99%。2700-4665的典型比放射性 mCi/μmol（100-180 μmol）；总合成时间约为1小时40 最小。

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来源期刊

Journal of labelled compounds & radiopharmaceuticals 医学-分析化学

CiteScore

3.30

自引率

0.00%

发文量

审稿时长

1 months

期刊介绍： The Journal of Labelled Compounds and Radiopharmaceuticals publishes all aspects of research dealing with labeled compound preparation and applications of these compounds. This includes tracer methods used in medical, pharmacological, biological, biochemical and chemical research in vitro and in vivo. The Journal of Labelled Compounds and Radiopharmaceuticals devotes particular attention to biomedical research, diagnostic and therapeutic applications of radiopharmaceuticals, covering all stages of development from basic metabolic research and technological development to preclinical and clinical studies based on physically and chemically well characterized molecular structures, coordination compounds and nano-particles.