Mohammed Bhuiyan, Jeffrey Souris, Anna Kucharski, Richard Freifelder, Jogeshwar Mukherjee, Chin-Tu Chen
{"title":"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。","authors":"Mohammed Bhuiyan, Jeffrey Souris, Anna Kucharski, Richard Freifelder, Jogeshwar Mukherjee, Chin-Tu Chen","doi":"10.1002/jlcr.4071","DOIUrl":null,"url":null,"abstract":"<p>The α4β2 nicotinic acetylcholine receptor (nAChR) ligand 2-[<sup>18</sup>F]fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine ([<sup>18</sup>F]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. [<sup>18</sup>F]Nifene was obtained in decay-corrected radiochemical yields of 10 ± 2% (<i>n</i> = 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.</p>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 1","pages":"31-36"},"PeriodicalIF":0.9000,"publicationDate":"2023-11-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4071","citationCount":"0","resultStr":"{\"title\":\"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\",\"authors\":\"Mohammed Bhuiyan, Jeffrey Souris, Anna Kucharski, Richard Freifelder, Jogeshwar Mukherjee, Chin-Tu Chen\",\"doi\":\"10.1002/jlcr.4071\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>The α4β2 nicotinic acetylcholine receptor (nAChR) ligand 2-[<sup>18</sup>F]fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine ([<sup>18</sup>F]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. [<sup>18</sup>F]Nifene was obtained in decay-corrected radiochemical yields of 10 ± 2% (<i>n</i> = 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.</p>\",\"PeriodicalId\":16288,\"journal\":{\"name\":\"Journal of labelled compounds & radiopharmaceuticals\",\"volume\":\"67 1\",\"pages\":\"31-36\"},\"PeriodicalIF\":0.9000,\"publicationDate\":\"2023-11-05\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4071\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of labelled compounds & radiopharmaceuticals\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://onlinelibrary.wiley.com/doi/10.1002/jlcr.4071\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"BIOCHEMICAL RESEARCH METHODS\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of labelled compounds & radiopharmaceuticals","FirstCategoryId":"3","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/jlcr.4071","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"BIOCHEMICAL RESEARCH METHODS","Score":null,"Total":0}
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
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.
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.
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