{"title":"功能良好的分子的放射性二氟甲基化。","authors":"Wei Zhang, Yinlong Li, Steven H Liang","doi":"10.62347/IIOG5660","DOIUrl":null,"url":null,"abstract":"<p><p>The strategic installation of a [<sup>18</sup>F]fluorine atom at the specific position of the lead molecule is a never-ending challenge for radiochemists in their endeavour to develop novel positron emission tomography (PET) imaging applications. Although the radiosynthesis of [<sup>18</sup>F]CF<sub>2</sub>H-containing molecules has been explored in the past decade, more methods need to be explored for various well-functionalized compounds. Recently, two novel strategies of radiodifluoromethylation were reported, namely the utilization of [<sup>18</sup>F]difluorocarbene building block and frustrated Lewis pair-mediated C-<sup>18</sup>F bond formation, respectively. These methods provide an efficient radiofunctionalization of complex CF<sub>2</sub>H-containing molecules for drug discovery and PET ligand development.</p>","PeriodicalId":7572,"journal":{"name":"American journal of nuclear medicine and molecular imaging","volume":null,"pages":null},"PeriodicalIF":2.0000,"publicationDate":"2024-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11087296/pdf/","citationCount":"0","resultStr":"{\"title\":\"Radiodifluoromethylation of well-functionalized molecules.\",\"authors\":\"Wei Zhang, Yinlong Li, Steven H Liang\",\"doi\":\"10.62347/IIOG5660\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>The strategic installation of a [<sup>18</sup>F]fluorine atom at the specific position of the lead molecule is a never-ending challenge for radiochemists in their endeavour to develop novel positron emission tomography (PET) imaging applications. Although the radiosynthesis of [<sup>18</sup>F]CF<sub>2</sub>H-containing molecules has been explored in the past decade, more methods need to be explored for various well-functionalized compounds. Recently, two novel strategies of radiodifluoromethylation were reported, namely the utilization of [<sup>18</sup>F]difluorocarbene building block and frustrated Lewis pair-mediated C-<sup>18</sup>F bond formation, respectively. These methods provide an efficient radiofunctionalization of complex CF<sub>2</sub>H-containing molecules for drug discovery and PET ligand development.</p>\",\"PeriodicalId\":7572,\"journal\":{\"name\":\"American journal of nuclear medicine and molecular imaging\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":2.0000,\"publicationDate\":\"2024-04-25\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11087296/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"American journal of nuclear medicine and molecular imaging\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.62347/IIOG5660\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/1/1 0:00:00\",\"PubModel\":\"eCollection\",\"JCR\":\"Q3\",\"JCRName\":\"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"American journal of nuclear medicine and molecular imaging","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.62347/IIOG5660","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/1/1 0:00:00","PubModel":"eCollection","JCR":"Q3","JCRName":"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING","Score":null,"Total":0}
引用次数: 0
摘要
在先导分子的特定位置战略性地安装[18F]氟原子,是放射化学家在开发新型正电子发射断层扫描(PET)成像应用过程中面临的一个永无止境的挑战。尽管在过去十年中已经探索了含[18F]CF2H分子的放射合成,但还需要探索更多的方法来合成各种功能良好的化合物。最近,有两种放射性碘氟甲基化的新策略被报道,即分别利用[18F]二氟碳结构单元和受挫路易斯对介导的 C-18F 键形成。这些方法为药物发现和 PET 配体开发提供了一种高效的含 CF2H 复杂分子放射性功能化方法。
Radiodifluoromethylation of well-functionalized molecules.
The strategic installation of a [18F]fluorine atom at the specific position of the lead molecule is a never-ending challenge for radiochemists in their endeavour to develop novel positron emission tomography (PET) imaging applications. Although the radiosynthesis of [18F]CF2H-containing molecules has been explored in the past decade, more methods need to be explored for various well-functionalized compounds. Recently, two novel strategies of radiodifluoromethylation were reported, namely the utilization of [18F]difluorocarbene building block and frustrated Lewis pair-mediated C-18F bond formation, respectively. These methods provide an efficient radiofunctionalization of complex CF2H-containing molecules for drug discovery and PET ligand development.
期刊介绍:
The scope of AJNMMI encompasses all areas of molecular imaging, including but not limited to: positron emission tomography (PET), single-photon emission computed tomography (SPECT), molecular magnetic resonance imaging, magnetic resonance spectroscopy, optical bioluminescence, optical fluorescence, targeted ultrasound, photoacoustic imaging, etc. AJNMMI welcomes original and review articles on both clinical investigation and preclinical research. Occasionally, special topic issues, short communications, editorials, and invited perspectives will also be published. Manuscripts, including figures and tables, must be original and not under consideration by another journal.