气候变化领域集成服务门户(CCPortal): A fluoride-derived electrophilic late-stage fluorination reagent for PET imaging

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DOI	10.1126/science.1212625
	A fluoride-derived electrophilic late-stage fluorination reagent for PET imaging
	Lee E.; Kamlet A.S.; Powers D.C.; Neumann C.N.; Boursalian G.B.; Furuya T.; Choi D.C.; Hooker J.M.; Ritter T.
发表日期	2011
ISSN	0036-8075
起始页码	639
结束页码	642
卷号	334 期号:6056
英文摘要	The unnatural isotope fluorine-18 (18F) is used as a positron emitter in molecular imaging. Currently, many potentially useful 18F-labeled probe molecules are inaccessible for imaging because no fluorination chemistry is available to make them. The 110-minute half-life of 18F requires rapid syntheses for which [18F]fluoride is the preferred source of fluorine because of its practical access and suitable isotope enrichment. However, conventional [18F]fluoride chemistry has been limited to nucleophilic fluorination reactions. We report the development of a palladium-based electrophilic fluorination reagent derived from fluoride and its application to the synthesis of aromatic 18F-labeled molecules via late-stage fluorination. Late-stage fluorination enables the synthesis of conventionally unavailable positron emission tomography (PET) tracers for anticipated applications in pharmaceutical development as well as preclinical and clinical PET imaging.
英文关键词	boric acid; fluorine 18; organometallic compound; palladium; drug development; fluoride; half life; imaging method; molecular analysis; palladium; tomography; tracer; article; catalysis; chemical interaction; chemical reaction; chemical structure; concentration (parameters); electron transport; electrophilicity; fluorination; nucleophilicity; oxidation; positron emission tomography; priority journal; radiochemistry; radioisotope decay; room temperature; structure analysis; synthesis
语种	英语
来源期刊	Science
文献类型	期刊论文
条目标识符	http://gcip.llas.ac.cn/handle/2XKMVOVA/244485
作者单位	Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, United States; Athinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, United States; Division of Nuclear Medicine and Molecular Imaging, Department of Radiology, Massachusetts General Hospital, Boston, MA 02114, United States
推荐引用方式 GB/T 7714	Lee E.,Kamlet A.S.,Powers D.C.,et al. A fluoride-derived electrophilic late-stage fluorination reagent for PET imaging[J],2011,334(6056).
APA	Lee E..,Kamlet A.S..,Powers D.C..,Neumann C.N..,Boursalian G.B..,...&Ritter T..(2011).A fluoride-derived electrophilic late-stage fluorination reagent for PET imaging.Science,334(6056).
MLA	Lee E.,et al."A fluoride-derived electrophilic late-stage fluorination reagent for PET imaging".Science 334.6056(2011).