期刊
SCIENCE
卷 334, 期 6056, 页码 639-642出版社
AMER ASSOC ADVANCEMENT SCIENCE
DOI: 10.1126/science.1212625
关键词
-
资金
- National Institute of General Medical Sciences [GM088237]
- National Institute of Biomedical Imaging and Bioengineering [EB013042]
- National Center for Research Resources [1S10RR017208-01A1]
- National Institute on Drug Abuse [5P30DA028800-02]
- Richard and Susan Smith Family Foundation
- Massachusetts Life Science Center
- Harvard Catalyst
- NSF [DGE0644491]
- Harvard Accelerator Fund
- Sloan Research Fellowship
- Eli Lilly and Co.
- AstraZeneca
- Camille Dreyfus
- Amgen
The unnatural isotope fluorine-18 (F-18) is used as a positron emitter in molecular imaging. Currently, many potentially useful F-18-labeled probe molecules are inaccessible for imaging because no fluorination chemistry is available to make them. The 110-minute half-life of F-18 requires rapid syntheses for which [F-18]fluoride is the preferred source of fluorine because of its practical access and suitable isotope enrichment. However, conventional [F-18]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 F-18-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.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据