A Fluoride-derived Electrophilic Late-Stage Fluorination Reagent for PET Imaging
SCIE
SCOPUS
- Title
- A Fluoride-derived Electrophilic Late-Stage Fluorination Reagent for PET Imaging
- Authors
- Lee, E; Kamlet, AS; Powers, DC; Neumann, CN; Boursalian, GB; Furuya, T; Choi, DC; Hooker, JM; Ritter, T
- Date Issued
- 2011-11-04
- Publisher
- American Association for the Advancement of Science
- Abstract
- 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.
- Keywords
- POSITRON-EMISSION-TOMOGRAPHY; REDUCTIVE ELIMINATION; RADIOSYNTHESIS; F-18
- URI
- https://oasis.postech.ac.kr/handle/2014.oak/15187
- DOI
- 10.1126/SCIENCE.1212625
- ISSN
- 0036-8075
- Article Type
- Article
- Citation
- SCIENCE, vol. 334, no. 6056, page. 639 - 642, 2011-11-04
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- There are no files associated with this item.
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