Invention Grant
US08742139B2 No-carrier-added nucleophilic [F-18] fluorination of aromatic compounds
有权
芳香族化合物的无载体添加亲核[F-18]氟化
- Patent Title: No-carrier-added nucleophilic [F-18] fluorination of aromatic compounds
- Patent Title (中): 芳香族化合物的无载体添加亲核[F-18]氟化
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Application No.: US13263333Application Date: 2010-04-01
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Publication No.: US08742139B2Publication Date: 2014-06-03
- Inventor: Nagichettiar Satyamurthy , Jorge R. Barrio
- Applicant: Nagichettiar Satyamurthy , Jorge R. Barrio
- Applicant Address: US CA Oakland
- Assignee: The Regents of The University of California
- Current Assignee: The Regents of The University of California
- Current Assignee Address: US CA Oakland
- Agency: Koppel, Patrick, Heybl & Philpott
- Agent Michael J. Ram
- International Application: PCT/US2010/001012 WO 20100401
- International Announcement: WO2010/117435 WO 20101014
- Main IPC: C07D319/06
- IPC: C07D319/06
![No-carrier-added nucleophilic [F-18] fluorination of aromatic compounds](/abs-image/US/2014/06/03/US08742139B2/abs.jpg.150x150.jpg)
Abstract:
Phenyliodonium ylide derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are shown for use as precursors in aromatic nucleophilic substitution reactions. The iodonium ylide group is substituted by nucleophiles such as halide ions to provide the corresponding haloaryl derivatives. No-carrier-added [F-18]fluoride ion exclusively substitutes the iodonium ylide moiety in these derivatives and provides high specific activity F-18 labeled fluoro derivatives. Protected L-dopa-6-iodonium ylide derivative have been synthesized as a precursors for the preparation of no-carrier-added 6-[F-18]fluoro-L-dopa. The iodonium ylide group in this L-dopa.derivative is nucleophilically substituted by no-carrier-added [F-18]fluoride ion to provide a [F-18]fluoro intermediates which upon acid hydrolysis yielded 6-[F-18]fluoro-L-dopa.
Public/Granted literature
- US20120123120A1 No-Carrier-Added Nucleophilic [F-18] Fluorination of Aromatic Compounds Public/Granted day:2012-05-17
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