发明授权
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
- 专利标题: No-carrier-added nucleophilic [F-18] fluorination of aromatic compounds
- 专利标题(中): 芳香族化合物的无载体添加亲核[F-18]氟化
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申请号: US13263333申请日: 2010-04-01
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公开(公告)号: US08742139B2公开(公告)日: 2014-06-03
- 发明人: Nagichettiar Satyamurthy , Jorge R. Barrio
- 申请人: Nagichettiar Satyamurthy , Jorge R. Barrio
- 申请人地址: US CA Oakland
- 专利权人: The Regents of The University of California
- 当前专利权人: The Regents of The University of California
- 当前专利权人地址: US CA Oakland
- 代理机构: Koppel, Patrick, Heybl & Philpott
- 代理商 Michael J. Ram
- 国际申请: PCT/US2010/001012 WO 20100401
- 国际公布: WO2010/117435 WO 20101014
- 主分类号: C07D319/06
- IPC分类号: C07D319/06
摘要:
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.
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