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1. (WO2010117435) NO-CARRIER-ADDED NUCLEOPHILIC [F-18] FLUORINATION OF AROMATIC COMPOUNDS

Pub. No.:    WO/2010/117435    International Application No.:    PCT/US2010/001012
Publication Date: Fri Oct 15 01:59:59 CEST 2010 International Filing Date: Fri Apr 02 01:59:59 CEST 2010
IPC: C07D 319/06
C07D 263/04
C07D 239/10
Applicants: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
SATYAMURTHY, Nagichettiar
BARRIO, Jorge, R.
Inventors: SATYAMURTHY, Nagichettiar
BARRIO, Jorge, R.
Title: NO-CARRIER-ADDED NUCLEOPHILIC [F-18] FLUORINATION OF AROMATIC COMPOUNDS
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.