No-carrier-added nucleophilic [F-18] fluorination of aromatic compounds

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.

主权项

1. A procedure for preparing an F-18 labeled aryl derivative comprising:
replacing an iodonium ylide group of a benzene derivative containing an iodonium ylide group with a no-carrier-added F-18 fluoride ion wherein the benzene derivative containing an iodonium ylide group is selected from the group consisting of: