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Nucleophilic fluorination of aromatic compounds

United States Patent

March 18, 2014
View the Complete Patent at the US Patent & Trademark Office
Iodylbenzene derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are used as precursors in aromatic nucleophilic substitution reactions. The iodyl group (IO.sub.2) is regiospecifically substituted by nucleophilic fluoride to provide the corresponding fluoroaryl derivatives. No-carrier-added [F-18]fluoride ion derived from anhydrous [F-18](F/Kryptofix, [F-18]CsF or a quaternary ammonium fluoride (e.g., Me.sub.4NF, Et.sub.4NF, n-Bu.sub.4NF, (PhCH.sub.2).sub.4NF) exclusively substitutes the iodyl moiety in these derivatives and provides high specific activity F-18 labeled fluoroaryl analogs. Iodyl derivatives of a benzothiazole analog and 6-iodyl-L-dopa derivatives have been synthesized as precursors and have been used in the preparation of no-carrier-added [F-18]fluorobenzothiazole as well as 6-[F-18]fluoro-L-dopa.
Satyamurthy; Nagichettiar (Los Angeles, CA), Barrio; Jorge R. (Agoura Hills, CA)
The Regents of the University of California (Oakland, CA)
13/ 054,458
July 13, 2009
This invention was made with Government support under Grant No. DE-FG02-06ER64249 awarded by the US Department of Energy. The federal government may have certain rights in the invention.