Nucleophilic fluorination of aromatic compounds
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.
- Research Organization:
- Univ. of California, Oakland, CA (United States)
- Sponsoring Organization:
- USDOE
- DOE Contract Number:
- FG02-06ER64249
- Assignee:
- The Regents of the University of California (Oakland, CA)
- Patent Number(s):
- 8,674,101
- Application Number:
- 13/054,458
- OSTI ID:
- 1127132
- Country of Publication:
- United States
- Language:
- English
Fluoridation method
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patent-application | April 2007 |
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