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Title: Nucleophilic fluorination of aromatic compounds

Abstract

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.

Inventors:
;
Issue Date:
Research Org.:
Univ. of California, Oakland, CA (United States)
Sponsoring Org.:
USDOE
OSTI Identifier:
1127132
Patent Number(s):
8,674,101
Application Number:
13/054,458
Assignee:
The Regents of the University of California (Oakland, CA)
DOE Contract Number:  
FG02-06ER64249
Resource Type:
Patent
Country of Publication:
United States
Language:
English
Subject:
37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY

Citation Formats

Satyamurthy, Nagichettiar, and Barrio, Jorge R. Nucleophilic fluorination of aromatic compounds. United States: N. p., 2014. Web.
Satyamurthy, Nagichettiar, & Barrio, Jorge R. Nucleophilic fluorination of aromatic compounds. United States.
Satyamurthy, Nagichettiar, and Barrio, Jorge R. Tue . "Nucleophilic fluorination of aromatic compounds". United States. https://www.osti.gov/servlets/purl/1127132.
@article{osti_1127132,
title = {Nucleophilic fluorination of aromatic compounds},
author = {Satyamurthy, Nagichettiar and Barrio, Jorge R},
abstractNote = {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.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {2014},
month = {3}
}

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