原创力文档synthesis of no-carrier-added 4-[18f]fluorophenol from 4-benzyloxyphenyl-(2-thienyl)iodonium bromide合成no-carrier-added 4 -[18 f]fluorophenol 4-benzyloxyphenyl -溴化碘鎓(2-thienyl).pdfVIP
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synthesis of no-carrier-added 4-[18f]fluorophenol from 4-benzyloxyphenyl-(2-thienyl)iodonium bromide合成no-carrier-added 4 -[18 f]fluorophenol 4-benzyloxyphenyl -溴化碘鎓(2-thienyl)
Molecules 2011, 16, 7621-7626; doi:10.3390/molecule
OPEN ACCESS
molecules
ISSN 1420-3049
/journal/molecules
Communication
Synthesis of No-Carrier-Added 4-[18F]Fluorophenol from
4-Benzyloxyphenyl-(2-thienyl)iodonium Bromide
Tobias L. Ross †, Johannes Ermert * and Heinz H. Coenen
Institute of Neuroscience and Medicine, INM-5: Nuclear Chemistry, Forschungszentrum Jülich
GmbH, 52425 Jülich, Germany
† Current address: Institute of Nuclear Chemistry, Johannes Gutenberg-University Mainz,
55128 Mainz, Germany.
* Author to whom correspondence should be addressed; E-Mail: j.ermert@fz-juelich.de;
Tel.: +49-2461-613110; Fax: +49-2461-612119.
Received: 11 August 2011; in revised form: 24 August 2011 / Accepted: 31 August 2011 /
Published: 6 September 2011
Abstract: 4-[18F]Fluorophenol is a versatile synthon for the synthesis of more complex
radiopharmaceuticals bearing a 4-[18F]fluorophenoxy moiety. In order to prepare
18
4-[ F]fluorophenol in no-carrier-added (n.c.a.) form only a nucleophilic labelling method
starting from [18F]fluoride is suitable. In this paper a new, two step radiosynthesis starting
from 4-benzyloxyphenyl-(2-thienyl)iodonium bromide and [18F]fluoride with subsequent
deprotection is described, yielding n.c.a. [18F]fluorophenol in 34 to 36% radiochemical yield.
Keywords: fluorine-18; 4-[18F]fluorophenol; diaryl iodonium salts; radiosynthesis;
positron emission tomography
1. Introduction
The introduction of fluorine into organi
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