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• Ermert, J
• Coenen, H
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• Ermert, J
• Coenen, H
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• Ermert, J
• Coenen, H

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Molecules 2011, 16(9), 7621-7626; doi:10.3390/molecules16097621

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.

Received: 11 August 2011; in revised form: 24 August 2011 / Accepted: 31 August 2011 / Published: 6 September 2011

(This article belongs to the Special Issue Fluorine Chemistry)

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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 4-[¹⁸F]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

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