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J Labelled Comp Radiopharm. 2013 Sep;56(11):539-43. doi: 10.1002/jlcr.3046. Epub 2013 May 3.

Synthesis of a phenolic precursor and its efficient O-[18F]fluoroethylation with purified no-carrier-added [18F]2-fluoroethyl brosylate as the labeling agent.

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  • 1Department of Radiology and Imaging Sciences, Emory University School of Medicine, Center for Systems Imaging, Wesley Woods Health Center, Atlanta, GA, USA.

Abstract

[(18)F]2-Fluoroethyl-p-toluenesulfonate also called [(18)F]2-fluoroethyl tosylate has been widely used for labeling radioligands for positron emission tomography (PET). [(18)F]2-Fluoroethyl-4-bromobenzenesulfonate, also called [(18)F]2-fluoroethyl brosylate ([(18)F]F(CH2)2OBs), was used as an alternative radiolabeling agent to prepare [(18)F]FEOHOMADAM, a fluoroethoxy derivative of HOMADAM, by O-fluoroethylating the phenolic precursor. Purified by reverse-phase HPLC, the no-carrier-added [(18)F]F(CH2)2OBs was obtained in an average radiochemical yield (RCY) of 35%. The reaction of the purified and dried [(18)F]F(CH2)2OBs with the phenolic precursor was performed by heating in DMF and successfully produced [(18)F]FEOHOMADAM, after HPLC purification, in RCY of 21%.

Copyright © 2013 John Wiley & Sons, Ltd.

KEYWORDS:

FEOHOMADAM; [18F]fluoroethyl brosylate; fluorine-18; fluoroethylation

PMID:
24285185
[PubMed - indexed for MEDLINE]
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