Synthesis of 18F-difluoromethylarenes using aryl boronic acids, ethyl bromofluoroacetate and [18F]fluoride

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Abstract

Herein, we report the radiosynthesis of 18F-difluoromethylarenes via the assembly of three components, a boron reagent, ethyl bromofluoroacetate, and cyclotron-produced non-carrier added [18F]fluoride. The two key steps are a copper-catalysed cross-coupling reaction, and a Mn-mediated 18F-fluorodecarboxylation.

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Sap, J. B. I., Wilson, T. C., Kee, C. W., Straathof, N. J. W., Ende, C. W. am, Mukherjee, P., … Gouverneur, V. (2019). Synthesis of 18F-difluoromethylarenes using aryl boronic acids, ethyl bromofluoroacetate and [18F]fluoride. Chemical Science, 10(11), 3237–3241. https://doi.org/10.1039/c8sc05096a

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