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


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.

SUBMITTER: Sap JBI 

PROVIDER: S-EPMC6429591 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature

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Synthesis of <sup>18</sup>F-difluoromethylarenes using aryl boronic acids, ethyl bromofluoroacetate and [<sup>18</sup>F]fluoride.

Sap Jeroen B I JBI   Wilson Thomas C TC   Kee Choon Wee CW   Straathof Natan J W NJW   Ende Christopher W Am CWA   Mukherjee Paramita P   Zhang Lei L   Genicot Christophe C   Gouverneur Véronique V  

Chemical science 20190129 11


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