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Synthesis of [18F]Arenes via the Copper-Mediated [18F]Fluorination of Boronic Acids.


ABSTRACT: A copper-mediated radiofluorination of aryl- and vinylboronic acids with K(18)F is described. This method exhibits high functional group tolerance and is effective for the radiofluorination of a range of electron-deficient, -neutral, and -rich aryl-, heteroaryl-, and vinylboronic acids. This method has been applied to the synthesis of [(18)F]FPEB, a PET radiotracer for quantifying metabotropic glutamate 5 receptors.

SUBMITTER: Mossine AV 

PROVIDER: S-EPMC4672358 | biostudies-literature | 2015 Dec

REPOSITORIES: biostudies-literature

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Synthesis of [18F]Arenes via the Copper-Mediated [18F]Fluorination of Boronic Acids.

Mossine Andrew V AV   Brooks Allen F AF   Makaravage Katarina J KJ   Miller Jason M JM   Ichiishi Naoko N   Sanford Melanie S MS   Scott Peter J H PJ  

Organic letters 20151114 23


A copper-mediated radiofluorination of aryl- and vinylboronic acids with K(18)F is described. This method exhibits high functional group tolerance and is effective for the radiofluorination of a range of electron-deficient, -neutral, and -rich aryl-, heteroaryl-, and vinylboronic acids. This method has been applied to the synthesis of [(18)F]FPEB, a PET radiotracer for quantifying metabotropic glutamate 5 receptors. ...[more]

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