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Copper-Mediated Radiofluorination of Arylstannanes with [18F]KF.

ABSTRACT: A copper-mediated nucleophilic radiofluorination of aryl- and vinylstannanes with [18F]KF is described. This method is fast, uses commercially available reagents, and is compatible with both electron-rich and electron-deficient arene substrates. This method has been applied to the manual synthesis of a variety of clinically relevant radiotracers including protected [18F]F-phenylalanine and [18F]F-DOPA. In addition, an automated synthesis of [18F]MPPF is demonstrated that delivers a clinically validated dose of 200 ± 20 mCi with a high specific activity of 2400 ± 900 Ci/mmol.

SUBMITTER: Makaravage KJ

PROVIDER: S-EPMC5078836 | biostudies-literature | 2016 Oct

REPOSITORIES: biostudies-literature

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Copper-Mediated Radiofluorination of Arylstannanes with [18F]KF.

Makaravage Katarina J KJ Brooks Allen F AF Mossine Andrew V AV Sanford Melanie S MS Scott Peter J H PJH

Organic letters 20161010 20

A copper-mediated nucleophilic radiofluorination of aryl- and vinylstannanes with [18F]KF is described. This method is fast, uses commercially available reagents, and is compatible with both electron-rich and electron-deficient arene substrates. This method has been applied to the manual synthesis of a variety of clinically relevant radiotracers including protected [18F]F-phenylalanine and [18F]F-DOPA. In addition, an automated synthesis of [18F]MPPF i ...[more]

PMID: 27718581

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