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

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.