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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. [ABSTRACT FROM AUTHOR]

A practical, rapid, and highly regioselectiveCu-catalyzed radiofluorinationof (mesityl)(aryl)iodonium salts is described. This protocol utilizes[18F]KF to access 18F-labeled electron-rich,-neutral, and -deficient aryl fluorides under a single set of mildconditions. This methodology is applied to the synthesis of protectedversions of two important radiotracers: 4-[18F]fluorophenylalanineand 6-[18F]fluoroDOPA. [ABSTRACT FROM AUTHOR]