Recent progress on radiofluorination using metals: strategies for generation of C–18F bonds

Abstract

C–F bond formation is an important research topic in organic synthesis because of the wide use of organofluorine compounds in various areas including pharmaceuticals, agricultural applications, and materials science. In particular, C–¹⁸F bond formation by incorporation of fluorine-18 (¹⁸F) with organic molecules is an important process to produce ¹⁸F-labeled radiotracers, which are commonly used in Positron Emission Tomography (PET). Several novel fluorination techniques have been developed due to the growing clinical demand for ¹⁸F radiotracers. Metal-mediated radiofluorination is a reliable method for the formation of C–¹⁸F bonds to produce ¹⁸F-labeled molecules compared to other methods. In this review, we summarize recent advances in the generation of C–¹⁸F bonds through metal-catalyzed radiofluorination.