Late-stage introduction of 18F and 11C into arenes is of importance in radiotracer development for positron emission tomography (PET). Recently developed copper-mediated methods have enabled radiolabeling of electronically diverse arenes, but the requirement for aryl precursors such as boronates, stannanes or hypervalent iodines remains a limitation. We have therefore developed Cu mediated radiofluorination and radiocyanation methods that use readily available and stable aryl halides as substrates. A broad scope of substrates is explored, including (hetero)arenes and bioactive molecules such as amino acids and peptides. Additionally, these methods are leveraged in operationally simple stepwise procedures to enable selective C-H radiolabeling of arenes.

Copper-mediated 18F and 11C radiolabeling of aryl halides

ACS Spring 2022

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