This report demonstrates electrophilic radiocyanation in (hetero)arenes, implying a new way to produce useful radiopharmaceuticals.
Radiocyanation is an attractive approach to introduce carbon-11 into radiopharmaceuticals, as nitriles and other acyl moieties. This report describes a Friedel-Crafts-type electrophilic radiocyanation of (hetero)aryltrimethylgermanes and trimethylstannanes as well as a direct C-H radiocyanation of (hetero)arenes. This approach leverages the in situ oxidation of [¹¹C]CN⁻ to [¹¹C]CNCl to enable electrophilic aromatic substitution pathways for accessing relevant ¹¹C-aryl nitrile scaffolds. This method proceeds in short reaction times with readily available, shelf-stable reagents and enables radiocyanation of diverse substrates in good radiochemical yields.
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McCarthy et al. (2026) studied this question.
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