C–H radiocyanation of bioactive molecules via sequential iodination/copper-mediated cross-coupling

We report a net C–H radiocyanation of electron-rich (hetero)aromatic substrates. This sequence is applied to a variety of substrates, including nucleobases, amino acids and LYRAGWRAFS peptide, which undergoes selective C–H radiocyanation at the tryptophan (W) residue.