Herein, we report a method for the isotopic labelling of hydantoins directly from CO by means of trimethyl-λ-phosphine diiodide mediated carbonyl insertion. The method is suitable for C-labelling of diverse substrates and was implementated for C-labelling in PET-imaging facilities for the synthesis of radiotracers. Isolated yields of 90% and radiochemical yields of 89% were achieved for hydantoin containing drug candidates in formulation within 30 min with high molar activity (>400 MBq nmol).
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