A direct fixation of CO2 for isotopic labelling of hydantoins using iodine-phosphine charge transfer complexes
John-Paul J Bow1, Valentina Adami2, Agostino Marasco2
1Section for Organic Chemistry Department of Chemistry, University of Oslo Sem Sælands vei 26, 0371 Oslo, Norway. Patrick.riss@kjemi.uio.no.
Abstract:
Herein, we report a method for the isotopic labelling of hydantoins directly from CO2 by means of trimethyl-λ5-phosphine diiodide mediated carbonyl insertion. The method is suitable for 13C-labelling of diverse substrates and was implementated for 11C-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-1).
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