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. 2022 Jul 5;58(54):7546-7549.
doi: 10.1039/d2cc01754g.

A direct fixation of CO2 for isotopic labelling of hydantoins using iodine-phosphine charge transfer complexes

John-Paul J Bow  1 , Valentina Adami  2 , Agostino Marasco  2 , Gaute Grønnevik  1 , Dean A Rivers  3 , Guiseppe Alvaro  3 , Patrick J Riss  1   4   5
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A direct fixation of CO2 for isotopic labelling of hydantoins using iodine-phosphine charge transfer complexes

John-Paul J Bow et al. Chem Commun (Camb). .

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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