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Scientific result | Chemistry
A SCBM Research Team, in collaboration with SHFJ, SIMOPRO and Karolinska Institute, has discovered a method inspired by the "click" chemistry which, from radioactive carbon dioxide, can synthesize in just five minutes radiolabeled molecules containing a cyclic urea moiety. This method has been used for the ultra-rapid isotope labeling of drugs, without modification of their structure and with an unequaled efficiency.
A robust, click chemistry inspired procedure for radiolabeling of cyclic ureas was developed. This protocol, suitable for all carbon isotopes (11C, 13C, 14C), is based on the direct functionalization of carbon dioxide: the universal building block for carbon radiolabeling. The strategy is operationally simple, reproducible in different radiochemistry centers, exhibits a remarkably wide substrate scope with short reaction times, and demonstrates superior reactivity compared to previously reported systems. With this procedure, a variety of pharmaceuticals and an unprotected peptide were labeled with high radiochemical efficiency.Read the French version.
Référence: A Del Vecchio, F Caillé, A Chevalier, O Loreau, K Horkka, C Halldin, M Schou, N Camus, P Kessler, B Kuhnast, F Taran, D Audisio Late-stage isotopic carbon labeling of pharmaceutically relevant cyclic ureas directly from CO2. Angew. Chem. Int. Ed. 2018, http://dx.doi.org/10.1002/anie.201804838
CEA is a French government-funded technological research organisation in four main areas: low-carbon energies, defense and security, information technologies and health technologies. A prominent player in the European Research Area, it is involved in setting up collaborative projects with many partners around the world.