Late‐Stage Isotopic Carbon Labeling of Pharmaceutically Relevant Cyclic Ureas Directly from CO(2)

A robust, click‐chemistry‐inspired procedure for radiolabeling of cyclic ureas was developed. This protocol, suitable for all carbon isotopes ((11)C, (13)C, (14)C), is based on the direct functionalization of carbon dioxide: the universal building block for carbon radiolabeling. The strategy is oper...

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Detalles Bibliográficos
Autores principales: Del Vecchio, Antonio, Caillé, Fabien, Chevalier, Arnaud, Loreau, Olivier, Horkka, Kaisa, Halldin, Christer, Schou, Magnus, Camus, Nathalie, Kessler, Pascal, Kuhnast, Bertrand, Taran, Frédéric, Audisio, Davide
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2018
Materias:
Communications
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6099343/
https://www.ncbi.nlm.nih.gov/pubmed/29862657
http://dx.doi.org/10.1002/anie.201804838
Descripción
Sumario:A robust, click‐chemistry‐inspired procedure for radiolabeling of cyclic ureas was developed. This protocol, suitable for all carbon isotopes ((11)C, (13)C, (14)C), is based on the direct functionalization of carbon dioxide: the universal building block for carbon radiolabeling. The strategy is operationally simple and reproducible in different radiochemistry centers, exhibits remarkably wide substrate scope with short reaction times, and demonstrates superior reactivity as compared to previously reported systems. With this procedure, a variety of pharmaceuticals and an unprotected peptide were labeled with high radiochemical efficiency.

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