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Journal Articles Angewandte Chemie International Edition Year : 2018

Late-stage isotopic carbon labeling of pharmaceutically relevant cyclic ureas directly from CO2

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Abstract

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.
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Dates and versions

cea-01818428 , version 1 (06-08-2018)

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Antonio del Vecchio, Fabien Caillé, Arnaud Chevalier, Olivier Loreau, Kaisa Horkka, et al.. Late-stage isotopic carbon labeling of pharmaceutically relevant cyclic ureas directly from CO2. Angewandte Chemie International Edition, 2018, ⟨10.1002/anie.201804838⟩. ⟨cea-01818428⟩
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