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Scientific result | Chemistry

A new method for ultra-rapid isotope labeling of drugs

​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.

Published on 19 June 2018


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.

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