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A simple method for carbon isotopic labeling with *CO2

Aarhus University researchers, in collaboration with industry partners, introduce a safer, cost-effective method for carbon-14 labeling in pharmaceuticals using CO2. This novel approach eliminates the need for hazardous CO and streamlines drug development.

Scientists from Aarhus University have unveiled a pioneering method for incorporating carbon isotopes into bioactive molecules, a process crucial for understanding the behavior and safety of new drug candidates. Together with partners from industry, this innovative procedure was demonstrated to be effective for the radiolabeling of pharmaceuticals, while also providing a practical and cost-effective approach to carbon isotope labeling.

In a newly published scientific paper the researchers introduce a novel electrocarboxylation setup catalyzed by palladium, enabling the precise incorporation of carbon-14 into pharmaceutically relevant molecules. Unlike previous methods that relied on carbon monoxide, a hazardous gas that requires an additional CO2-to-CO reduction step, this new approach utilizes near-stoichiometric amounts of labeled carbon dioxide directly, streamlining the labeling process and minimizing waste.

The introduction of carbon isotopes into bioactive molecules provides invaluable insights into their metabolic pathways and pharmacological properties, guiding researchers in the development of safer and more effective drugs. With this new method, scientists can now conduct late-stage carbon labeling with unprecedented efficiency, facilitating the rapid synthesis of labeled compounds. Moreover, the simplicity and affordability of the electrocarboxylation setup make it accessible to researchers worldwide, promising widespread adoption by the pharmaceutical industry.

About the research

Study type:

Experimental chemistry

External funding:

The authors appreciate the financial support from the Danish National Research Foundation (grant no. DNRF118), NordForsk (grant no. 85378), the Independent Research Fund Denmark/Technology and Production Sciences, and Aarhus University. Support from the European Union’s Horizon 2020 research and innovation programme under grant agreement no. 862179 and Marie Sklodowska-Curie grant agreement no. 859910 is also gratefully acknowledged. The authors also appreciate the financial support from The Novo Nordisk Foundation CO2 Research Center (CORC). The authors are also highly thankful to CSCAA for the computing hours for the DFT study. K.H.H. additionally thanks the Research Council of Norway (no. 300769) and Sigma2 (no. nn9330k). C.S.D additionally thanks the Novo Nordisk Foundation under the grant agreement NNF23OC0081745.

Conflicts of interest:

Troels Skrydstrup is co-owner of SyTracks A/S, which commercialises COware®. The remaining authors declare no competing interests.

Link to the scientific article:

Efficient palladium-catalyzed electrocarboxylation enables late-stage carbon isotope labelling

Gabriel M. F. Batista, Ruth Ebenbauer, Craig Day, Jonas Bergare, Karoline T. Neumann, Kathrin H. Hopmann, Charles S. Elmore, Alonso Rosas-Hernández & Troels Skrydstrup

Nature Communications, 2024, 15, 2592, https://www.nature.com/articles/s41467-024-46820-9

Contact information:

Professor Troels Skrydstrup
Aarhus University
Department of Chemistry and Interdisciplinary Nanoscience Centre (iNANO)
Email: ts@chem.au.dk