Successful scale-up studies on a key intermediate for antimalaria drugs

In a successful collaboration, the team of Prof. Marti from ChemTech and of Prof. Trombini from the University of Bologna has developed and successfully scaled up to multigram scale the key step in the synthesis of a novel antimalarial drug.

The unique endoperoxide structure was synthesized in a radical [2 + 2 + 2] annulation with pure oxygen. Elemental oxygen is a sustainable reagent but unfortunately has major drawbacks in its safely application in the synthesis laboratory, as it can potentially make dangerous explosive mixtures. As part of his Master's thesis in the laboratories of the ChemTech Institute, Davide Lardani has extensively studied and optimized this reaction first at the g-scale and then to perform a safe scale-up at the multigram scale. This work has just been published in the leading journal of process chemistry, Organic Process Research & Development.

These results allow a safe production of a key intermediate for new antimalarial drugs, which can now be further investigated in clinical studies.

To read the entire paper: https://pubs.acs.org/doi/10.1021/acs.oprd.1c00309?ref=PDF