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Palladium-Catalyzed Regioselective Allylic Oxidation of Amorphadiene, a Precursor of Artemisinin. 2021
Andrea Zanetti, and
Geoffrey Schwertz, and
Marllon Nascimento de Oliveira, and
Mario Andrés Gomez Fernandez, and
Zacharias Amara, and
Janine Cossy
Molecular, Macromolecular Chemistry and Materials (C3M), ESPCI Paris/CNRS/PSL Research University, Paris 75005 Cedex 5, France.
A regioselective Pd-catalyzed allylic oxidation of amorphadiene, a key precursor to the antimalarial drug artemisinin, is described. Amorphadiene can be obtained in high yields by fermentation, but it is currently treated as a waste in the industrial semisynthetic artemisinin process. The catalytic step described here is a substitute for the P450 enzymes involved in the artemisinin biosynthesis and opens up new opportunities to supplement a critical step in the current semisynthetic route and increase the potential of the fermentation process.
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