OPRD PAPER-An Improved Manufacturing Process for the Antimalaria Drug artemether

New Drug Approvals

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Novartis Pharma AG, Chemical and Analytical Development and Chemical Operations, CH-4002 Basel, Switzerland.
Org. Process Res. Dev., 2007, 11 (3), pp 336–340
DOI: 10.1021/op0602425
Artemisinin and its derivatives, such as artemether, are highly sensitive compounds, which require careful optimized production processes for their manufacture. Due to robustness issues, the manufacturing procedure of the reduction of artemisinin with potassium borohydride to dihydroartemisinin was reinvestigated. The most important factor for obtaining optimal yields is to ensure low levels of contamination of potassium hydroxide in potassium borohydride. Application of a lower reaction temperature, fast addition rate of potassium borohydride, and careful control of the pH during the quench with acid are further important parameters in guaranteeing a robust process. In the redesign of the conversion of dihydroartemisinin to artemether, the yield was increased, and dichloromethane was replaced by the ecologically…

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