OPRD PAPER-Streamlined Process for the Conversion of Artemisinin to Artemether

New Drug Approvals

Abstract Image
Clinton Health Access Initiative, 383 Dorchester Avenue, Suite 400, Boston, Massachusetts 02127, United States
Org. Process Res. Dev., 2012, 16 (5), pp 764–768
DOI: 10.1021/op300037e
PAPER reports an improvement to the previously published manufacturing process for artemether, a key antimalarial drug, utilizing readily available reagents, easily controlled manufacturing conditions, and a greatly simplified workup and isolation. New analytical methods and in-process controls allow for optimization of yield through control of side product formation. A 70% overall yield from the two-step conversion of naturally or synthetically derived artemisinin to pure β-artemether is obtained. This corresponds to a usage factor of 1.35 kg of artemisinin needed to produce 1 kg of β-artemether, compared to the current industry average of 1.59 kg.
Org. Process Res. Dev.2012

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