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Synfacts 2014; 10(6): 0555
DOI: 10.1055/s-0033-1341264
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Industrial Production of Artemisinin

Rezensent(en):
Philip Kocienski
Turconi J, * Griolet F, Guevel R, Oddon G, Villa R, Geatti A, Hvala M, Rossen K, Göller R, Burgard A. * Sanofi, Sisteron, Marcy L’Etoile and Neuville sur Saône, France; Sanofi-Aventis, Garessio, Italy; Sanofi-Aventis, Frankfurt am Main, Germany
Semisynthetic Artemisinin, the Chemical Path to Industrial Production.

Org. Process Res. Dev. 2014;
18: 417-422
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Publikationsverlauf

Publikationsdatum:
16. Mai 2014 (online)

 
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Key words

artemisinin - artemisinic acid - diastereoselective hydrogenation - photooxidation

Significance

Artemisinin is an antimalarial agent extracted from the leaves of Artemisia annua. The quest for a more reliable and economic supply of the drug resulted in the large-scale synthesis depicted, which is based on two key steps: (1) the diastereoselective hydrogenation of artemisinic acid (A) and (2) the photooxidation of dihydroartemisinic acid derivative D.


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Comment

A major breakthrough was the discovery of a highly efficient biosynthetic route to artemisinic acid (A) in engineered Saccharomyces cerevisiae (C. J. Paddon et al. Nature 2013, 496, 528). This commercial synthesis delivers 365 kg batches of artemisinin starting from 600 kg of A (55% overall) and is expected to produce 60 tons per annum.


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