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
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.
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.
