Total synthesis of artemisinin, WO 2012154906 (A1) 15th nov 2012

Total synthesis of artemisinin, WO2012154906  (A1) 15th nov 2012

link at espacenet

Indiana University Research And Technology Corporation

Inventors Cook, Silas; Zhu, Chun-Yin
Application number: WO2012US37214 2012 05 10
Priority number(s): US201161484317P 2011 05 10

Oxidative synthesis; Rearrangement synthesis, The present invention provides a method for manufacturing artemisinin and its congeners from cyclohexenone as a starting material.

Systematic (IUPAC) name
1,2-benzodioxepin-10(3H)-oneArtemisinin also known as Qinghaosu (Chinese青蒿素), and its derivatives are a group of drugs that possess the most rapid action of all current drugs against Plasmodium falciparum malaria.[1] Treatments containing an artemisinin derivative (artemisinin-combination therapies, ACTs) are now standard treatment worldwide for P. falciparum malaria. The starting compound artemisinin is isolated from the plant Artemisia annua, sweet wormwood, a herb employed in Chinese traditional medicine.

Chemically, artemisinin is a sesquiterpene lactone containing an unusual peroxide bridge. This peroxide is believed to be responsible for the drug’s mechanism of action. Few other natural compounds with such a peroxide bridge are known.[2] (Ascaridole is another.)

Use of the drug by itself as a monotherapy is explicitly discouraged by the World Health Organization, as there have been signs that malarial parasites are developing resistance to the drug. Therapies that combine artemisinin with some other antimalarial drug are the preferred treatment for malaria and are both effective and well tolerated in patients. The drug is also increasingly being used in Plasmodium vivax malaria,[3] as well as being a topic of research in cancer treatment.


  1. White NJ (July 1997). “Assessment of the pharmacodynamic properties of antimalarial drugs in vivo”Antimicrob. Agents Chemother. 41 (7): 1413–22. PMC 163932PMID 9210658.
  2.  a b “Artemisinin and a new generation of antimalarial drugs”Education in Chemistry. July 2006.
  3. Douglas NM, Anstey NM, Angus BJ, Nosten F, Price RN (June 2010). “Artemisinin combination therapy for vivax malaria”.Lancet Infect Dis 10 (6): 405–16. doi:10.1016/S1473-3099(10)70079-7PMID 20510281.


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