Method and apparatus for the synthesis of dihydroartemisinin and artemisinin derivatives

Inventors: Daniel Kopetzki, David Tyler McQuade, Peter H. Seeberger, Kerry Gilmore

• Assignee: Max-Planck-Gesellschaft zur Forderung der Wissenschaften

The present invention is directed to a method for continuous production of dihydroartemisinin and also artemisinin derivatives derived from dihydroartemisinin by using artemisinin or dihydroartemisinic acid (DHAA) as starting material as well as to a continuous flow reactor for producing dihydroartemisinin as well as the artemisinin derivatives. It was found that the reduction of artemisinin to dihydroartemisinin in a continuous process requires a special kind of reactor and a special combination of reagents comprising a hydride reducing agent, at least one activator such as an inorganic activator, at least one solid base, at least one aprotic solvent and at least one C1-C5 alcohol.

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