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Method and apparatus for the synthesis of dihydroartemisinin and artemisinin derivatives

MPS-Authors
/persons/resource/persons121504

Kopetzki,  Daniel
Biomolekulare Systeme, Max Planck Institute of Colloids and Interfaces, Max Planck Society;

/persons/resource/persons121636

McQuade,  D. Tyler
Biomolekulare Systeme, Max Planck Institute of Colloids and Interfaces, Max Planck Society;

/persons/resource/persons121849

Seeberger,  Peter H.
Peter H. Seeberger - Automated Systems, Biomolekulare Systeme, Max Planck Institute of Colloids and Interfaces, Max Planck Society;

/persons/resource/persons127138

Gilmore,  Kerry
Kerry Gilmore, Biomolekulare Systeme, Max Planck Institute of Colloids and Interfaces, Max Planck Society;

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2156634.pdf
(Publisher version), 968KB

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Citation

Kopetzki, D., McQuade, D. T., Seeberger, P. H., & Gilmore, K.(2015). Method and apparatus for the synthesis of dihydroartemisinin and artemisinin derivatives.


Cite as: https://hdl.handle.net/11858/00-001M-0000-0027-120E-C
Abstract
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.