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A continuous-flow process for the synthesis of artemisinin
Daniel Kopetzki1, François Lévesque, Peter H Seeberger
1Department for Biomolecular Systems, Max Planck Institute of Colloids and Interfaces, 14424 Potsdam, Germany.
Chemistry (Weinheim an Der Bergstrasse, Germany)
|March 23, 2013
Summary
Semisynthesis of the antimalarial drug artemisinin from plant waste increases production. A new continuous-flow process efficiently converts dihydroartemisinic acid into artemisinin, improving drug availability.
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
- Chemical Engineering
Background:
- Artemisinin is a crucial antimalarial drug, but natural sourcing from sweet wormwood is insufficient for global demand.
- Supply shortages lead to high drug prices and the proliferation of counterfeit antimalarials, particularly in Africa.
- Semisynthesis from precursors like dihydroartemisinic acid (DHAA) offers a viable alternative to boost artemisinin production.
Purpose of the Study:
- To develop an efficient, scalable photochemical process for artemisinin semisynthesis from DHAA.
- To optimize the continuous-flow process for high yield and short residence times.
- To establish a method for recovering DHAA from waste streams for sustainable production.
Main Methods:
- A one-pot photochemical continuous-flow reactor was designed and implemented for DHAA conversion.
- Process parameters were carefully optimized to maximize artemisinin yield.
- A novel extraction method was developed to isolate DHAA from discarded mother liquors.
Main Results:
- The continuous-flow process achieved a 65% yield of artemisinin from DHAA.
- The optimized process demonstrated short residence times, suitable for large-scale production.
- An effective method for recovering DHAA from waste was successfully developed.
Conclusions:
- The developed photochemical continuous-flow process provides an effective route for artemisinin semisynthesis.
- This method can significantly supplement the limited natural supply of artemisinin.
- The process contributes to ensuring a more reliable and accessible supply of essential antimalarial medication.
