Concise Synthesis of Artemisinin from a Farnesyl Diphosphate Analogue

Publication date: Available online 4 April 2017
Source:Bioorganic & Medicinal Chemistry
Author(s): Xiaoping Tang, Melodi Demiray, Thomas Wirth, Rudolf K. Allemann
Artemisinin is one of the most potent anti-malaria drugs and many often-lengthy routes have been developed for its synthesis. Amorphadiene synthase, a key enzyme in the biosynthetic pathway of artemisinin, is able to convert an oxygenated farnesyl diphosphate analogue directly to dihydroartemisinic aldehyde, which can be converted to artemisinin in only four chemical steps, resulting in an efficient synthetic route to the anti-malaria drug.

Graphical abstract

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