| Summary: | Artemisinin, a natural sesquiterpene isolated from the Artemisia annua L. plant, represents a remarkable achievement in the treatment against malaria. Since its discovery in the 1970’s, researchers readily started synthesizing this complex natural product containing an unusual endoperoxide fragment. Despite various total syntheses reported, only in the last decade the production jumped from extraction/bench scale to industrial manufacturing. In this sense, the objective of this contribution is to highlight the discovery, the most representative works towards the synthesis of artemisinin and its main derivatives used worldwide against malaria, and the path to the industrial production of these compounds.
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