The endoperoxide sesquiterpene lactone, artemisinin, and its derivatives have become increasingly important as antimalarial drugs with impressive activity against multidrug resistant forms of Plasmodium falciparum. Artemisinin has a novel structure among known antimalarial compounds with a unique 1,2,4-trioxane ring that is essential for activity. This paper gives an overview of the chemistry of artemisinin and comments on future prospects for artemisinin and its derivatives.