Alkylation of heme by the antimalarialdrugartemisinin

Abstract

The peroxide function of artemisinin has been activated by iron(II)-heme generated in situ from iron(III)-protoporphyrin-IX and glutathione, a biologically relevant reductant. In mild conditions, this reaction produced a high yield (85%) of heme derivatives alkylated at α-, β-, and δ-meso positions by a C4-centered radical derived from artemisinin.