The reaction of dihydroartemisinin (I) with benzoyl chloride in pyridine gives the benzoate (II), which is treated with alyltrimethylsilane (III) and ZnCl2 in dichloroethane to yield the allyl-artemisinin derivative (IV). The ozonolysis of the vinyl group of (IV), followed by reduction with NaBH4, affords the 2-hydroxyethyl derivative (V). The reaction of (V) with Ms-Cl and TEA provides the mesylate (VI), which is finally condensed with 1-[3-(trifluoromethyl)phenyl]piperazine (VII) in refluxing benzene to furnish the target piperazinylethyl derivative.