Dihydroartemisinin (II) was prepared by NaBH4 reduction of artemisinin (I). Condensation of (II) with 2-bromoethanol (A) in the presence of boron trifluoride etherate yielded the 10beta-bromoethyl acetal (III). Finally, reaction of (III) with dimethylamine in DMF provided the desired amine, which was finally converted to the oxalate salt.