Abstract

The synthesis of C-12 deuterated and tritiated deoxoartemisinins is described. Tritiated deoxoartemisinin which could be incubated with the protein of Plasmodium falciparum for binding mechanism study was obtained by direct reduction of the carbonyl group of artemisinin using NaBT4 and BF3×Et2O in dried THF.

Keywords: sodium borohydride, deuterium labeling, tritium labeling, malaria, artemisinin, deoxoartemisinin