Synthesis of Qinghaosu Analogues as Potential Antiparasitic Agents. Phase 1

摘要

The synthesis of a series of Qinghaosu analogues as potential anti-parasiticagents was studied. The key precursors to three intermediates were prepared and exposed to reaction with singlet oxygen. The expected ether endoperoxide functional group, essential to the activity of the parent structure, was obtained in one instance. This product, as well as another possible endoperoxide side product, was submitted to the USAMROC for in vitro biological evaluation. Characterization of the other products obtained from the singlet oxygen reaction have provided valuable information which is expected to lead to much improved yields for a number of analogues during the Phase II study.