Drug Development Against Parasitic Diseases: Synthesis of the Antimalarial Agent Qinghaosu and Analogs.

摘要

A stereoselective total synthesis of (+)-artemisinin has been improved from 18 steps to 13 steps with a resultant 12-fold increase in the overall yield. A new class of tricyclic analogs of artemisinin has been discovered that possesses good in vitro antimalarial activity. U.S. and foreign patents have been filed. One paper has been published and three others are in preparation.