Industrial stereospecific synthesis of beta-artemether by using artemisinin as raw material

Abstract

The invention discloses stereospecific synthesis of beta-artemether by using artemisinin as a raw material through a one-pot method, which comprises the following steps of: in a system of alkaline solution of dichloromethane, taking sodium borohydride as a reducing agent and aluminium tert-butoxide as a catalyst, and reducing to obtain dihydroartemisinin; and separating out a water phase, adding methanol, sodium acid sulfate, aluminum perchlorate nonahydrate, nickelousperchlorate and the like serving as catalysts for methyl etherification, and reacting at room temperature for 2 hours to obtain the beta-artemether, wherein the maximum yield rate of the beta-artemether is 85 percent and the maximum total yield rate of artemether is 93.5 percent. The method has the characteristics of low cost, high yield, short time and simple and safe operation, and is completely suitable for industrial production.

Description

technical field

[0001] The invention relates to an antimalarial drug artemisinin derivative artemether, in particular to a semi-synthetic method for artemether. Background technique

[0002] According to the latest report of the World Health Organization, malaria is an infectious disease with a clear upward trend in the world except AIDS. It is a communicable disease in tropical and subtropical regions, endangering the health of two billion people; Many people were infected and about 3 million people (mostly children) died, especially in Africa has become the number one killer. For this reason, in 2004, Nature magazine published a number of reviews and prospects, discussing how to prevent and treat malaria and related research progress (Nature, 2004, 430:7002).

[0003] Artemisinin is a new effective antimalarial compound that was isolated from Artemisia annua L. on the basis of Chinese scholars' research on "Elbow Reserve Emergency Prescription" written by Han Dynasty phar...