METHOD AND APPARATUS FOR THE SYNTHESIS OF DIHYDROARTEMISININ AND ARTEMISININ DERIVATIVES
申请人:MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V.
公开号:US20160145265A1
公开(公告)日:2016-05-26
The present invention is directed to a method for continuous production of dihydroartemisinin and also artemisinin derivatives derived from dihydroartemisinin by using artemisinin or dihydroartemisinic acid (DHAA) as starting material as well as to a continuous flow reactor for producing dihydroartemisinin as well as the artemisinin derivatives. It was found that the reduction of artemisinin to dihydroartemisinin in a continuous process requires a special kind of reactor and a special combination of reagents comprising a hydride reducing agent, at least one activator such as an inorganic activator, at least one solid base, at least one aprotic solvent and at least one C
1
-C
5
alcohol.
本发明涉及一种用青蒿素或二氢青蒿酸(DHAA)作为起始材料连续生产二氢青蒿素和由二氢青蒿素衍生的青蒿素衍生物的方法,以及用于生产二氢青蒿素和青蒿素衍生物的连续流反应器。发现在连续过程中将青蒿素还原为二氢青蒿素需要一种特殊的反应器和一种特殊的试剂组合,包括一种氢化还原剂,至少一种活化剂,如无机活化剂,至少一种固体碱,至少一种无极溶剂和至少一种C1-C5醇。