Efficient Preparation of Novel Qinghaosu (Artemisinin) Derivatives: Conversion of Qinghao (Artemisinic) Acid into Deoxoqinghaosu Derivatives and 5-Carba-4-deoxoartesunic Acid1
- 1 January 1992
- journal article
- letter
- Published by Georg Thieme Verlag KG in Synlett
- Vol. 1992 (06) , 481-483
- https://doi.org/10.1055/s-1992-21384
Abstract
Qinghao acid (1) is converted via dihydroqinghao aldehyde (6) into secondary alcohols, each of which upon photooxygenation followed by treatment with copper(II) trifluoromethanesulfonate in dichloromethane-acetonitrile under oxygen in a "one-pot" operation affords ethyldeoxoqinghaosu (10), phenyldeoxoqinghaosu (11), allyldeoxoqinghaosu (12) and the β- and α-epimers 17 and 18 of 5-carba-4-deoxoartesunic acid, novel carbon analogues of artesunate.Keywords
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