Series of artemisinin derivatives and process for preparation thereof

摘要

This invention relates to the synthesis of certain novel Baylis-Hillman adducts of artremisinin derived aldehyde 2-[10′β-deoxoartemisininyl]-ethanal. The capabilities of introduction of three functional groups into a molecule in one step using Baylis-Hillman reaction encouraged us to synthesize some highly functionalized derivatives of artemisinin. These highly functionalized artemisinin derivatives embodied in this document are found to be active against various cancer cell-lines.

主权项

1. A compound of general formula 3wherein R is selected from:wherein;
R′ is methyl, ethyl, i-propyl, t-butyl, or aryl; and R″ is methyl, ethyl, or i-propyl.