新产品编号:2447863

Chemical Name: Succinic acid 3,4-bis[(3R,5aS,6R,8aS,9R,10R,12R,12aR)-3,6,9-trimethylperhydro-3,12-epoxy[1,2]dioxepino[4,3-i]-2-benzopyran-10-ylmethyl]isobutyl monoester
项目整合开发状态: Preclinical
项目研究机构: Johns Hopkins University (Originator)
合成路线:Reduction of artemisinin (I) with DIBAL,followed by acetylation of the resultant lactol (II) with Ac2O/DMAP leads to dihydroartemisinin acetate (III).Treatment of the allylic dichloride (IV) with trimethylsilyllithium provides the bis-silane derivative (V).Then,coupling of dihydroartemisinin acetate (III) with bis-silane (V) in the presence of SnCl4 gives rise to the artemisinin dimer (VI).

合成路线:Hydroboration of the double bond of (VI),followed by quenching with NaBO3 yields the primary alcohol (VII).This is then acylated by succinic anhydride (VIII) in the presence of DMAP to provide the target succinate ester.