【药物名称】
化学结构式(Chemical Structure):
参考文献No.719544
标题:Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers with high stability and efficacy
作者:Posner, G.H.; Paik, I.-P.; Sur, S.; McRiner, A.J.; Borstnik, K.; Xie, S.; Shapiro, T.A.
来源:J Med Chem 2003,46(6),1060
合成路线图解说明:

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).

合成路线图解说明:

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.

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