Camptothecin-1-oxide derivatives and process for preparing same

Details Camptothecin-1-oxide derivatives and process for preparing same Camptothecin-1-oxide derivatives and process for preparing same

C - Chemistry, Metallurgy

07

D

260/272.5

C07D 491/22 (2006.01)

Patent

CA 1246577

Abstract New 5- and/or 7-substituted camptothecin-1-oxide derivatives possessing anti-tumor activity with slight toxicity, represented by the general formula: Image (I) wherein R stands for a hydrogen atom, an alkyl group, a hydroxyl group, an alkoxy group or an acyloxy group and R' for a hydrogen atom, an alkyl group, an aralkyl group, a hydroxymethyl group, an acyloxymethyl group or a carboxy- methyl group, with the proviso that both of R and R' should not be hydrogen atoms. These 5- and/or 7-substituted camptothecin-1-oxide derivatives are prepared by treating the corresponding 5- and/or 7-substituted camptothecins with a peroxidant as N-oxidizing reagent. - 1 -

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