Camptothecin derivatives and process for preparing same

C - Chemistry – Metallurgy – 07 – D

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260/271.3

C07D 491/147 (2006.01) C07D 491/22 (2006.01)

Patent

CA 1332414

ABSTRACT The present invention is directed to camptothecin derivatives represented by the general formula: Image (I) wherein R1 represents a lower alkyl group, R2 represents a hydrogen atom or an amino, hydroxyl, lower acylamino or lower alkoxy group, R3 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, nitro, amino, cyano or di(lower alkyl)amino group, R4 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, lower alkylthio, amino, cyano or di(lower alkyl)amino group, and R5 represents a hydrogen or halogen atom or a hydroxyl or lower alkoxy group, with the proviso that all of the R2, R3, R4 and R5 substituents should not be a hydrogen atom and also that if any one of the R2, R3, R4 and R5 is aa hydroxyl or lower alkoxy group, all of the other three substituens should not be a hydrogen atom. The invention is also directed to preparing the camptothecin derivatives of the general formula (I). Such compounds are useful as anti-tumor drugs and intermediates therefor. - 1 -

588680

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