| 摘要 |
FIELD: organic chemistry and chemical technology. SUBSTANCE: invention relates to water-soluble derivatives of camptothecine of the formula (I): <EMI ID=0.108 HE=30 WI=63 TI=CHI> where n = 1 or 2; (1) R and R taken separately are hydrogen, lower alkyl, (C<SB>3-7</SB>)-cycloalkyl, (C<SB>3-7</SB>)-cycloalkyl(lower)alkyl, lower alkenyl, hydroxy(lower)alkyl, lower(alkoxy)lower alkyl; (2) R means hydrogen, lower alkyl, (C<SB>3-7</SB>)-cycloalkyl, (C<SB>3-7</SB>)-cycloalkyl(lower)alkyl, lower alkenyl, hydroxy(lower)alkyl or lower(alkoxy)lower alkyl; R means COP where P is hydrogen, lower alkyl, perhaloid-lower alkyl, (C<SB>3-7</SB>)-cycloalkyl, (C<SB>3-7</SB>)-cycloalkyl, lower alkyl, lower alkenyl, hydroxy(lower)alkyl, lower alkoxy, lower(alkoxy)lower alkyl; (3) R and R taken together with connecting nitrogen atom form saturated 3-7-atomic heterocyclic group of the formula IA: <EMI ID=0.109 HE=9 WI=9 TI=CHI> where Y means O, S, CH<SB>2</SB>, NR where R is hydrogen, lower alkyl, perhaloid-lower alkyl, aryl, aryl substituted with one or some substituents taken from the group involving lower alkyl, halogen, nitro-, amino-group, lower(alkyl)amino, perhaloid-lower alkyl, hydroxy(lower)alkyl, lower alkoxy, lower(alkoxy)lower alkyl or COR where R is hydrogen, lower alkyl, perhaloid-lower alkyl, lower alkoxy, aryl, aryl substituted with one or some substituents taken from the group involving: lower alkyl, perhaloid-lower alkyl, hydroxy(lower)-alkyl, lower(alkoxy)lower alkyl. Invention relates to also pharmaceutically acceptable salts of these compounds, their use for treatment of patients with tumors and methods of their preparing. EFFECT: improved methods of synthesis. 14 cl, 2 tbl, 4 dwgf
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