DERIVATIVES OF CAMPTOTHECINE, METHODS OF SYNTHESIS, COMPOUNDS, PHARMACEUTICAL COMPOSITION Russian patent published in 1998 - IPC

FIELD: organic chemistry and chemical technology. SUBSTANCE: invention relates to water-soluble derivatives of camptothecine of the formula (I): where n = 1 or 2; (1) R¹ and R² taken separately are hydrogen, lower alkyl, (C_3-7)-cycloalkyl, (C_3-7)-cycloalkyl(lower)alkyl, lower alkenyl, hydroxy(lower)alkyl, lower(alkoxy)lower alkyl; (2) R¹ means hydrogen, lower alkyl, (C_3-7)-cycloalkyl, (C_3-7)-cycloalkyl(lower)alkyl, lower alkenyl, hydroxy(lower)alkyl or lower(alkoxy)lower alkyl; R² means COP³ where P³ is hydrogen, lower alkyl, perhaloid-lower alkyl, (C_3-7)-cycloalkyl, (C_3-7)-cycloalkyl, lower alkyl, lower alkenyl, hydroxy(lower)alkyl, lower alkoxy, lower(alkoxy)lower alkyl; (3) R¹ and R² taken together with connecting nitrogen atom form saturated 3-7-atomic heterocyclic group of the formula IA: where Y means O, S, CH₂, NR⁴ where R⁴ 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 COR⁵ where R⁵ 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 dwg