7-HALO- AND 7β, 8β--METHANOTAXOLS, PHARMACEUTICAL COMPOSITION, INTERMEDIATE COMPOUNDS AND METHODS OF SYNTHESIS OF INTERMEDIATE COMPOUNDS Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of taxols of the general formula (I) where R₁ - methyl or phenyl; R₂ is H, NHC(O)H, NHC(O)-alkyl, NHC(O)-phenyl, NHC(O)O-CH₂-phenyl, NH₂, NHC(O)-1-adamantyl, NHCOO-3-tetrahydrofuranyl, NHCOO-4- -tetrahydropyranyl, NHCO-CH₂C(CH₃)₃, NHCO--C(CH₃)₃, NHCONHPh, NHCOC-(CH₂CH₃)CH₃, NHCOC--(CH₃)₂CH₂Cl, NHCOC--(CH₃)₂CH₂CH₃, phthalimido-group, NHC(O)-1-phenyl-1- -cyclopentyl, NHC(O)-1-methyl-1-cyclohexyl, NHC(S)NHC-(CH₃)₃, NHC(O)NHC-(CH₃)₃ or NHCONHPh; R₃ is H, NHCO-phenyl or NHC(O)OC-(CH₃)₃; R₄ is H, OC(O)O-CH₂CCl₃ or NHC(O)-phenyl; R₅ is H or OH; R₆ is H when R₇ means α-R₇₁ or β-R₇₂ where one of R₇₁,R₇₂ is H and other - X; X - halogen atom; R₈ - methyl; R₁₀ is H or C(O)-CH₃, or their pharmaceutically acceptable salts. Compounds of the formula (I) show antitumor activity and can be used in medicine. EFFECT: improved methods of synthesis, enhanced efficiency of compounds. 18 cl, 2 tbl