FIELD: organic chemistry, pharmacy. SUBSTANCE: invention proposes 7-deoxyderivatives of taxol of the formula (I) where R1 means a group of the formula -C(O)Rz where Rz is a group of the formula RO or R and R means C1-C6--alkyl, phenyl; Rg is phenyl or 5-membered heteroaryl containing one atom of oxygen or sulfur; R2 means hydrogen atom or a group of the formula: -COOR where R means C1-C6-alkyl. Also, invention relates to derivatives of baccatine-III (II) that are intermediate compounds in synthesis of 7-deoxyderivatives of taxol of the formula (I) and particular intermediate compounds: 10-penta-fluorothioncarbonate-7-triethylsilylhydroxybaccatine-III of the formula (III), 7-[(methylthio)carbonothioylhydroxy]-10- -deacetylhydroxybaccatine-III of the formula (IV) and 7-[(methylthio)carbonothioylhydroxy] -13-triethylsilhydroxy-baccatine-III of the formula (V) using for synthesis of derivatives of baccatine-III of the formula (II). Also, invention proposes a pharmaceutical composition containing a compound of the formula (I) that shows antitumor activity and can be used for treatment of mammals with tumors. EFFECT: improved method of synthesis, enhanced effectiveness. 14 cl, 1 tbl, 42 ex
Authors
Dates
1998-11-27—Published
1993-07-30—Filed