| 摘要 |
FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of taxols of the general formula (I) <EMI ID=0.288 HE=42 WI=75 TI=CHI> where R<SB>1</SB> - methyl or phenyl; R<SB>2</SB> is H, NHC(O)H, NHC(O)-alkyl, NHC(O)-phenyl, NHC(O)O-CH<SB>2</SB>-phenyl, NH<SB>2</SB>, NHC(O)-1-adamantyl, NHCOO-3-tetrahydrofuranyl, NHCOO-4- -tetrahydropyranyl, NHCO-CH<SB>2</SB>C(CH<SB>3</SB>)<SB>3</SB>, NHCO--C(CH<SB>3</SB>)<SB>3</SB>, NHCONHPh, NHCOC-(CH<SB>2</SB>CH<SB>3</SB>)CH<SB>3</SB>, NHCOC--(CH<SB>3</SB>)<SB>2</SB>CH<SB>2</SB>Cl, NHCOC--(CH<SB>3</SB>)<SB>2</SB>CH<SB>2</SB>CH<SB>3</SB>, phthalimido-group, NHC(O)-1-phenyl-1- -cyclopentyl, NHC(O)-1-methyl-1-cyclohexyl, NHC(S)NHC-(CH<SB>3</SB>)<SB>3</SB>, NHC(O)NHC-(CH<SB>3</SB>)<SB>3</SB> or NHCONHPh; R<SB>3</SB> is H, NHCO-phenyl or NHC(O)OC-(CH<SB>3</SB>)<SB>3</SB>; R<SB>4</SB> is H, OC(O)O-CH<SB>2</SB>CCl<SB>3</SB> or NHC(O)-phenyl; R<SB>5</SB> is H or OH; R<SB>6</SB> is H when R<SB>7</SB> means alpha-R<SB>71</SB> or beta-R<SB>72</SB> where one of R<SB>71</SB>,R<SB>72</SB> is H and other - X; X - halogen atom; R<SB>8</SB> - methyl; R<SB>10</SB> is H or C(O)-CH<SB>3</SB>, 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
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