| 摘要 |
PURPOSE: Provided are a fluorinated taxol derivative of formula(I). Further, provided are pharmaceutical formulations and useful intermediates for the fluorinated taxols of the formula(I). A method of treating mammalian tumors using a compound of the formula(I) is also provided. CONSTITUTION: A fluorinated taxol derivative is represented by the formula(I) in which R¬1 is -COR¬z in which R¬z is RO- or R; R¬g is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, or a radical of the formula -W-R¬x in which W is a bond, C2-6 alkenediyl, or -(CH2)t-, in which t is one to six; and R¬x is naphthyl, furyl, thienyl or phenyl, and furthermore R¬x can be optionally substituted with one to three same or different C1-6 alkyl, C1-6 alkoxy, halogen or -CF3 groups; R¬2 is -OCOR, H, OH, -OR, -OSO2R, -OCONR¬oR, -OCONHR, -OCOO(CH2)tR, or -OCOOR; and R and R¬o are independently C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, C2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C1-6 alkyl, C1-6 alkoxy, halogen or -CF3 groups.
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