Fluoro taxols

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C - Chemistry, Metallurgy

07

D

C07D 305/14 (2006.01) A61K 31/335 (2006.01) A61K 31/38 (2006.01) C07D 407/12 (2006.01) C07D 409/12 (2006.01) C07F 7/18 (2006.01) C07F 9/655 (2006.01) C07F 9/6558 (2006.01) H01L 21/48 (2006.01) H05K 1/16 (2006.01) H05K 1/03 (2006.01) H05K 1/09 (2006.01) H05K 3/40 (2006.01)

Patent

CA 2099232

This invention relates to a fluorinated taxol ~ of formula I (see formula I) in which R1 is -COR2 in which R2 is RO- or R; R8 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; R2 is -OCOR, H, OH, -OR, -OSO2R, -OCONRR, -OCONHR, -OCOO(CH2)t R, 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. Further provided by this invention are pharmaceutical formulations and useful intermediates for the fluorinated taxols ~ of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.

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