DERIVATIVES OF TAXANE FUNCTIONED BY POSITION 14 AND METHOD FOR THEIR PREPARING Russian patent published in 2008 - IPC C07D305/14 

FIELD: organic chemistry of natural compounds, medicine.

SUBSTANCE: invention relates to novel derivatives of taxane functioned by position 14 of the formula (III): wherein X represents -N₃, -NH₂, -NH-R₃, =CH-R₈ or -O-R₃ when R₆ is distinct from phenyl; R₂ represents hydrogen atom or acyl; R₃ represents (C₁-C₄)-alkoxycarbonyl or taken in common with R₄ it forms carbonyl, thiocarbonyl, -SO, -SO₂ group; R₄ represents hydrogen atom or taken in common with R₃ or R₈ it forms groups indicated in corresponding determinations for R₃ and R₈; R₅ represents hydrogen atom or alcohol-protective group; R represents aryl, substituted aryl under condition that it differs from phenyl when X means -O-R₃; R₈ represents hydrogen atom, (C₁-C)-alkyl, (C₁-C₄)-alkoxycarbonyl or taken in common with R₄ it forms carbonyl group; R₉ represents acyl group, such as (C₂-C₆)-aliphatic acyl group or hydroxyaminoacyl group, such as β-isobutylisoserine residue or phenylisoserine. Also, invention relates to a method for synthesis of these compounds, intermediate compounds and methods for their synthesis. Synthesized compounds possess the improved anti-tumor properties.

EFFECT: improved method of synthesis, valuable medicinal properties of compounds.

8 cl, 45 ex