METHOD OF SYNTHESIS OF TAXOL DERIVATIVES Russian patent published in 1994 - IPC

FIELD: organic chemistry. SUBSTANCE: product: derivatives of taxol of formula (I), where R₁ and R₂ - H or the group of formula (III) , where n= 1-3; R₃ and R₄ is C₁-C₃-alkyl at condition that at least one of R₁ and R₂ is not hydrogen atom. Reagent 1: taxol. Reagent 2: compound of the general formula (II) , where R₃ and R₄ as indicated above. Process conditions: in the presence of condensing agent and catalyst (the presence of latter does not obligatory). At the ratio of compound (II) and taxol 1:1 2-substituted compound of formula (I) is prepared, where R₁ is a group of formula (III) and R₂ - H. At the case of synthesis of 2,7-di(substituted) of compound of formula (I), where R₁ and R₂ - a group of formula (III), is reacted with compound of formula (II). If necessary, 2,7-di(substituted) compounds of formula (I) is split at pH 7-7.4, and 7-substituted compound of formula (I) is prepared, where R₁ - H, and R₂ - a group of formula (III). Compound of formula (I) shows high antitumor activity at the dose 1.88-7.50 mg/kg and water solubility. Synthesized compounds are used in medicine. EFFECT: enhanced antitumor activity. 6 cl, 2 tbl