WATER-SOLUBLE POLYMER DERIVATIVES OF TRITERPENOIDS AND A METHOD FOR PREPARATION THEREOF Russian patent published in 2005 - IPC

FIELD: organic synthesis.

SUBSTANCE: invention provides novel triterpenoid derivatives having general formula:

(I), wherein, as polymer carrier, are used water-soluble copolymers of N-vinylpyrrolidone with α,β-(methyl)acrylic acid alkyl esters and quaternary ammonium salts thereof having general formula: (II), in which formulas A represents triterpenoid residue belonging to series of acids: betulinic {1}, betulonic {2}, glycyrrhetinic {3}, glycyrrhisic {4}, ursolic {5}, ursonic {6}, oleanolic {7}, oleanonic {8}, meristothropic {9}, diketomeristothropic {10}, macedonic {11}, diketomacedonic {12},equinocystic {13}, or mixture of above-indicated carboxyl-containing triterpenoids, where R₁ and R₂ are hydrogen or methyl; R₃ methyl or ethyl; R₄ is C₆-C₁₆-alkyl; Hal is iodine, bromine, or chlorine atom; k = 65-95 mol %; l = 0.1-34 mol %; n = 0.5-5.4 mol %; molecular weight is equal to (7-100)·10³. Polymer derivatives of above-defined triterpenoids are prepared by reaction of terpolymer II, wherein k = 65-95 mol %; l = 0.1-34 mol %; x = 1.0-34.9 mol %; R₁-R₄, Hal and molecular weight as above. Reaction is carried out in organic solvent at concentration of terpolymer 1 to 30%, concentration of triterpenoid 0.05 to 3.4%, and molar ratio of motif containing quaternary nitrogen to triterpenoid between 1 and 10. Products are isolated by removing solvent.

EFFECT: expanded synthetic possibilities.