TRIPHENYLPHOSPHONIUM SALTS OF LUPANE TRITERPERNOIDS, METHOD FOR PRODUCING AND USING AS ANTICANCER AGENTS Russian patent published in 2015 - IPC A61K31/66 C07F9/54 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to betulinic acid derivatives, producing them and using for cancer. For producing derivatives of formulas

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1.R¹=OAc; R²=H; R³=Me; X=Br 2. R¹=H; R²= OAc; R³=Me; X=Br 3. R¹=OH; R²= OAc; R³=Me; X=Br 4. R¹=H; R²= OH; R³=Me; X=I 5. R¹=OAc; R²=H; R³=H; X=Br 6. R¹=OAc; R²=H; R³=Bn; X=I betulin is transformed into betulonic acid, then into dihydrobetulonic acid and respective dihydrobetulonates to be acetylated; the produced compounds are hydroborated and oxidised, then transformed into respective halogen derivatives; that is followed by hydrogenolysis and triphenylphosphine reaction to produce the derivatives of the above formulas. Cytotoxic activity of all the derivatives exceeds anticancer activity of betulinic acid substantially.

EFFECT: there are presented new effective anticancer agents.

6 cl, 1 dwg, 3 tbl, 11 ex