METHOD FOR PREPARING CAMPTOTHECIN ESTERS Russian patent published in 2012 - IPC C07D491/22 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a method for preparing aliphatic camptothecin ester that involves a reaction of a parent compound of camptothecin with at least one alkylating agent and at least one acid, in which said parent compound of camptothecin represents 20(S)-camptothecin and said alkylating agent has formula R¹COX¹ or (R¹CO)₂O, where R¹ represents CH₃, C₂H₅; C₃H₇; C₄H₉; C₆H₁₃; C₈H₁₇ or CH=CHCH₃; X¹ represents halogenide; and where said acid represents sulphuric acid; and in which the parent compound of camptothecin represents 9-nitro-camptothecin and said alkylating agent has formula R¹COX¹ or (R¹CO)₂O, where R¹ represents C₂H₅; C₃H₇; C₄H₉; C₆H₁₃ or i-C₃H₇; X¹ represents halogenide; and where said acid represents sulphuric acid. Also, the invention refers to crystalline camptothecin-20-propionate which can find application as an antineoplastic drug.

EFFECT: method provides preparing high-yield products.

4 cl, 1 tbl, 2 ex