METHOD FOR PRODUCING BETULINIC ACID

摘要

FIELD: chemistry.SUBSTANCE: in first step of synthesis of betulinic acid (1)from betulin, the primary C-hydroxyl is protected using a vinyl group which is incorporated via selective C-O-vinylation of betulin with acetylene in a super-basic DMSO-KOH medium. Subsequent C-O-acetylation of 28-O-vinyl ester of betulin and treatment of 3?-acetoxy-28-O-vinyl ester of betulin without extracting concentrated HCl from the reaction mass yields 3?-acetoxybetulin, whose two-step oxidation into a corresponding aldehyde, then into an acid and via hydrolysis of 3?-acetoxybetulinic acid yields the desired acid (1).EFFECT: method cuts time, financial and labour costs when producing the acid and increases output.1 ex