METHODS FOR PREPARATION OF BENZOXAZOLE ANALOGUES HAVING ANTICANCER ACTIVITY, ANTIMICROBIAL ACTIVITY AND FLUORESCENT BLEACHING ACTIVITY

摘要

PURPOSE: Methods for preparation of benzoxazole analogues are provided, thereby easily preparing benzoxazole analogues which have anticancer activity, antimicrobial activity and fluorescent bleaching activity, and easily preparing a large quantity of library of benzoxazole analogues. CONSTITUTION: The method for preparation of benzoxazole analogues represented by formula (1) comprises the steps of: (1) reacting a compound of formula (2) with a compound of formula (3) in organic solvent to prepare a compound of formula (4); and (2) reacting the compound of formula (4) with acid, wherein X is nitrogen or carbon; Y is sulfur when X is nitrogen, or oxygen when X is carbon; R1 is hydrogen, nitro, C1-C3 alkyl, C1-C3 alkoxy or halogen; R2 is hydrogen, halogen, C1-C3 alkyl, phenylazo, C1-C3 alkoxy, C1-C3 alkylthio, or C1-C3 alkoxycarbonyl; the organic solvent is selected from methanol, ethanol and ether; and the acid is selected from trifluoroacetic acid, phosphate, hydrochloric acid, nitric acid and sulfuric acid.