2-ARYL-2-METHYL-2,3-DIHYDROBENZOFURAN WITH ANTIOXIDANT ACTIVITY

摘要

PURPOSE: Provided is 2-aryl-2-methyl-2,3-dihydrobenzofuran with antioxidant activity which is useful for the prevention and treatment of various diseases associated with active oxygen species. CONSTITUTION: The 2-aryl-2-methyl-2,3-dihydrobenzofuran with antioxidant activity represented by formula(1) and its pharmaceutically acceptable salts are provided, wherein R' is hydrogen, acetyl, or t-butyldimethylsilyl; R is NO2, NH2, COOR1, CONR2R3 or NHC(Z)R4; R1 is hydrogen, C1 to C8 alkyl, C3 to C10 alkenyl, C3 to C6 cycloalkyl, phenyl or pyrimidine; R2 and R3 are independently C1 to C8 alkyl, phenyl, or pyridine; R4 is C1 to C8 alkyl, C3 to C10 alkenyl, phenyl, pyridine, C1 to C6 alkylamine, aniline, or aminopyridine; and Z is oxygen or sulfur. Its preparing method comprises the steps of: alkylation of a compound of formula(2) with a compound of formula(3) to form a compound of formula(4); Claisen reaction of the compound of formula(4) to form a compound of formula(5); and cyclization of the compound of formula(5) to prepare a compound of formula(1).