摘要
以2-羟基-3-氰甲基-5-甲基苯乙酮为原料,通过缩合、I2/DMSO/H2SO4关环氧化及酸性条件下水解合成目标产物4-溴-6-甲基-8-黄酮醋酸、3,4-亚甲二氧基-6-甲基-8-黄酮醋酸及4’-溴-6-甲基-8-氰甲基黄酮,3,4-亚甲二氧基-6-甲基-8-氰甲基黄酮,该合成方法具有反应时间短、操作简便、收率好等优点。药理实验表明,上述合成所得到的黄酮醋酸及衍生物均具有抗炎活性。
The preparation of the derivatives of substituted flavone-8-acetic acid and evaluating of their biological activities were studied. The synthesis of 4-bromo, 3, 4-methylenedioxy-6-methyl flavone-8-acetic acids and 4-bromo, 3, 4-methylenedioxy-8-cyanomethyl-6-methylflavone have been prepared by condensation, I2/DMSO/H2SO4 cyclization-oxidation and acid hydrolyzing using 3 -cynomethyl - 2 - hydroxy-5-methyl acetophenone as material. Being compared with other synthetic methods of flavone-8-acetic acids, this method is charactered by the reaction time being short, the operation process being simple and the yield being good. Moreover, anti-inflammatory activities of cyanomethylflavones and flavone - 8 -acetic acids were also investigated through their pharmacological experiments. The results show that these new substituted flavone-8- acetic acids have good anti-inflammatory activities.
出处
《黑龙江大学自然科学学报》
CAS
2004年第2期122-127,共6页
Journal of Natural Science of Heilongjiang University