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以藜芦醛(Ⅰ)为起始原料,经过溴代、还原、傅克烷基化、脱甲基4步反应,合成了化合物4,5-二-(2-溴-4,5-二羟基苯甲基)-1,2-二苯酚(Ⅵ),总产率为53.5%。采用1HNMR、13CNMR、HREIMS等进行了结构表征。通过比色法对化合物Ⅵ及中间产物4,5-二-(2-溴-4,5-二甲氧基苯甲基)-1,2-二甲氧基苯(Ⅴ)进行蛋白酪氨酸磷酸酶1B(protein tyrosine phosphatase 1B,PTP1B)抑制活性测定,结果显示化合物质量浓度为20 mg/L时,化合物Ⅴ和Ⅵ的PTP1B酶抑制率分别为25.08%和79.48%,表明化合物Ⅵ具有较好的PTP1B酶抑制活性。
Using the resveratrol (Ⅰ) as the starting material, the compound 4, 5-bis- (2-bromo-4,5-dihydroxybenzene) was synthesized by bromination, reduction, Frieff alkylation and demethylation. Methyl) -1,2-diphenol (Ⅵ) in a total yield of 53.5%. 1HNMR, 13CNMR, HREIMS and other structural characterization. Compound tyrosine was assayed by colorimetry for compound VI and the intermediate 4,5-di- (2-bromo-4,5-dimethoxybenzyl) -1,2-dimethoxybenzene The results showed that the inhibitory rates of PTP1B were 25.08% and 79.48% when the compound concentration was 20 mg / L, respectively, indicating that compound Ⅵ was more potent than PTP1B Good PTP1B enzyme inhibitory activity.