白藜芦醇及其水溶性衍生物的合成

Synthesis of resveratrol and its water-soluble analogue

目的:合成白藜芦醇及其水溶性衍生物。方法:以3,5-二甲氧基苯甲醛和4-甲氧基碘苯为原料,经Wittig反应,Heck偶联,脱甲基反应,连接侧链等合成白藜芦醇及其衍生物,并使用紫外法测定其在水中的溶解度大小。结果:目标化合物经核磁共振氢谱,质谱等确证为白藜芦醇及其水溶性衍生物,且水溶性提高3倍。结论:该方法的反应路线步骤短,操作简便,对反式产物选择性高。

Objective： To synthesize resveratrol and its water-soluble analogue. Methods： 3,5-dimethoxybenzaldehyde and 4-Methoxyiodobenzene were used as starting materials to prepare resveratrol and its water-soluble analogue via Wittig reaction, Heck reaction, deprotection and modification with mPEG side chain. Results： The structure of target compounds were confirmed by 1H NMR and MS; the overall yields of resveratrol were about 47%. Conclusion： This synthetic route presented requires only three steps and it is easy to operate with high stereoselectivity of trans conformation.