黄芩素乙酰化衍生物的合成工艺优化

Synthesis of baicalein acetyl derivative and technology optimizing

目的:以天然产物黄芩素为先导化合物合成其乙酰化衍生,并对其合成工艺进行优化,确定最佳合成工艺。方法:吡啶作为有机碱和催化剂,乙酸酐作为酰化剂和反应溶剂与黄芩素在室温下反应制备黄芩素乙酰化衍生物。结果:对黄芩素容易被氧化的酚羟基进行保护以提高其稳定性,同时提高黄芩素的脂溶性,扩大黄芩素的临床应用范围。结论:黄芩素与乙酸酐在吡啶条件下,室温反应2h,得到目标化合物,收率为69%,并通过核磁共振谱图对其进行结构确正。

Objective：Baicalein was used as a lead compound for synthesizing the acetylated derivative and its synthesizing process was optimized in order to determine the optimum synthesis process. Methods： Pyridine was asthe organic alkali and catalyst and acetic anhydride was also used as the acetyl agent and reaction solvent. The acetyl derivative of baicalein was prepared with the treatment of baicalein and acetic anhydride stirred at the roomtemperature. Results： The three phenolic hydroxyls, which was easily oxidized, was protected by acetyl reaction to enhance the stability and improve the baicalein fat-soluble and the range of clinical application of baicalein wasexpand. Conclusion： Baicalein was treated with acetic anhydride and pyridine at room temperature for 2h and the target compound was obtained, the yield is 69%. The structure of the derivative was elucidated with the aid of nu-clear magnetic resonance spectrum.