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目的:通过Erlenmeyer-Plchl反应制备药物合成的重要中间体3,4,5-三甲氧基苯乙酸。方法:在醋酸、醋酐和醋酸钠存在的条件下,将3,4,5-三甲氧基苯甲醛与马尿酸缩合,得到二氢噁唑酮中间体,再经氢氧化钠水解、过氧化氢氧化得到3,4,5-三甲氧基苯乙酸。结果:所得产物经红外光谱、核磁共振氢谱和质谱确证;总收率约为58%。结论:本方法路线短,原料易得,操作简单,避免了剧毒试剂的使用,更适于工业化生产。
OBJECTIVE: To prepare 3,4,5-trimethoxyphenylacetic acid, an important intermediate of pharmaceutical synthesis, by Erlenmeyer-Plchl reaction. Methods: Condensation of 3,4,5-trimethoxybenzaldehyde with hippuric acid in the presence of acetic acid, acetic anhydride and sodium acetate gave the oxadiazolone intermediate which was hydrolyzed by sodium hydroxide and peroxidized Hydroxylation gives 3,4,5-trimethoxyphenylacetic acid. Results: The obtained product was confirmed by IR, 1H NMR and MS; The total yield was about 58%. Conclusion: This method has short route, easy to get raw materials, simple operation, avoids the use of highly toxic reagents and is more suitable for industrial production.