无水氯化镁和三乙胺催化合成β-酮酸酯

A Safe and Economical Method for the Preparation of β-Keto Esters

以丙二酸二乙酯为原料,在氢氧化钾条件下将其转变为丙二酸单乙醇酯钾盐,研究丙二酸单乙醇酯钾盐在无水氯化镁-三乙胺碱体系作用下,与酰氯反应制备β-酮酸酯的方法。产物结构经1H NMR、质谱、元素分析确证。该方法避免使用格氏试剂、氢化钠、丁基锂等强碱,条件温和,操作简单,成本低,适合在实验室和工业生产中制备β-酮酸酯。

β-Keto esters is a series of important and versatile intermediates in organic synthesis. In this paper, an economical method with high yield for the preparation ofβ-keto ester was developed starting from diethyl malonate via potassium ethyl malonate, which was reacted with acyl chloride under catalysis of anhydrous magnesium chloride-triethylamine system. This process avoids using of Grignard reagent, sodium hydride and n-butyl lithium. Therefore it can be conducted under mild conditions with low costs and suitable for commercial production of β-keto esters with high purity.