(2-苯硫基乙基)丙二酸二乙酯的合成方法研究

Research of synthesis of Diethyl [2-(phenylthio)ethyl] malonate

以苯硫酚为原料,在碱性条件下与1,1-环丙基二羧酸二乙酯反应,一步制得了抗痛风药苯磺唑酮的重要中间体(2-苯硫基乙基)丙二酸二乙酯,收率为55%。本工艺将原有路线缩短一步,极大缩短了反应时间,提高了产品收率,用1H NMR和MS对产品进行了结构表征。

Diethyl [2-（phenylthio）ethyl] malonate was synthesized by one step reaction of thiophenol and diethyl cyclopropane-1,1-dicarboxylate in alkaline condition,and the yield of product was 55%.Under the optimized conditions,the reaction time was significantly reduced and the yield increased.The structure of the product was characterized by1H-NMR and MS.