非甾体抗炎药洛索洛芬钠的合成研究

目的研究洛索洛芬钠的合成新工艺。方法以苯乙烯为原料,经氯化、格氏加成、酯化、氯甲基化、缩合、脱羧等7步反应制得洛索洛芬钠(2-4-(2-氧代环戊基甲基)苯基]丙酸钠二水合物)。结果与结论目标化合物的结构经1H-NMR和ESI-MS谱确证,总收率为35.0%(以苯乙烯计)。改进后的制备工艺具有原料价廉易得、反应条件温和、收率高、操作简便的特点,适合于工业化生产。

Study on the synthesis of nonsteroidal anti-inflammatory drug loxoprofen sodium

Loxoprofen sodium, an important nonsteroidal anti-inflammatory drug （ NSAIDs）, is a representative of a series of 2-aryl propionic acids anti-inflammatory drugs, which has possessed the characteristics of quick and finer curative effect in treating disease with a little dosage. Loxoprofen sodium was introduced into the market which led to the need for a high-yielding, economical and environmentall sound process. The synthesis of loxoprofen sodium has been accomplished from commercially available styrene as starting material through seven steps in 35.0% overall yield（ based on styrene）, which involved chlorination, Grignard addition, esterification, chloromethylation, condensation and decarboxylation. The structure of loxoprofen sodium has been characterized by ^1H-NMR and ESI-MS. This synthetic method has some advantages such as cheap available material, mild reaction conditions, high yield and simple operation, which is suitable for the largescale production.