非甾体抗炎药洛索洛芬钠的合成工艺研究

Study of synthetic process of loxoprofen sodium

目的 :改进合成工艺 ,缩短合成路线 ,提高总收率。方法 :以甲苯为原料 ,合成 2 对溴代甲基苯基丙酸。再在乙醇、DMF溶剂和氢氧化钠的条件下 ,与 2 乙氧羰基环戊酮进行烷基化后直接水解 ,脱羧成盐得洛索洛芬钠。结果 :经IR ,1 H NMR光谱鉴定 ,产品结构与洛索洛芬钠一致。结论 :该合成路线较短 ,总收率 40 %以上。

Objective:For improving and shortening synthetic process and raising yield.Methods:2-(p-bromomrthyl phenyl)propionic acid is prepared from toluene,and alkylated with 2-oxocyclopentane carboxylate in medium of ethanol,DMF,and sodium hydroxide,and loxoprofen sodium is obtained following the product of the former reaction is hydrolyzed and decarboxylated.Results:The product thus obtained is identified with IR and JH1,D,Z-NMR.Conclusion:A shorter new process for synthesis of loxoprofen sodium is established with a yield of >40%. [