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目的研究消炎镇痛药洛索洛芬钠的关键中间体2-(4-溴甲基)苯基丙酸的合成新方法。方法以4-甲基苯乙酮为原料,经还原、氯化、氰化得到2-(4-甲基)苯基丙腈(Ⅲ),然后经水解、溴化得到关键中间体2-(4-溴甲基)苯基丙酸(Ⅴ),该中间体再经过4步反应可制得洛索洛芬钠。结果与结论关键中间体2-(4-溴甲基)苯基丙酸的结构经1H-NMR、FT-IR、MS谱确证,目标化合物的总收率为38%。该工艺路线具有原料易得、操作简便、副产物少、收率高的特点,适合于工业化生产。
AIM: To study a new method for the synthesis of 2- (4-bromomethyl) phenylpropionic acid, the key intermediate of loxoprofen sodium, an anti-inflammatory analgesic. Methods 4- (4-Methyl) phenylpropionitrile (Ⅲ) was obtained by the reduction, chlorination and cyanidation of 4-methylacetophenone, which was then hydrolyzed and brominated to obtain the key intermediate 2- 4-bromomethyl) phenylpropionic acid (V), this intermediate can be obtained after 4 steps of loxoprofen sodium. Results and Conclusions The structure of 2- (4-bromomethyl) phenylpropionic acid, a key intermediate, was confirmed by 1H-NMR, FT-IR and MS spectra. The overall yield of target compound was 38%. The process has the advantages of raw materials, easy operation, less by-products, high yield, suitable for industrial production.