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目的为加强塞来昔布原料药的质量控制,合成了塞来昔布的有关物质。方法以甲基取代的苯乙酮为起始原料,经Claisen缩合,再分别与水合肼和对氨磺酰基苯肼盐酸盐缩合,制得目标化合物。结果与结论目标化合物的结构经1H-NMR、MS确证,合成的杂质可以作为塞来昔布原料药质量控制的有关物质对照品。该方法条件温和、原料易得、操作简单。
Objective To improve the quality control of celecoxib’s drug substance and to synthesize the related substances of celecoxib. Methods Methyl substituted acetophenone was used as the starting material, which was condensed with Claisen and then with hydrazine hydrate and p-sulfamoyl phenylhydrazine hydrochloride respectively to obtain the target compound. RESULTS AND CONCLUSIONS The structures of target compounds were confirmed by 1H-NMR and MS. The synthesized impurities could be used as reference substance for quality control of celecoxib. The method is mild, easy to get raw materials, easy to operate.