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中文摘要：
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。
英文摘要：
To improve the quality control of celecoxib, the related substances （2a, 3b, 3c, 4a, 5a, 6a） were synthesized. Based on the reported synthetic route of celecoxib, we developed a one-pot synthetic method to prepare the related compounds of celecoxib. Starting from methyl substituted acetophenone, a convenient synthetic route was designed including Claisen condensation, condensation of the 1,3-butanedione with hydrazine hydrate or 4-sulfonamidophenylhydrazine hydrochloride. The raw materials were cheap and easy to obtain and the reaction conditions were mild. The structures of the target compounds were confirmed by 1H-NMR and MS. The target compounds can be used as the related substances in the quality control of celecoxib.
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