New efficient and convenient approaches have been devised for the synthesis of sitagliptin impurities. As a part of impurity profile study of an antidiabetic drug substance sitagliptin 1, we encountered with six process related impurities. These impurities were detected by utilizing simple techniques such as high performance liquid chromatography (HPLC) and liquid chromatography‐mass spectrometry (LC–MS). All these impurities were synthesized and their presence in the sitagliptin sample was confirmed by co‐injection and matching the retention time with spiked impurities. The formation and control of these impurities during sitagliptin manufacture and synthesis of these impurities is discussed in detail. Synthesis of these impurities was accomplished by utilizing readily accessible starting materials, simple, convenient and concise reaction sequence.

中文翻译：

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西格列汀杂质的高效便捷合成途径

已经设计出用于合成西他列汀杂质的新的有效且方便的方法。作为抗糖尿病药物西他列汀1杂质谱研究的一部分，我们遇到了六种与工艺有关的杂质。利用高效液相色谱（HPLC）和液相色谱等简单技术检测了这些杂质-质谱（LC-MS）。所有这些杂质均已合成，并且通过共进样并将保留时间与加标的杂质相匹配，证实了它们在西他列汀样品中的存在。详细讨论了西他列汀生产和这些杂质的合成过程中这些杂质的形成和控制。这些杂质的合成是通过利用容易获得的原料，简单，方便和简明的反应顺序完成的。