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    • Development of a Practical Manufacturing Process to Relebactam Via Thorough Understanding of the Origin and Control of Oligomeric Impurities

    Jungchul Kim,Tetsuji Itoh,Feng Xu,Zachary E. X. Dance,Jacob H. Waldman,Debra J. Wallace, Feiyue Wu,Roman Kats-Kagan,Anil R. Ekkati,Andrew P. J. Brunskill,Feng Peng,Patrick S. Fier,Jennifer Obligacion,Benjamin D. Sherry,Zhijian Liu,Khateeta M. Emerson,Adam J. Fine,Anna Jenks,Marco Euclide Armenante

    Organic Process Research & Development（2021）

    Merck & Co Inc

    Cited 3|Views23
    Abstract
    The development of a robust manufacturing process to relebactam, a potent beta-lactamase inhibitor, is described. The origin and control strategy of oligomer impurities formed during hydrogenolysis of benzyl urea intermediate 9 and deprotection of Boc-sulfate intermediate 11 have been thoroughly studied and developed. The optimal manufacturing process has been successfully implemented for commercialization, preparing relebactam (1) in >99% purity with a non-detectable level of oligomers.
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    Key words
    relebactam,oligomers,hydrogenolysis,sulfation,SO3 center dot triethylamine,bromotrimethylsilane
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    【要点】：本文详述了通过深入理解β-内酰胺酶抑制剂relebactam在合成过程中寡聚体杂质的来源和控制策略，开发出一种高效的实际制造工艺，实现了高纯度产品的商业化生产。
    

    【方法】：作者通过详细研究relebactam在氢解反应和去保护步骤中产生的寡聚体杂质，制定了一套控制杂质的有效策略。
    

    【实验】：实验通过氢解反应和去保护步骤优化了制造工艺，使用具体的数据集（未提及数据集名称）成功制备了纯度大于99%的relebactam，并且实现了寡聚体杂质不可检测的水平。