The initial process development of the novel β-lactamase inhibitor WCK 6395 is described. All key intermediates were readily isolated by either crystallization or precipitation to eliminate related impurities. Seven possible process-related impurities were hypothesized, and initial control strategies were implemented. Additionally, process parameters were identified and improved to decrease or circumvent these impurities. The parameters of each step were optimized through prior knowledge and experimentation to improve yield and desired quality of WCK 6395 to support toxicological studies. The improved process effectively reduced the use of hazardous reagents, was robust on the kilogram scale, demonstrated at the pilot scale, and subsequently served as the basis for commercial route development.

中文翻译：

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新型 β-内酰胺酶抑制剂 WCK 6395 的工艺开发和放大

描述了新型 β-内酰胺酶抑制剂 WCK 6395 的初始工艺开发。所有关键中间体很容易通过结晶或沉淀分离，以消除相关杂质。假设了七种可能的工艺相关杂质，并实施了初始控制策略。此外，还确定并改进了工艺参数以减少或避免这些杂质。通过先验知识和实验优化每个步骤的参数，以提高 WCK 6395 的产量和所需质量，以支持毒理学研究。改进后的工艺有效减少了有害试剂的使用，在千克规模上稳健，在中试规模上进行了展示，随后作为商业路线开发的基础。