The plasma kallikrein inhibitor ASP5069 is a promising drug candidate for the treatment of edema and hematoma and for the prevention of bleeding during surgery. Here, we report the development of a practical and scalable process for manufacturing ASP5069 that features a convergent synthetic approach, suppression of impurity formation, effective purification of the amine compound by extraction, improved reproducibility of the reductive amination reaction, and a drying process for the dihydrate form. This process was successfully used to prepare >100 g of ASP5069.

中文翻译：

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血浆激肽释放酶抑制剂ASP5069的实用且可扩展的生产工艺

血浆激肽释放酶抑制剂ASP5069是用于治疗水肿和血肿以及预防手术中出血的有前途的候选药物。在这里，我们报告开发一种实用且可扩展的ASP5069制造工艺，该工艺具有收敛的合成方法，抑制杂质形成，通过萃取有效纯化胺化合物，提高还原性胺化反应重现性以及干燥工艺的特点。二水合物形式。此过程已成功用于制备> 100 g的ASP5069。