Practical and Scalable Manufacturing Process for Plasma Kallikrein Inhibitor ASP5069

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...

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Bibliographic Details
Published inOrganic process research & development Vol. 24; no. 12; pp. 2830 - 2839
Main Authors Hirasawa, Shun, Kohmura, Yoshinori
Format Journal Article
LanguageEnglish
Published American Chemical Society 18.12.2020
Subjects
dihydrate form
ASP5069
reductive amination
plasma kallikrein inhibitor
Mannich reaction
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Summary: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.
ISSN:1083-6160
1520-586X
DOI:10.1021/acs.oprd.0c00291