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...
Saved in:
Published in | Organic process research & development Vol. 24; no. 12; pp. 2830 - 2839 |
---|---|
Main Authors | , |
Format | Journal Article |
Language | English |
Published |
American Chemical Society
18.12.2020
|
Subjects | |
Online Access | Get full text |
Cover
Loading…
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 |