Title:
NOVEL PRODUCTION METHOD FOR APIXABAN
Document Type and Number:
WIPO Patent Application WO/2021/261172
Kind Code:
A1
Abstract:
The present invention addresses the problem of providing a simple production method that can be industrially applied and that enables direct production of apixaban. Through usage of said simple production method, apixaban, which is the objective, is directly prepared from a one-pot reaction without involving isolation of production intermediates, by causing a reaction to a compound represented by formula (I) after adding thereto formamide and, as a base, preferably sodium methoxide in the presence of, as a reaction solvent, preferably acetonitrile, methanol, or ethanol.
Inventors:
HORI YOHEI (JP)
CHUDA YU (JP)
CHUDA YU (JP)
Application Number:
PCT/JP2021/020478
Publication Date:
December 30, 2021
Filing Date:
May 28, 2021
Export Citation:
Assignee:
DAITO PHARMACEUICAL CO LTD (JP)
International Classes:
C07D471/04; A61K31/4545; A61P7/02
Foreign References:
| JP2017521437A | 2017-08-03 | |||
| CN110862389A | 2020-03-06 | |||
| CN104045637A | 2014-09-17 | |||
| JP2005511712A | 2005-04-28 | |||
| JP2008514712A | 2008-05-08 |
Other References:
WANG, Y. ET AL.: "Design, synthesis, and structure-activity relationship of novel and effective apixaban derivatives as FXa inhibitors containing 1,2,4-triazole/pyrrole derivatives as P2 binding element", BIOORG. MED. CHEM., vol. 24, 2016, pages 5646 - 5661, XP029763093, DOI: 10.1016/j.bmc.2016.09.024
Attorney, Agent or Firm:
KUSAMA, Osamu (JP)
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