Title:
METHOD FOR PRODUCING AZILSARTAN USING ENVIRONMENT-FRIENDLY SOLVENT AND KEY INTERMEDIATE COMPOUND RELATED THERETO
Document Type and Number:
WIPO Patent Application WO/2021/230691
Kind Code:
A1
Abstract:
The present invention relates to synthesizing azilsartan dihexylamine salt, which is a key intermediate, through an efficient one-pot reaction, and then synthesizing azilsartan medoxomil through an ionic liquid and a eutectic solvent, which are environmentally-friendly solvents. The present invention achieves the effects of shortening a reaction time and reducing manufacturing costs by continuously performing a cyclization reaction and a hydrolysis reaction during the production of azilsartan medoxomil. The present invention also synthesizes azilsartan dicyclohexylamine salt, which is a key intermediate, through a one-pot reaction, uses an ionic liquid and a eutectic solvent as environmentally-friendly solvents instead of an organic solvent to increase reactivity such that a reaction can be performed even at less than 50℃, and thus reduces production of related substances, and can mass-produce high-purity, high-yield, and competitive azilsartan medoxomil.
Inventors:
PARK EUN JU (KR)
JI HYUN (KR)
PARK JIN OH (KR)
JI HYUN (KR)
PARK JIN OH (KR)
Application Number:
PCT/KR2021/006039
Publication Date:
November 18, 2021
Filing Date:
May 13, 2021
Export Citation:
Assignee:
DAEBONG LS CO LTD (KR)
International Classes:
C07D413/10; A61K31/4245; A61P9/12; C07D413/14
Domestic Patent References:
| WO2012107814A1 | 2012-08-16 |
Foreign References:
| US20120238606A1 | 2012-09-20 | |||
| US20050032854A1 | 2005-02-10 | |||
| US20140113942A1 | 2014-04-24 |
Other References:
STANISLAV RÁDL; JOSEF ČERNÝ; JAN STACH; AND ZUZANA GABLÍKOVÁ: "Improved Process for Azilsartan Medoxomil: A New Angiotensin Receptor Blocker", ORGANIC PROCESS RESEARCH & DEVELOPMENT, 1 January 2013 (2013-01-01), pages 77 - 86, XP002716686, ISSN: 1083-6160, DOI: 10.1021/op3002867
Attorney, Agent or Firm:
KOH, Bong Jin (KR)
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