Title:
METHOD FOR PREPARATION OF EFINACONAZOLE IN IONIC LIQUID MEDIUM
Document Type and Number:
WIPO Patent Application WO/2021/060948
Kind Code:
A1
Abstract:
The present invention relates to a novel method for preparation of efinaconazole in an ionic liquid medium, the method comprising: reacting 1-[[(2R,3S)-2-(2,4-difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole, and 4-methylenepiperidine or an organic chemically acceptable salt thereof, wherein the 4-methylenepiperidine or the organic chemically acceptable salt thereof is anionized on a base; and performing a coupling reaction with the 1-[[(2R,3S)-2-(2,4-difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole in the presence of an ionic liquid compound. The present invention uses an ionic liquid instead of an organic solvent when preparing efinaconazole, thereby reducing related substances compared to the conventional method, shortens the reaction time, thereby making it possible to easily obtain the final compound, efinaconazole, with high purity and high yield, and may be very suitably used for mass production.
Inventors:
PARK EUN JU (KR)
JI HYUN (KR)
LEE JI EUN (KR)
PARK JIN OH (KR)
JI HYUN (KR)
LEE JI EUN (KR)
PARK JIN OH (KR)
Application Number:
PCT/KR2020/013162
Publication Date:
April 01, 2021
Filing Date:
September 25, 2020
Export Citation:
Assignee:
DAEBONG LS LTD (KR)
International Classes:
C07D401/06; A61K31/454; A61P3/10
Domestic Patent References:
| WO2016193917A1 | 2016-12-08 | |||
| WO2016079728A1 | 2016-05-26 | |||
| WO2016079728A1 | 2016-05-26 | |||
| WO2005014583A1 | 2005-02-17 |
Foreign References:
| US20160376253A1 | 2016-12-29 | |||
| IN201741018119A | 2018-11-30 | |||
| KR20150075187A | 2015-07-03 | |||
| KR20090036349A | 2009-04-14 |
Other References:
See also references of EP 3915981A4
Attorney, Agent or Firm:
KOH, Bong Jin (KR)
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