Title:
PRODUCTION AND PURIFICATION METHODS FOR EFINACONAZOLE
Document Type and Number:
WIPO Patent Application WO/2018/212333
Kind Code:
A1
Abstract:
Production and purification methods for efinaconazole are provided by which high-purity efinaconazole can be obtained in high yield through a simple procedure using a specific impurity as an index, the methods being suitable for industrial scale. The production method for efinaconazole is characterized by comprising step A, in which a toluene solution comprising compound (II), compound (III), an inorganic base, and toluene is formed, the amount of the toluene in volume (L) being 2-5 times the mass (Kg) of the compound (II), step B, in which the toluene solution is reacted with heating, and step C, in which the liquid reaction mixture obtained in step B is washed to obtain a crude toluene solution of efinaconazole which has a residual 4-MP content of 5 wt% or less with respect to the efinaconazole.
Inventors:
WATANABE MASAHITO (JP)
KANAYAMA TAKESHI (JP)
KANAYAMA TAKESHI (JP)
Application Number:
PCT/JP2018/019324
Publication Date:
November 22, 2018
Filing Date:
May 18, 2018
Export Citation:
Assignee:
KAKEN PHARMA CO LTD (JP)
International Classes:
C07D401/06; A61P31/10; C07D401/14; C07D487/10; A61K31/4439
Domestic Patent References:
| WO2016193917A1 | 2016-12-08 | |||
| WO2016181306A1 | 2016-11-17 | |||
| WO2016116919A1 | 2016-07-28 | |||
| WO2016079728A1 | 2016-05-26 | |||
| WO2012029836A1 | 2012-03-08 | |||
| WO1994026734A1 | 1994-11-24 | |||
| WO1994026734A1 | 1994-11-24 | |||
| WO2012029836A1 | 2012-03-08 | |||
| WO2016079728A1 | 2016-05-26 | |||
| WO2016116919A1 | 2016-07-28 | |||
| WO2016181306A1 | 2016-11-17 | |||
| WO2016193917A1 | 2016-12-08 |
Foreign References:
| US20170129874A1 | 2017-05-11 | |||
| JP2017036262A | 2017-02-16 | |||
| EP3091007A1 | 2016-11-09 | |||
| CN106928186A | 2017-07-07 | |||
| US20160376253A1 | 2016-12-29 |
Other References:
TIEZTE L. F. , EICHER T., PRECISE ORGANIC SYNTHESIS [EXPERIMENT MANUAL], 15 January 1995 (1995-01-15), pages 27 - 31, XP009517592, ISBN: 4-524-40131-8
See also references of EP 3628668A4
See also references of EP 3628668A4
Attorney, Agent or Firm:
ONO, Shinjiro et al. (JP)
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