Title:
METHOD FOR PRODUCING CENTANAFADINE
Document Type and Number:
WIPO Patent Application WO/2021/075494
Kind Code:
A1
Abstract:
The present invention addresses the problem of finding a method for reliably producing (1R,5S)-1-(naphthalen-2-yl)-3-azabicyclo[3.1.0]hexane hydrochloride, wherein crystalline polymorphs can be controlled with industrially easy operations. Provided is a method for producing a crystalline form of (1R,5S)-1-(naphthalen-2-yl)-3-azabicyclo[3.1.0]hexane hydrochloride, the method comprising: step (a) for heating and dissolving (1R,5S)-1-(naphthalen-2-yl)-3-azabicyclo[3.1.0]hexane hydrochloride in a solvent including an alcohol-based solvent; step (b) for cooling the dissolved product of step (a) to a temperature, at which crystals of (1R,5S)-1-(naphthalen-2-yl)-3-azabicyclo[3.1.0]hexane hydrochloride precipitate, to nucleate the crystals; step (c) for heating a mixture containing the crystals obtained by nucleation to a temperature at which only a specific crystalline form selectively remains; and step (d) for cooling the mixture heated in step (c) to obtain the crystalline form.
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Inventors:
OTSUKA REI (JP)
ANNAKA KIMIYOSHI (JP)
MITANI HIKARU (JP)
ANNAKA KIMIYOSHI (JP)
MITANI HIKARU (JP)
Application Number:
PCT/JP2020/038896
Publication Date:
April 22, 2021
Filing Date:
October 15, 2020
Export Citation:
Assignee:
OTSUKA PHARMA CO LTD (JP)
International Classes:
A61P25/00; A61K31/403; A61P43/00; C07D209/52
Domestic Patent References:
| WO2001014037A1 | 2001-03-01 | |||
| WO2018119291A1 | 2018-06-28 | |||
| WO2016205762A1 | 2016-12-22 | |||
| WO2018119291A1 | 2018-06-28 |
Foreign References:
| JP2018517742A | 2018-07-05 | |||
| JPH11267402A | 1999-10-05 | |||
| JP2005508383A | 2005-03-31 | |||
| JP2019147794A | 2019-09-05 | |||
| US20070082940A1 | 2007-04-12 | |||
| JP2019147794A | 2019-09-05 |
Attorney, Agent or Firm:
YAMAO, Norihito et al. (JP)
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