Invention Publication
- Patent Title: METHOD FOR PRODUCING CENTANAFADINE
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Application No.: US17769250Application Date: 2020-10-15
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Publication No.: US20240140910A1Publication Date: 2024-05-02
- Inventor: Rei Otsuka , Kimiyoshi Annaka , Hikaru Mitani
- Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
- Applicant Address: JP Tokyo
- Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
- Current Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
- Current Assignee Address: JP Tokyo
- Priority: JP 19189407 2019.10.16
- International Application: PCT/JP2020/038896 2020.10.15
- Date entered country: 2022-04-14
- Main IPC: C07D209/52
- IPC: C07D209/52

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.
Public/Granted literature
- US2607624A Telescopic sprinkler Public/Granted day:1952-08-19
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