Invention Grant
- Patent Title: Process for the preparation of 2-(5-methoxyisochroman-1-yl)-4,5-dihydro-1H-imidazole and the hydrogensulfate salt thereof
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Application No.: US16768093Application Date: 2018-11-30
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Publication No.: US11352346B2Publication Date: 2022-06-07
- Inventor: Ilpo Laitinen , Mikko Leskinen , Mikko Mäkelä
- Applicant: ORION CORPORATION
- Applicant Address: FI Espoo
- Assignee: ORION CORPORATION
- Current Assignee: ORION CORPORATION
- Current Assignee Address: FI Espoo
- Agency: Finnegan, Henderson, Farabow, Garrett & Dunner, LLP
- Priority: FI20176085 20171201
- International Application: PCT/FI2018/050864 WO 20181130
- International Announcement: WO2019/106238 WO 20190606
- Main IPC: C07D405/04
- IPC: C07D405/04 ; C07D311/76 ; C07F7/10

Abstract:
The present disclosure relates to an improved process for the preparation of isochroman structured alpha2A adrenoceptor agonist, namely 2-(5-methoxyisochroman-1-yl)-4,5-dihydro-1H-imidazole of formula (I) and a pharmaceutically acceptable salts thereof, such as 2-(5-methoxyisochroman-1-yl)-4,5-dihydro-1H-imidazole hydrogensulfate of formula (Ia), and to a novel intermediate compound used in the process, namely N-(2-aminoethyl)-5-methoxyisochroman-1-carboxamide monohydrate of formula (V). Alpha2A agonists are useful in the treatment of anxiety, and for use as a sedative or analgesic agent, and other diseases where alpha2A agonism is desired.
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