Invention Application
- Patent Title: Manufacture of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol
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Application No.: US15559630Application Date: 2016-03-22
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Publication No.: US20180065984A1Publication Date: 2018-03-08
- Inventor: Carla De Faveri , Florian Anton Martin Huber
- Applicant: H. Lundbeck A/S
- Applicant Address: DK Valby
- Assignee: H. Lundbeck A/S
- Current Assignee: H. Lundbeck A/S
- Current Assignee Address: DK Valby
- Priority: DKPA201500181 20150324
- International Application: PCT/EP2016/056244 WO 20160322
- Main IPC: C07D498/04
- IPC: C07D498/04 ; C07D211/78 ; C07D491/113 ; C07C227/18 ; C07C227/22 ; C07C249/02 ; C07C269/04 ; C07C271/22
![Manufacture of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol](/abs-image/US/2018/03/08/US20180065984A1/abs.jpg.150x150.jpg)
Abstract:
The present invention relates to a process for synthesis of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol abbreviated THIP, having the INN name gaboxadol, starting from pyrrolidin-2-one. The process comprises a new direct process to obtain the intermediate dimethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-5 dicarboxylate or the intermediate diethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate.
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