Invention Grant
- Patent Title: Process for preparing 5R-[(benzyloxy) amino] piperidine-2S-carboxylate and oxalates thereof
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Application No.: US16345744Application Date: 2018-03-02
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Publication No.: US10662190B2Publication Date: 2020-05-26
- Inventor: Baolin Wang , Yuxin Qi , Yinlong Zhao , Yuqi Teng , Jun Chen , Lizhu Ju , Xinfa Li
- Applicant: XINFA PHARMACEUTICAL CO., LTD
- Applicant Address: CN Dongying
- Assignee: XINFA PHARMACEUTICAL CO., LTD
- Current Assignee: XINFA PHARMACEUTICAL CO., LTD
- Current Assignee Address: CN Dongying
- Agency: CBM Patent Consulting, LLC
- Priority: com.zzzhc.datahub.patent.etl.us.BibliographicData$PriorityClaim@d415d77
- International Application: PCT/CN2018/077915 WO 20180302
- International Announcement: WO2019/033746 WO 20190221
- Main IPC: C07D471/08
- IPC: C07D471/08 ; C07D211/60 ; C07C51/41 ; C07C55/07
![Process for preparing 5R-[(benzyloxy) amino] piperidine-2S-carboxylate and oxalates thereof](/abs-image/US/2020/05/26/US10662190B2/abs.jpg.150x150.jpg)
Abstract:
It relates to improved processes of preparing 5R-[(benzyloxy) amino] piperidine-2S-carboxylate and oxalate thereof. In the present invention, L-glutamic acid or L-glutamic acid sodium salt as the starting material is reacted with chloroactic acid under an alkaline condition via a substitution reaction to obtain compound III; then, compound III is reacted with alcohol in the presence of acid reagent via esterification reaction to obtain compound IV; under the action of strong base, compound IV is subjected to intramolecular condensation into ring, hydrolysis-decarboxylation, and esterification to obtain compound V; compound V is condensed with benzyloxy amine hydrochloride salt in the presence of alkaline to obtain compound VI; compound VI is subjected to reduction and chiral resolution to obtain 5R-[(benzyloxy) amino] piperidine-2S-carboxylate oxalate (IIb) which is then neutralized to obtain 5R-[(benzyloxy) amino] piperidine-2S-carboxylate (IIa).
Public/Granted literature
- US20190256514A1 Process for Preparing 5R-[(benzyloxy) amino] piperidine-2S-carboxylate and Oxalates Thereof Public/Granted day:2019-08-22
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