Invention Grant
- Patent Title: Industrial process of mono-alkylating piperidine nitrogen in piperidine derivative with deuterated-lower-alkyl
-
Application No.: US16644084Application Date: 2018-09-06
-
Publication No.: US11214545B2Publication Date: 2022-01-04
- Inventor: Yuya Nakai , Masashi Hayashi , Wataru Mitsuhashi
- 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
- Agency: Sughrue Mion, PLLC
- Priority: JPJP2017-172351 20170907
- International Application: PCT/JP2018/032983 WO 20180906
- International Announcement: WO2019/049918 WO 20190314
- Main IPC: C07D221/28
- IPC: C07D221/28

Abstract:
The present invention relates to a method of mono-alkylating a piperidine nitrogen in a piperidine derivative with a deuterated lower-alkyl, which comprises protecting the piperidine nitrogen with an aralkyl protective group, lower-alkylating the piperidine nitrogen with a deuterated-lower-alkylating agent under neutral or basic condition, and then deprotecting the aralkyl protective group.
Information query