Invention Grant
US09481680B2 Process for the preparation of key intermediates of omarigliptin
有权
omarigliptin的重要中间体的制备方法
- Patent Title: Process for the preparation of key intermediates of omarigliptin
- Patent Title (中): omarigliptin的重要中间体的制备方法
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Application No.: US14900858Application Date: 2015-01-19
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Publication No.: US09481680B2Publication Date: 2016-11-01
- Inventor: Ottorino De Lucchi , Enrico Rosso , Simone Zaramella , Stefano Tartaggia
- Applicant: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A.
- Applicant Address: IT Montecchio Maggiore (VI)
- Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A
- Current Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A
- Current Assignee Address: IT Montecchio Maggiore (VI)
- Agency: Lucas & Mercanti, LLP
- Priority: ITVI2014A0064 20140320
- International Application: PCT/EP2015/050858 WO 20150119
- International Announcement: WO2015/139859 WO 20150924
- Main IPC: C07C271/18
- IPC: C07C271/18 ; C07C221/00 ; C07C225/10 ; C07C245/24 ; C07D309/14 ; C07D487/04 ; C07C225/16 ; C07C269/08

Abstract:
An improved process for the preparation of a key intermediate for the synthesis of the active ingredient Omarigliptin is provided. The key intermediate is a compound having the following formula (I) wherein R1 is propargyl or allyl group and P is an amine protecting group. The compound of formula (I) is prepared by converting a compound of formula (IV) by an amination reaction to a compound of formula (III), which is then protected to provide a compound of formula (II), which is then alkylated to provide the compound of formula (I).
Public/Granted literature
- US20160200727A1 PROCESS FOR THE PREPARATION OF KEY INTERMEDIATES OF OMARIGLIPTIN Public/Granted day:2016-07-14
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