Invention Grant
- Patent Title: Process for preparing roflumilast
- Patent Title (中): 罗氟司特制备方法
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Application No.: US14426881Application Date: 2013-10-16
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Publication No.: US09321726B2Publication Date: 2016-04-26
- Inventor: Josep Salaet Ferre , Francisco Marquillas Olondriz
- Applicant: INTERQUIM, S.A.
- Applicant Address: ES Barcelona
- Assignee: Interquim, S.A.
- Current Assignee: Interquim, S.A.
- Current Assignee Address: ES Barcelona
- Agency: Birch, Stewart, Kolasch & Birch, LLP
- Priority: ES201231598 20121017
- International Application: PCT/EP2013/071607 WO 20131016
- International Announcement: WO2014/060464 WO 20140424
- Main IPC: C07D213/75
- IPC: C07D213/75 ; C07D233/60 ; C07D249/08 ; C07D207/408 ; C07D209/48 ; C07D295/104 ; C07D233/90 ; C07D249/10

Abstract:
The invention relates to a process for the preparation of Roflumilast by reaction of an activated form of 3-(cyclopropylmethoxy)-4-(difluoromethoxy)-benzoic acid with an activating agent selected from (a) carbonyldiimidazole (CDI), (b) 1,1′-carbonyl-di-(1,2,4-triazol) (CDT), (c) 1,1′-carbonyl-bis-(2-methylimidazol), (d), 1′-carbonyl-dipyperidin, (e) N,N′-dicyclohexylcarbodiimide (DCC), (f) N,N′-diisopropylcarbodiimide (DIC), (g) 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) and a combination of one of the previous (a)-(g) with (h) N-hydroxysuccinimide or (i) N-hydroxyphthalimide, and the subsequent reaction with 3,5-dichloropyridine-4-amine in the presence of an inorganic base. The invention also relates to the synthesis intermediates.
Public/Granted literature
- US20150246884A1 PROCESS FOR PREPARING ROFLUMILAST Public/Granted day:2015-09-03
Information query
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