Invention Grant
- Patent Title: Process for the preparation of Efavirenz
- Patent Title (中): 制备依法韦仑的方法
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Application No.: US13060839Application Date: 2009-01-30
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Publication No.: US08420808B2Publication Date: 2013-04-16
- Inventor: Alessandro Leganza , Marco Galvagni
- Applicant: Alessandro Leganza , Marco Galvagni
- Applicant Address: IT Alte di Montecchio Maggiore
- 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 Alte di Montecchio Maggiore
- Agency: Dickstein Shapiro LLP
- International Application: PCT/EP2009/000612 WO 20090130
- International Announcement: WO2010/085978 WO 20100805
- Main IPC: C07D265/12
- IPC: C07D265/12

Abstract:
The present invention is directed to a process for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one, of formula (I) comprising reacting the intermediate of formula (II) [0045] as a free base or a salt thereof, with diphosgene (TCMCF, trichlormethylchloroformate) Cl3CO—COCl in an organic solvent or in a biphasic medium comprised of an organic solvent and water, preferably but not mandatorily in the presence of a weak base in an amount sufficient to neutralise the reaction mixture or in an up to 30% molar excess of such amount.
Public/Granted literature
- US20110196151A1 PROCESS FOR THE PREPARATION OF EFAVIRENZ Public/Granted day:2011-08-11
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