Invention Grant
- Patent Title: Production method for 3,3-dimethyl-3,4-dihydro-1H-quinoxalin-2-one derivative and intermediate for said production method
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Application No.: US14910971Application Date: 2014-08-08
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Publication No.: US09676703B2Publication Date: 2017-06-13
- Inventor: Kazuhiro Kudou , Masato Nagatsuka
- Applicant: SANTEN PHARMACEUTICAL CO., LTD.
- Applicant Address: JP Osaka
- Assignee: SANTEN PHARMACEUTICAL CO., LTD.
- Current Assignee: SANTEN PHARMACEUTICAL CO., LTD.
- Current Assignee Address: JP Osaka
- Agency: Buchanan, Ingersoll & Rooney PC
- Priority: JP2013-166643 20130809
- International Application: PCT/JP2014/071053 WO 20140808
- International Announcement: WO2015/020204 WO 20150212
- Main IPC: C07D241/44
- IPC: C07D241/44 ; C07C227/18

Abstract:
An object is to provide a novel production method suitable for industrial production of a 3,3-dimethyl-3,4-dihydro-1H-quinoxalin-2-one derivative and a synthetic intermediate for the method. Provided is a method for producing a compound represented by formula (1): wherein R1 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aryl group, R2 represents a hydrogen atom, an optionally substituted alkyl group, a hydroxy group, or nitrogen atom-protecting group, R3 represents a hydrogen atom, an optionally substituted alkyl group, a hydroxy group, or a nitrogen atom-protecting group, and X represents a hydroxy group or a leaving group, or a salt thereof, the method comprising the steps of: reacting a compound represented by formula (2): wherein R1, R2, and X are the same as defined in formula (1), R4represents an optionally substituted alkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aryl group, or a salt thereof with a nitrating agent to obtain a compound represented by formula (3): wherein R1 , R2 , R4, and X are the same as defined in formulae (1) and (2), or a salt thereof, and reducing the compound represented by formula (3) or the salt therof to obtain the compound represented by formula (1) or the salt thereof.
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