Invention Grant
US07872007B2 Process for the preparation of 2-(4-hydroxy-3-morfolynil)-2-cyclohexenone
失效
2-(4-羟基-3-吗啉代)-2-环己烯酮的制备方法
- Patent Title: Process for the preparation of 2-(4-hydroxy-3-morfolynil)-2-cyclohexenone
- Patent Title (中): 2-(4-羟基-3-吗啉代)-2-环己烯酮的制备方法
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Application No.: US12279323Application Date: 2007-02-12
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Publication No.: US07872007B2Publication Date: 2011-01-18
- Inventor: Elio Napolitano
- Applicant: Elio Napolitano
- Applicant Address: IT Pisa
- Assignee: Abiogen Pharma S.p.A.
- Current Assignee: Abiogen Pharma S.p.A.
- Current Assignee Address: IT Pisa
- Agency: Knobbe Martens Olson & Bear LLP
- Priority: ITMI2006A0258 20060213
- International Application: PCT/IT2007/000088 WO 20070212
- International Announcement: WO2007/094022 WO 20070823
- Main IPC: A61K31/5375
- IPC: A61K31/5375 ; C07D265/30

Abstract:
It is disclosed a process for the preparation of 2-(4-hydroxy-3-morfolinyl)-2-cycloesenone (BTG-1675A) comprising the steps of: i) reacting N-hydroxymorpholine with cycloesanone in the presence of an oxidation agent thus obtaining an isoxazolidine of Formula IV; and ii) converting the isoxazolidine of Formula IV into 2-(4-hydroxy-3-morfolinyl)-2-cycloesenone. Advantageously, the oxidation agent of the step i) is selected from the group consisting of metal oxides, esters and amides of the azodicarboxylic acid and the step ii) of conversion is carried out by basic catalysis followed by trituration in an aromatic hydrocarbon, preferably toluene. The process disclosed allows to obtain BTG-1675A according to the invention in an amount of hundreds of grams and on an industrial scale. The invention further concerns a new process for preparing hydroxylamines, particularly N-hydroxymorpholine, which is used in the process for preparing BTG-1675A.
Public/Granted literature
- US20090030199A1 PROCESS FOR THE PREPARATION OF 2-(4-HYDROXY-3-MORFOLYNIL)-2-CYCLOHEXENONE Public/Granted day:2009-01-29
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