发明授权
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

  • 专利标题: Process for the preparation of 2-(4-hydroxy-3-morfolynil)-2-cyclohexenone
  • 专利标题(中): 2-(4-羟基-3-吗啉代)-2-环己烯酮的制备方法
  • 申请号: US12279323
    申请日: 2007-02-12
  • 公开(公告)号: US07872007B2
    公开(公告)日: 2011-01-18
  • 发明人: Elio Napolitano
  • 申请人: Elio Napolitano
  • 申请人地址: IT Pisa
  • 专利权人: Abiogen Pharma S.p.A.
  • 当前专利权人: Abiogen Pharma S.p.A.
  • 当前专利权人地址: IT Pisa
  • 代理机构: Knobbe Martens Olson & Bear LLP
  • 优先权: ITMI2006A0258 20060213
  • 国际申请: PCT/IT2007/000088 WO 20070212
  • 国际公布: WO2007/094022 WO 20070823
  • 主分类号: A61K31/5375
  • IPC分类号: A61K31/5375 C07D265/30
Process for the preparation of 2-(4-hydroxy-3-morfolynil)-2-cyclohexenone
摘要:
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.
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