发明授权
US08685996B2 Methods for making 3-O-protected morphinones and 3-O-protected morphinone dienol carboxylates 有权
制备3-O-保护的吗啡酮和3-O-保护的吗啡酮二烯酚羧酸酯的方法

  • 专利标题: Methods for making 3-O-protected morphinones and 3-O-protected morphinone dienol carboxylates
  • 专利标题(中): 制备3-O-保护的吗啡酮和3-O-保护的吗啡酮二烯酚羧酸酯的方法
  • 申请号: US13472227
    申请日: 2012-05-15
  • 公开(公告)号: US08685996B2
    公开(公告)日: 2014-04-01
  • 发明人: Andreas Stumpf
  • 申请人: Andreas Stumpf
  • 申请人地址: US CT Stamford
  • 专利权人: Purdue Pharma L.P.
  • 当前专利权人: Purdue Pharma L.P.
  • 当前专利权人地址: US CT Stamford
  • 代理机构: Dechert LLP
  • 主分类号: A61K31/485
  • IPC分类号: A61K31/485 C07D489/02
Methods for making 3-O-protected morphinones and 3-O-protected morphinone dienol carboxylates
摘要:
Disclosed are methods for making aldehydes and ketones comprising allowing the corresponding primary or secondary alcohol to react in the presence of trichoroisocyanuric acid, a compound of formula R1SR2 and a base. In one embodiment, the alcohol is a compound of formula (I): wherein R3 is a protecting group. Also disclosed are methods for making 3-O-protected morphine dienol carboxylates comprising allowing a compound of formula (I) to oxidize in the presence of a chlorine-containing compound and a compound of formula R1SR2; and allowing the product of the oxidation step to react with an acylating agent.
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