发明公开
EP0491538A1 Stereocontrolled production of hydroxyester, hydroxyamide, and lactone compounds from chiral alpha-amino aldehydes 失效
Stereokontrollierte Herstellung von Hydroxyester-,Hydroxyamid- und Lactonverbindungen aus chiralen alpha-Aminoaldehyden。

  • 专利标题: Stereocontrolled production of hydroxyester, hydroxyamide, and lactone compounds from chiral alpha-amino aldehydes
  • 专利标题(中): Stereokontrollierte Herstellung von Hydroxyester-,Hydroxyamid- und Lactonverbindungen aus chiralen alpha-Aminoaldehyden。
  • 申请号: EP91311659.6
    申请日: 1991-12-16
  • 公开(公告)号: EP0491538A1
    公开(公告)日: 1992-06-24
  • 发明人: Decamp, Ann E.Shinkai, IchiroKawaguchi, Alan T.Volante, Ralph P.
  • 申请人: MERCK & CO. INC.
  • 申请人地址: 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
  • 专利权人: MERCK & CO. INC.
  • 当前专利权人: MERCK & CO. INC.
  • 当前专利权人地址: 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
  • 代理机构: Thompson, John Dr.
  • 优先权: US628045 19901217
  • 主分类号: C07D307/33
  • IPC分类号: C07D307/33 C07D263/52 C07C237/22
Stereocontrolled production of hydroxyester, hydroxyamide, and lactone compounds from chiral alpha-amino aldehydes
摘要:
A process for stereocontrolled preparation of a medicinally significant hydroxyester, hydroxyamide or lactone compound of structural formula:

comprises the addition of homoenolate equivalents to chiral α-amino aldehydes. The hydroxyester, hydroxyamide, or lactone reaction products are useful as inhibitors of the HIV protease or of renin, or as intermediates in the preparation of inhibitors of the HIV protease or renin.
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