METHOD FOR PRODUCING (1S,4S,5S)-4-BROMO-6-OXABICYCLO[3.2.1]OCTAN-7-ONE
    4.
    发明申请
    METHOD FOR PRODUCING (1S,4S,5S)-4-BROMO-6-OXABICYCLO[3.2.1]OCTAN-7-ONE 审中-公开
    (1S,4S,5S)-4-溴-6-氧杂环戊二烯[3.2.1]哒嗪酮的制备方法

    公开(公告)号:US20150353577A1

    公开(公告)日:2015-12-10

    申请号:US14762393

    申请日:2014-03-28

    摘要: It is an object of the present invention to provide a method for efficiently producing (1S,4S,5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one (1), which is important as an intermediate compound for the production of an FXa-inhibiting compound. A method for producing (1S,4S,5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one (1), which comprises treating an (R)-α-phenylethylamine salt of (S)-3-cyclohexene-1-carboxylic acid with 1,3-dibromo-5,5-dimethylhydantoin or N-bromosuccinimide in a solvent.

    摘要翻译: 本发明的目的是提供一种有效制备(1S,4S,5S)-4-溴-6-氧杂双环[3.2.1]辛-7-酮(1)的方法,该方法作为中间体 用于生产FXa抑制化合物的化合物。 (1S,4S,5S)-4-溴-6-氧杂双环[3.2.1]辛-7-酮(1)的制备方法,该方法包括处理(R)-α-苯基乙胺盐(S) - 3-环己烯-1-羧酸与1,3-二溴-5,5-二甲基乙内酰脲或N-溴代琥珀酰亚胺在溶剂中反应。