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    • 1. 发明公开
    • PROCESS FOR PREPARING CHIRAL AMINES
    • 制备手性胺的方法
    • EP3301087A1
    • 2018-04-04
    • EP16191845.3
    • 2016-09-30
    • DPx Fine Chemicals Austria GmbH & Co KG
    • de Vries, AndreLefort, LaurentVerzijl, Gerard
    • C07D211/56
    • C07D211/56
    • The invention pertains to a process for the preparation of an amine having at least two chiral centers from a ketone having a chiral center at the α position and an amine comprising the steps of:
      (a) contacting a ketone having a chiral center at the α position and a primary amine thereby forming an imine;
      (b) contacting the imine with a reducing agent in the presence of an enantioselective catalyst to form an amine having at least two chiral centers,
      wherein step (a) and/or step (b) are conducted under racemization-enhancing conditions, wherein the racemization-enhancing conditions are achieved by addition of an acid and/or by addition of a salt of a primary amine and an acid, which salt is added in addition to or instead of the primary amine, and wherein the reducing agent is hydrogen.
    • 本发明涉及由α位具有手性中心的酮和胺制备具有至少两个手性中心的胺的方法,该方法包括以下步骤:(a)使在α位具有手性中心的酮与α 位置和伯胺从而形成亚胺; (b)使亚胺与还原剂在对映选择性催化剂存在下接触以形成具有至少两个手性中心的胺,其中步骤(a)和/或步骤(b)在外消旋化增强条件下进行,其中 通过加入酸和/或通过加入伯胺和酸的盐实现外消旋化增强条件,除了伯胺之外或代替伯胺添加盐,并且其中还原剂是氢。