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Stereoselective method for producing a 1,3-amino alcohol derivative

机译:立体选择性制备1,3-氨基醇衍生物的方法

摘要

PROBLEM TO BE SOLVED: To provide a method for highly stereoselectively producing an optically active 1,3-amino alcohol derivative with ease in a high yield by the catalytically asymmetric nucleophilic addition reaction of the aldol addition reaction type using an aldehyde compound and an enamine or its derivative.;SOLUTION: The method for producing an optically active 1,3-amino alcohol derivative having an N, O-acetal structure comprises treating a polymer formed as an intermediate with a Lewis acid such as scandium triflate in ethanol to effectively decompose the polymer in the asymmetric nucleophilic addition reaction for reacting an aldehyde with an enamine derived from an aldehyde in the presence of an asymmetric catalyst composed of a monovalent copper compound and a chiral diamine ligand. Furthermore, the method for producing the corresponding optically active 1,3-amino alcohol derivative comprises treating the above polymer with an allylating agent or a reducing agent in the presence of a Lewis acid.;COPYRIGHT: (C)2007,JPO&INPIT
机译:解决的问题:提供一种通过醛类加成反应或烯醛或烯胺加成反应进行的醛醇加成反应类型的催化不对称亲核加成反应,以高收率容易地高度立体选择性地制备光学活性的1,3-氨基醇衍生物的方法。解决方案:制备具有N,O-乙缩醛结构的旋光的1,3-氨基醇衍生物的方法包括用路易斯酸如三氟甲磺酸in在乙醇中处理作为中间体形成的聚合物,以有效地分解其衍生物。在不对称亲核加成反应中使聚合物与醛反应,使醛与衍生自醛的烯胺在由一价铜化合物和手性二胺配体组成的不对称催化剂存在下反应。此外,制备相应的旋光的1,3-氨基醇衍生物的方法包括在路易斯酸存在下用烯丙基化剂或还原剂处理上述聚合物。COPYRIGHT:(C)2007,JPO&INPIT

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