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    • 4. 发明申请
    • ALPHA-CARBOLINE DERIVATIVES AND METHODS FOR PREPARATION THEREOF
    • ALPHA-CARBOLINE衍生物及其制备方法
    • US20090326229A1
    • 2009-12-31
    • US12376068
    • 2007-08-02
    • Masahiro MizunoHideya MizufuneMisayo SeraMasahiro MinenoTsuyoshi Ueda
    • Masahiro MizunoHideya MizufuneMisayo SeraMasahiro MinenoTsuyoshi Ueda
    • C07D471/02C07D213/72
    • C07D471/04C07D213/74C07D213/75C07D405/12
    • To provide methods for preparing alpha-carboline derivatives in few steps, as well as conveniently and industrially advantageously. A method for preparation of a compound represented by Formula (II) or a salt thereof, comprising subjecting a compound represented by Formula (I) or a salt thereof to a ring closure reaction in the presence of a palladium catalyst, a ligand, and a base; a method for preparation of a compound represented by Formula (IX) or a salt thereof, comprising subjecting a compound represented by Formula (VII) or a salt thereof to a ring closure reaction in the presence of a palladium catalyst, a ligand, and a base, and subsequently to an aromatization reaction; and methods for preparation of compounds represented by Formulae (XV), (XVII), and (XIX) or a salt thereof, comprising subjecting respective compounds represented by Formulae (II) and (IX) or a salt thereof to a reaction for introducing a leaving group when necessary, and subsequently to a coupling reaction: wherein the symbols respectively represent the same meaning as defined in the present specification.
    • 提供在几个步骤中以及方便和工业上有利地制备α-咔啉衍生物的方法。 一种制备由式(II)表示的化合物或其盐的方法,包括在钯催化剂,配体和配体存在下,将式(I)表示的化合物或其盐进行闭环反应 基础; 一种制备由式(Ⅸ)表示的化合物或其盐的方法,包括在钯催化剂,配体和配体存在下使式(Ⅶ)表示的化合物或其盐进行闭环反应 碱,然后进行芳构化反应; 以及由式(XV),(XVII)和(XIX)表示的化合物或其盐制备化合物或其盐的方法,包括使由式(Ⅱ)和(Ⅸ)表示的各种化合物或其盐进行引入 在必要时离去基团,随后进行偶联反应:其中符号分别表示与本说明书中定义的相同的含义。