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    • 14. 发明授权
    • Method for producing oxyindoles
    • 氧吲哚的制备方法
    • US5679799A
    • 1997-10-21
    • US553022
    • 1995-11-03
    • Katsuhisa IsogaiKohei Hasegawa
    • Katsuhisa IsogaiKohei Hasegawa
    • C07D209/34C07D209/32
    • C07D209/34
    • There is disclosed a method for producing oxyindoles, which comprises reacting a 2-halogenophenylacetic acid or its salt with ammonia in the presence of a copper salt catalyst, and heating a mixture of the produced 2-aminophenylacetic acid or its salt and oxyindoles in the presence of an acid catalyst, to subject the 2-aminophenylacetic acid or its salt to a ring-closure reaction. According to this method, relatively readily available 2-halogenophenylacetic acids are used as a starting raw material to industrially produce highly pure oxyindoles in high yield in one pot without involving complicated steps. Further, since the amination is carried out at a temperature greatly lower than that of the conventional art, the lowering of the pH of the reaction liquid can be suppressed. Therefore, the restrictions on the specifications of the reaction apparatus, such as corrosion prevention and pressure resistance, can be mitigated.
    • 公开了一种制备羟吲哚的方法,其包括在铜盐催化剂存在下使2-卤代苯基乙酸或其盐与氨反应,并在所存在的条件下加热所产生的2-氨基苯乙酸或其盐与羟基吲哚的混合物 的酸催化剂,以使2-氨基苯基乙酸或其盐进行闭环反应。 根据该方法,使用相对容易获得的2-卤代苯基乙酸作为起始原料,在一锅中以高产率工业生产高纯度的氧吲哚,而不涉及复杂的步骤。 此外,由于胺化在比现有技术大大降低的温度下进行,所以可以抑制反应液的pH降低。 因此,可以减轻对反应装置的规格的限制,例如防腐蚀和耐压性。