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    • 10. 发明申请
    • PROCESS FOR PREPARING AMINOARYLACETYLENES
    • 制备氨基乙酰丙酮的方法
    • WO9903803A2
    • 1999-01-28
    • PCT/US9814253
    • 1998-07-08
    • CATALYTICA PHARMACEUTICALS INCGRUBER JOHN M
    • GRUBER JOHN M
    • B01J31/24B01J31/30C07B61/00C07C209/62C07C211/45C07C249/02C07C251/24C07C
    • C07C249/02C07C251/24
    • This invention provides a process for preparing aminoarylacetylenes comprising reacting an N-arylmethylidene aminoarylhalide with a terminal acetylene in the presence of a base and a catalyst system comprising a palladium catalyst and a cuprous salt to produce a novel N-arylmethylidene aminoarylacetylene, and hydrolyzing the N-arylmethylidene aminoarylacetylene to the aminoarylacetylene. In one embodiment, the invention provides a process for preparing aminophenylacetylenes comprising reacting an N-benzylidene aminophenylhalide with a terminal acetylene in the presence of a base and the catalyst system to produce a novel N-benzylidene aminophenylacetylene, and hydrolyzing the N-benzylidene aminophenylacetylene to the aminophenylacetylene.
    • 本发明提供了一种制备氨基芳基乙炔的方法,该方法包括使N-芳基亚甲基氨基芳基卤化物与末端乙炔在碱和包含钯催化剂和亚铜盐的催化剂体系存在下反应以制备新的N-芳基亚甲基氨基芳基乙炔并将N - 芳基亚甲基氨基芳基乙炔转化为氨基芳基乙炔。 在一个实施方案中,本发明提供了一种制备氨基苯基乙炔的方法,包括在碱和催化剂体系存在下使N-亚苄基氨基苯基卤与末端乙炔反应以制备新的N-亚苄基氨基苯基乙炔,并将N-亚苄基氨基苯基乙炔水解为 氨基苯乙炔。