申请人:Catalytica Pharmaceuticals, Inc.
公开号:US06100429A1
公开(公告)日:2000-08-08
This invention provides a process for preparing aminoarylacetylenes comprising reacting a 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 a 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
该发明提供了一种制备氨基芳基乙炔的过程,包括在碱和催化剂体系(包括钯催化剂和铜盐)的存在下,将N-芳基甲基亚胺氨基芳基卤化物与末端炔反应,以产生新型的N-芳基甲基亚胺氨基芳基乙炔,并水解N-芳基甲基亚胺氨基芳基乙炔为氨基芳基乙炔。在一种实施方式中,该发明提供了一种制备氨基苯乙炔的过程,包括在碱和催化剂体系的存在下,将N-苄亚甲基氨基苯卤化物与末端炔反应,以产生新型的N-苄亚甲基氨基苯乙炔,并水解N-苄亚甲基氨基苯乙炔为氨基苯乙炔。