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    • 3. 发明授权
    • Process for the preparation of 5-(4-[4-(5-cyano-3-indolyl)butyl]-1-piperazinyl)benzofuran-2-carboxamide
    • 制备5-(4- [4-(5-氰基-3-吲哚基)丁基] -1-哌嗪基)苯并呋喃-2-甲酰胺的方法
    • US07799916B2
    • 2010-09-21
    • US11912584
    • 2006-04-12
    • Andreas Bathe
    • Andreas Bathe
    • C07D405/12
    • C07D307/84C07D405/12
    • The invention relates to a process for the preparation of 5-(4-[4-(5-cyano-3-indolyl)butyl]-1-piperazinyl)benzofuran-2-carboxamide and/or one of its physiologically acceptable salts, characterized in that a compound of the formula (I), in which L denotes Cl, Br, I, SO2F, SO2CF3, SO2C2F5, is reacted with 3-(4-piperazin-1-ylbuyl)indole-5-carbonitrile by transition-metal-catalyzed coupling by means of Pd complexes, and/or in that the 5-(4[4-(5-cyano-3-indolyl)butyl]-1-piperazinyl)benzofuran-2-carboxamide formed is converted into one of its acid-addition salts by treatment with an acid, and to a second process, characterized in that a compound of the formula (II), as the base or HX salt (where X=Cl, BR), is reacted with 3-(4-oxobutyl)-1H-indole-5-carbonitrile by reductive amination, and/or in that 5-(4-[4-(5-cyano-3-indolyl)butyl]-1-piperazinyl)benzofuran-2-carboxamide is converted into one of its acid-addition salts by treatment with an acid.
    • 本发明涉及制备5-(4- [4-(5-氰基-3-吲哚基)丁基] -1-哌嗪基)苯并呋喃-2-甲酰胺和/或其生理上可接受的盐之一的方法,其特征在于 其中L表示Cl,Br,I,SO2F,SO2CF3,SO2C2F5的式(I)化合物与3-(4-哌嗪-1-基丁基)吲哚-5-甲腈通过过渡金属反应 通过Pd络合物的催化偶联,和/或由形成的5-(4 [4-(5-氰基-3-吲哚基)丁基] -1-哌嗪基)苯并呋喃-2-甲酰胺转化为其中的一种 通过用酸处理酸加成盐,以及第二种方法,其特征在于将式(II)化合物作为碱或HX盐(其中X = Cl,BR)与3-(4 - (4- [4-(5-氰基-3-吲哚基)丁基] -1-哌嗪基)苯并呋喃-2-甲酰胺为(4-氧代丁基)-1H-吲哚-5-甲腈,和/ 通过用酸处理转化为其酸加成盐之一。