首页> 外国专利> N- 3-Dimethylamino-2-(4-pyridinyl)-2-propenylidene!-N- methylmethaniminium chloride hydrochloride, its use in preparing 5-(cyano or carbamyl)- 3,4'- bipyridin!-6(1H)-one and its use as a cardiotonic

N- 3-Dimethylamino-2-(4-pyridinyl)-2-propenylidene!-N- methylmethaniminium chloride hydrochloride, its use in preparing 5-(cyano or carbamyl)- 3,4'- bipyridin!-6(1H)-one and its use as a cardiotonic

机译:N-3-二甲基氨基-2-(4-吡啶基)-2-丙烯基!-N-甲基甲基氯化铵盐酸盐,其用于制备5-(氰基或氨基甲酰基)-3,4'-联吡啶!-6(1H)-一种及其作为强心剂的用途

摘要

Amrinone intermediates are prepared by reacting 4-picoline with at least three mole equivalents of phosgene per mole of 4-picoline and excess dimethylformamide to produce N-[3-dimethylamino-2-(4-pyridinyl)-2-propenylidene]-N-methylmethaniminium chloride hydrochloride, then reacting the latter with Q-CH2CONH2 and at least three mole equivalents of base in anhydrous medium and then neutralizing the reaction mixture to produce 5-Q-[3,4'-bipyridin]-6(1H)-one, where Q is cyano or carbamyl. Other aspects of the invention are the separate steps of preparing said iminium salt and then converting it to said 5-Q-[3,4'-bipyridin]-6(1H)-one, and also cardiotonic composition and method for increasing cardiac contractility using said iminium salt or pharmaceutically-acceptable acid-addition salt thereof as the active cardiotonic.
机译:通过使4-甲基吡啶与至少三摩尔当量的光气/摩尔4-甲基吡啶和过量的二甲基甲酰胺反应以生成N- [3-二甲基氨基-2-(4-吡啶基)-2-丙烯基] -N-来制备氨力农中间体。甲基甲基氯化铵盐酸盐,然后使后者与Q-CH2CONH2和至少三摩尔当量的碱在无水介质中反应,然后中和反应混合物以生成5-Q- [3,4'-联吡啶] -6(1H)- ,其中Q是氰基或氨基甲酰基。本发明的其他方面是制备所述亚胺盐然后将其转化为所述5-Q- [3,4'-联吡啶] -6(1H)-one的单独步骤,以及用于增强心脏收缩力的强心剂组合物和方法使用所述亚胺盐或其药学上可接受的酸加成盐作为活性强心药。

著录项

  • 公开/公告号NO156689B

    专利类型

  • 公开/公告日1987-07-27

    原文格式PDF

  • 申请/专利权人 STERLING DRUG INC.;

    申请/专利号NO19810000639

  • 申请日1981-02-25

  • 分类号C07D213/53;C07D213/84;

  • 国家 NO

  • 入库时间 2022-08-22 07:19:53

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