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    Butadiene derivatives, their preparation and use as an antithrombotic agent
    2.
    发明公开
    Butadiene derivatives, their preparation and use as an antithrombotic agent 失效
    Butadienderivate，ihre Herstellung und Verwendung als antithrombotisches Mittel。

    公开(公告)号：EP0563798A1

    公开(公告)日：1993-10-06

    申请号：EP93104977.9

    申请日：1993-03-25

    申请人： TANABE SEIYAKU CO., LTD.

    发明人： Iwasaki, Tameo ,  Nishitani, Takashi ,  Ohtani, Akio ,  Inamasu, Masanori

    IPC分类号： C07D207/02 ,  C07C235/34 ,  A61K31/40 ,  A61K31/225 ,  C07D213/40 ,  C07D295/125 ,  A61K31/44 ,  A61K31/535 ,  C07D207/46 ,  C07D207/50 ,  C07D401/06 ,  C07C69/602

    CPC分类号： C07D207/02 ,  A61K31/225 ,  A61K31/40 ,  C07C235/34 ,  C07C243/32 ,  C07D401/06

    摘要： Novel butadiene derivatives of the formula [I]:

    wherein Ring A is tri-lower alkoxyphenyl, R¹ and R² combine each other to form a group of the formula:



            〉N-R³



    or one of R¹ and R² is lower alkoxy, and the other is group of the formula: -NHR³, in which R³ is hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted amino, hydroxy or pyridylcarbonyl, or salts thereof.
    Among the desired butadiene derivatives [I] of the present invention, the 3-butenoic acid-type compounds per se have antithrombotic activity, but they can also be used as an intermediate for preparing the 2,5-pyrrolidinedione-type compounds having excellent antithrombotic activity. And additionally a butenoic acid ester of the formula [II]:

    wherein Ring A is a tri-lower alkoxyphenyl group, and one of R¹² and R²² is a lower alkoxy group, and the other is hydroxy group, or a salt thereof, as synthetic intermediate.

    摘要翻译： 式[I]的新型丁二烯衍生物：其中环A是三低级烷氧基苯基，R 1和R 2彼此结合形成下式的基团：其中R 1和R 3之一或 R 1和R 2是低级烷氧基，另一个是式-NHR 3的基团，其中R 3是氢，取代或未取代的低级烷基，取代或未取代的低级烷氧基，取代的 或未取代的氨基，羟基或吡啶基羰基，或其盐。 在本发明的所需丁二烯衍生物[I]中，3-丁烯酸类化合物本身具有抗血栓形成活性，但也可以用作制备具有优异抗血栓形成的2,5-吡咯烷二酮型化合物的中间体 活动。 另外，式[II]的丁烯酸酯：其中环A是三低级烷氧基苯基，R 1和R 2之一是低级烷氧基 ，另一种是羟基，或其盐作为合成中间体。