Thiazinobenzimidazole derivatives
    1.
    发明授权
    Thiazinobenzimidazole derivatives 失效
    噻嗪基苯并咪唑衍生物

    公开(公告)号:US4450109A

    公开(公告)日:1984-05-22

    申请号:US417596

    申请日:1982-09-13

    CPC分类号: C07D513/04

    摘要: The specification describes novel thiazinobenzimidazole derivatives represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2 and X represent a wide variety of substituent groups respectively. The above thiazinobenzimidazole derivatives may be prepared by reacting corresponding 2-hydroxymethyl thiazinobenzimidazole derivatives with corresponding reactive derivatives of carboxylic acid or halogenide or by reacting 2-p-toluenesulfonyloxymethyl-thiazinobenzimidazole derivatives with sodium azides, thiols, phenols or amines. The above thiazinobenzimidazole derivatives wherein X is OH may be prepared by reducing their corresponding 2-alkoxycarbonyl derivatives. Where X represents a p-toluenesulfonyloxy group, the thiazinobenzimidazole derivatives may be obtained by reacting corresponding 2-hydroxymethyl-thiazinobenzimidazole derivatives with p-toluenesulfonyl chloride. Where X stands for an N-substituted 2-(homo)piperazinomethyl group, 2-(homo)piperazinomethyl-thiazinobenzimidazole derivatives are reacted with reactive compounds to introduce the desired substituent groups. The thiazinobenzimidazole derivatives according to this invention are useful as medicament for circulatory systems.

    摘要翻译: 该说明书描述了由以下通式表示的新型噻唑并苯并咪唑衍生物:其中R1,R2和X分别代表多种取代基。 上述噻唑并苯并咪唑衍生物可以通过使相应的2-羟甲基噻嗪基苯并咪唑衍生物与羧酸或卤化物的相应反应性衍生物反应或通过2-对甲苯磺酰氧甲基 - 噻嗪基苯并咪唑衍生物与叠氮化钠,硫醇,酚或胺的反应来制备。 其中X是OH的上述噻嗪基苯并咪唑衍生物可以通过还原它们相应的2-烷氧基羰基衍生物来制备。 当X代表对甲苯磺酰氧基时,噻吩并苯并咪唑衍生物可以通过相应的2-羟甲基 - 噻嗪基苯并咪唑衍生物与对甲苯磺酰氯反应而得到。 其中X代表N-取代的2-(均)哌嗪基甲基,2-(高)哌嗪基甲基 - 噻嗪基苯并咪唑衍生物与反应性化合物反应以引入所需的取代基。 根据本发明的噻嗪基苯并咪唑衍生物可用作循环系统的药物。

    Thiazinobenzimidazole derivatives
    2.
    发明授权
    Thiazinobenzimidazole derivatives 失效
    噻嗪基苯并咪唑衍生物

    公开(公告)号:US4369309A

    公开(公告)日:1983-01-18

    申请号:US240219

    申请日:1981-03-03

    CPC分类号: C07D513/04

    摘要: The specification describes novel thiazinobenzmidazole derivatives represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2 and X represent a wide variety of substituent groups respectively. The above thiazinobenzimidazole derivatives may be prepared by reacting corresponding 2-hydroxymethyl thiazinobenzimidazole derivatives with corresponding reactive derivatives of carbonylic acid or halogenide or by reacting 2-p-toluenesulfonyloxymethyl-thiazinobenzimidazole derivatives with sodium azides, thiols, phenols or amines. The above thiazinobenzimidazole derivatives wherein X in OH may be prepared by reducing their corresponding 2-alkoxycarbonyl derivatives. Where X represents a p-toluenesulfonyloxy group, the thiazinobenzimidazole derivatives may be obtained by reacting corresponding 2-hydroxymethyl-thiazinobenzimidazole derivatives with p-toluenesulfonyl chloride. Where X stands for an N-substituted 2-(homo)piperazinomethyl group, 2-(homo)piperazinomethyl-thiazinobenzimidazole derivatives are reacted with reactive compounds to introduce the desired substituent groups. The thiazinobenzimidazole derivatives according to this invention are useful as medicament for circulatory systems.

    摘要翻译: 该说明书描述了由以下通式表示的新型噻嗪并咪唑衍生物:其中R1,R2和X分别代表各种各样的取代基。 上述噻唑并苯并咪唑衍生物可以通过使相应的2-羟甲基噻嗪基苯并咪唑衍生物与羰基酸或卤化物的相应反应性衍生物反应,或通过2-对甲苯磺酰氧基甲基 - 噻嗪基苯并咪唑衍生物与叠氮化钠,硫醇,酚或胺反应来制备。 其中X中的X可以通过还原其相应的2-烷氧基羰基衍生物来制备上述噻唑并苯并咪唑衍生物。 当X代表对甲苯磺酰氧基时,噻吩并苯并咪唑衍生物可以通过相应的2-羟甲基 - 噻嗪基苯并咪唑衍生物与对甲苯磺酰氯反应而得到。 其中X代表N-取代的2-(均)哌嗪基甲基,2-(高)哌嗪基甲基 - 噻嗪基苯并咪唑衍生物与反应性化合物反应以引入所需的取代基。 根据本发明的噻嗪基苯并咪唑衍生物可用作循环系统的药物。