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    Process for the preparation of imino-bridged benzocycloheptapyridines
    3.
    发明授权
    Process for the preparation of imino-bridged benzocycloheptapyridines 失效
    亚氨基桥联苯并环庚三烯的制备方法

    公开(公告)号：US4256889A

    公开(公告)日：1981-03-17

    申请号：US93410

    申请日：1979-11-13

    申请人： Kenneth L. Shepard ,  Daniel G. Brenner

    发明人： Kenneth L. Shepard ,  Daniel G. Brenner

    IPC分类号： C07D221/16 ,  C07D471/18

    CPC分类号： C07D221/16 ,  Y02P20/55 ,  Y10S514/906

    摘要： Benzocycloheptapyridines with an imine bridge in the cycloheptane ring, derivatives and pharmaceutically acceptable salts thereof are useful as anxiolytics, antidepressants, anticonvulsants, muscle relaxants and in the treatment of mixed anxiety-depression, minimal brain dysfunction and extrapyramidal disorders such as Parkinson's disease. They are prepared, for example, by treatment of a benzo[5,6]cyclohepta[1,2-c]pyridin-11-one with ammonia to give the 11-imine, acylation of the imine, treatment of the protected imine with an alkyllithium to provide the 11-alkyl-11-acylamino compound, treatment with acid or base to cause ring closure to an 11-alkyl-6,11-acylimino compound followed by removal of the protecting group, either hydrolytically or hydrogenolytically.

    摘要翻译： 在环庚烷环中具有亚胺桥的苯并环庚三烯类，其衍生物和药学上可接受的盐可用作抗焦虑剂，抗抑郁药，抗惊厥药，肌肉松弛剂和治疗混合焦虑抑郁症，最小脑功能障碍和锥体外系疾病如帕金森病。 它们例如通过用氨处理苯并[5,6]环庚并[1,2-c]吡啶-11-酮来制备，得到亚胺的11-亚胺，酰化，用保护的亚胺处理 烷基锂以提供11-烷基-11-酰氨基化合物，用酸或碱处理以引起闭环到11-烷基-6,11-酰亚氨基化合物，然后去除保护基团，水解或氢解。

    10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines
    4.
    发明授权
    10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines 失效
    10,11-二氢-5H-二苯并[a，d]环庚烯-5,10-亚胺

    公开(公告)号：US4232158A

    公开(公告)日：1980-11-04

    申请号：US045494

    申请日：1979-06-04

    申请人： Kenneth L. Shepard ,  Daniel G. Brenner

    发明人： Kenneth L. Shepard ,  Daniel G. Brenner

    IPC分类号： C07D221/02 ,  C07D451/02 ,  C07D487/08

    CPC分类号： C07D451/00 ,  Y02P20/55 ,  Y10S514/906

    摘要： 10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines, derivatives and pharmaceutically acceptable salts thereof are useful as antianxiety agents, as muscle relaxants and in the treatment of extrapyramidal disorders such as in Parkinson's disease. They are prepared by treatment of a 5H-dibenzo[a,d]cyclohepten-5-one with ammonia to give the 5-imine, acylation of the imine, treatment of the protected imine with an organolithium to provide the 5-substituted-5-acylamino compound, treatment with acid or base to cause ring closure to a 5-substituted-5,10-acylimino compound followed by removal of the protecting group, either hydrolytically or hydrogenolytically.

    摘要翻译： 10,11-二氢-5H-二苯并[a，d]环庚烯-5,10-亚胺，其衍生物和药学上可接受的盐可用作抗焦虑剂，肌肉松弛剂和治疗锥体外系疾病如帕金森氏病。 它们通过用氨处理5H-二苯并[a，d]环庚烯-5-酮制备，得到亚胺的5-亚胺酰化，用有机锂处理被保护的亚胺，得到5-取代-5 - 酰基氨基化合物，用酸或碱处理以使5-取代的5,10-酰亚氨基化合物闭环，然后除去水解或氢解的保护基。