Method of preparation of halogenated diazines
    2.
    发明授权
    Method of preparation of halogenated diazines 失效
    卤代二嗪的制备方法

    公开(公告)号:US5304647A

    公开(公告)日:1994-04-19

    申请号:US572676

    申请日:1990-08-24

    摘要: A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof.The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product.The substituted halogenodiazines are used as intermediates in the synthesis of unfused heterobicyclic compounds containing an aromatic moiety, diazine, and another aromatic moiety, such as thiophene, benzene, or naphthalene, which have biological activity.

    摘要翻译: 一种制备取代的卤代二氮的方法,其可用作合成新型未取代杂双环化合物的中间体及其产物。 该反应包括加入有机锂试剂,随后加成产物脱氢。 反应在一个反应​​容器中进行,而不分离取代的卤代二氢二嗪中间体。 反应在中等温度和短时间内进行,这降低了副反应的可能性并提高了产率。 此外,后处理步骤在两相条件下进行以防止取代的卤代二嗪水解成取代的羟基二嗪。 该方法简单,高效,产品成品率高。 取代的卤代二嗪用作合成含有芳族部分,二嗪和其它具有生物活性的其它芳族部分如噻吩,苯或萘的未稠合的杂双环化合物的中间体。

    Di-substituted phthalazines
    4.
    发明授权
    Di-substituted phthalazines 失效
    二取代酞嗪

    公开(公告)号:US4963676A

    公开(公告)日:1990-10-16

    申请号:US400502

    申请日:1989-08-30

    摘要: A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof.The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product.The substituted halogenodiazines are used as intermediates in the synthesis of novel unfused heterobicyclic compounds containing an aromatic moiety, diazine, and another aromatic moiety, such as thiophene, benzene, or naphthalene, which have biological activity.

    摘要翻译: 一种制备取代的卤代二氮的方法,其可用作合成新型未取代杂双环化合物的中间体及其产物。 该反应包括加入有机锂试剂,随后加成产物脱氢。 反应在一个反应​​容器中进行,而不分离取代的卤代二氢二嗪中间体。 反应在中等温度和短时间内进行,这降低了副反应的可能性并提高了产率。 此外,后处理步骤在两相条件下进行以防止取代的卤代二嗪水解成取代的羟基二嗪。 该方法简单,高效,产品成品率高。 取代的卤代二嗪用作合成含有芳族部分,二嗪和另外具有生物活性的其它芳族部分如噻吩,苯或萘的新型未稠合的杂双环化合物的中间体。

    Novel diazines and their method of preparation
    8.
    发明授权
    Novel diazines and their method of preparation 失效
    新型二嗪类及其制备方法

    公开(公告)号:US4929726A

    公开(公告)日:1990-05-29

    申请号:US153998

    申请日:1988-02-09

    摘要: A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof.The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product.The substituted halogenodiazines are used as intermediates in the synthesis of novel unfused heterobicyclic compounds containing an aromatic moiety, diazine, and another aromatic moiety, such as thiophene, benzene, or naphthalene, which have biological activity.

    摘要翻译: 一种制备取代的卤代二氮的方法,其可用作合成新型未取代杂双环化合物的中间体及其产物。 该反应包括加入有机锂试剂,随后加成产物脱氢。 反应在一个反应​​容器中进行,而不分离取代的卤代二氢二嗪中间体。 反应在中等温度和短时间内进行,这降低了副反应的可能性并提高了产率。 此外,后处理步骤在两相条件下进行以防止取代的卤代二嗪水解成取代的羟基二嗪。 该方法简单,高效,产品成品率高。 取代的卤代二嗪用作合成含有芳族部分,二嗪和另外具有生物活性的其它芳族部分如噻吩,苯或萘的新型未稠合的杂双环化合物的中间体。