Benzodiazepine-diones, a process for their production and their use as
medicaments
    1.
    发明授权
    Benzodiazepine-diones, a process for their production and their use as medicaments 失效
    苯二氮卓类药物,其生产过程及其用作药物

    公开(公告)号:US4187306A

    公开(公告)日:1980-02-05

    申请号:US922419

    申请日:1978-07-06

    摘要: The invention covers compounds of the formula ##STR1## in which R.sup.1 and R.sup.5 each represents 0, 1, 2, 3 or 4 of the following substituents: alkyl, hydroxyl, acyloxy, alkoxy, nitro, amino, alkylamino, dialkylamino, acylamino, acylalkylamino, alkoxycarbonylamino, halogen, trifluoromethyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, aminosulphonyl, alkylaminosulphonyl, dialkylaminoamino, R.sup.2 is hydrogen, optionally substituted alkyl, aralkyl or aryl or heterocyclo-alkyl, acyl or alkoxycarbonyl, and R.sup.3 and R.sup.4 are each hydrogen, or optionally substituted alkyl, aralkyl, aryl or hetero-aryl, are useful as medicaments which have an action on the central nervous system, in particular as, for example, tranquilizers and/or antiamnesics. Also included in the invention are methods for preparing said compounds, compositions containing them and methods for the use of said compounds and compositions.

    摘要翻译: 本发明涵盖下式的化合物,其中R 1和R 5各自表示0,1,2,3或4个以下取代基:烷基,羟基,酰氧基,烷氧基,硝基,氨基,烷基氨基,二烷基氨基,酰氨基,酰基烷基氨基 烷氧基羰基,氨基羰基,氨基磺酰基,烷基氨基磺酰基,二烷基氨基氨基,R2是氢,任意取代的烷基,芳烷基或芳基或杂环烷基,酰基或烷氧基羰基,R3和R4是 每个氢或任选取代的烷基,芳烷基,芳基或杂芳基可用作对中枢神经系统具有作用的药物,特别是例如镇定剂和/或抗病毒药物。 本发明还包括制备所述化合物的方法,含有它们的组合物和使用所述化合物和组合物的方法。

    Process for the preparation of tetrachloropyrimidine
    3.
    发明授权
    Process for the preparation of tetrachloropyrimidine 失效
    四氯嘧啶的制备方法

    公开(公告)号:US4125722A

    公开(公告)日:1978-11-14

    申请号:US842976

    申请日:1977-10-17

    IPC分类号: C07D239/30 C07D239/24

    CPC分类号: C07D239/30

    摘要: Process for the preparation of tetrachloropyrimidine, characterized in that compounds of the formula ##STR1## wherein R = a radical which can be split off under the reaction conditions,Are reacted with chlorine or agents which release chlorine, preferably at temperatures from 0.degree.-150.degree. C and using more than 7 mols of chlorine, in particular using 11-13 mols of chlorine.

    摘要翻译: 制备四氯嘧啶的方法,其特征在于下式化合物其中R =可在反应条件下分离的基团,与氯离子反应,或在0°-150℃温度下优选释放出氯离子 DEG,并使用大于7摩尔的氯,特别是使用11-13摩尔的氯。

    Process for the preparation of 2,4,5-trichloropyrimidine
    6.
    发明授权
    Process for the preparation of 2,4,5-trichloropyrimidine 失效
    制备2,4,5-三氯嘧啶的方法

    公开(公告)号:US4171442A

    公开(公告)日:1979-10-16

    申请号:US913119

    申请日:1978-06-06

    IPC分类号: C07D239/30 C07D239/20

    CPC分类号: C07D239/30

    摘要: Process for the preparation of 2,4,5-trichloropyrimidine, characterized in that compounds of the formula ##STR1## wherein R a radical which can be split off under the reaction conditions andR' an optionally substituted lower alkyl radical,Are reacted at temperatures from 0.degree. to 50.degree. C. with less than 7.5 mols of chlorine, in particular 3.5 to 7.0 mols of chlorine, and the reaction products are then after-heated to temperatures of 100.degree.-150.degree. C., in particular 110.degree.-140.degree. C., in the absence of chlorine.

    摘要翻译: 制备2,4,5-三氯嘧啶的方法,其特征在于下式化合物其中R为在反应条件下可分离的基团,R'为任选取代的低级烷基,在温度下反应 从0℃至50℃,小于7.5摩尔氯,特别是3.5至7.0摩尔氯,然后将反应产物后加热至100-150℃,特别是110℃ - 140℃,没有氯气。

    2,5-Dichloro-thiazolo[4,5-d]thiazole and process for making same
    7.
    发明授权
    2,5-Dichloro-thiazolo[4,5-d]thiazole and process for making same 失效
    2,5-Dichloro-thiazolo {8 4,5-d {9噻唑及其制备方法

    公开(公告)号:US3994913A

    公开(公告)日:1976-11-30

    申请号:US626410

    申请日:1975-10-28

    IPC分类号: A01N43/90 C07D513/04

    CPC分类号: C07D513/04

    摘要: 2,5-Dichloro-thiazolo[4,5-d]thiazole, which is useful as a fungicide, is prepared by reacting compounds having the formula ##EQU1## wherein X.sub.1 is Cl, andX.sub.2 is H or Cl orX.sub.1 and X.sub.2 together form a C-C bondIn the temperature range of 150.degree. to 300.degree. C, with at least the stoichiometrically required amount of sulphur.

    摘要翻译: 可用作杀真菌剂的2,5-二氯 - 噻唑并[4,5-d]噻唑通过使具有下式的化合物N = CCl 2 CCl 2 -CCl-CH 2 N 2 CCl 2 / XX 2(其中X 1为Cl)和 X 2是H或Cl或X 1和X 2在一般的150℃至300℃的温度范围内一起形成CC键,至少具有所需的化学计量量的硫。

    Process for the preparation of 2,4,5-trichloropyrimidine
    9.
    发明授权
    Process for the preparation of 2,4,5-trichloropyrimidine 失效
    制备2,4,5-三氯嘧啶的方法

    公开(公告)号:US4140857A

    公开(公告)日:1979-02-20

    申请号:US868727

    申请日:1978-01-11

    IPC分类号: C07D239/30 C07D239/02

    CPC分类号: C07D239/30

    摘要: Process for the preparation of 2,4,5-trichloropyrimidine, characterized in that compounds of the formula ##STR1## wherein R = a radical which can be split off under the reaction conditionsAre reacted with more than 7 and less than 13 mols of chlorine, in particular 11 mols of chlorine, at temperatures from 0 - 40.degree. C. and the reaction mixture is then subsequently heated in the absence of chlorine to temperatures from about 100 - 150.degree. C., in particular 110 - 140.degree. C.

    摘要翻译: 制备2,4,5-三氯嘧啶的方法,其特征在于下式化合物其中R =可在反应条件下分解的基团反应多于7,氯化物少于13摩尔 ,特别是氯化钠,在0-40℃的温度下,然后将反应混合物随后在不存在氯的情况下加热至约100-150℃,特别是110-140℃的温度。