Benzazocine derivatives
    1.
    发明授权
    Benzazocine derivatives 失效
    苯并噻唑衍生物

    公开(公告)号:US3686167A

    公开(公告)日:1972-08-22

    申请号:US3686167D

    申请日:1969-02-10

    CPC classification number: C07D307/14

    Abstract: BENZAZOCINE DERIVATIVES OF THE FORMULA:

    3-R4,6,6-DI(R2-),(R1)M-1,2,3,4,5,6-HEXAHYDRO-3-BENZAZOCINE

    WHEREIN R1 REPRESENTS METHOXY, HYDROXY, OR AN ACYLOXY GROUP, WITH THE PROVISO THAT TWO R1 GROUPS MAY TOGETHER FORM A ALKYLENEDIOXY GROUP, M IS AM INTEGER OF 1 TO 3, EACH R2 REPRESENTS AN ALKYL GROUP HAVING AT MOST 4 CARBON ATOMS, AND R4 STANDS FOR HYDROGEN, AN ALIPHATIC OR CYCLOALIPHATIC GROUP HAVING AT MOST 6 CARBON ATOMS, AN ARALKYL GROUP HAVING UP TO 10 CARBON ATOMS, AN ALKYLAMINOCARBONYLALKYL OR MONO-OR DI-ALKYLAMINOALKYL GROUP WHEREIN THE ALKYL HAS AT MOST 3 CARBON ATOMS, ALKYLCARBONYL OF UP TO 5 CARBON ATOMS, CYCLOPROPYLCARBONYL, BENZOYL, PHENYLACETYL, TOSSYL OR TETRAHYDROFURFURYL GROUP, ARE NON-NARCOTIC ANALGESIC COMPOUNDS.

    Process for preparing 1,4-benzodiazepin-2-ones
    5.
    发明授权
    Process for preparing 1,4-benzodiazepin-2-ones 失效
    制备1,4-苯并二苯并[2-ONES]的方法

    公开(公告)号:US3692772A

    公开(公告)日:1972-09-19

    申请号:US3692772D

    申请日:1969-09-03

    Abstract: The process for preparing benzodiazepin-2-one derivatives of the formula

    WHEREIN R1 is hydrogen or lower alkyl, and rings A and B are either unsubstituted or substituted by one or more groups of nitro, trifluoromethyl, halogen, alkyl and alkoxy groups, which comprises subjecting a 2-amino- Alpha phenylbenzylideneaminoacetal derivative to ring-closure, hydrolyzing the resultant product to obtain the 2hydroxybenzodiazepine derivative, and subjecting such derivative to oxidation to yield the benzodiazepin-2-one derivative. Also provided are novel 1-alkyl-2-hydroxybenzodiazepine derivatives of the formula

    WHEREIN R''1 is lower alkyl and rings A and B may be either unsubstituted or substituted as defined above, such derivatives being useful as intermediates in the above process and also as tranquilizing agents.

    Abstract translation: 制备式WHEREIN R1的苯并二氮杂-2-酮衍生物的方法是氢或低级烷基,环A和B是未取代的或被一个或多个硝基,三氟甲基,卤素,烷基和烷氧基基团取代,其包括 使2-氨基-α-苯基亚苄基氨基缩醛衍生物闭环,水解所得产物,得到2-羟基苯并二氮杂衍生物,并使该衍生物氧化得到苯并二氮杂-2-酮衍生物。 还提供了式WHEREIN R'1是低级烷基的新的1-烷基-2-羟基苯并二氮杂衍生物,A和B环可以是未取代的或如上所定义的取代基,这些衍生物可用作上述方法中的中间体,也可用作 镇静剂。

    2-iminobenzodiazepine derivatives
    6.
    发明授权
    2-iminobenzodiazepine derivatives 失效
    2-咪唑烷酮衍生物

    公开(公告)号:US3687941A

    公开(公告)日:1972-08-29

    申请号:US3687941D

    申请日:1969-07-08

    CPC classification number: C07C255/00

    Abstract: WITH A COMPOUND OF THE FORMULA
    Compounds of the formula

    WHEREIN R1 has the same meaning as above and the respective benzene rings A and B may have one or more substituents as defined above to a ring closure reaction. Compounds of the formula II are produced by reacting a compound of the formula

    WHEREIN R1 is hydrogen or alkyl and the respective benzene rings A and B may have one or more substituents which are the same or different and selected from the group consisting of halogen, nitro, trifluoromethyl, alkyl and alkoxy are prepared by subjecting a compound of the formula

    WHEREIN R1 has the same meaning as defined above and R2 is hydrogen, alkyl, hydroxyalkyl or aralkyl with aminoacetonitrile. Compounds of the formula III are produced by reacting a compound of the formula

    Abstract translation: 式WHERE R1的化合物是氢或烷基,相应的苯环A和B可以具有一个或多个相同或不同的取代基,选自卤素,硝基,三氟甲基,烷基和烷氧基,通过使 式WHEREIN R 1具有与上述相同含义的化合物,并且相应的苯环A和B可具有一个或多个如上定义的取代基进行闭环反应。 通式II的化合物通过使式WHEREIN R 1具有与上述相同的含义并且R 2是氢,烷基,羟基烷基或芳烷基与氨基乙腈反应来制备。 式III的化合物通过使下式的化合物与其中R2是氢,烷基,羟基烷基或芳烷基的式R2NH2的化合物反应来制备。

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