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    1,4-Benzodiazepin-2-ones and their synthesis
    1.
    发明授权
    1,4-Benzodiazepin-2-ones and their synthesis 失效
    1,4-苯并二氮杂-2-酮及其合成

    公开(公告)号：US3926952A

    公开(公告)日：1975-12-16

    申请号：US43811574

    申请日：1974-01-30

    Applicant: AMERICAN HOME PROD

    Inventor： MCCAULLY RONALD J

    IPC: C07D243/24 ,  C07D243/28 ,  C07D243/26

    CPC classification number: C07D243/24

    Abstract: 2-Aminobenzophenone anti-oximes are converted to heretofore undescribed dihydroxyacetanilide derivatives, which are useful for preparing known 1,4-benzodiazepin-2-ones.

    Abstract translation: 将2-氨基二苯甲酮抗肟转化为迄今未描述的二羟基乙酰替苯胺衍生物，其可用于制备已知的1,4-苯并二氮杂-2-酮。

    Intermediates for the preparation of 1,3-dihydro-2H-1,4-benzodiazepin-2-ones
    2.
    发明授权
    Intermediates for the preparation of 1,3-dihydro-2H-1,4-benzodiazepin-2-ones 失效
    用于制备1,3-二氢-2H-1,4-苯并二氮杂-2-酮的中间体

    公开(公告)号：US3899527A

    公开(公告)日：1975-08-12

    申请号：US33286173

    申请日：1973-02-15

    Applicant: AMERICAN HOME PROD

    Inventor： MCCAULLY RONALD J

    IPC: C07D243/24 ,  C07C69/16 ,  C07C69/28

    CPC classification number: C07D243/24

    Abstract: Two routes for the preparation of 2-(2-acylamido-2-amino)acetamidophenyl aryl ketones, used as intermediates in the synthesis of psycholeptic 1,3-dihydro-2H-1,4-benzodiazepin-2-ones are described. The first of these routes involves the formation of a 2-(2,2-diacyloxy)acetamidophenyl aryl ketone from glyoxylic acid and an aryl phenyl ketone via either a 2,2-diacyloxy acetyl halide or a 2,2-diacyloxy acetyl anhydride, conversion thereof to the corresponding 2-(2-acylamido-2-hydroxy) acetamidophenyl aryl ketone directly or via the 2-(2,2-dihydroxy)acetamidophenyl aryl ketone, formation of the corresponding 2-(2-acylamido-2halo)acetamidophenyl aryl ketone, and conversion to the 2-(2acylamido-2-amino)acetamidophenyl aryl ketone. The second route forms the 2-(2,2-dihydroxy)acetamidophenyl aryl ketone by reacting a 2,3-dicarboxylicacyl tartaric anhydride with a 2aminophenyl aryl ketone to obtain a 2-(3-carboxy-2,3acyloxy)propionamidophenyl aryl ketone, selectively hydrolyzing the so-obtained ketone and selectively oxidizing the product with a vic glycol cleaving agent.

    Abstract translation: 描述了用于合成心律肽1,3-二氢-2H-1,4-苯并二氮杂-2-酮的2-（2-酰基氨基-2-氨基） - 乙酰氨基苯基芳基酮的两条途径。 这些路线中的第一个涉及通过2,2-二酰氧基乙酰卤或2,2-二酰氧基乙酰酐从乙醛酸和芳基苯基酮形成2-（2,2-二酰氧基）乙酰氨基苯基芳基酮， 直接或通过2-（2,2-二羟基）乙酰氨基苯基芳基酮将其转化成相应的2-（2-酰基酰氨基-2-羟基）乙酰氨基苯基芳基酮，形成相应的2-（2-酰基酰胺基-2-卤代 ）乙酰氨基苯基芳基酮，并转化成2-（2-酰基氨基-2-氨基）乙酰氨基苯基芳基酮。 第二种途径通过2,3-二甲酰基酒石酸酐与2-氨基苯基芳基酮反应形成2-（2,2-二羟基）乙酰氨基苯基芳基酮，得到2-（3-羧基-2,3-酰氧基） 丙酰胺基苯基芳基酮，选择性水解所得酮并用维生素二醇裂解剂选择性氧化产物。

    1,3-Dihydro-3 -hydroxy-5-phenyl-2H-1,4-benzodiazepin-2-one, substituted diamino acetate esters and their acid salts in compositions and methods for inducing a calming effect
    7.
    发明授权
    1,3-Dihydro-3 -hydroxy-5-phenyl-2H-1,4-benzodiazepin-2-one, substituted diamino acetate esters and their acid salts in compositions and methods for inducing a calming effect 失效
    1,3-二氢-3-羟基-5-苯基-2H-1,4-苯并二氮杂-2-酮，取代二氨基乙酸酯及其酸盐，用于诱导镇静作用的组合物和方法

    公开(公告)号：US3886276A

    公开(公告)日：1975-05-27

    申请号：US41074173

    申请日：1973-10-29

    Applicant: AMERICAN HOME PROD

    Inventor： MCCAULLY RONALD J ,  NUDELMAN ABRAHAM ,  BELL STANLEY C

    IPC: A61K31/55 ,  C07D243/24 ,  C07D403/06 ,  A61K27/00

    CPC classification number: C07D243/24 ,  A61K31/55 ,  C07D403/06

    Abstract: This invention is directed to novel central nervous system depressants of Formula I:

    wherein R1 is selected from the group consisting of (lower)alkyl and ar(lower)alkyl; R2 is selected from the group consisting of di(lower)alkylamino(lower)alkyl and diaryl(lower)alkylamino(lower)alkyl; R1 and R2 may be concatenated to form a radical selected from the group consisting of

    WHEREIN R4 is selected from the group consisting of (lower)alkyl, aryl, hydroxy(lower)alkyl, ar(lower)alkyl and (lower)alkoxy(lower)alkyl; R5 is selected from the group consisting of (lower)-alkylamino and piperidino; n is an integer from 3 to 5; m is an integer from 1 - 2; r is an integer from 2 to 3; s is an integer from 0 to 6; t is an integer from 0 - 6; with the proviso that the sum of s and t is 3 to 6; R3 is selected from the group consisting of hydrogen, (lower)alkyl, ar(lower)alkyl and (lower)alkoxy(lower)alkyl; X is selected from the group consisting of halogen, cyano, trifluoromethyl, nitro and (lower)alkylthio; Y is selected from the group consisting of hydrogen, halogen, trifluoromethyl, nitro and (lower)alkylthio; and the pharmaceutically acceptable salts thereof, in addition to the method of their preparation and administration and administrable compositions containing the active compounds.

    Abstract translation: 本发明涉及式I的新型中枢神经系统抑制剂：

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