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    PROCESS FOR THE PREPARATION OF 2-HYDROXY ETHYLIDENE-CYANO ACETIC ANILIDE
    1.
    发明授权
    PROCESS FOR THE PREPARATION OF 2-HYDROXY ETHYLIDENE-CYANO ACETIC ANILIDE 失效

    公开(公告)号：KR800000742B1

    公开(公告)日：1980-08-02

    申请号：KR760001516

    申请日：1976-06-18

    Applicant: HOECHST AG

    Inventor： HEUBACH G ,  ERTEL H ,  WOLF E

    IPC: C07C121/417

    Abstract: Title compds. (I, R1, R2, R3 = C1-3 alkyl, C1-3 alkoxy, C1-3 alkylthio, halogen, nitro, cyano, alkoxycarbonyl; M = H, alkali metal, ammonium), useful as an antiphlogistics or an anodyne, were prepd. by heating acetoacetic anilide(II) with formic ester(III) and followed by treating with acetic anhydride to give 2-alkixy-methylene-acetoacetic anilide(IV). The reaction of IV with hydroxyamine in org. solvent gave isoxazole(V), which was reacted with base and followed by reacting with org. strong acid to give I.

    Tranquilizer composition and method of treatment
    4.
    发明授权
    Tranquilizer composition and method of treatment 失效
    TRANQUILIZER组合物和处理方法

    公开(公告)号：US3849559A

    公开(公告)日：1974-11-19

    申请号：US34020973

    申请日：1973-03-12

    Applicant: HOECHST AG

    Inventor： HAERTFELDER G ,  WOLF E ,  KOHL H

    IPC: C07F9/53 ,  C07F9/645 ,  A61K27/00

    CPC classification number: C07F9/645 ,  C07F9/5304

    Abstract: 1. PHARMACEUTICAL PREPARATION HAVING TRANQUILIZING PROPERTIES CONTAINING AN EFFECTIVE AMOUNT OF AN ACTIVE COMPOUND OF THE FORMULA

    1-((R3)2-P(=O)-(CH2)N-),2-(O=),5-(R2-PHENYL-),R1-1,2-

    DIHYDRO-3H-1,4-BENZODIAZEPINE

    IN WHICH R1 AND R2, WHICH MAY BE IDENTICAL OR DIFFERENT, EACH REPRESENT A HYDROGEN ATOM, A NITRO GROUP, A HALOGEN ATOM OR THE TRIFLUOROMETHYL GROUP AND R2 IN ADDITION MAY REPRESENT A STRAIGHT CHAIN OR BRANCHED ALKYL GROUP HAVIN 1 TO 6 CARBON ATOMS, R3 REPRESENTS A STRAIGHT CHAIN OR BRANCHED ALKYL GROUP HAVING 1 TO 3 CARBON ATOMS, AND N IS A NUMBER FROM 1 TO 6, AND A PHARMACEUTICALLY TOLERABLE 0022ADJUVANT OR EXCIPIENT.

    7.
    发明专利
    未知

    公开(公告)号：SE374115B

    公开(公告)日：1975-02-24

    申请号：SE587471

    申请日：1971-05-06

    Applicant: HOECHST AG

    Inventor： WOLF E ,  KOHL H ,  HERTFELDER G

    IPC: C07F9/53 ,  C07F9/645 ,  C07D53/06 ,  C07F9/50

    Abstract: 1345443 Phosphorus-containing benzodiazepine derivatives FARBWERKE HOECHST AG 5 May 1971 [8 May 1970 23 Sept 1970] 13207/71 Heading C2P [Also in Division A5] The invention comprises a phosphorus-containing benzodiazepine derivative of the general formula wherein R 1 is H, NO 2 , a halogen atom, or CF 3 , R 2 is a straight or branched chain alkyl group having up to 8 carbon atoms, a hydrogen atom, a halogen atom, NO 2 or CF 3 , R 3 is a straight chain or branched chain alkyl group having up to 3 carbon atoms and n is an integer from 1 to 6: They may be obtained by (a) reacting a metal derivative of the formula wherein M is a metal cation with a phosphine oxide of the formula X(CH 2 ) n P(O)(R 3 ) 2 , wherein X is a halogen atom or an alkyl (or aryl-) sulphonyloxy group, or (b) by reacting a compound of the formula with a derivative of amino acetic acid (preferably an ester, e.g. an imino or ortho ester derivative) or (c) by reacting a compound of the above Formula IV with a halide or azide of a halogenoacetic acid, treating the product with ammonia and then cyclizing the compound so obtained. In reaction (a) the metal compound can first be formed by heating the appropriate 1-unsubstituted benzodiazepine with, e.g., Ca-, Na- or Li-hydride or with potassium tertbutylate or sodium methylate in an inert organic solvent and the product may then be formed directly by reaction with the compound X(CH 2 ) n P(O)(R 3 ) 2 in the same solvent without isolation of the metal derivative. The products are useful as tranquillizers.

    8.
    发明专利
    未知

    公开(公告)号：CH552020A

    公开(公告)日：1974-07-31

    申请号：CH631074

    申请日：1971-05-05

    Applicant: HOECHST AG

    Inventor： WOLF E ,  KOHL H ,  HERTFELDER G

    IPC: C07F9/53 ,  C07F9/645 ,  C07F9/28

    Abstract: 1345443 Phosphorus-containing benzodiazepine derivatives FARBWERKE HOECHST AG 5 May 1971 [8 May 1970 23 Sept 1970] 13207/71 Heading C2P [Also in Division A5] The invention comprises a phosphorus-containing benzodiazepine derivative of the general formula wherein R 1 is H, NO 2 , a halogen atom, or CF 3 , R 2 is a straight or branched chain alkyl group having up to 8 carbon atoms, a hydrogen atom, a halogen atom, NO 2 or CF 3 , R 3 is a straight chain or branched chain alkyl group having up to 3 carbon atoms and n is an integer from 1 to 6: They may be obtained by (a) reacting a metal derivative of the formula wherein M is a metal cation with a phosphine oxide of the formula X(CH 2 ) n P(O)(R 3 ) 2 , wherein X is a halogen atom or an alkyl (or aryl-) sulphonyloxy group, or (b) by reacting a compound of the formula with a derivative of amino acetic acid (preferably an ester, e.g. an imino or ortho ester derivative) or (c) by reacting a compound of the above Formula IV with a halide or azide of a halogenoacetic acid, treating the product with ammonia and then cyclizing the compound so obtained. In reaction (a) the metal compound can first be formed by heating the appropriate 1-unsubstituted benzodiazepine with, e.g., Ca-, Na- or Li-hydride or with potassium tertbutylate or sodium methylate in an inert organic solvent and the product may then be formed directly by reaction with the compound X(CH 2 ) n P(O)(R 3 ) 2 in the same solvent without isolation of the metal derivative. The products are useful as tranquillizers.

    9.
    发明专利
    未知

    公开(公告)号：FR2100639B1

    公开(公告)日：1974-04-12

    申请号：FR7116571

    申请日：1971-05-07

    Applicant: HOECHST AG

    Inventor： WOLF E ,  KOHL H ,  HERTFELDER G

    IPC: C07F9/53 ,  C07F9/645 ,  A61K27/00 ,  C07F9/00

    Abstract: 1345443 Phosphorus-containing benzodiazepine derivatives FARBWERKE HOECHST AG 5 May 1971 [8 May 1970 23 Sept 1970] 13207/71 Heading C2P [Also in Division A5] The invention comprises a phosphorus-containing benzodiazepine derivative of the general formula wherein R 1 is H, NO 2 , a halogen atom, or CF 3 , R 2 is a straight or branched chain alkyl group having up to 8 carbon atoms, a hydrogen atom, a halogen atom, NO 2 or CF 3 , R 3 is a straight chain or branched chain alkyl group having up to 3 carbon atoms and n is an integer from 1 to 6: They may be obtained by (a) reacting a metal derivative of the formula wherein M is a metal cation with a phosphine oxide of the formula X(CH 2 ) n P(O)(R 3 ) 2 , wherein X is a halogen atom or an alkyl (or aryl-) sulphonyloxy group, or (b) by reacting a compound of the formula with a derivative of amino acetic acid (preferably an ester, e.g. an imino or ortho ester derivative) or (c) by reacting a compound of the above Formula IV with a halide or azide of a halogenoacetic acid, treating the product with ammonia and then cyclizing the compound so obtained. In reaction (a) the metal compound can first be formed by heating the appropriate 1-unsubstituted benzodiazepine with, e.g., Ca-, Na- or Li-hydride or with potassium tertbutylate or sodium methylate in an inert organic solvent and the product may then be formed directly by reaction with the compound X(CH 2 ) n P(O)(R 3 ) 2 in the same solvent without isolation of the metal derivative. The products are useful as tranquillizers.

    10.
    发明专利
    未知

    公开(公告)号：BE765790A

    公开(公告)日：1971-08-30

    申请号：BE765790

    申请日：1971-04-15

    Applicant: HOECHST AG

    Inventor： WOLF E ,  KOHL H ,  HERTFELDER G

    IPC: C07F9/53 ,  C07F9/645 ,  C07D

    Abstract: 1345443 Phosphorus-containing benzodiazepine derivatives FARBWERKE HOECHST AG 5 May 1971 [8 May 1970 23 Sept 1970] 13207/71 Heading C2P [Also in Division A5] The invention comprises a phosphorus-containing benzodiazepine derivative of the general formula wherein R 1 is H, NO 2 , a halogen atom, or CF 3 , R 2 is a straight or branched chain alkyl group having up to 8 carbon atoms, a hydrogen atom, a halogen atom, NO 2 or CF 3 , R 3 is a straight chain or branched chain alkyl group having up to 3 carbon atoms and n is an integer from 1 to 6: They may be obtained by (a) reacting a metal derivative of the formula wherein M is a metal cation with a phosphine oxide of the formula X(CH 2 ) n P(O)(R 3 ) 2 , wherein X is a halogen atom or an alkyl (or aryl-) sulphonyloxy group, or (b) by reacting a compound of the formula with a derivative of amino acetic acid (preferably an ester, e.g. an imino or ortho ester derivative) or (c) by reacting a compound of the above Formula IV with a halide or azide of a halogenoacetic acid, treating the product with ammonia and then cyclizing the compound so obtained. In reaction (a) the metal compound can first be formed by heating the appropriate 1-unsubstituted benzodiazepine with, e.g., Ca-, Na- or Li-hydride or with potassium tertbutylate or sodium methylate in an inert organic solvent and the product may then be formed directly by reaction with the compound X(CH 2 ) n P(O)(R 3 ) 2 in the same solvent without isolation of the metal derivative. The products are useful as tranquillizers.

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