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    21.
    发明专利
    未知

    公开(公告)号：NO129568B

    公开(公告)日：1974-04-29

    申请号：NO277070

    申请日：1970-07-15

    Applicant: HOECHST AG

    Inventor： KOENIG W ,  GEIGER R ,  WOLF E

    IPC: A61K38/00 ,  C07D253/08 ,  C07K1/10 ,  C07K5/068 ,  C07K14/695 ,  C07C103/52

    Abstract: 1318963 1,2,3 - Benzo triazines FARBWERKE HOECHST AG 3 Aug 1970 [1 Aug 1969] 37320/70 Heading C2C A 3 - hydroxy - 4 - oxo - 3,4 - dihydro - 1,2,3- benzo triazine ester of a protected amino acid or a protected peptide, which is prepared from the free 3-hydroxy benzo triazine and a protected amino acid or peptide containing a free carboxyl group in the presence of a carbo diimide, is used in the preparation of peptides wherein a carboxylic ester of a protected amino acid or peptide is reacted with an amino acid or peptide having a free amino group and protecting groups are subsequently removed. The following starting materials are prepared. Z - Asn(Mbh)OH, Z - Gln(Mbh)OH and its methyl ester and H Gln(Mbh)OMe, HCl, Z-Gly- NH-MbH, and BOC-Leu-Phe-OH, where "Mbh" is 4,4 1 -dimethoxy benzhydryl.

    22.
    发明专利
    未知

    公开(公告)号：FR2100639A1

    公开(公告)日：1972-03-24

    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.

    24.
    发明专利
    未知

    公开(公告)号：DK137861C

    公开(公告)日：1978-10-23

    申请号：DK220771

    申请日：1971-05-06

    Applicant: HOECHST AG

    Inventor： WOLF E ,  KOHL H ,  HAERTFELDER G

    IPC: C07F9/53 ,  C07F9/645 ,  C07F9/65

    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.

    26.
    发明专利
    未知

    公开(公告)号：BG20801A3

    公开(公告)日：1975-12-20

    申请号：BG2164671

    申请日：1971-05-04

    Applicant: HOECHST AG

    Inventor： WOLF E ,  KOHL H ,  HERTFELDER G

    IPC: C07F9/53 ,  C07F9/645 ,  C07D53/04

    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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