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    DERIVATIVES OF BICYCLIC AMINO ACIDS, PROCESSES FOR THEIR PREPARATION, AGENTS CONTAINING THEM AND THEIR USE AS WELL AS BICYCLIC AMINO ACIDS AS INTERMEDIATES AND PROCESS FOR THEIR PREPARATION
    21.
    发明专利
    DERIVATIVES OF BICYCLIC AMINO ACIDS, PROCESSES FOR THEIR PREPARATION, AGENTS CONTAINING THEM AND THEIR USE AS WELL AS BICYCLIC AMINO ACIDS AS INTERMEDIATES AND PROCESS FOR THEIR PREPARATION 未知

    公开(公告)号：DE3280014D1

    公开(公告)日：1989-12-14

    申请号：DE3280014

    申请日：1982-12-24

    Applicant: HOECHST AG

    Inventor： URBACH HANSJORG DR ,  HENNING RAINER DR ,  TEETZ VOLKER DR ,  GEIGER ROLF PROF DR ,  BECKER REINHARD DR ,  GAUL HOLGER

    IPC: A61K38/55 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K38/00 ,  A61P7/10 ,  A61P9/08 ,  A61P9/12 ,  C07D209/02 ,  C07D209/08 ,  C07D209/32 ,  C07D209/34 ,  C07D209/42 ,  C07D209/52 ,  C07D215/22 ,  C07D215/227 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06

    Abstract: 1. Claims for the Contracting states ; BE, CH, DE, FR, GB, IT, Li, Lu, NL, SE A compound of the formula I see diagramm : EP0084164,P21,F7 in which the hydrogen atoms on the bridgehead C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2, R1 denotes methyl, R2 denotes hydrogen, (C1 -C4 )-alkyl or benzyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes phenyl, and its physiologically acceptable salts. 1. Claims for the Contracting state : Austria A process for the preparation of the compounds of the formula I see diagramm : EP0084164,P24,F4 in which the hydrogen atoms on the bridgehead C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2, R1 denotes methyl, R2 denotes hydrogen, (C1 -C4 )-alkyl or benzyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes phenyl, and its physiologically acceptable salts, which a) comprises reacting a compound of the formula II see diagramm : EP0084164,P24,F6 wherein R1 , R2 , X, Y and Z have the meanings as in formula I, with a compound of the formula III see diagramm : EP0084164,P25,F1 in which the H atoms on the C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2 and W denotes a radical which can be cleaved off by hydrogenolysis or by acid, and subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl groups, or b) for the preparation of compounds of the formula I, in which Y and Z together denote oxygen, comprises b1 ) reacting a compound of the formula IV see diagramm : EP0084164,P25,F3 in which the H atoms on the C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n and R1 have the meanings as in formula I and W has the meaning as in formula III, with a compound of the formula V, R2 O2 C-CH = CH-CO-X wherein R2 and X have the meanings as in formula I, and subsequently splitting off the radical W and, if appropriate, also the radical R2 to form the free carboxyl groups, or, b2 ) reacting a compound of the formula IV mentioned under b1 ) with a compound of the general formula VI, wherein R2 has the meaning as in formula I, and with a compound of the general formula VII OHC-CO2 R2 X-CO-CH3 wherein X has the meaning as in formula I, subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl group, or c) for the preparation of compounds of the formula I, in which Y and Z each denote hydrogen, comprises c1 ) reacting a compound of the formula IV mentioned under b1 ) with a compound of the formula VIII see diagramm : EP0084164,P25,F2 wherein R2 and X have the meanings as in formula I, reducing the Schiff's bases obtained and subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl groups, or c2 ) catalytically reducing a compound of the formula I in which Y and Z together denote oxygen, with hydrogen, or d) for the preparation of compounds of the formula I, in which Y denotes hydroxyl and Z denotes hydrogen, comprises reducing a compound of the formula I, in which Y and Z together denote oxygen, catalytically with hydrogen or with a reducing agent, such as sodium borohydride, and, if appropriate, converting the compounds obtained according to (a)-(d) into their physiologically acceptable salts.

    PROCESS FOR THE PREPARATION OF N-ALKYLATED AMINO ACIDS AND THEIR ESTERS
    28.
    发明专利
    PROCESS FOR THE PREPARATION OF N-ALKYLATED AMINO ACIDS AND THEIR ESTERS 未知

    公开(公告)号：DE3460578D1

    公开(公告)日：1986-10-09

    申请号：DE3460578

    申请日：1984-01-31

    Applicant: HOECHST AG

    Inventor： URBACH HANSJORG DR ,  HENNING RAINER DR

    IPC: A61K31/255 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/12 ,  A61P43/00 ,  C07C20060101 ,  C07C67/00 ,  C07C215/00 ,  C07C227/00 ,  C07C227/14 ,  C07C227/18 ,  C07C229/02 ,  C07C229/06 ,  C07C229/16 ,  C07C229/24 ,  C07C229/26 ,  C07C229/28 ,  C07C229/36 ,  C07C233/43 ,  C07C253/00 ,  C07C255/58 ,  C07C271/06 ,  C07C279/18 ,  C07C301/00 ,  C07C303/28 ,  C07C309/03 ,  C07C309/19 ,  C07C309/63 ,  C07C309/64 ,  C07C309/65 ,  C07C309/70 ,  C07C313/00 ,  C07C323/58 ,  C07C325/00 ,  C07C381/00 ,  C07D207/323 ,  C07D209/14 ,  C07D209/18 ,  C07D209/26 ,  C07D209/44 ,  C07D213/36 ,  C07D217/12 ,  C07D231/38 ,  C07D233/88 ,  C07D237/26 ,  C07D239/26 ,  C07D239/74 ,  C07D241/36 ,  C07D261/08 ,  C07D263/32 ,  C07D275/02 ,  C07D277/58 ,  C07D307/52 ,  C07D307/81 ,  C07D309/34 ,  C07D317/48 ,  C07D317/60 ,  C07D333/20 ,  C07D333/58 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D521/00 ,  C07K5/06 ,  C07K14/81 ,  C07C99/00 ,  C07C101/00 ,  C07C143/68 ,  C07C149/243 ,  C07C149/43

    Abstract: For the Contracting states : BE, CH, DE, FR, GB, IT, LU, NL, SE 1. A process for preparing compounds of the formula I see diagramm : EP0117448,P21,F1 in which n = 1 or 2, R denotes, hydrogen, carboxy, carbamoyl, an optionally substituted aliphatic radical having 2-8 carbon atoms, an optionally substituted cycloaliphatic radical having 3-9 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms, an OR**4 or SR**4 radical in which R**4 represents an optionally substituted aliphatic radical having 1-4 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms or an optionally substituted heteroaromatic radical having 5-10 ring atoms, or an optionally substituted heteroaromatic radical having 5-10 ring atoms, R**1 denotes hydrogen, an optionally substituted aliphatic radical having 1-6 carbon atoms, an optionally substituted cycloaliphatic radical having 3-9 carbon atoms, an optionally substituted cycloaliphatic-aliphatic radical having 4-13 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms, an optionally substituted araliphatic radical having 7-16 carbon atoms, an optionally substituted heteroaromatic radical having 5-10 ring atoms or the side chain of an optionally protected naturally occuring alpha-amino acid, R**2 and R**3 are identical or different and denote hydrogen, an optionally substituted aliphatic radical having 1-6 carbon atoms, an optionally substituted cycloaliphatic radical having 3-9 carbon atoms, an optionally substituted cycloaliphatic-aliphatic radical having 4-12 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms or an optionally substituted araliphatic radical having 7-16 carbon atoms, which comprises reacting compounds of the formulae II ou III see diagramm : EP0117448,P22,F2 in which n, R, R**1, R**2 and R**3 have the abovementioned meanings, with compounds of the formulae IV or V see diagramm : EP0117448,P22,F3 in which R, R**1, R**2, R**3 and n have the abovementioned meanings, if desired eliminating ester groups by hydrolysis or if desired esterifying free carboxyl groups in a manner known per se. For the Contracting state : Austria 1. A process for preparing compounds of the formula see diagramm : EP0117448,P25,F1 in which n = 1 or 2, R denotes, carbamoyl, hydrogen, carboxy an optionally substituted aliphatic radical having 2-8 carbon atoms, an optionally substituted cycloaliphatic radical having 3-9 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms, an OR**4 or SR**4 radical in which R**4 represents an optionally substituted aliphatic radical having 1-4 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms or an optionally substituted heteroaromatic radical having 5-10 ring atoms, or an optionally substituted heteroaromatic radical having 5-10 ring atoms, R**1 denotes hydrogen, an optionally substituted aliphatic radical having 1-6 carbon atoms, an optionally substituted cycloaliphatic radical having 3-9 carbon atoms, an optionally substituted cycloaliphatic-aliphatic radical having 4-13 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms, an optionally substituted araliphatic radical having 7-16 carbon atoms, an optionally substituted heteroaromatic radical having 5-10 ring atoms or the side chain of an optionally protected naturally accuring alpha-amino acid, R**2 and R**3 are identical or different and denote hydrogen, an optionally substituted aliphatic radical having 1-6 carbon atoms, an optionally substituted cycloaliphatic radical having 3-9 carbon atoms, an optionally substituted cycloaliphatic-aliphatic radical having 4-12 carbon atoms, an optionally substituted aromatic radical having 6-12 carbon atoms or an optionally substituted araliphatic radical having 7-16 carbon atoms, which comprises reacting compounds of the formulae II or III see diagramm : EP0117448,P26,F2 in which n, R, R**1, R**2 and R**3 have the abovementioned meanings, with compounds of the formulae IV or V see diagramm : EP0117448,P26,F3 in which R, R**1, R**2, R**3 and n have the abovementioned meanings, if desired eliminating ester groups by hydrolysis or hydrogenolysis or if desired esterifying free carboxyl groups in a manner known per se.

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