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    2-AMINOMETHYL-PHENOL DERIVATIVES, PROCESS FOR THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    10.
    发明专利
    2-AMINOMETHYL-PHENOL DERIVATIVES, PROCESS FOR THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知

    公开(公告)号：DE3360236D1

    公开(公告)日：1985-07-11

    申请号：DE3360236

    申请日：1983-03-02

    Applicant: HOECHST AG

    Inventor： ENGLERT HEINRICH CHRISTIAN DR ,  LANG HANS-JOCHEN DR ,  HROPOT MAX DR ,  KAISER JOACHIM DR

    IPC: A61K31/135 ,  A61K31/40 ,  A61K31/535 ,  A61K31/54 ,  A61P3/00 ,  A61P7/10 ,  A61P9/12 ,  C07C43/21 ,  C07C67/00 ,  C07C313/00 ,  C07C315/04 ,  C07C317/00 ,  C07C317/22 ,  C07C317/32 ,  C07C317/36 ,  C07D277/04 ,  C07D295/08 ,  C07D295/096 ,  C07D307/52 ,  C07C147/14 ,  C07C147/12 ,  C07C147/10

    Abstract: 1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE 2-Aminomethylphenols of the formula I see diagramm : EP0088346,P33,F2 in which R represents hydrogen or alkyl having 1 or 2 C atoms, R**1 represents alkyl having 1 to 8 C atoms, cycloalkyl having 3 to 12 C atoms and up to 8 ring members, alkenyl having 2 to 8 C atoms or cycloalkenyl having 5 to 12 C atoms and up to 8 ring members, it being possible for each of the aforementioned radicals to be substituted with 1 to 5 identical or different halogen atoms, R**2 and R**4 are identical or different and denote hydrogen, halogen, alkyl having 1 or 2 C atoms or alkoxy having 1 or 2 C atoms, R**3 denotes halogen, alkyl having 1 to 12 C atoms or cycloalkyl having 3 to 12 C atoms and up to 8 ring members, R**5 and R**6 are identical or different and represent hydrogen, alkyl having 1 to 6 C atoms, cycloalkyl having 3 to 10 C atoms and up to 8 ring members or the radical -[CH2 ]o -Ar, wherein o = 1 or 2, the -[CH2 ]o - chain can be substituted by 1 or 2 (C1 or C2 )-alkyl groups and Ar is a 5- or 6- membered aromatic or heteroaromatic system, which is optionally substituted by 1 to 3 identical or different radicals (C1 or C2 )-alkyl, (C1 or C2 )-alkoxy or halogen, and n is 1 or 2, it being possible for the radicals R**5 and R**6 and/or two of the radicals R**2 , R**3 and R**4 also to form a -[CH2 ]m - chain having m = 3 to 6, which can optionally be substituted by 1 or 2 methyl groups and, in the case of R**5 and R**6 , can also be interrupted by 1 or 2 oxygen atoms, sulfur atoms and/or imino groups, and their physiologically tolerated salts. 1. Claims for the Contracting State : AT A process for the preparation of the 2-aminomethylphenols of the formula I see diagramm : EP0088346,P35,F4 in which R represents hydrogen or alkyl having 1 or 2 C atoms, R**1 represents alkyl having 1 to 8 C atoms, cycloalkyl having 3 to 12 C atoms and up to 8 ring members, alkenyl having 2 to 8 C atoms or cycloalkenyl having 5 to 12 C atoms and up to 8 ring members, it being possible for each of the aforementioned radicals to be substituted with 1 to 5 identical or different halogen atoms, R**2 and R**4 are identical or different and denote hydrogen, halogen, alkyl having 1 or 2 C atoms or alkoxy having 1 or 2 C atoms, R**3 denotes halogen, alkyl having 1 to 12 C atoms or cycloalkyl having 3 to 12 C atoms and up to 8 ring members, R**5 and R**6 are identical or different and represent hydrogen, alkyl having 1 to 6 C atoms, cycloalkyl having 3 to 10 C atoms and up to 8 ring members or the radical -[CH2 ]o -Ar, wherein o = 1 or 2, the -[CH2 ]o - chain can be substituted by 1 or 2 (C1 or C2 )-alkyl groups and Ar is a 5- or 6-membered aromatic or heteroaromatic system, which is optionally substituted by 1 to 3 identical or different radicals (C1 or C2 )-alkyl, (C1 or C2 )-alkoxy or halogen, and n is 1 or 2, it being possible for the radicals R**5 and R**6 and/or two of the radicals R**2 , R**3 and R**4 also to form a -[CH2 ]m - chain having m = 3 to 6, which can optionally be substituted by 1 or 2 methyl groups and, in the case of R**5 and R**6 , can also be interrupted by 1 or 2 oxygen atoms, sulfur atoms and/or imino groups, and their physiologically tolerated salts, which comprises a) reacting a compound of the formula II see diagramm : EP0088346,P36,F1 wherein n, R**1 , R**2 , R**3 and R**4 have the abovementioned meanings, with an N-hydroxymethylcarboxamide of the general formula III see diagramm : EP0088346,P36,F2 in which R has the abovementioned meaning, R**5 denotes hydrogen or alkyl having 1 to 4 C atoms and R**7 represents hydrogen, optionally halogen-substituted alkyl having 1 to 4 C atoms or aryl having 6 to 10 C atoms, or in which R**5 and the radical COR**7 together represent the o-phthaloyl radical, to give a compound of the general formula IV see diagramm : EP0088346,P36,F3 and removing the acyl radical R**7 -CO by hydrolysis, b) reacting a compound of the formula II, in which the radicals R**1 to R**4 and n have the abovementioned meanings, in the presence of formaldehyde, with an amine of the general formula V see diagramm : EP0088346,P36,F4 in which R**5 and R**6 have the meanings mentioned in claim 1 with the exception of hydrogen, c) reacting a compound of the general formula VI see diagramm : EP0088346,P36,F5 in which n and R to R**4 have the abovementioned meanings and Z represents a leaving group, with an amine of the general formula H-N = Y, wherein Y represents an amine-protective group or the radicals R**5 and R**6 defined in claim 1, it being possible for R**6 also to be an amine-protective group, to give a compound of the general formula VII see diagramm : EP0088346,P37,F1 and, if appropriate, removing the amine-protective group by hydrolysis or hydrogenolysis, or d) reacting compounds of the general formula XIV see diagramm : EP0088346,P37,F2 in which n and R to R**4 have the abovementioned meanings, with an amine of the formula R**5 -NH2 , with R**5 having the abovementioned meaning, to give Schiff's bases of the formula XV see diagramm : EP0088346,P37,F3 in which n and R to R**5 have the abovementioned meanings, and reducing the latter to give a compound of the formula I, and optionally converting the compound of the formula I obtained according to one of the variants a) - d) into its physiologically tolerated salts.

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