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    54.
    发明专利
    未知

    公开(公告)号：NO20020328L

    公开(公告)日：2002-01-31

    申请号：NO20020328

    申请日：2002-01-22

    Applicant: BASF AG

    Inventor： KNOPP MONIKA ,  KOSER STEFAN ,  SCHAEFER BERND

    IPC: C07D277/20 ,  C07D277/56

    Abstract: The invention relates to processes for preparing 2-aminomethyl-4-cyanothiazole and its salts of the formulae Ia and Ibin whichn=1 or 2 andfor n=1, X is chloride, bromide, triflate and hydrogen sulfate andfor n=2, X is sulfate, which comprises the process step where the aminonitrile of the formula IIis stirred with a cysteine ester of the formula III,in which R is branched or linear C1-10-alkyl orwhere n=0, 1 or 2 and R is branched or linear C1-C10C10-alkyl or C1-C4-alkoxy or C1-C4-dialkylamino in an inert solvent in the presence of a base at from 0° C. to 80° C. until the reaction has essentially proceeded to completion, and to the compounds of the formulae Ia and Ib.

    NEW SUBSTITUTED AMIDES, THEIR PRODUCTION AND THEIR USE
    57.
    发明专利
    NEW SUBSTITUTED AMIDES, THEIR PRODUCTION AND THEIR USE 未知

    公开(公告)号：HRP20000787A2

    公开(公告)日：2001-08-31

    申请号：HRP20000787

    申请日：2000-11-17

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED ,  MOELLER ACHIM ,  TREIBER HANS-JOERG ,  KNOPP MONIKA

    IPC: C07D295/08 ,  A61K31/16 ,  A61K31/166 ,  A61K31/27 ,  A61K31/395 ,  A61K31/40 ,  A61K31/455 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61P9/00 ,  A61P13/12 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/28 ,  A61P27/12 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P37/02 ,  A61P43/00 ,  C07C229/38 ,  C07C237/20 ,  C07C237/22 ,  C07C237/32 ,  C07C237/36 ,  C07D209/14 ,  C07D213/82 ,  C07D233/64 ,  C07D237/32 ,  C07D237/36 ,  C07D295/14 ,  C07D295/155 ,  C07D237/00

    Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH═CH—, —C═C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, —NHSO2—C1-C4-alkyl and —SO2—C1-C4-alkyl; and Y is phenyl, pyridine, pyrimidine and pyrazine and R4 is hydrogen, COOR9 and CO—Z in which Z is NR10R11 and R9 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and R10 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which itself may also be substituted by one or two R12 radicals, and R11 is hydrogen, C1-C6-alkyl, branched or unbranched, which may also be and substituted by a phenyl ring which may also carry an R9 radical, and R12 can be hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, J, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, —NHCO—C1-C4-alkyl, —NHCO-phenyl, —NHSO2—C1-C4-alkyl, NHSO2-phenyl, —SO2—C1-C4-alkyl and —SO2-phenyl, R13 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and R14 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.

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