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    (2H)-3-benzazepin-2-ones, their pharmaceutical compositions and their pharmaceutical uses
    1.
    发明授权
    (2H)-3-benzazepin-2-ones, their pharmaceutical compositions and their pharmaceutical uses 失效

    公开(公告)号：US4737495A

    公开(公告)日：1988-04-12

    申请号：US868986

    申请日：1986-05-30

    申请人： Andreas Bomhard ,  Manfred Psiorz ,  Joachim Heider ,  Norbert Hauel ,  Klaus Noll ,  Berthold Narr ,  Walter Kobinger ,  Christian Lillie

    发明人： Andreas Bomhard ,  Manfred Psiorz ,  Joachim Heider ,  Norbert Hauel ,  Klaus Noll ,  Berthold Narr ,  Walter Kobinger ,  Christian Lillie

    IPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D491/04 ,  C07D521/00 ,  A61K31/445 ,  A61K31/47 ,  A61K31/55 ,  C07D233/16

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D491/04

    摘要： The invention relates to new heteroaromatic amine derivatives of formula ##STR1## wherein A represents a --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--or ##STR2## group and B represents a methylene, carbonyl or thiocarbonyl group or A represents a --CO--CO or ##STR3## group and B represents a methylene group, in which the carbon atom marked x is linked to the phenyl nucleus,E represents a straight-chained alkylene group optionally substituted by an alkyl group,G represents a straight-chained alkylene group optionally substituted by an alkyl group,R.sub.1 represents a hydrogen, fluorine, chlorine or bromine atom, a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, alkylmercapto, hydroxy, alkoxy or phenylalkoxy group,R.sub.2 represents a hydrogen, chlorine or bromine atom or a hydroxy, alkoxy, phenylalkoxy or alkyl group orR.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen atom, an alkenyl group, an alkyl or phenylalkyl group, andHet represents a 5- or 6-membered heteroaromtic ring bonded via a carbon or nitrogen atom, which contains an oxygen, sulphur or nitrogen atom, two nitrogen atoms or a nitrogen atom and an oxygen or sulphur atom, and onto which additionally a phenyl ring can be condensed, in which case the bond can also be via the phenyl nucleus, or an imidazo[1,2-a]pyridyl group wherein the carbon structure of the above-mentioned groups can be substituted by a methylenedioxy or ethylenedioxy group or can be mono- or disubstituted by a halogen atom or an alkyl, hydroxy, alkoxy, phenylalkoxy, phenyl, dimethoxyphenyl, nitro, amino, acetylamino, carbamoylamino, N-alkyl-carbamoylamino, hydroxymethyl, mercapto, alkylmercapto, alkylsulphinyl, alkylsulphonyl, alkylsulphonyloxy, alkylsulphonylamino, alkoxycarbonylmethoxy, carboxymethoxy or alkoxymethyl group, and at the same time any imino group present in the above-mentioned heteroaromatic groups can be substituted by an alkyl, phenylalkyl or phenyl group, the N-oxides and the acid addition salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly the effect of lowering heart rate and oxygen requirement of the heart. They can be used to treat sinus tachycardia or ischaemic heart disease.

    Process for preparing (s)- and (r) -but-3-en-2-ol and the derivatives thereof from l-or d-lactic acid esters
    7.
    发明授权
    Process for preparing (s)- and (r) -but-3-en-2-ol and the derivatives thereof from l-or d-lactic acid esters 失效
    用于从1-或D-乳酸酯制备（ - ）和（R） - 丁-3-烯-2-醇及其衍生物的方法

    公开(公告)号：US5457247A

    公开(公告)日：1995-10-10

    申请号：US361250

    申请日：1994-12-21

    申请人： Franz D. Klingler ,  Manfred Psiorz

    发明人： Franz D. Klingler ,  Manfred Psiorz

    IPC分类号： C07B61/00 ,  C07C29/32 ,  C07C29/44 ,  C07C33/03 ,  C07C29/00 ,  C07C33/02

    CPC分类号： C07C29/103 ,  C07C29/32 ,  C07B2200/07

    摘要： A novel process for preparing enantiomerically pure (S)- or (R)-but-3-en-2-ol compounds includes the following reaction steps:(a) reacting an alkyl ester of D- or L-lactic acid with a hydropyran compound to obtain a lactate ester having a hydropyranyl ether group,(b) reducing the lactate ester with an aluminum hydride at a temperature below 0.degree. C. to obtain a propionaldehyde having a hydropyranyl ether group,(c) reacting the propionaldehyde with an alkyl phosphonium salt to obtain a 3-butene having a hydropyranyl ether group, and(d) cleaving the hydropyranyl ether group to prepare the enantiomerically pure (S)- or (R)- but-3-en-2-ol.

    摘要翻译： 制备对映体纯的（S） - 或（R） - 丁-3-烯-2-醇化合物的新方法包括以下反应步骤：（a）使D-或L-乳酸的烷基酯与氢吡喃 化合物，得到具有氢吡喃基醚基团的乳酸酯，（b）用氢化铝在低于0℃的温度下还原乳酸酯，得到具有氢吡喃基醚基团的丙醛，（c）使丙醛与烷基 得到具有氢吡喃基醚基团的3-丁烯，（d）裂解氢吡喃基醚基团以制备对映体纯的（S） - 或（R） - 丁-3-烯-2-醇。

    Process for preparing 1,3-dialkyl-5-hydroxyoxindoles and the ether derivatives thereof
    8.
    发明授权
    Process for preparing 1,3-dialkyl-5-hydroxyoxindoles and the ether derivatives thereof 失效
    制备1,3-二烷基-5-羟基吲哚及其醚衍生物的方法

    公开(公告)号：US5614637A

    公开(公告)日：1997-03-25

    申请号：US448222

    申请日：1995-05-23

    申请人： Rainer Sobotta ,  Rainer Schwarz ,  Manfred Psiorz

    发明人： Rainer Sobotta ,  Rainer Schwarz ,  Manfred Psiorz

    IPC分类号： C07D209/34

    CPC分类号： C07D209/34

    摘要： The invention is directed to a process for preparing a 1,3-dialkyl-5-hydroxyoxindole of formula 1: ##STR1## comprising heating an N-alkyl-p-alkoxy-(.alpha.-haloacyl)anilide of formula 2: ##STR2## wherein the substituents are as defined herein, in the presence of an anhydrous zinc halide to a temperature in the range from about 120.degree. C. to about 160.degree. C., and isolating the 1,3-dialkyl-5-hydroxyoxindole prepared.

    摘要翻译： 本发明涉及制备式1的1,3-二烷基-5-羟基吲哚的方法：式2的xy-（α-卤代酰基）酰苯胺：其中取代基如本文所定义，在存在下 的无水卤化锌至约120℃至约160℃的温度，并分离所制备的1,3-二烷基-5-羟基羟吲哚。