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    Process for the preparation of diacylated 4-imidazolin-2-ones
    92.
    发明授权
    Process for the preparation of diacylated 4-imidazolin-2-ones 失效
    二酰化4-咪唑啉-2-酮的制备方法

    公开(公告)号：US4238618A

    公开(公告)日：1980-12-09

    申请号：US884520

    申请日：1978-03-08

    申请人： Karl-Heinz Scholz ,  Willy Hartmann ,  Hans-Georg Heine

    发明人： Karl-Heinz Scholz ,  Willy Hartmann ,  Hans-Georg Heine

    IPC分类号： C07D233/70 ,  C07D235/02 ,  C07D235/26

    CPC分类号： C07D235/02 ,  C07D233/70 ,  C07D235/26

    摘要： A process for the preparation of a diacylated 4-imidazolin-2-one of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen, optionally substituted alkyl, cycloalkyl, aryl and alkoxy, which comprises contacting a compound of the formula of II ##STR2## wherein R.sup.1 and R.sup.2 of the previously assigned significance with a source of chlorine at a temperature from 20.degree. to 150.degree. C. in the presence of a radical forming agent or under ultra-violet light and thereafter dehydrohalogenating or dehalogenating the resultant chlorinated product the diacylated 4-imidazolin-2-ones prepared by the process are useful for photochemical cycloadditions and as intermediates for the preparation of compounds in the biotin series.

    摘要翻译： 制备式（I）的二酰化4-咪唑啉-2-酮的方法，其中R 1和R 2独立地表示氢，任选取代的烷基，环烷基，芳基和烷氧基，其包括使式 的II（II）化合物，其中在自由基形成剂存在下或在紫外光下，在20至150℃的温度下，将具有氯源的先前指定的含义的R 1和R 2在脱卤化氢 或脱卤化所得氯化产物，通过该方法制备的二酰化4-咪唑啉-2-酮可用于光化学环加成和作为制备生物素系列中化合物的中间体。

    Process for the preparation of monoaryl thioureas
    94.
    发明授权
    Process for the preparation of monoaryl thioureas 失效
    制备单芳基硫脲的方法

    公开(公告)号：US4234513A

    公开(公告)日：1980-11-18

    申请号：US36687

    申请日：1979-05-07

    申请人： Theodor Papenfuhs

    发明人： Theodor Papenfuhs

    IPC分类号： C07C67/00 ,  C07C325/00 ,  C07C335/16 ,  C07D235/26 ,  C07C157/09 ,  C07C69/14 ,  C07C69/78

    CPC分类号： C07C335/16 ,  C07D235/26

    摘要： An improved process for the preparation of monoaryl thiourea compounds, in which a salt of an arylamine is reacted with ammonium rhodanide or an alkali metal rhodanide in an aqueous medium; the improvement consists in that the reaction is carried out in a reaction mixture which at the start contains a higher amount by weight of the salt of the arylamine than of water and contains 1 to 1.25 times the equivalent amount of the rhodanide calculated on the arylamine, and which does not contain any excess acid, and that the reaction is carried out at a temperature which is below the boiling point of the reaction mixture by at least 5.degree. C. It is advantageous, but not compulsory, to effect the reaction while using from 5 to 10 mol % of hydrogeno-sulfite ions, in order to remove sulfur-containing by-products which are formed as a consequence of the acid spontaneous decomposition of the rhodanide in an inevitable side reaction.By means of the improved novel process, homogeneous monoaryl thioureas are obtained in a high yield with a reduced charge of the waste water.

    摘要翻译： 制备单芳基硫脲化合物的改进方法，其中芳基胺的盐与水性介质中的硫氰酸铵或碱金属的硫化物反应; 改进之处在于反应在反应混合物中进行，反应混合物在起始时含有比水重量更多的芳胺盐，而不是水，并且含有按芳基胺计算的当量量的1至1.25倍的硫化铑， 并且其不含任何过量的酸，并且反应在低于反应混合物沸点的温度下进行至少5℃。使用时有利但不是强制性地进行反应 5至10摩尔％的亚硫酸氢根离子，以便除去由于不可避免的副反应中的硫酸根的酸自发分解而形成的含硫副产物。 通过改进的新方法，可以以高产率获得均匀的单芳基硫脲，并减少废水的装入量。

    Aminoalkyl-substituted benzimidazolidin-2-ones
    96.
    发明授权
    Aminoalkyl-substituted benzimidazolidin-2-ones 失效
    氨基烷基取代的苯并咪唑烷-2-酮

    公开(公告)号：US4215119A

    公开(公告)日：1980-07-29

    申请号：US26608

    申请日：1979-04-03

    申请人： Anton Mentrup ,  Kurt Schromm ,  Ernst-Otto Renth ,  Richard Reichl ,  Werner Traunecker ,  Wolfgang Hoefke

    发明人： Anton Mentrup ,  Kurt Schromm ,  Ernst-Otto Renth ,  Richard Reichl ,  Werner Traunecker ,  Wolfgang Hoefke

    IPC分类号： C07D215/02 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/536 ,  A61P9/08 ,  A61P9/12 ,  A61P11/00 ,  A61P25/24 ,  A61P25/26 ,  C07D215/22 ,  C07D215/227 ,  C07D223/04 ,  C07D233/32 ,  C07D233/36 ,  C07D235/04 ,  C07D235/22 ,  C07D235/26 ,  C07D263/54 ,  C07D263/58 ,  C07D265/22 ,  C07D265/36 ,  C07D405/04 ,  C07D405/12 ,  C07D413/12 ,  A61K31/535

    CPC分类号： C07D215/227 ,  C07D233/36 ,  C07D235/26 ,  C07D263/58 ,  C07D265/36 ,  Y10S514/929

    摘要： Racemic and optically active compounds of the formulaQ-C.sub.n H.sub.2n -NH-Rwherein Q is ##STR1## where R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, trifluoromethyl or amino,R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or trifluoromethyl,R.sub.1 and R.sub.2, together with each other, are methylenedioxy or ethylenedioxy, andA is --O--, --CH.sub.2 --CH.sub.2 --, or --NR.sub.3 -- where R.sub.3 is hydrogen or alkyl or 1 to 4 carbon atoms,n is an integer from 2 to 6, inclusive, andR is hydrogen, benzyl or ##STR2## where R.sub.4 is hydrogen, methyl or ethyl,R.sub.5, R.sub.6 and R.sub.7, which may be identical to or different from each other, are each hydrogen, halogen, hydroxymethyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, nitro, cyano, --CONHR.sub.3, --CONHOH, --COOR.sub.3, R.sub.8 O--, methylsulfonylmethyl or, when one or two of R.sub.5 through R.sub.7 are other than halogen or trifluoromethyl, also --NR.sub.3 R.sub.9,whereR.sub.3 has the meanings defined above,R.sub.8 is hydrogen, alkanoyl of 1 to 20 carbon atoms, alkyl of 1 to 4 carbon atoms, or aralkyl, andR.sub.9 is hydrogen, lower alkanoyl, methanesulfonyl, carbamoyl, dimethylsulfamoyl, or alkoxycarbonyl of 2 to 5 carbon atoms, andR.sub.5 and R.sub.6, together with each other, are --O--CH.sub.2 --O, --O--CH.sub.2 --CH.sub.2 --O--, --CH.dbd.CH--CH.dbd.CH--, --O--CH.sub.2 --CONH--, --CH.sub.2 --CH.sub.2 --COHN-- or --O--CO--NH--,and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as vasodilators and CNS-stimulators.

    摘要翻译： 其中Q为氢，卤素，1至4个碳原子的烷基，1至4个碳原子的烷氧基，三氟甲基或氨基，R 2为式Q-C n H 2n-NH-R的外消旋和旋光活性化合物 氢，卤素，1至4个碳原子的烷基，1至4个碳原子的烷氧基或三氟甲基，R 1和R 2彼此一起是亚甲二氧基或亚乙二氧基，A是-O-，-CH 2 -CH 2 - 或 -NR 3 - ，其中R 3是氢或烷基或1至4个碳原子，n是2-6的整数，包括2和6，R是氢，苄基或者其中R 4是氢，甲基或乙基，R 5，R 6和 R 7可以相同或不同，分别为氢，卤素，羟甲基，三氟甲基，1至4个碳原子的烷基，1至4个碳原子的烷氧基，硝基，氰基，-CONHR 3，-CONHOH， - COOR 3，R8O-，甲基磺酰基甲基，或当R 5至R 7中的一个或两个不同于卤素或三氟甲基时，也可以是-NR 3 R 9，其中R 3具有上述定义，R 8是氢， 1至20个碳原子的烷酰基，1至4个碳原子的烷酰基或芳烷基，R 9是氢，低级烷酰基，甲磺酰基，氨基甲酰基，二甲基氨磺酰基或2至5个碳原子的烷氧基羰基，以及R5和R6， 另一个是-O-CH 2 -O，-O-CH 2 -CH 2 -O - ， - CH = CH-CH = CH-，-O-CH 2 -CONH-，-CH 2 -CH 2 -COOH-或-O-CO -NH-和无毒的药学上可接受的酸加成盐。 化合物及其盐可用作血管扩张剂和CNS刺激剂。

    Dicarboxylic acids and dicarboxylic acid esters containing a benzimidazolone radical
    98.
    发明授权
    Dicarboxylic acids and dicarboxylic acid esters containing a benzimidazolone radical 失效
    含有苯并咪唑酮基团的二羧酸和二羧酸酯

    公开(公告)号：US4161603A

    公开(公告)日：1979-07-17

    申请号：US794694

    申请日：1977-05-06

    申请人： Jurgen Habermeier

    发明人： Jurgen Habermeier

    IPC分类号： C07D233/72 ,  C07D233/74 ,  C07D233/96 ,  C07D235/26 ,  C07D239/22 ,  C07D239/62 ,  C08G63/00 ,  C08G63/685

    CPC分类号： C08G63/6854 ,  C07D233/74 ,  C07D233/96 ,  C07D235/26 ,  C07D239/22 ,  C07D239/62

    摘要： Dicarboxylic acids or dicarboxylic acid esters, containing a N,N-heterocyclic radical, of the formula ##STR1## in which the two R.sub.1 independently of one another each denote hydrogen, an alkyl with 1 to 4 C atoms or a phenyl, the two R.sub.2 independently of one another each denote hydrogen or an alkyl with 1 to 10 C atoms, the two n represent identical or different numbers from 2 to 12 and X denotes a divalent monocyclic N,N-heterocyclic radical of benzimidazolone, parabanic acid, 2,2-dimethylimidazolidine-4,5-dione, 6-ethyluracil or barbituric acid are prepared by reacting 1 mol of the corresponding N,N-heterocyclic compounds with 2 mols of a compound of the formula ##STR2## wherein Y.sub.1 denotes a chlorine or bromine atom. The dicarboxylic acid compounds have a high stability to heat and therefore are very suited for the manufacture of polycondensates by the melt condensation process.

    摘要翻译： 含有式（IMAGE）的N，N-杂环基的二羧酸或二羧酸酯，其中两个R 1彼此独立地表示氢，具有1-4个C原子的烷基或苯基，二个R2 彼此独立地表示氢或具有1至10个C原子的烷基，两个n表示2至12个相同或不同的数字，X表示苯并咪唑酮的二价单环N，N-杂环基，对苯乙酸，2,2 - 二甲基咪唑烷-4,5-二酮，6-乙基尿嘧啶或巴比妥酸是通过使1摩尔相应的N，N-杂环化合物与2摩尔下式化合物反应制备的，其中Y1表示氯或溴原子 。 二羧酸化合物对热的稳定性高，因此非常适用于通过熔融缩合方法制备缩聚物。

    Aminoalkyl-substituted benzoxazine derivatives
    99.
    发明授权
    Aminoalkyl-substituted benzoxazine derivatives 失效
    氨基烷基取代的苯并恶嗪衍生物

    公开(公告)号：US4154829A

    公开(公告)日：1979-05-15

    申请号：US773394

    申请日：1977-03-02

    申请人： Anton Mentrup ,  Kurt Schromm ,  Ernst-Otto Renth ,  Richard Reichl ,  Werner Traunecker ,  Wolfgang Hoefke

    发明人： Anton Mentrup ,  Kurt Schromm ,  Ernst-Otto Renth ,  Richard Reichl ,  Werner Traunecker ,  Wolfgang Hoefke

    IPC分类号： C07D215/02 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/536 ,  A61P9/08 ,  A61P9/12 ,  A61P11/00 ,  A61P25/24 ,  A61P25/26 ,  C07D215/22 ,  C07D215/227 ,  C07D223/04 ,  C07D233/32 ,  C07D233/36 ,  C07D235/04 ,  C07D235/22 ,  C07D235/26 ,  C07D263/54 ,  C07D263/58 ,  C07D265/22 ,  C07D265/36 ,  C07D405/04 ,  C07D405/12 ,  C07D413/12 ,  C07D265/30 ,  A61K31/535

    CPC分类号： C07D215/227 ,  C07D233/36 ,  C07D235/26 ,  C07D263/58 ,  C07D265/36 ,  Y10S514/929

    摘要： Racemic and optically active compounds of the formulaQ--C.sub.n H.sub.2n --NH--Rwherein Q is ##STR1## where R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, trifluoromethyl or amino,R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or trifluoromethyl,R.sub.1 and R.sub.2, together with each other, are methylenedioxy or ethylenedioxy, andA is --O--, --CH.sub.2 --CH.sub.2 --, --O--CH.sub.2 -- where the oxygen is bonded to the benzene ring, or --NR.sub.3 -- where R.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms,N is an integer from 2 to 6, inclusive, andR is hydrogen, benzyl or ##STR2## where R.sub.4 is hydrogen, methyl or ethyl,R.sub.5, r.sub.6 and R.sub.7, which may be identical to or different from each other, are each hydrogen, halogen, hydroxymethyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, nitro, cyano, --CONHR.sub.3, --CONHOH, --COOR.sub.3, R.sub.8 O--, methylsulfonylmethyl or, when one or two of R.sub.5 through R.sub.7 are other than halogen or trifluoromethyl, also --NR.sub.3 R.sub.9,whereR.sub.3 has the meanings defined above,R.sub.8 is hydrogen, alkanoyl of 1 to 20 carbon atoms, alkyl of 1 to 4 carbon atoms or aralkyl, andR.sub.9 is hydrogen, lower alkanoyl, methanesulfonyl, carbamoyl, dimethylsulfamoyl, or alkoxycarbonyl of 2 to 5 carbon atoms, andR.sub.5 and R.sub.6, together with each other, are --O--CH.sub.2 --O, --O--CH.sub.2 --CH.sub.2 --O--, --CH.dbd.CH--CH.dbd.CH--, --O--CH.sub.2 --CONH--, --CH.sub.2 --CH.sub.2 --CONH-- or --O--CO--NH--,and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as vasodilators and CNS-stimulators.

    摘要翻译： 其中Q为氢，卤素，1至4个碳原子的烷基，1至4个碳原子的烷氧基，三氟甲基或氨基，R 2为式Q-C n H 2n-NH-R的外消旋和旋光活性化合物 氢，卤素，1至4个碳原子的烷基，1至4个碳原子的烷氧基或三氟甲基，R 1和R 2彼此一起是亚甲二氧基或亚乙二氧基，A是-O-，-CH 2 -CH 2 - ， - O-CH2-，其中氧与苯环结合，或-NR 3 - ，其中R 3是氢或1至4个碳原子的烷基，N是2至6，INCLUSIVE和R R的整数是氢，苄基或 其中R 4是氢，甲基或乙基，R 5，R 6和R 7可以彼此相同或不同，各自为氢，卤素，羟甲基，三氟甲基，1至4个碳原子的烷基，1至 4个碳原子，硝基，氰基，-CONHR 3，-CONHOH，-COOR 3，R 8 O - ，甲基磺酰基甲基，或当R 5至R 7中的一个或两个不同于卤素或三氟甲基时，也可以是-NR 3 R 9， R 3具有上述定义，R 8为氢，1至20个碳原子的烷酰基，1至4个碳原子的烷基或芳烷基，R 9为氢，低级烷酰基，甲磺酰基，氨基甲酰基，二甲基氨磺酰基或烷氧基羰基2至5 碳原子和R 5和R 6彼此一起是-O-CH 2 -O，-O-CH 2 -CH 2 -O - ， - CH = CH-CH = CH-，-O-CH 2 -CONH-， - CH2-CH2-CONH-或-O-CO-NH-，及其无毒的药学上可接受的酸加成盐; 化合物及其盐可用作血管扩张剂和CNS刺激剂。