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113 条记录 (耗时 0.033 秒)

    Quinolone- and 1,8-naphthyridin-4-one-carboxylic acids which are C-bonded in the 7-position
    62.
    发明授权
    Quinolone- and 1,8-naphthyridin-4-one-carboxylic acids which are C-bonded in the 7-position 失效
    在7-位C键合的喹诺酮和1,8-萘啶-4-酮羧酸

    公开(公告)号：US4956465A

    公开(公告)日：1990-09-11

    申请号：US252631

    申请日：1988-10-03

    申请人： Michael Schriewer ,  Klaus Grohe ,  Uwe Petersen

    发明人： Michael Schriewer ,  Klaus Grohe ,  Uwe Petersen

    IPC分类号： C07D215/56 ,  C07D471/04

    CPC分类号： C07D471/04 ,  C07D215/56

    摘要： As novel intermediates for antibacterials, the quinolone- and 1,8-naphthyridine-4-one-carboxylic acids which are C-bonded in the 7-position of the formula ##STR1## in which Y represents a carboxyl group, a nitrile group, an ester group --COOR.sup.3, or an acid amide group --CONR.sup.4 R.sup.5, where R.sup.3 stands for C.sub.1 -C.sub.4 -alkyl,X.sup.2 stands for hydrogen, nitro, alkyl having 1 to 3 carbon atoms and halogen, in particularR.sup.1 can be alkyl having 1-4 carbon atoms, vinyl, halogenoalkyl, hydroxyalkyl, cycloalkyl having 1-6 carbon atoms or optionally substituted phenyl,R.sup.2 stands for hydrogen, alkyl having 1-3 carbon atoms which is optionally substituted by halogen, alkoxy having 1-2 carbon atoms or nitro, phenyl and for a radical ##STR2## and Z.sup.1 and Z.sup.2 can each be hydrogen or various organic radicals or together form a ring,and salts and esters thereof.

    摘要翻译： 作为抗细菌剂的新型中间体，在其中Y表示羧基的式“I”的7-位上与C键合的喹诺酮和1,8-二氮杂萘-4-酮羧酸，腈基 ，酯基-COOR3或酰胺基-CONR4R5，其中R3代表C1-C4-烷基，X2代表氢，硝基，具有1至3个碳原子的烷基和卤素，特别是R1可以是具有1个 -4个碳原子，乙烯基，卤代烷基，羟基烷基，具有1-6个碳原子的环烷基或任选取代的苯基，R 2代表氢，具有1-3个碳原子的烷基，其任选被卤素，具有1-2个碳原子的烷氧基或 硝基，苯基和基团，并且Z 1和Z 2各自可以是氢或各种有机基团或一起形成环，以及它们的盐和酯。

    Process for the preparation of benzoic acid derivatives
    63.
    发明授权
    Process for the preparation of benzoic acid derivatives 失效
    苯甲酸衍生物的制备方法

    公开(公告)号：US4851160A

    公开(公告)日：1989-07-25

    申请号：US90888

    申请日：1987-08-28

    申请人： Uwe Petersen ,  Michael Schriewer ,  Ernst Kysela ,  Klaus Grohe

    发明人： Uwe Petersen ,  Michael Schriewer ,  Ernst Kysela ,  Klaus Grohe

    IPC分类号： C07C63/72 ,  C07C51/363 ,  C07C51/60 ,  C07C63/00 ,  C07C63/70 ,  C07C67/00 ,  C07C227/00 ,  C07C229/60

    CPC分类号： C07C51/363 ,  C07C51/60

    摘要： A process for the preparation of a compound of the formula ##STR1## in which X.sup.1 and X.sup.2 each independently is chlorine or fluorine, andY is chlorine, bromine, fluorine or iodine, comprising subjecting a compound of the formula ##STR2## to a Sandmeyer or Balz-Schiemann reaction thereby to produce a carboxylic acid of the formula ##STR3## and converting the carboxylic acid (Ia) into an acyl chloride of the formula ##STR4## The compound (II) is new. The products are known intermediates for anti-bacterials.

    摘要翻译： 一种制备式（I）的化合物的方法，其中X1和X2各自独立地为氯或氟，Y为氯，溴，氟或碘，其包括使式（VI）化合物 （II）转化为Sandmeyer或Balz-Schiemann反应，从而产生下式的羧酸（Ia），并将羧酸（Ia）转化成式（Ⅰb）的酰氯化合物（ II）是新的。 该产品是已知的抗细菌中间体。

    4-Hydroxy-quinoline-3-carboxylic
    67.
    发明授权
    4-Hydroxy-quinoline-3-carboxylic 失效
    4-羟基 - 喹啉-3-羧酸

    公开(公告)号：US4870182A

    公开(公告)日：1989-09-26

    申请号：US189559

    申请日：1988-05-03

    申请人： Michael Schriewer ,  Klaus Grohe

    发明人： Michael Schriewer ,  Klaus Grohe

    IPC分类号： C07C227/00 ,  C07C45/46 ,  C07C49/807 ,  C07C59/215 ,  C07C67/00 ,  C07C69/738 ,  C07C205/56 ,  C07C205/58 ,  C07C205/61 ,  C07C227/08 ,  C07C229/34 ,  C07C255/42 ,  C07C255/58 ,  C07C317/48 ,  C07C323/63 ,  C07C323/65 ,  C07D215/56

    CPC分类号： C07D215/56 ,  C07C205/56 ,  C07C205/58 ,  C07C205/61 ,  C07C45/46 ,  C07C49/807

    摘要： A process for the preparation of a compound of the formula ##STR1## in which Y is a nitrile group, an ester group COOR.sup.1 or an acid amide CONR.sup.2 R.sup.3,R.sup.1, R.sup.2 and R.sup.3 each independently is hydrogen or C.sub.1 -C.sub.4 -alkyl, and R.sup.3 may also be phenyl, andX.sup.2, X.sup.3, X.sup.4 and X.sup.5 each independently is hydrogen, halogen, nitro, cyano, alkyl having 1-3 carbon atoms, alkoxy having 1-3 carbon atoms, alkylmercapto having 1-3 carbon atoms, alkylsulphonyl having 1-3 carbon atoms, or a phenylsulphonyl group which is optionally substituted in the aryl radical,comprising reacting an aminoacrylate of the formulain whichX.sup.1 is halogen, a nitro group, an alkoxy, alkoxy, alkylmercapto or alkylsulphonyl group having 1-3 carbon atoms in each case, or an arylsulphonyl group,W is hydrogen or a --CH.sub.2 CH.sub.2 Z radical,Z is is a nitrile group, an ester group COOR.sup.4 or an acid amide group CONR.sup.5 R.sup.6, andR.sup.4, R.sup.5 and R.sup.6 each independently is hydrogen or C.sub.1 -C.sub.4 -alkyl, and R.sup.5 may also be phenyl,with an acid acceptor in an aprotic solvent. Some of the reactants are new, as are the products which are intermediates for antibacterially active 1-alkyl-4-quinolone-3-carboxylic acids.

    摘要翻译： 制备其中Y为腈基，酯基COOR1或酰胺CONR2R3，R1，R2和R3各自独立地为氢或C1-C4烷基的式“IMAGE”化合物的方法，R3 也可以是苯基，X2，X3，X4和X5各自独立地是氢，卤素，硝基，氰基，具有1-3个碳原子的烷基，具有1-3个碳原子的烷氧基，具有1-3个碳原子的烷基巯基，烷基磺酰基具有 1-3个碳原子，或任选在芳基中被取代的苯基磺酰基，包括使下式的氨基丙烯酸酯与其中X 1是卤素，硝基，烷氧基，烷氧基，烷基巯基或具有1-3个碳原子的烷基磺酰基反应 每个情况下的原子或芳基磺酰基，W是氢或-CH 2 CH 2 Z基团，Z是腈基，酯基COOR 4或酰胺基CONR 5 R 6，并且R 4，R 5和R 6各自独立地是氢或C1- C4烷基和R5也可以是苯基，在非质子传递溶剂中与酸受体结合。 一些反应物是新的，作为抗菌活性1-烷基-4-喹诺酮-3-羧酸的中间体的产物也是新的。

    Preparation of 1,8-bridged 4-quinoline-3-carboxylic acids
    68.
    发明授权
    Preparation of 1,8-bridged 4-quinoline-3-carboxylic acids 失效
    制备1,8-桥接的4-喹啉-3-羧酸

    公开(公告)号：US4859773A

    公开(公告)日：1989-08-22

    申请号：US172612

    申请日：1988-03-24

    申请人： Klaus Grohe ,  Michael Schriewer

    发明人： Klaus Grohe ,  Michael Schriewer

    IPC分类号： A61K31/495 ,  A61K31/535 ,  A61P31/04 ,  C07C67/00 ,  C07C229/34 ,  C07C231/00 ,  C07C237/04 ,  C07C237/06 ,  C07C237/16 ,  C07C237/20 ,  C07C253/00 ,  C07C255/26 ,  C07C255/27 ,  C07C255/42 ,  C07C301/00 ,  C07C311/00 ,  C07C313/00 ,  C07C317/48 ,  C07C323/25 ,  C07C323/29 ,  C07D215/56 ,  C07D471/06 ,  C07D498/06

    CPC分类号： C07D215/56 ,  C07D471/06

    摘要： A process for the preparation of a 1,8-bridged 4-quinolone-3-carboxylic acid of the formula ##STR1## comprising in a first reaction step reacting an enamine of the formula ##STR2## in an anhydrous, aprotic solvent with one equivalent of a base, at a temperature form 80.degree. C. to 180.degree. C., to give a 4-quinolone-3-carboxylic acid derivative of the formula ##STR3## and, in a second reaction step, reacting that with another equivalent of a base, to give the 1,8-bridged 4-quinolone-3-carboxylic acid derivative of the formula (I) and optionally converting the group Y into a carboxyl group or salt thereof. Both steps may be effected simultaneously in a one-pot process without intermediate isolation of the compound II. Some of the compounds are new. The old and new compounds are antibacterials and promote animal growth.

    摘要翻译： 制备式IMA IMA的1,8桥桥4-喹诺酮-3-羧酸的方法包括在第一反应步骤中使式IMA的烯胺（II）在无水非质子溶剂 与一当量的碱反应，在80℃至180℃的温度下，得到式“IMAGE”的4-喹诺酮-3-羧酸衍生物，并且在第二反应步骤中，使其与 另一当量的碱，得到式（I）的1,8桥桥4-喹诺酮-3-羧酸衍生物，并任选将基团Y转化为羧基或其盐。 两个步骤可以在一锅法中同时进行，而不中间分离化合物II。 一些化合物是新的。 老化合物和新化合物是抗菌药物，促进动物生长。

    Process for the preparation of 4-hydroxy-quinoline-3-carboxylic acids
    69.
    发明授权
    Process for the preparation of 4-hydroxy-quinoline-3-carboxylic acids 失效
    制备4-羟基 - 喹啉-3-羧酸的方法

    公开(公告)号：US4804760A

    公开(公告)日：1989-02-14

    申请号：US43663

    申请日：1987-04-28

    申请人： Michael Schriewer ,  Klaus Grohe

    发明人： Michael Schriewer ,  Klaus Grohe

    IPC分类号： C07C227/00 ,  C07C45/46 ,  C07C49/807 ,  C07C59/215 ,  C07C67/00 ,  C07C69/738 ,  C07C205/56 ,  C07C205/58 ,  C07C205/61 ,  C07C227/08 ,  C07C229/34 ,  C07C255/42 ,  C07C255/58 ,  C07C317/48 ,  C07C323/63 ,  C07C323/65 ,  C07D215/56 ,  C07D215/36 ,  C07D215/38 ,  C07D215/40

    CPC分类号： C07D215/56 ,  C07C205/56 ,  C07C205/58 ,  C07C205/61 ,  C07C45/46 ,  C07C49/807

    摘要： A process for the preparation of a compound of the formula ##STR1## in which Y is a nitrile group, an ester group COOR.sup.1 or an acid amide CONR.sup.2 R.sup.3,R.sup.1, R.sup.2 and R.sup.3 each independently is hydrogen or C.sub.1 -C.sub.4 -alkyl, and R.sup.3 may also be phenyl, andX.sup.2, X.sup.3, X.sup.4 and X.sup.5 each independently is hydrogen, halogen, nitro, cyano, alkyl having 1-3 carbon atoms, alkoxy having 1-3 carbon atoms, alkylmercapto having 1-3 carbon atoms, alkyl-sulphonyl having 1-3 carbon atoms, or a phenylsulphonyl group which is optionally substituted in the aryl radical,comprising reacting an aminoacrylate of the formulain whichX.sup.1 is halogen, a nitro group, an alkoxy, alkoxy, alkylmercapto or alkylsulphonyl group having 1-3 carbon atoms in each case, or an arylsulphonyl group,W is hydrogen or a --CH.sub.2 CH.sub.2 Z radical,Z is a nitrile group, an ester group COOR.sup.4 or an acid amide group CONR.sup.5 R.sup.6, andR.sup.4, R.sup.5 and R.sup.6 each independently is hydrogen or C.sub.1 -C.sub.4 -alkyl, and R.sup.5 may also be phenyl, with an acid acceptor in an aprotic solvent. Some of the reactants are new, as are the products which are intermediates for antibacterially active 1-alkyl-4-quinolone-3-carboxylic acids.

    摘要翻译： 制备其中Y为腈基，酯基COOR1或酰胺CONR2R3，R1，R2和R3各自独立地为氢或C1-C4烷基的式“IMAGE”化合物的方法，R3 也可以是苯基，X2，X3，X4和X5各自独立地是氢，卤素，硝基，氰基，具有1-3个碳原子的烷基，具有1-3个碳原子的烷氧基，具有1-3个碳原子的烷基巯基， 包括具有1-3个碳原子的磺酰基或在芳基中任选取代的苯基磺酰基，包括使下式的氨基丙烯酸酯与其中X 1为卤素，硝基，烷氧基，烷氧基，烷基巯基或具有1- 3个碳原子或芳基磺酰基，W为氢或-CH 2 CH 2 Z基，Z为腈基，酯基COOR4或酰胺基CONR5R6，R4，R5和R6各自独立地为氢或C1 -C 1-4 - 烷基和R 5也可以是苯基，在非质子溶剂中与酸受体反应。 一些反应物是新的，作为抗菌活性1-烷基-4-喹诺酮-3-羧酸的中间体的产物也是新的。