Process for the preparation of quinoline carboxylic acids
    5.
    发明授权
    Process for the preparation of quinoline carboxylic acids 失效
    制备喹啉羧酸的方法

    公开(公告)号:US4981966A

    公开(公告)日:1991-01-01

    申请号:US295439

    申请日:1989-01-10

    CPC分类号: C07D215/56 C07F5/022 C07F5/04

    摘要: The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.The advantage of the process of the present invention is that it makes the desired compounds of the Formula I available in a simple manner, with high yields and in a short reaction time.

    摘要翻译: 本发明涉及制备式I化合物(I)(其中R代表氢或甲基)及其药学上可接受的盐的新方法,其包括使式V化合物(V )(其中R 1和R 2表示包含2-6个碳原子并且任选被卤素取代的脂族酰氧基或对于包含7-11个碳原子的芳族酰氧基)与式VI的胺VI, (其中R具有与上述相同的含义)或其盐,并且如此获得的式VII(VII)化合物(其中R,R 1和R 2如上所述)在分离之后或在不分离之前进行水解,以及 如果需要将由此获得的式I的化合物转化成其盐或使其与其盐相同。 式I的化合物是已知的抗菌剂。 本发明方法的优点在于使得所需的式I化合物可以简单的方式得到,产率高,反应时间短。

    Isatin derivatives, processes for the preparation thereof and
pharmaceutical composition comprising the same
    6.
    发明授权
    Isatin derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same 失效
    靛红衍生物,其制备方法和包含其的药物组合物

    公开(公告)号:US4382934A

    公开(公告)日:1983-05-10

    申请号:US83271

    申请日:1979-10-10

    摘要: A compound of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen, halogen, lower alkyl, lower alkoxy, halo (lower) alkyl, lower alkanoylamino, lower alkoxyalylamino, or a 5 to 6 membered saturated or unsaturated heterocyclic group having at least one imino group, and selected from the group consisting of pyrrolidinyl, pyrrolinyl, imidazolidinyl, piperazinyl, piperidyl, and morpholynyl,or R.sup.1 and R.sup.2 are combined together to form a benzene ring,R.sup.3 is oxo or a group of the formula .dbd.N--OR.sup.5, in which R.sup.5 is hydrogen or lower alkyl,R.sup.4 is mono- or di- or triphenyl (lower) alkyl,A is C.sub.1 to C.sub.7 alkylene and its hydroxy derivatives,Y is (C.sub.1 to C.sub.3) alkylene,or a pharmaceutically acceptable salt thereof.Said compounds having antiallergic properties represent inclusively all of the possible optical and/or geometrical isomers due to the asymmetric carbon and carbon-nitrogen double bond.

    摘要翻译: 下式的化合物:其中R 1和R 2是氢,卤素,低级烷基,低级烷氧基,卤代(低级)烷基,低级烷酰氨基,低级烷氧基氨基或5至6元饱和或不饱和杂环基, 至少一个亚氨基,并且选自吡咯烷基,吡咯啉基,咪唑烷基,哌嗪基,哌啶基和吗啉基,或者R 1和R 2结合在一起形成苯环,R 3是氧代或式= N- OR5,其中R5是氢或低级烷基,R4是一或二或三苯基(低级)烷基,A是C1-C7亚烷基及其羟基衍生物,Y是(C1-C3)亚烷基或其药学上可接受的盐 其中。 由于不对称碳和碳 - 氮双键,所述具有抗过敏性质的化合物包括所有可能的光学和/或几何异构体。

    Nitroalkyl-piperazines for inhibiting bacteria fungi and nematodes
    9.
    发明授权
    Nitroalkyl-piperazines for inhibiting bacteria fungi and nematodes 失效
    用于抑制真菌和NEMATODES的NITROALKYL-PIPERAZINES

    公开(公告)号:US3678168A

    公开(公告)日:1972-07-18

    申请号:US3678168D

    申请日:1968-06-21

    申请人: MERCK & CO INC

    发明人: GRIER NATHANIEL

    IPC分类号: C07D295/067 A01N9/22

    CPC分类号: C07D295/067

    摘要: Antimicrobial compositions containing piperazine nitroalkanes useful as soil sterilants and algicides, etc., for agricultural and industrial application.

    摘要翻译: 含有可用作土壤杀菌剂和杀藻剂等的哌嗪硝基烷烃的抗微生物组合物,用于农业和工业应用。