Imidazolylacetic acid amides, their production, antimycotic compositions
comprising said compounds and their use as antimycotic agents
    2.
    发明授权
    Imidazolylacetic acid amides, their production, antimycotic compositions comprising said compounds and their use as antimycotic agents 失效
    咪唑啉酸,它们的生产,含有化合物的抗微生物组合物及其作为抗菌剂的用途

    公开(公告)号:US4032636A

    公开(公告)日:1977-06-28

    申请号:US651419

    申请日:1976-01-22

    CPC分类号: C07D417/06 A61K31/415

    摘要: Imidazolylacetic acid amides of the formula: ##STR1## or pharmaceutically acceptable nontoxic salts thereof wherein either R.sup.1 is phenyl or cycloalkyl, unsubstituted or substituted by one or more substituents; andR.sup.2 is hydrogen; orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are attached, form a saturated 5 to 7-membered heterocyclic ring which ring may contain an --SO.sub.2 -- or --NY-- moiety wherein Y is alkoxycarbonyl, dialkylaminocarbonyl, or phenyl or diphenylmethyl, unsubstituted or substituted by one or more substituents and wherein said 5 to 7-membered heterocyclic ring itself is otherwise unsubstituted or substituted by one or more substituents; andX.sup.1, x.sup.2, x.sup.3 and X.sup.4 are the same or different and are each hydrogen or halogen,Are produced byA. reacting a halodiphenylacetic acid amide of the formula: ##STR2## wherein R.sup.1, R.sup.2, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as above defined, and Hal is halogen,With imidazole; orB. reacting a halodiphenylacetic acid halide of the formula- ##STR3## WHEREIN X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as above defined and Hal is halogenWith imidazole to produce an imidazolide of the formula: ##STR4## wherein X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as above defined which in turn is transaminated by reaction with an amine of the formula:NHR.sup.1 R.sup.2whereinR.sup.1 and R.sup.2 are as above defined.

    Chlorinated imidazole derivatives and a process for preparing them
    5.
    发明授权
    Chlorinated imidazole derivatives and a process for preparing them 失效
    氯化咪唑衍生物及其制备方法

    公开(公告)号:US3997552A

    公开(公告)日:1976-12-14

    申请号:US602948

    申请日:1975-08-07

    申请人: Karl Heinz Buchel

    发明人: Karl Heinz Buchel

    摘要: Imidazole derivatives, useful as intermediates for making herbicides, having the formula ##STR1## wherein X is chlorine, lower alkyl mono- or polysubstituted by chlorine, or aryl which is optionally mono- or polysubstituted by halogen and/or lower alkyl andR.sub.1 and R.sub.2 are identical or different and are chlorine or phenyl optionally substituted by halogen and/or lower alkyl. The imidazole derivatives are prepared by converting an imidazole derivative having the formula ##STR2## wherein X' is hydrogen, lower alkyl or aryl optionally substituted by halogen atom and/or lower alkyl andR'.sub.1 and R'.sub.2 are identical and represent hydrogen and/or phenyl optionally substituted by halogen and/or lower alkylBy means of hydrogen chloride, in the absence of water, into the corresponding hydrochloride, subsequently reacting with hydrochloride with an excess of chlorine at elevated temperature.

    摘要翻译: 可用作制备除草剂的中间体的咪唑衍生物,其具有下式:其中X为氯,被氯单取代或多取代的低级烷基或芳基,其任选被卤素和/或低级烷基和R1和R2单取代或多取代 是相同或不同的,并且是任选被卤素和/或低级烷基取代的氯或苯基。 咪唑衍生物通过将具有式(IV)的式(IV)的咪唑衍生物转化为其中X'为氢,任选被卤素原子和/或低级烷基取代的低级烷基或芳基,R 1和R 2相同, 表示氢和/或任选被卤素和/或低级烷基取代的苯基。在氢的存在下,氯化氢与相应的氯化氢反应,随后在高温下用氯化氢过量反应。

    N-methyl-imidazole derivatives for treating mycotic infections
    9.
    发明授权
    N-methyl-imidazole derivatives for treating mycotic infections 失效
    用于治疗真菌感染的N-甲基 - 咪唑衍生物

    公开(公告)号:US4062959A

    公开(公告)日:1977-12-13

    申请号:US554009

    申请日:1975-02-28

    摘要: N-methyl-imidazole derivatives of the formula: ##STR1## or a pharmaceutically acceptable non-toxic salt thereof, wherein X is an unsubstituted or substituted 6-membered heteroaromatic moiety having two nitro heteroatoms,Y is an unsubstituted or substituted aliphatic moiety, an unsubstituted or substituted cycloaliphatic moiety, an unsubstituted or substituted aralkyl moiety or an unsubstituted or substituted aryl moiety, andZ is an unsubstituted or substituted aliphatic moiety, an unsubstituted or substituted cycloaliphatic moiety, an unsubstituted or substituted aralkyl moiety, an unsubstituted or substituted aryl moiety, an unsubstituted or substituted pyridyl moiety or an alkoxycarbonyl moiety,Are useful as antimycotic agents.

    摘要翻译: 式(I)的N-甲基 - 咪唑衍生物或其药学上可接受的无毒盐,其中X是具有两个硝基杂原子的未取代或取代的6元杂芳族部分,Y是未取代或取代的脂族 未取代或取代的脂环族部分,未取代或取代的芳烷基部分或未取代或取代的芳基部分,Z为未取代或取代的脂族部分,未取代或取代的脂环族部分,未取代或取代的芳烷基部分,未取代或取代的芳烷基部分, 取代的芳基部分,未取代或取代的吡啶基部分或烷氧基羰基部分,可用作抗生药剂。