Process for the synthesis of N-hydroxypyrroles, N-hydroxyimidazoles, and
derivatives thereof
    83.
    发明授权
    Process for the synthesis of N-hydroxypyrroles, N-hydroxyimidazoles, and derivatives thereof 失效
    N-羟基吡咯,N-羟基咪唑及其衍生物的合成方法

    公开(公告)号:US4006160A

    公开(公告)日:1977-02-01

    申请号:US578895

    申请日:1975-05-19

    CPC分类号: C07D215/60 C07D207/34

    摘要: A process is described for the preparation of N-hydroxypyrrole-2-carbonitriles, N-hydroxyimidazole-2-carbonitriles, pyrrole-2-carbonitriles, and 3-substituted-2, 3-dihydro-2-pyrrolones by thermally decomposing 2-azidoheteroaromatic N-oxides. In the process a 2-azidoheteroaromatic N-oxide is heated in a suitable solvent for a period of time sufficient to bring the reaction to completion. Removal of the solvent by conventional methods gives the desired product. Which product is obtained is determined by the choice of solvents. In non-polar aprotic solvents, N-hydroxypyrrole-2-carbonitriles or N-hydroxyimidazole-2-carbonitriles are obtained. In nucleophilic solvents capable of undergoing Michael-type additions pyrrole-2-carbonitriles, imidazole-2-carbonitriles, and 3-substituted-2,3-dihydro-2-pyrrolone derivatives are obtained where a solvent molecule comprises the 3-substituent. These compounds are useful as anti-bacterials, e.g., against E. Coli.

    摘要翻译: 描述了通过热分解2-叠氮基异芳族化合物制备N-羟基吡咯-2-腈,N-羟基咪唑-2-腈,吡咯-2-腈和3-取代-2,3-二氢-2-吡咯烷酮的方法 N-氧化物。 在该方法中,将2-叠氮基不饱和N-氧化物在合适的溶剂中加热足以使反应完成的时间。 通过常规方法去除溶剂得到所需产物。 获得的产品是由溶剂的选择决定的。 在非极性非质子溶剂中,得到N-羟基吡咯-2-腈或N-羟基咪唑-2-腈。 在能够进行迈克尔型加成的亲核溶剂中,得到吡咯-2-腈,咪唑-2-腈和3-取代-2,3-二氢-2-吡咯酮衍生物,其中溶剂分子包含3-取代基。 这些化合物可用作抗细菌剂,例如抗大肠杆菌。

    Mercapto quinoline n-oxides and their use in combatting dandruff
    85.
    发明授权
    Mercapto quinoline n-oxides and their use in combatting dandruff 失效
    MERCAPTO喹啉N氧化物及其在组合DANDRUFF中的应用

    公开(公告)号:US3862151A

    公开(公告)日:1975-01-21

    申请号:US32571273

    申请日:1973-01-22

    申请人: CIBA GEIGY CORP

    IPC分类号: C07D215/60 C07D33/62

    摘要: Novel compounds having the structural formula in tautomeric form:

    AND METAL SALTS AND COMPLEXES THEREOF WHEREIN R1 and R2 are hydrogen, alkyl, cycloalkyl, aryl, alkylthio, halogen, nitro, trifluoromethyl or alkoxy; x is an integer from 1 to 4 and y is an integer from 1 to 2. The invention also includes anti-dandruff shampoos containing the above metal salts and complexes and to a method of combatting dandruff comprising applying to the hair and scalp a detergent composition containing the above metal complexes.

    摘要翻译: 具有互变异构形式的结构式的新型化合物:

    Derivatives of 4-{8 2-(carbocycloalkoxymethyl) phenylimino{9 -1,4-dihydroquinolines
    86.
    发明授权
    Derivatives of 4-{8 2-(carbocycloalkoxymethyl) phenylimino{9 -1,4-dihydroquinolines 失效
    4- {8 2-(碳氧烷基甲基)苯基] {9-1,4-二氢喹啉的衍生物

    公开(公告)号:US3679687A

    公开(公告)日:1972-07-25

    申请号:US3679687D

    申请日:1970-09-11

    申请人: CIBA GEIGY CORP

    摘要: 4-(2-(Carbocycloalkoxymethyl)phenylimino)-1,4-dihydroquinolines bearing a chloro or trifluoromethyl group in the 7-position of the quinoline nucleus are anti-inflammatory and anti-malarial agents and can be prepared through treatment of a cycloalkyl 2aminophenylacetate with the appropriate 4-chloroquinoline. A typical embodiment is 7-chloro-4-(2(carbocyclohexyloxymethyl)phenylimino)-1,4-dihydroquinoline.

    摘要翻译: 在喹啉核的7-位带有氯或三氟甲基的4- [2-(羧基环烷氧基甲基)苯基亚氨基] -1,4-二氢喹啉是抗炎和抗疟药,可以通过环烷基2 - 氨基苯基乙酸乙酯与适当的4-氯喹啉。 典型的实施方案是7-氯-4- [2-(碳环己基氧基甲基)苯基亚氨基] -1,4-二氢喹啉。