Substituted naphthyridinyl hydrazines as anti-liver cancer agents

    公开(公告)号:US09855255B1

    公开(公告)日:2018-01-02

    申请号:US15607397

    申请日:2017-05-26

    CPC classification number: A61K31/4375 C07D201/06

    Abstract: The substituted naphthyridinyl hydrazine compounds as anti-liver cancer agents are anti-liver cancer agents that inhibit proliferative pathways of cancer cells, thereby exhibiting potent in vitro and in vivo anticancer activity. The compounds have the formula: wherein R1 and R2 each are selected independently from hydrogen, mercapto, and C1-C5-alkyl, preferably methyl, ethyl, propyl, isopropyl or halogen; R3 and R4 each are selected independently from hydrogen, alkyl or halogen; and R5 is selected from substituted or unsubstituted aryl, more preferably from substituted phenyl, naphthyl, and substituted or unsubstituted heteroaryl, more preferably from furyl, pyrrolyl, thienyl, imidazolyl, thiadiazolyl, pyridinyl, pyridazinyl, pyrimidinyl, benzothiazolyl, oxadiazolyl or sugar moities. These agents exert their action through topoisomerase II inhibition.

    METHOD FOR PRODUCING AMIDE COMPOUND
    45.
    发明申请
    METHOD FOR PRODUCING AMIDE COMPOUND 有权
    生产酰胺化合物的方法

    公开(公告)号:US20130005960A1

    公开(公告)日:2013-01-03

    申请号:US13635092

    申请日:2011-03-15

    CPC classification number: C07D201/06 C07D201/04 C07D225/02

    Abstract: The present invention relates to a method for producing a high purity, high quality amide compound, particularly, lactam. A first embodiment of the present invention is characterized in that an amount of each of a halide, an aldehyde compound, an alcohol compound and a nitrile compound contained in a solution recycled into an oxime-forming step is controlled to an amount of 0.4 mol % or less based on the ketone as a starting material. A second embodiment of the present invention is characterized in that one or more compounds selected from the group consisting of a ketone, an oxime and an amide compound are purified by hydrogenation and/or crystallization for eliminating impurities containing a double bond. A third embodiment of the present invention is characterized in that a content of impurities having a cyclic bridge structure is controlled by using a cycloalkanone purified by recrystallization.

    Abstract translation: 本发明涉及一种生产高纯度,优质酰胺化合物,特别是内酰胺的方法。 本发明的第一实施方案的特征在于,将再循环到肟形成步骤的溶液中所含的卤化物,醛化合物,醇化合物和腈化合物中的每一种的量控制为0.4mol% 基于酮作为原料。 本发明的第二个实施方案的特征在于,通过氢化和/或结晶纯化一种或多种选自酮,肟和酰胺化合物的化合物,以消除含有双键的杂质。 本发明的第三实施方案的特征在于通过使用通过重结晶纯化的环烷酮来控制具有环状桥结构的杂质的含量。

    Process for producing lactam
    46.
    发明授权
    Process for producing lactam 失效
    生产内酰胺的方法

    公开(公告)号:US07045622B2

    公开(公告)日:2006-05-16

    申请号:US10469533

    申请日:2001-03-23

    CPC classification number: C07D201/06 C07D201/04 C07D223/10

    Abstract: It is an object of the present invention to provide a method of continuously producing a lactam in high-temperature high-pressure water, and the present invention relates to a method for producing a lactam characterized by selectively synthesizing the lactam without bringing about hydrolysis by introducing an oxime into flowing high-temperature high-pressure water, wherein the lactam is continuously synthesized at a high rate from the oxime in water at a high temperature of at least 250° C. and a high pressure of at least 12 MPa.

    Abstract translation: 本发明的目的是提供一种在高温高压水中连续生产内酰胺的方法,本发明涉及一种制备内酰胺的方法,其特征在于,通过引入不引起水解而选择性合成内酰胺 将肟流入高温高压水中,其中在至少250℃的高温和至少12MPa的高压下,从肟在水中以高速连续合成内酰胺。

    Process for producing laurolactam from cyclododecanone
    47.
    发明授权
    Process for producing laurolactam from cyclododecanone 有权
    从环十二酮生产十二内酰胺的方法

    公开(公告)号:US06649757B2

    公开(公告)日:2003-11-18

    申请号:US10345548

    申请日:2003-01-16

    CPC classification number: C07D201/06 C07D201/04

    Abstract: Laurolactam having high quality is produced by reacting cyclododecanone with a hydroxylamine salt of a mineral acid, and converting the resultant cyclododecanoneoxime to laurolactam through the Beckmann rearrangement reaction, wherein a content of each of oxygen atom-containing C12 organic compounds, for example, cyclododecenone or epoxycyclododecane, and cycloaliphatic unsaturated C12 hydrocarbon compounds, contained, as an impurity, in the staring cyclododecanone material, is controlled to 1,000 ppm or less.

    Abstract translation: 通过使环十二酮与无机酸的羟胺盐反应,通过贝克曼重排反应将所得的环十二烷酮肟转化为十二内酰胺,生成具有高品质的月桂内酰胺,其中各含氧原子的C12有机化合物,例如环十二酮或 环氧环十二烷和环脂肪族不饱和C12烃化合物被控制在1000ppm以下,作为杂质,在起始环十二烷酮材料中。

    Catalyst and process for oxidation of organic substrates by hydrogen
peroxide
    49.
    发明授权
    Catalyst and process for oxidation of organic substrates by hydrogen peroxide 失效
    通过过氧化氢氧化有机底物的催化剂和方法

    公开(公告)号:US4286068A

    公开(公告)日:1981-08-25

    申请号:US144073

    申请日:1980-04-28

    Abstract: A process for oxidizing organic substrates such as ketones and ethylenically unsaturated compounds. The substrate is contacted with aqueous hydrogen peroxide in a solution or in a two-phase liquid system, in the presence of a polymeric catalyst containing chemically bonded arsenic. This process can lead to lactones or hydroxy acids from cyclic ketones or to esters or mixtures of alcohol and carboxylic acid from open chain ketones. Unsaturated compounds afford epoxides and/or diols. Preparations of certain polymers substituted by arsenic groups, particularly from polystyrene, poly(vinylpyridine) and copolymers thereof, useful as catalysts in such oxidation process, are described. For example, polystyrene is brominated, bromine therein is replaced by lithium and the resulting lithiated polymer is converted into a polymer containing an arsenic group, such as arsono, --As(O)(OH).sub.2, as substituent group, by reaction with arsine triethoxide followed by oxidation and hydrolysis by aqueous hydrogen peroxide. The aromatic polymers, polyphenylene and polymers and copolymers of vinylpyridine, can be used similarly as the catalyst.

    Abstract translation: 氧化有机底物如酮和烯属不饱和化合物的方法。 在含有化学键合的砷的聚合催化剂的存在下,将底物与溶液或两相液体体系中的过氧化氢水溶液接触。 这个过程可以导致来自环酮的内酯或羟基酸或来自开链酮的酯或醇和羧酸的混合物。 不饱和化合物提供环氧化物和/或二醇。 描述了在这种氧化过程中用作催化剂的由砷基特别是聚苯乙烯,聚(乙烯基吡啶)及其共聚物取代的某些聚合物的制备。 例如,聚苯乙烯被溴化,其中的溴被锂代替,所得到的锂化聚合物通过与胂酸反应转化成含有砷基团的聚合物,例如arsono -As(O)(OH)2作为取代基) 然后用过氧化氢水溶液进行氧化和水解。 芳族聚合物,聚苯和乙烯基吡啶的聚合物和共聚物可以类似地用作催化剂。

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