디페닐 유도체를 포함하는 항균제
    53.
    发明公开
    디페닐 유도체를 포함하는 항균제 失效
    含有二苯甲基衍生物的抗菌剂

    公开(公告)号:KR1020120079616A

    公开(公告)日:2012-07-13

    申请号:KR1020110000897

    申请日:2011-01-05

    Abstract: PURPOSE: An antibacterial agent containing novel diphenyl derivative or pharmaceutically acceptable salt thereof is provided to suppress bacterial fatty acid biosynthesis. CONSTITUTION: An antibacerial agent against mycobacteria contains a compound of chemical formula I or pharmaceutically acceptable salt thereof as an active ingredient. The mycobacteria are Mycobacterium tuberculosis. A composition for preventing or treating mycobacterium infections contains the compound or salt as an active ingredient. The mycobacterium infections are tuberculosis. The composition is manufactured in the form of a pharmaceutical composition administered to mammals and birds.

    Abstract translation: 目的:提供含有新二苯衍生物或其药学上可接受的盐的抗菌剂以抑制细菌脂肪酸生物合成。 构成:抗分枝杆菌的抗菌剂含有化学式I的化合物或其药学上可接受的盐作为活性成分。 分枝杆菌是结核分枝杆菌。 用于预防或治疗分枝杆菌感染的组合物含有化合物或盐作为活性成分。 分枝杆菌感染是结核病。 该组合物以施用于哺乳动物和鸟类的药物组合物的形式制造。

    베이커 이스트를 이용한 피라진 화합물의 제조 방법
    56.
    发明公开
    베이커 이스트를 이용한 피라진 화합물의 제조 방법 失效
    通过使用巴克氏酵母在水稻条件下制备水溶性四聚物的方法

    公开(公告)号:KR1020040095889A

    公开(公告)日:2004-11-16

    申请号:KR1020030026907

    申请日:2003-04-29

    Abstract: PURPOSE: Methods for preparing tetrasubstitued pyrazines using baker's yeast are provided, thereby easily and environment-friendly preparing tetrasubstitued pyrazines in water under mild condition. CONSTITUTION: The method for preparing tetrasubstitued pyrazines of formula (2) using baker's yeast comprises the steps of: (1) preparing a solution of baker's yeast; and (2) dissolving beta-keto alpha-oxime carbonyl derivatives of formula (1) in hydrophilic organic solvent and adding the solution into the baker's yeast solution to carry out chemoselective microbial reduction, wherein R1 is methyl, ethyl or phenyl; R2 is hydrogen, methyl or benzyl; R3 is methoxy, ethoxy, benzyloxy or phenylamine; the organic solvent is selected from benzene, toluene and hexane.

    Abstract translation: 目的:提供使用面包酵母制备四取代吡嗪的方法,由此在温和条件下在水中制备四取代吡嗪容易且环境友好。 构成:使用面包酵母制备式(2)的四取代吡嗪的方法包括以下步骤:(1)制备面包酵母溶液; 将式(1)的β-酮基α-肟羰基衍生物溶解在亲水性有机溶剂中,并将溶液加入面包酵母溶液中进行化学选择性微生物还原,其中R1为甲基,乙基或苯基; R2是氢,甲基或苄基; R3是甲氧基,乙氧基,苄氧基或苯胺; 有机溶剂选自苯,甲苯和己烷。

    아세틸콜린 수용체에 작용하는 이소옥사졸 또는이소옥사졸린 치환된 1,2,5,6-테트라하이드로피리딘 유도체
    57.
    发明授权
    아세틸콜린 수용체에 작용하는 이소옥사졸 또는이소옥사졸린 치환된 1,2,5,6-테트라하이드로피리딘 유도체 失效
    아세틸콜린수용체체에작용하는이소옥사졸또는이소옥사졸린치환된1,2,5,6-테트라하이드로피리딘유도체

    公开(公告)号:KR100437973B1

    公开(公告)日:2004-07-02

    申请号:KR1020010066579

    申请日:2001-10-27

    Abstract: PURPOSE: Isoxazole or isoxazoline substituted 1,2,5,6-tetrahydropyridine derivative having high affinity for an acetylcholine receiptor is provided, which compound is useful as a muscarine type acetylcholine receiptor agonist, a recognition improving agent and a treating agent of cerebral nervous disease such as Alzheimer's disease. CONSTITUTION: The isoxazole or isoxazoline substituted 1,2,5,6-tetrahydropyridine derivative represented by formula(1) and a pharmaceutically acceptable salt thereof are provided, wherein R2 is C1-4 alkyl; one of R3 and R4 is one functional group in claim 1 and another of them is H; R5 is hydrogen, hydroxy, hydroxy C1-6 alkyl, C1-6 alkoxymethyl, C1-6 alkoxy, acetoxy, C1-4 alkyl ester, nitrile, aryl, phenylthio, methylthiomethyl, phenylsulfoxide, dimethylthiomethyl, C1-4 alkylketo, C1-4 alkylketo oxime, C1-4 alkylketo C1-5 alkyl oxime, and N-pyrrolidine-2-on; R6 is hydrogen; and R5 and F6 form -CH2OCH2 together. The process for preparing the isoxazole or isoxazoline substituted 1,2,5,6-tetrahydropyridine derivative represented by formula comprises the steps of: reacting 3- or 4-pyridine aldehyde oxime compound of formula(2) with chlorox to prepare nitrile oxide of formula(4); and cycloadddition reaction of nitrile oxide of formula(4) with alkene or alkyne compound of formula(8) or formula(9) to prepare a compound of formula(5) or formula(6); reacting the compound of formula(5) or formula(6) with alkyl iodide to prepare alkyl pyridine salt of formula(7); and reducing the alkyl pyridine salt of formula(7).

    Abstract translation: 目的:提供了对乙酰胆碱接受者具有高亲和力的异恶唑或异恶唑啉取代的1,2,5,6-四氢吡啶衍生物,该化合物可用作毒蕈碱型乙酰胆碱接受者激动剂,识别改善剂和脑神经疾病治疗剂 如阿尔茨海默病。 本发明提供了由式(1)表示的异恶唑或异恶唑啉取代的1,2,5,6-四氢吡啶衍生物及其药学上可接受的盐,其中R2为C1-4烷基; R 3和R 4中的一个是权利要求1中的一个官能团,另一个是H; R5是氢,羟基,羟基C1-6烷基,C1-6烷氧基甲基,C1-6烷氧基,乙酰氧基,C1-4烷基酯,腈,芳基,苯硫基,甲硫基甲基,苯基亚砜,二甲基硫代甲基,C1-4烷基酮基,C1-4 烷基酮肟,C 1-4烷基酮基C 1-5烷基肟和N-吡咯烷-2-酮; R6是氢; R5和F6一起形成-CH2OCH2。 制备由下式表示的异恶唑或异恶唑啉取代的1,2,5,6-四氢吡啶衍生物的方法包括以下步骤:使式(2)的3-或4-吡啶醛肟化合物与氯化氧反应以制备式 (4); 和式(4)的氧化腈与式(8)或式(9)的烯烃或炔烃化合物的环加成加成反应以制备式(5)或式(6)的化合物; 使式(5)或式(6)的化合物与烷基碘反应以制备式(7)的烷基吡啶盐; 和还原式(7)的烷基吡啶盐。

    알릴화된 7-히드록시쿠마린 유도체의 제조방법
    58.
    发明公开
    알릴화된 7-히드록시쿠마린 유도체의 제조방법 失效
    制备所有的7-羟基喹啉衍生物的方法

    公开(公告)号:KR1020020068475A

    公开(公告)日:2002-08-27

    申请号:KR1020020036479

    申请日:2002-06-27

    Abstract: PURPOSE: Provided is a method for preparing allylated 7-hydroxycoumarin derivatives effectively and economically in high yield. CONSTITUTION: The method for preparing allylated 7-hydroxycoumarin is characterized by reacting allylhalide of the formula(1) with 7-hydroxycoumarin of the formula(2) to manufacture allylated 7-hydroxycoumarin derivative of the formula(3).

    Abstract translation: 目的:提供以高产率有效和经济地制备烯丙基化的7-羟基香豆素衍生物的方法。 构成:制备烯丙基化7-羟基香豆素的方法的特征在于使式(1)的烯丙基卤与式(2)的7-羟基香豆素反应制备式(3)的烯丙基化的7-羟基香豆素衍生物。

    알릴화된 방향족 화합물 및 피라노쿠마린 화합물의 제조방법
    59.
    发明公开
    알릴화된 방향족 화합물 및 피라노쿠마린 화합물의 제조방법 失效
    所有芳族化合物和吡咯烷酮衍生物的制备方法

    公开(公告)号:KR1020010096074A

    公开(公告)日:2001-11-07

    申请号:KR1020000019995

    申请日:2000-04-17

    Abstract: PURPOSE: A method for preparing an allyl aromatic compound and a pyranocoumarin derivative are provided, to use an indium metal catalyst which is stable in water and atmosphere, environment-friendly and recyclable and MMPP or hydrogen peroxide as an oxidizing agent which is cheap, for the economical efficiency. CONSTITUTION: The allyl aromatic compound of the formula 3 is prepared by reacting the allyl halogen compound of the formula 1 with the aromatic compound of the formula 2 in the presence of an indium metal catalyst. The allyl aromatic compound of the formula 5 is prepared by reacting the allyl halogen compound of the formula 1 with the aromatic compound of the formula 4 in the presence of an indium metal catalyst. The decursinol of the formula 6 is prepared by the oxidation cyclization of the allyl aromatic compound of the formula 5 and magnesium monoperoxyphthalate hexahydrate(MMPP) or hydrogen peroxide. In the formulas 1, 2, 3, 4, 5 and 6, X is a halogen atom; R1 and R2 are independent each other and are H or a straight of branched hydrocarbon group of C1-C5; R3 is H or OH; and R4 is H, a methyl group or a phenyl group. Preferably an acid catalyst is added further in the case of MMPP used, and a phase transfer catalyst is added further in the case of hydrogen peroxide used.

    Abstract translation: 目的:提供一种制备烯丙基芳族化合物和吡喃香豆素衍生物的方法,使用在水和大气中稳定的环境友好和可回收的铟金属催化剂和廉价的MMPP或过氧化氢作为氧化剂,用于 经济效益。 构成:式3的烯丙基芳族化合物通过在铟金属催化剂的存在下使式1的烯丙基卤素化合物与式2的芳族化合物反应来制备。 式5的烯丙基芳族化合物通过在铟金属催化剂的存在下使式1的烯丙基卤素化合物与式4的芳族化合物反应来制备。 式6的前胡烯醇通过式5的烯丙基芳族化合物和单过氧邻苯二甲酸镁(MMPP)或过氧化氢的氧化环化来制备。 在式1,2,3,4,5和6中,X是卤原子; R1和R2彼此独立,为H或C1-C5的支链烃基的直链; R3是H或OH; R4为H,甲基或苯基。 在使用MMPP的情况下,优选添加酸催化剂,并且在使用过氧化氢的情况下进一步加入相转移催化剂。

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