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    • 3. 发明公开
    • 신규 3-페녹시-4-파이론, 3-페녹시-4-피리돈 또는 4-피리돈 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 항균 조성물
    • 新型3-苯基-4-吡喃酮,3-苯氧基-4-吡啶酮或4-吡啶酮衍生物,其制备方法和含有其作为活性成分的抗生物组合物
    • KR1020110011271A
    • 2011-02-08
    • KR1020090068834
    • 2009-07-28
    • 한국과학기술연구원서울대학교산학협력단
    • 신계정노은주정민경차현주서선희
    • C07D309/34C07D213/06A61K31/351A61P31/00
    • C07D213/06A61K31/351C07D309/34
    • PURPOSE: A novel 3-phenoxy-4-pyrone, 3-penoxy-4-pyridone or 4-pyridoen derivative and an antibacterial composition are provided to effectively suppress enoyl-ACP reductase(Fabl). CONSTITUTION: A novel 3-penoxy-4-pyrone, 3-phenoxy-4-pyridone or 4-pyridone derivative is denoted by chemical formula 1. A method for preparing the novel 3-phenoxy-4-pyrone derivative of chemical formula 1 comprises: a step of performing Ullmann reaction of kojic acid compound of chemical formula 4 to obtain a compound of chemical formula 5; a step of substituting the compound of chemical formula 5 with a chloride group to prepare a compound of chemical formula 6; a step of performing Arbuzov reation of the compound of chemical formula 6 to obtain a compound of chemical formula 7; and a step of performing Horner-Emmons reaction of compound of chemical formula 7 to introduce a double bond structure to prepare a compound of chemical formula 1a. An antibacterial composition contains the novel 3-phenoxy-4-pyrone, 3-phenoxy-4-pyridone or 4-pyridone derivative or pharmaceutically acceptable salt thereof as an active ingredient.
    • 目的:提供新颖的3-苯氧基-4-吡喃酮,3-缩氧-4-吡啶酮或4-吡啶酮衍生物和抗菌组合物,以有效抑制烯酰-ACP还原酶(Fab1)。 构成:化学式1表示新的3-氧羰基-4-吡喃酮,3-苯氧基-4-吡啶酮或4-吡啶酮衍生物。制备化学式1的新型3-苯氧基-4-吡喃酮衍生物的方法包括 :进行化学式4的曲酸化合物的乌尔曼反应以获得化学式5的化合物的步骤; 用氯化物基团取代化学式5的化合物制备化学式6的化合物的步骤; 进行化学式6的化合物的Arbuzov化合以获得化学式7的化合物的步骤; 并进行化学式7化合物的霍纳 - 埃蒙斯反应以引入双键结构以制备化学式1a的化合物的步骤。 抗菌组合物含有新型3-苯氧基-4-吡喃酮,3-苯氧基-4-吡啶酮或4-吡啶酮衍生物或其药学上可接受的盐作为活性成分。
    • 7. 发明公开
    • 아지리디닐퀴놀린디온 유도체와 그의 제조방법
    • 亚胺基喹啉衍生物及其制备方法
    • KR1020020031909A
    • 2002-05-03
    • KR1020000062695
    • 2000-10-24
    • 한국과학기술연구원
    • 김동진박상우유경호신계정김동찬
    • C07D403/04
    • C07D401/04
    • PURPOSE: The aziridinyl quinolinedion derivatives and a producing method thereof are provided, which compounds have improved anticancer activity. CONSTITUTION: The aziridinyl quinolinedion derivatives are represented by formula(1), wherein R1 is hydrogen or C1 to C4 alkyl; and any one of R2 and R3 is aziridinyl or 2-methylaziridinyl and the other is halogen, C1 to C4 alkoxy, azido or amino. The aziridinyl quinolinedion derivatives are prepared by reacting 6,7-dihalo-quinolinedion compounds of formula(2) with aiziridine compounds of formula(3) in the presence of organic base and a nonpolar solvent selected from benzene and dioxane at 0 to 20 deg.C to prepare 6-halo-7-aziridinyl quinolinedion of formula(1a) having substituted aziridinyl at C-7 site.
    • 目的:提供吖丙啶喹啉衍生物及其制备方法,该化合物具有改善的抗癌活性。 构成:吖丙啶喹啉衍生物由式(1)表示,其中R 1是氢或C 1至C 4烷基; 并且R2和R3中的任一个是氮丙啶基或2-甲基氮丙啶基,另一个是卤素,C 1至C 4烷氧基,叠氮基或氨基。 氮杂环丁烷基喹啉衍生物通过在有机碱和选自苯和二恶烷的非极性溶剂的存在下,在0至20℃下,使式(2)的6,7-二卤代喹啉化合物与式(3)的氮杂环丁烷化合物反应来制备。 制备在C-7位具有取代的氮丙啶基的式(1a)的6-卤代-7-氮杂环丁烷基喹啉。