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    • 3. 发明公开
    • 페닐프로피온산 유도체 또는 그의 염의 제조방법
    • 制备苯丙酸衍生物的方法及其制备方法
    • KR1020000033172A
    • 2000-06-15
    • KR1019980049926
    • 1998-11-20
    • 주식회사 코오롱
    • 조은정김맹섭조성민
    • C07C59/86
    • PURPOSE: A method for preparing phenylpropionic acid derivatives as an anti-imflammatory and pain-killing agent and salts thereof are provided. CONSTITUTION: The method for preparing 2-(4-(2-oxocyclopentane-1-mono methyl)propionic acid of formula 1 comprises the steps: reacting 2-(4-halomethyl)phenylpropionic acid of formula 2 with alkyl 2-oxocyclopentanone carboxylate of formula 3 in the presence of bases selected from the group consisting of sodium hydroxide, potassium hydroxide, sodium methoxide, and sodium ethoxide, in organic solvents selected from the group consisting of methylene chloride, chloroform, carbon tetrachloride, 1,2-dichloroethane, benzene, toluene, xylene, acetonitrile, 1,4-dioxane, tetrahydrofuran, and N,N-dimethylformamide; hydrolysing and decarbonizing the resulting compound in the presence of acids such as sulfonic acid, chloric acid, and bromic acid; extracting and concentrating the reaction solution; and crystallizing by addition of solvents or developing on silica gel chromatography.
    • 目的:提供一种制备苯丙酸衍生物作为抗炎和止痛剂及其盐的方法。 构成:制备式1的2-(4-(2-氧代环戊烷-1-单甲基)丙酸的方法包括以下步骤:使式2的2-(4-卤代甲基)苯基丙酸与2-氧代环戊烷-1-羧酸烷基酯 式3在选自氢氧化钠,氢氧化钾,甲醇钠和乙醇钠的碱存在下,在选自二氯甲烷,氯仿,四氯化碳,1,2-二氯乙烷,苯 ,甲苯,二甲苯,乙腈,1,4-二恶烷,四氢呋喃和N,N-二甲基甲酰胺;在酸如磺酸,氯酸和溴酸的存在下水解和脱碳所得化合物;提取并浓缩反应 溶液;通过加入溶剂结晶或在硅胶色谱上显影。
    • 6. 发明公开
    • 페닐프로피온산 유도체 또는 그의 염의 제조방법
    • 苯甲酸衍生物或其盐的制备方法
    • KR1020000033173A
    • 2000-06-15
    • KR1019980049927
    • 1998-11-20
    • 주식회사 코오롱
    • 조은정김맹섭조성민양재권
    • C07C59/86
    • PURPOSE: A method of preparing phenyl propionic acid derivatives or their salts useful for anti-inflammatory and analgesic agent, more specifically a method of preparing 2-(4-(2-oxocyclopentane-1-ylmethyl)phenyl)propionic acid of the following chemical formula 1 or its pharmaceutically acceptable salts is provided the reaction process of which is simple and which is also excellent in yield rate and purity: (chemical formula 1). CONSTITUTION: The method of preparing 2-(4-(2-oxocyclopentane-1-ylmethyl)phenyl)propionic acid or its pharmaceutically acceptable salts is characterized by reacting 2-(4-halomethyl)phenyl propionic acid of the following chemical formula 2 as a starting material with cyclopentanone of the following chemical formula 3: (chemical formula 2), (chemical formula 3), wherein X is Cl, Br or I.
    • 目的:制备苯基丙酸衍生物或其盐可用于抗炎和止痛剂的方法,更具体地说是制备以下化学品的2-(4-(2-(2-氧代环戊烷-1-基甲基)苯基)丙酸的方法 提供式1或其药学上可接受的盐,其反应过程简单并且产率和纯度也优异:(化学式1)。 构成:制备2-(4-(2-氧代环戊烷-1-基甲基)苯基)丙酸或其药学上可接受的盐的方法的特征在于使下列化学式2的2-(4-卤代甲基)苯基丙酸反应为 具有下列化学式3的环戊酮的原料:(化学式2),(化学式3),其中X为Cl,Br或I.
    • 10. 发明授权
    • 치환된 페닐아세트산 유도체의 제조방법
    • KR102393122B1
    • 2022-05-02
    • KR1020207006285
    • 2018-08-07
    • C07C255/41C07C255/40C07C253/14C07C253/30C07C45/67C07C49/693C07C51/00C07C51/08C07C59/86C07C67/30C07C69/716
    • 본발명은약학적제조분야에속하며, 치환된페닐아세트산유도체의신규한제조방법에관한것으로, 특히 2-(4-(2-옥소사이클로펜틸)페닐) 프로판산의제조에관한것이다. 출발물질로서 1,4-디-할로벤질화합물또는이치환된벤질화합물을사용하는전구체형태의록소프로펜을제조하는방법은사이클로펜타논기또는그의전구체화합물의치환반응을통해이루어진다. JPEG112020022554510-pct00049.jpg89108 여기서, X는할로겐이고, L1은할로겐, OH, OMs, OTs, OTf 등에서선택된적합한이탈기이고; L2는할로겐, CN, OH, -CH2OH, -CHO, CH3NO2, 에스테르기, -NR4R5, OTf, OTs, OMs, -C=CR6, -C≡CR7 등에서선택된적합한이탈기이고, 여기서, R4, R5, R6, R7은단쇄알킬기이고; Z는 JPEG112020022554510-pct00050.jpg19101등에서선택된사이클로펜타논기및 그의전구체형태이고; R3은단쇄알킬기이며; L3은할로겐, OH, OMs, OTs, OTf 등, 또는유기금속기에서선택된적합한이탈기이다. 또한, 본발명은사이클로펜타논기의전구체화합물을사이클로펜타논으로전환시킨후, 록소프로펜의전구체화합물을록소프로펜으로전환시키는상세한절차도포함한다.