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    • 13. 发明公开
    • 로큐로니움 브로마이드의 제조방법
    • 制备溴化硼的方法
    • KR1020100063370A
    • 2010-06-11
    • KR1020080121867
    • 2008-12-03
    • (주) 성운파마코피아
    • 정인화박성진이수철최왕근
    • C07J11/00C07J43/00
    • C07J11/00C07J13/00C07J43/00
    • PURPOSE: A method for preparing high quality and high purity rocuronium bromide is provided, which is industrially useful. CONSTITUTION: A method for preparing rocuronium bromide comprises the steps of: obtaining the compound of the chemical formula V by reacting the compound of IV with morpholine; obtaining the compound of the chemical formula VI by reacting the compound of the chemical formula V with an acetate compound; obtaining a compound of the chemical formula VII by reacting the compound of the chemical formula VI with pyrrolidine; and obtaining the compound of the chemical formula VIII by reacting the compound of the chemical formula VII with acetyl chloride.
    • 目的:提供一种制备高品质,高纯度罗库溴铵的方法,在工业上有用。 构成:制备罗库溴铵的方法包括以下步骤:通过使IV化合物与吗啉反应获得化学式V的化合物; 通过使化学式V的化合物与乙酸酯化合物反应获得化学式VI的化合物; 通过使化学式VI的化合物与吡咯烷反应获得化学式VII的化合物; 并通过化学式Ⅶ化合物与乙酰氯反应得到化学式Ⅷ化合物。
    • 14. 发明公开
    • 세펨 화합물의 결정형 산 부가염의 직접 제조방법
    • 制备CEPHEM衍生物的晶体酸添加盐的直接方法
    • KR1020090063817A
    • 2009-06-18
    • KR1020070131322
    • 2007-12-14
    • (주) 성운파마코피아우진비엔지 주식회사
    • 정인화박성진이수철최왕근강석진
    • C07D501/34
    • A method for manufacturing a crystalline acid-added salt of cephem compound which is used for antibiotics is provided to easily introduce nitrogen-containing heterocyclic group and directly obtain from the acid-added salt. A method for producing a crystalline acid-added salt of cephem compound comprises: a step of reacting a cepotaxim derivative of the chemical formula 2 or its salt and heterocycle compound of R1-H under the presence of base and halogenation silyl compound to obtain the acid-added salt of cephem compound of the chemical formula 1; and a step of crystallizing the acid-added salt of cephem compound using sulphuric acid(H2SO4). The cephem compound of the chemical formula 1 is cefepime, cefpirome, or cefquinome. The base is dimethylaniline or diethylaniline. The reaction solvent is acetonitrile, dichloromethane, dimethylformamide or dimethylacetamide.
    • 提供了用于抗生素的头孢烯化合物的结晶性酸加成盐的制造方法,容易地导入含氮杂环基,并直接从酸加成盐得到。 一种头孢烯化合物的结晶性酸加成盐的制造方法,其特征在于,使化学式2的头孢噻肟衍生物或其盐与R1-H的杂环化合物在碱和卤化甲硅烷基化合物的存在下反应,得到酸 化学式1的头孢烯化合物的添加盐; 和使用硫酸(H 2 SO 4)使头孢烯化合物的酸加成盐结晶的步骤。 化学式1的头孢烯化合物是头孢吡肟,头孢匹罗或头孢喹肟。 碱为二甲基苯胺或二乙基苯胺。 反应溶剂为乙腈,二氯甲烷,二甲基甲酰胺或二甲基乙酰胺。
    • 18. 发明公开
    • 엔테카비어 제조방법
    • ENTECAVIR的准备方法
    • KR1020120091971A
    • 2012-08-20
    • KR1020110023232
    • 2011-03-16
    • (주) 성운파마코피아주식회사 한서켐
    • 정인화장명식김기남
    • C07D473/18A61K31/522A61P31/20
    • Y02P20/55C07D473/18A61K31/522
    • PURPOSE: A method for preparing entecavir is provided to cheaply obtain the entecavir of high purity and high content. CONSTITUTION: A method for preparing entecavir comprises: a step of reacting a compound of chemical formula 2 with alpha-hydroxy acetyl halide to prepare a ketene cyclic compound of chemical formula 3; a step of ring opending and reducing the keten cyclic compound under the presence of a base catalyst to prepare a compound of chemical formula 4; a step of esterification, sharpless epoxidation, and ring opening of the compound of chemical formula 4 and introducing R2 as an alcohol protection group to prepare a compound of chemical formula 5; a step of alkylation of the compounds of chemical formulas 5 and 6 to prepare a compound of chemical formula 7; a step of introducing amine protection group R3 to the compound of chemical formula 7 to prepare a compound of chemical formula 8; a step of preparing alkene compound of chemical formula 10 through Witting or under the presence of acid catalyst; and a step of deprotecting the compound of chemical formula 10.
    • 目的:提供一种制备恩替卡韦的方法,以便廉价地获得高纯度和高含量的恩替卡韦。 构成:制备恩替卡韦的方法包括:使化学式2的化合物与α-羟基乙酰卤反应制备化学式3的烯酮环状化合物的步骤; 在碱催化剂存在下,使环化合物和环酮化合物还原,制备化学式4的化合物; 化学式4化合物的酯化,无水环氧化和开环步骤,引入R2作为醇保护基,制备化学式5的化合物; 化学式5和化合物6的烷基化步骤以制备化学式7的化合物; 向化学式7化合物引入胺保护基团R3以制备化学式8的化合物的步骤; 通过配制或在酸催化剂存在下制备化学式10的烯烃化合物的步骤; 和使化学式10的化合物脱保护的步骤。