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1. 发明公开

KR1020130077458A 벤조디아제핀 유도체의 제조방법 无效
标题翻译：制备苯二酸衍生物的方法
公开(公告)号：KR1020130077458A
公开(公告)日：2013-07-09
申请号：KR1020110146178
申请日：2011-12-29
申请人： 코오롱생명과학 주식회사
发明人： 최윤환 , 신영균 , 장원태 , 최태근 , 박상후
IPC分类号： C07D243/14 , C07D243/26 , A61K31/5513 , A61P25/18
摘要： PURPOSE: A manufacturing method of the benzodiazepine derivative is provided to offer a simple production process and economic benefits not by using the expensive catalyst, and to safely mass-produce the high-yield of benzodiazepine derivative as there is not in danger of ignition or explosion. CONSTITUTION: A manufacturing method of the benzodiazepine derivative comprises the step of manufacturing the compound which is represented by the chemical formula 1 by the reduction reaction between a reducing agent and the compound represented by chemical formula 2. The above manufacturing method of the benzodiazepine derivative is performed by reacting the compound represented by chemical formula 2 with the reducing agent at a mol ratio of 1:0.5-1:10. The above reduction reaction occurs at 0 through 100°C. The above compound represented by chemical formula 2 is manufactured by cyclizing the compound represented by chemical formula 3 under the presence of base basic condition. The base is the one of the group comprised of sodium hydroxide and potassium hydroxide.
摘要翻译：目的：提供苯并二氮杂衍生物的制造方法，以提供简单的生产工艺和经济效益，而不是使用昂贵的催化剂，并且安全地大量生产高产量的苯并二氮杂衍生物，因为没有点燃或爆炸的危险。构成：苯并二氮杂衍生物的制造方法包括通过还原剂与化学式2所示的化合物的还原反应制造由化学式1表示的化合物的步骤。上述苯并二氮杂衍生物的制造方法为通过使化学式2表示的化合物与还原剂以摩尔比为1:0.5-1:10反应而进行。上述还原反应发生在0〜100℃。由化学式2表示的上述化合物通过在碱性碱性条件的存在下使由化学式3表示的化合物环化来制备。碱是由氢氧化钠和氢氧化钾组成的组中的一种。

2. 发明公开

KR1020120058314A 스타틴 화합물의 제조방법 및 이에 사용되는 중간체 화합물 无效
标题翻译：制备其化合物的方法及其使用的中间体化合物
公开(公告)号：KR1020120058314A
公开(公告)日：2012-06-07
申请号：KR1020100120032
申请日：2010-11-29
申请人： 코오롱생명과학 주식회사
发明人： 신영균 , 최윤환 , 장원태 , 최태근
IPC分类号： C07D215/14 , C07D405/06 , C07F9/50 , C07C309/79
CPC分类号： C07D215/14 , C07C309/79 , C07D405/06 , C07F9/50
摘要： PURPOSE: A method for preparing statin compounds and an intermediate compound are provided to ensure working stability and to easily remove reaction by-production. CONSTITUTION: A method for preparing statin compounds comprises: a step of reacting a starting material and sulfonyl compounds to prepare a first intermediate compound; a step of reacting the first intermediate compounds with phosphine compounds to prepare a second intermediate compound; and a step of reacting the second intermediate compounds with carbonyl compounds under the presence of base.
摘要翻译：目的：提供一种制备他汀类化合物和中间体化合物的方法，以确保工作稳定性，并易于除去反应副产物。构成：制备他汀类化合物的方法包括：使原料和磺酰化合物反应制备第一中间体化合物的步骤; 使第一中间体化合物与膦化合物反应以制备第二中间体化合物的步骤; 以及在碱存在下使第二中间体化合物与羰基化合物反应的步骤。

3. 发明公开

KR1020130077451A 아미노벤질아민의 제조방법 无效
标题翻译：制备氨基苯胺的方法
公开(公告)号：KR1020130077451A
公开(公告)日：2013-07-09
申请号：KR1020110146169
申请日：2011-12-29
申请人： 코오롱생명과학 주식회사
发明人： 신영균 , 최윤환 , 장원태 , 김관희 , 최태근 , 박상후
IPC分类号： C07C209/66 , C07C211/49 , C07B31/00
摘要： PURPOSE: A producing method of aminobenzylamine is provided to simplify production processes, and to mass-produce aminobenzylamine with high yield by not using an expensive catalyst. CONSTITUTION: A producing method of aminobenzylamine comprises the following steps: producing a compound denoted by chemical formula 2 by the substitution reaction between a compound denoted by chemical formula 3 and metallic azide; and a producing a compound denoted by chemical formula 1 by the reduction reaction between a nitro group of the compound denoted by the chemical formula 2 with an azide group. In the chemical formula 1: R1 is an alkyl group, an aryl group, a cycloalkyl group, and a heteroaryl group; l is a fixed number selected from 0-4; and R2 is selected from hydrogen, an alkyl group, an aryl group, a cycloalkyl group, and a heteroaryl group.
摘要翻译：目的：提供氨基苄胺的生产方法以简化生产工艺，并通过不使用昂贵的催化剂以高产率大量生产氨基苄胺。构成：氨基苄胺的制造方法包括以下步骤：通过化学式3表示的化合物与金属叠氮化物之间的取代反应来制造由化学式2表示的化合物; 通过化学式2表示的化合物的硝基与叠氮基的还原反应来制造由化学式1表示的化合物。在化学式1中：R 1是烷基，芳基，环烷基和杂芳基; l是0-4的固定数; 并且R 2选自氢，烷基，芳基，环烷基和杂芳基。

4. 发明公开

KR1020130087153A 로수바스타틴의 제조방법 및 이에 사용되는 중간체 화합물 无效
标题翻译：用于制备罗哌沙星及其使用的中间体化合物的方法
公开(公告)号：KR1020130087153A
公开(公告)日：2013-08-06
申请号：KR1020120008215
申请日：2012-01-27
申请人： 코오롱생명과학 주식회사
发明人： 신영균 , 정원택 , 김관희 , 최태근
IPC分类号： C07D239/42 , A61K31/505 , A61K31/495
CPC分类号： A61K31/495 , C07D239/42 , A61K31/505
摘要： PURPOSE: A method for preparing rosuvastatin is provided to obtain a large amount of high purity rosuvastatin using an intermediate compound without a separate purification process. CONSTITUTION: An intermediate compound is denoted by chemical formula 1. A method for preparing the intermediate compound comprises the steps of: reacting a compound of chemical formula 2 with a phosphine-based compound to prepare a compound of chemical formula 3; and reacting the compound of chemical formula 3 with a compound of chemical formula 4 under the presence of a base. A method for preparing a rosuvastatin compound of chemical formula 6 or a pharmaceutically acceptable salt thereof comprises the steps of: deprotecting the intermediate compound of chemical formula 1 under the presence of acid; hydrolyzing the treated compound under the presence of a base; and neutralizing and reacting with a pharmaceutically acceptable salt.
摘要翻译：目的：提供一种制备瑞舒伐他汀的方法，使用中间体化合物获得大量的高纯度瑞舒伐他汀，无需单独的纯化过程。构成：中间体化合物由化学式1表示。制备中间体化合物的方法包括以下步骤：使化学式2的化合物与膦类化合物反应，制备化学式3的化合物; 并在碱的存在下使化学式3的化合物与化学式4的化合物反应。制备化学式6的瑞舒伐他汀化合物或其药学上可接受的盐的方法包括以下步骤：在酸存在下使化学式1的中间体化合物脱保护; 在碱的存在下水解处理的化合物; 并中和并与药学上可接受的盐反应。

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