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1. 发明授权

US08232389B2 Method for crystallization of azetidinonecarboxylic acid 失效
标题翻译：氮杂环丁烷羧酸结晶方法
公开(公告)号：US08232389B2
公开(公告)日：2012-07-31
申请号：US12308413
申请日：2007-06-13
申请人： Keita Nishino , Teruyoshi Koga , Masafumi Fukae , Yasuyoshi Ueda
发明人： Keita Nishino , Teruyoshi Koga , Masafumi Fukae , Yasuyoshi Ueda
IPC分类号： C07F7/18
CPC分类号： C07F7/1804
摘要： The present invention relates to a method for crystallization of (2R)-2-{(3S,4S)-3-[(1R)-1-(tert-butyldimethylsilyloxy)ethyl]-2-oxoazetidin-4-yl}propionic acid, and is characterized in that crystallization is carried out by mixing a solution containing the compound with a substituted aromatic hydrocarbon solvent and/or a halogenated hydrocarbon solvent. The method can provide a crystal of the compound with a high purity and a high yield while the content of 2S isomer is kept at a low level.
摘要翻译：本发明涉及（2R）-2 - {（3S，4S）-3 - [（1R）-1-（叔丁基二甲基甲硅烷氧基）乙基] -2-氧代氮杂环丁烷-4-基}丙酸其特征在于，通过将含有该化合物的溶液与取代的芳烃溶剂和/或卤代烃溶剂混合来进行结晶。该方法可以提供具有高纯度和高产率的化合物的晶体，而2S异构体的含量保持在低水平。

2. 发明申请

US20100240886A1 PROCESS FOR PRODUCING CARBAPENEM COMPOUND 审中-公开
标题翻译：生产碳化合物的方法
公开(公告)号：US20100240886A1
公开(公告)日：2010-09-23
申请号：US12294665
申请日：2007-03-27
申请人： Keita Nishino , Teruyoshi Koga
发明人： Keita Nishino , Teruyoshi Koga
IPC分类号： C07D487/04
CPC分类号： C07D477/08
摘要： The present invention has its object to provide an easy process for producing (4R,5S,6S)-3-[[(3S,5S)-5-(dimethylaminocarbonyl)-3-pyrrolidinyl]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid, excellent in antimicrobial activity. The present invention relates to a process for continuously producing (4R,5S,6S)-3-[[(3S,5S)-5-(dimethylaminocarbonyl)-3-pyrrolidinyl]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid without isolating/purifying the reaction intermediate.
摘要翻译：本发明的目的是提供一种制备（4R，5S，6S）-3 - [[（3S，5S）-5-（二甲基氨基羰基）-3-吡咯烷基]硫基] -6 - [（1R） -1-羟乙基] -4-甲基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸，抗菌活性优异。本发明涉及连续生产（4R，5S，6S）-3 - [[（3S，5S）-5-（二甲基氨基羰基）-3-吡咯烷基]硫基] -6 - [（1R）-1- 羟乙基] -4-甲基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸，无需分离/纯化反应中间体。

3. 发明授权

US07524952B2 Process for producing carbapenem compound for oral administration 有权
标题翻译：生产用于口服给药的碳青霉烯类化合物的方法
公开(公告)号：US07524952B2
公开(公告)日：2009-04-28
申请号：US10533183
申请日：2003-11-13
申请人： Keita Nishino , Teruyoshi Koga
发明人： Keita Nishino , Teruyoshi Koga
IPC分类号： C07D477/06 , C07D477/20 , C07D477/04
CPC分类号： C07D477/06 , C07F7/1892 , Y02P20/55
摘要： The present invention provides a process for efficiently producing a 1β-methylcarbapenem compound for oral administration. The process, which is for producing a 1β-methylcarbapenem compound represented by general formula (2), is characterized by reacting a β-lactam compound represented by general formula (1) as a starting material with a thiol compound (R3—SH) in the presence of a base and optionally eliminating the protective group R1. In the formulae (1) and (2), R1 denotes a hydrogen atom, a trimethylsilyl group or a triethylsilyl group; R2 denotes an alkyl group having 1 to 10 carbon atoms or a cycloalkyl group having 3 to 10 carbon atoms; R3 denotes an organic group; and R4 denotes hydrogen, a trimethylsilyl group or a triethylsilyl group.
摘要翻译：本发明提供一种有效地制备口服给药的1β-甲基碳青霉烯化合物的方法。用于制备由通式（2）表示的1β-甲基碳青霉烯化合物的方法的特征在于使由通式（1）表示的β-内酰胺化合物作为起始原料与硫醇化合物（R3-SH）在碱的存在和任选地除去保护基团R1。在式（1）和（2）中，R 1表示氢原子，三甲基甲硅烷基或三乙基甲硅烷基; R2表示碳原子数1〜10的烷基或碳原子数3〜10的环烷基。 R3表示有机基团; R4代表氢，三甲基甲硅烷基或三乙基甲硅烷基。

4. 发明申请

US20060252929A1 Novel intermediate for carbapenem compound for oral administration and process for producing the same 失效
标题翻译：用于口服给药的碳青霉烯类化合物的新型中间体及其制备方法
公开(公告)号：US20060252929A1
公开(公告)日：2006-11-09
申请号：US10533868
申请日：2003-11-13
申请人： Keita Nishino , Teruyoshi Koga
发明人： Keita Nishino , Teruyoshi Koga
IPC分类号： C07F9/572
CPC分类号： C07F9/65611 , C07D205/08 , C07D477/18 , Y02P20/55
摘要： The present invention provides a novel intermediate for efficiently producing a 1β-methylcarbapenem compound for oral administration, and a process for producing the intermediate. That is, the present invention provides a process for producing a novel β-lactam compound represented by general formula (4), the process including allowing a lactam compound represented by general formula (5) as a starting material to react with a compound represented by general formula (6) in the presence of a base to obtain a novel β-lactam compound represented by general formula (1), protecting the hydroxyl group, subsequently performing cyclization in the presence of a strong base, allowing the cyclized compound to react with diphenylphosphoryl chloride to obtain a novel β-lactam compound represented by general formula (3), and eliminating the protecting group therefrom. (In the formulae, R1 represents a trimethylsilyl group or a triethylsilyl group; R2 represents an aryl group or a heteroaryl group; R3 represents an alkyl group having 1 to 10 carbon atoms or a cycloalkyl group having 3 to 10 carbon atoms; and X represents a halogen atom.)
摘要翻译：本发明提供了一种用于口服给药的高效制备1β-甲基碳青霉烯化合物的新型中间体及其制备方法。也就是说，本发明提供一种制备由通式（4）表示的新型β-内酰胺化合物的方法，该方法包括使通式（5）表示的内酰胺化合物作为起始原料与由通式（6）的化合物，得到通式（1）表示的新型β-内酰胺化合物，保护羟基，随后在强碱存在下进行环化，使环化的化合物与二苯基磷酰氯，得到通式（3）表示的新型β-内酰胺化合物，除去保护基。（式中，R 1表示三甲基甲硅烷基或三乙基甲硅烷基; R 2表示芳基或杂芳基; R 3' 表示碳原子数1〜10的烷基或碳原子数3〜10的环烷基，X表示卤素原子。

5. 发明申请

US20060009442A1 Process for producing carbapenem compound for oral administration 有权
标题翻译：生产用于口服给药的碳青霉烯类化合物的方法
公开(公告)号：US20060009442A1
公开(公告)日：2006-01-12
申请号：US10533183
申请日：2003-11-13
申请人： Keita Nishino , Teruyoshi Koga
发明人： Keita Nishino , Teruyoshi Koga
IPC分类号： A61K31/407 , A61K31/43
CPC分类号： C07D477/06 , C07F7/1892 , Y02P20/55
摘要： The present invention provides a process for efficiently producing a 1β-methylcarbapenem compound for oral administration. The process, which is for producing a 1β-methylcarbapenem compound represented by general formula (2), is characterized by reacting a β-lactam compound represented by general formula (1) as a starting material with a thiol compound (R3—SH) in the presence of a base and optionally eliminating the protective group R1. In the formulae (1) and (2), R1 denotes a hydrogen atom, a trimethylsilyl group or a triethylsilyl group; R2 denotes an alkyl group having 1 to 10 carbon atoms or a cycloalkyl group having 3 to 10 carbon atoms; R3 denotes an organic group; and R4 denotes hydrogen, a trimethylsilyl group or a triethylsilyl group.
摘要翻译：本发明提供一种有效地制备口服给药的1β-甲基碳青霉烯化合物的方法。用于制备由通式（2）表示的1β-甲基碳青霉烯化合物的方法的特征在于使由通式（1）表示的β-内酰胺化合物作为起始原料与硫醇化合物（R 3）在碱的存在下，并任选地除去保护基R 1。在式（1）和（2）中，R 1表示氢原子，三甲基甲硅烷基或三乙基甲硅烷基; R 2表示碳原子数1〜10的烷基或碳原子数3〜10的环烷基， R 3表示有机基团; 并且R 4表示氢，三甲基甲硅烷基或三乙基甲硅烷基。

6. 发明授权

US07538212B2 Intermediate for carbapenem compound for oral administration and process for producing the same 失效
标题翻译：用于口服给药的碳青霉烯类化合物的中间体及其制备方法
公开(公告)号：US07538212B2
公开(公告)日：2009-05-26
申请号：US10533868
申请日：2003-11-13
申请人： Keita Nishino , Teruyoshi Koga
发明人： Keita Nishino , Teruyoshi Koga
IPC分类号： C07F9/572 , C07D205/08
CPC分类号： C07F9/65611 , C07D205/08 , C07D477/18 , Y02P20/55
摘要： The present invention provides a novel intermediate represented by formula (1), (3), or (4) for efficiently producing a 1β-methylcarbapenem compound for oral administration, and a process for producing the intermediate. That is, the present invention provides a process for producing a novel β-lactam compound represented by formula (4), the process including allowing a β-lactam compound represented by formula (5) as a starting material to react with a compound represented by formula (6) in the presence of a base to obtain a novel β-lactam compound represented by formula (1), protecting the hydroxyl group, subsequently performing cyclization in the presence of a strong base, allowing the cyclized compound to react with diphenylphosphoryl chloride to obtain a novel β-lactam compound represented by formula (3), and eliminating the protecting group therefrom. The formulae referred to are diagrammed as follows: (In the formulae, R1 represents a trimethylsilyl group or a triethylsilyl group; R2 represents an aryl group or a heteroaryl group; R2 represents an aryl group or a heteroaryl group; R3 represents an alkyl group having 1 to 10 carbon atoms or a cycloalkyl group having 3 to 10 carbon atoms; and X represents a halogen atom.)
摘要翻译：本发明提供了一种用于高效制备口服给药的1β-甲基碳青霉烯化合物的式（1），（3）或（4）所示的新型中间体及其制备方法。也就是说，本发明提供一种制备由式（4）表示的新型β-内酰胺化合物的方法，该方法包括使由式（5）表示的β-内酰胺化合物作为起始原料与由式（6）的化合物，得到由式（1）表示的新型β-内酰胺化合物，保护羟基，随后在强碱存在下进行环化，使环化的化合物与二苯基磷酰氯得到式（3）所示的新型β-内酰胺化合物，除去保护基。所用的化合物如下：（式中，R1表示三甲基甲硅烷基或三乙基甲硅烷基; R2表示芳基或杂芳基; R2表示芳基或杂芳基; R3表示具有 1至10个碳原子或具有3至10个碳原子的环烷基; X表示卤素原子。

7. 发明授权

US08093378B2 Crystallization method for intermediates of carbapenem antibiotics 有权
标题翻译：碳青霉烯类抗生素中间体的结晶方法
公开(公告)号：US08093378B2
公开(公告)日：2012-01-10
申请号：US12226771
申请日：2007-04-18
申请人： Keita Nishino , Teruyoshi Koga , Masafumi Fukae , Yasuyoshi Ueda
发明人： Keita Nishino , Teruyoshi Koga , Masafumi Fukae , Yasuyoshi Ueda
IPC分类号： C07F9/568
CPC分类号： C07F9/65611 , C07D477/18
摘要： An improved crystallization method for an azetidinone compound represented by the formula 1: , which is extremely useful as a common intermediate for the synthesis of 1β-methylcarbapenem compounds. The present method provides crystals having higher quality and stability than conventional crystals and excellent filterability at the time of recovery; and an azetidinone compound having a low content of impurity, and which has a controlled particle size distribution of crystals and improved handleability and stability. The crystallization is carried out by adding a hydrocarbon solvent to a solution in which an azetidinone compound extremely useful as a common intermediate for the synthesis of 1β-methylcarbapenem compounds is dissolved in the presence of a seed crystal in an amount of 200% by weight or less based on the weight of the azetidinone compound.
摘要翻译：用于由式1表示的氮杂环丁酮化合物的改进的结晶方法：其作为合成1'-溴代 - 甲基碳青霉烯化合物的常用中间体非常有用。本方法提供比常规晶体更高的质量和稳定性的晶体，并且在回收时具有优异的过滤性; 和具有低杂质含量的氮杂环丁酮化合物，其具有可控的晶体粒度分布和改进的可操作性和稳定性。结晶是通过将烃溶剂加入到其中作为合成1'-溴代 - 碳代青霉烯化合物的常用中间体的氮杂环丁酮化合物在种子存在下溶解200重量％的溶液或更少，基于氮杂环丁酮化合物的重量。

8. 发明申请

US20100298556A1 Method for crystallization of azetidinonecarboxylic acid 失效
标题翻译：氮杂环丁烷羧酸结晶方法
公开(公告)号：US20100298556A1
公开(公告)日：2010-11-25
申请号：US12308413
申请日：2007-06-13
申请人： Keita Nishino , Teruyoshi Koga , Masafumi Fukae , Yasuyoshi Ueda
发明人： Keita Nishino , Teruyoshi Koga , Masafumi Fukae , Yasuyoshi Ueda
IPC分类号： C07D205/04
CPC分类号： C07F7/1804
摘要： The present invention relates to a method for crystallization of (2R)-2-{(3S, 4S)-3-[(1R)-1-(tert-butyldimethylsilyloxy)ethyl]-2-oxoazetidin-4-yl}propionic acid, and is characterized in that crystallization is carried out by mixing a solution containing the compound with a substituted aromatic hydrocarbon solvent and/or a halogenated hydrocarbon solvent. The method can provide a crystal of the compound with a high purity and a high yield while the content of 2S isomer is kept at a low level.
摘要翻译：本发明涉及（2R）-2 - {（3S，4S）-3 - [（1R）-1-（叔丁基二甲基甲硅烷氧基）乙基] -2-氧代氮杂环丁烷-4-基}丙酸其特征在于，通过将含有该化合物的溶液与取代的芳烃溶剂和/或卤代烃溶剂混合来进行结晶。该方法可以提供具有高纯度和高产率的化合物的晶体，而2S异构体的含量保持在低水平。

9. 发明申请

US20090118496A1 Crystallization Method for Intermediates of Carbapenem Antibiotics 有权
标题翻译：碳青霉烯类抗生素中间体的结晶方法
公开(公告)号：US20090118496A1
公开(公告)日：2009-05-07
申请号：US12226771
申请日：2007-04-18
申请人： Keita Nishino , Teruyoshi Koga , Masafumi Fukae , Yasuyoshi Ueda
发明人： Keita Nishino , Teruyoshi Koga , Masafumi Fukae , Yasuyoshi Ueda
IPC分类号： C07D487/04
CPC分类号： C07F9/65611 , C07D477/18
摘要： The present invention relates to an azetidinone compound extremely useful as a common intermediate for the synthesis of 1β-methylcarbapenem compounds. The present invention provides a crystallization method to obtain a crystal which has a higher quality and a higher stability than a conventional crystal and is excellent in filterability at the time of recovering crystal; an azetidinone compound having a low content of impurity; and an azetidinone compound which has a controlled particle size distribution of crystals and improved handleability and stability. The crystallization is carried out by adding a hydrocarbon solvent to a solution in which an azetidinone compound extremely useful as a common intermediate for the synthesis of 1β-methylcarbapenem compounds is dissolved in the presence of a seed crystal in an amount of 200% by weight or less based on the weight of the azetidinone compound. According to the method, the crystal having a high quality and a high stability and excellent filterability at the time of recovering the crystal can be obtained.
摘要翻译：本发明涉及作为合成1'-甲基碳青霉烯化合物的常用中间体非常有用的氮杂环丁酮化合物。本发明提供一种获得具有比常规晶体更高质量和更高稳定性的晶体的结晶方法，并且在回收晶体时的过滤性优异; 具有低杂质含量的氮杂环丁酮化合物; 和具有可控的晶体粒度分布和改进的可操作性和稳定性的氮杂环丁酮化合物。结晶是通过将烃溶剂加入到其中作为合成1,1-甲基碳青霉烯化合物的常用中间体非常有用的氮杂环丁酮化合物在200重量％的种子晶种存在下溶解的溶液进行的，或少于氮杂环丁酮化合物的重量。根据该方法，可以获得在回收晶体时具有高质量和高稳定性以及优异的过滤性的晶体。

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