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公开(公告)号：US08883968B2
公开(公告)日：2014-11-11
申请号：US13876734
申请日：2011-09-30
摘要： The method for producing a surfactin or a salt thereof according to the present invention comprises the steps of adding an organic solvent containing a branched alkyl alcohol to a culture fluid containing the surfactin or the salt thereof, or to a solution obtained by removing an insoluble component from the culture fluid, and extracting the surfactin or the salt thereof with the organic solvent,wherein the surfactin or the salt thereof is represented by the formula (1): wherein * indicates an optically active center; X is an amino acid selected from leucine, isoleucine and valine; R is a C9-13 alkyl group or a C9-13 branched alkyl group; and M is an alkali metal, an alkaline earth metal, an optionally-substituted amine or the like.
摘要翻译： 本发明的表面活性素或其盐的制造方法包括将含有支链烷基醇的有机溶剂添加到含有所述表面活性素或其盐的培养液中的步骤，或者将除去不溶成分 从所述培养液中提取所述表面活性素或其盐，其中所述表面活性素或其盐由式（1）表示：其中*表示光学活性中心; X是选自亮氨酸，异亮氨酸和缬氨酸的氨基酸; R为C 9-13烷基或C 9-13支链烷基; M是碱金属，碱土金属，任意取代的胺等。
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公开(公告)号：US20130197190A1
公开(公告)日：2013-08-01
申请号：US13876734
申请日：2011-09-30
摘要： The method for producing a surfactin or a salt thereof according to the present invention comprises the steps of adding an organic solvent containing a branched alkyl alcohol to a culture fluid containing the surfactin or the salt thereof, or to a solution obtained by removing an insoluble component from the culture fluid, and extracting the surfactin or the salt thereof with the organic solvent,wherein the surfactin or the salt thereof is represented by the formula (1): wherein * indicates an optically active center; X is an amino acid selected from leucine, isoleucine and valine; R is a C9-13 alkyl group or a C9-13 branched alkyl group; and M is an alkali metal, an alkaline earth metal, an optionally-substituted amine or the like.
摘要翻译： 本发明的表面活性素或其盐的制造方法包括将含有支链烷基醇的有机溶剂添加到含有所述表面活性素或其盐的培养液中的步骤，或者将除去不溶成分 从所述培养液中提取所述表面活性素或其盐，其中所述表面活性素或其盐由式（1）表示：其中*表示光学活性中心; X是选自亮氨酸，异亮氨酸和缬氨酸的氨基酸; R为C 9-13烷基或C 9-13支链烷基; M是碱金属，碱土金属，任意取代的胺等。
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3.发明申请METHOD FOR STABILIZING CARBODIIMIDE DERIVATIVE AND STABILIZED COMPOSITION THEREOF 审中-公开用于稳定碳二亚胺衍生物和稳定化合物的方法公开(公告)号：US20100016634A1
公开(公告)日：2010-01-21
申请号：US12439005
申请日：2007-08-30
IPC分类号： C07C267/00
CPC分类号： C07C267/00
摘要： Disclosed is a method for stabilizing a carbodiimide derivative (1) which is a condensing agent useful for production of general synthetic chemical products. Also disclosed is a stabilized composition of the carbodiimide derivative. The method is characterized in that the carbodiimide derivative (1) is handled in an atmosphere wherein the concentration of molecular oxygen in the gas phase within a container is set at not more than 3% by volume and/or in the co-presence of at least one compound selected from the group consisting of antioxidants, N-oxyl compounds, sulfur compounds, amines and Lewis acids.
摘要翻译： 公开了一种稳定碳二亚胺衍生物（1）的方法，碳二亚胺衍生物（1）是可用于生产一般合成化学产品的缩合剂。 还公开了碳二亚胺衍生物的稳定化组合物。 该方法的特征在于，将碳二亚胺衍生物（1）在容器内气相中的分子氧浓度设定为3体积％以下和/或共存于 选自抗氧化剂，N-氧基化合物，硫化合物，胺和路易斯酸的至少一种化合物。
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公开(公告)号：US08183408B2
公开(公告)日：2012-05-22
申请号：US12734661
申请日：2008-11-07
IPC分类号： C07C273/18
CPC分类号： C07C273/1827 , C07C275/16
摘要： The present invention relates to a process for producing an N-carbamoyl-tert-leucine, characterized in mixing tert-leucine with an isocyanic acid compound while a pH of the mixture is kept at not less than 8.0 and not more than 13.5, wherein an amount of the isocyanic acid compound is not less than 0.9 times by mole and not more than 1.1 times by mole relative to an amount of the tert-leucine. According to the present invention, it becomes possible to easily produce an N-carbamoyl-tert-leucine with high efficiency, while the generation of by-products such as a dipeptide-like compound and a urea compound is prevented.
摘要翻译： 本发明涉及一种N-氨基甲酰基 - 叔 - 亮氨酸的制备方法，其特征在于，将所述混合物的pH值保持在8.0以上且13.5以下的条件下，将叔亮氨酸与异氰酸化合物混合， 异氰酸化合物的量相对于叔亮氨酸的量为0.9倍摩尔以上1.1倍以下。 根据本发明，可以高效率地容易地制造N-氨基甲酰基 - 叔 - 亮氨酸，同时防止二肽类化合物和尿素化合物等副产物的产生。
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公开(公告)号：US20100256416A1
公开(公告)日：2010-10-07
申请号：US12734661
申请日：2008-11-07
IPC分类号： C07C229/26
CPC分类号： C07C273/1827 , C07C275/16
摘要： The present invention relates to a process for producing an N-carbamoyl-tert-leucine, characterized in mixing tert-leucine with an isocyanic acid compound while a pH of the mixture is kept at not less than 8.0 and not more than 13.5, wherein an amount of the isocyanic acid compound is not less than 0.9 times by mole and not more than 1.1 times by mole relative to an amount of the tert-leucine. According to the present invention, it becomes possible to easily produce an N-carbamoyl-tert-leucine with high efficiency, while the generation of by-products such as a dipeptide-like compound and a urea compound is prevented.
摘要翻译： 本发明涉及一种N-氨基甲酰基 - 叔 - 亮氨酸的制备方法，其特征在于，将所述混合物的pH值保持在8.0以上且13.5以下的条件下，将叔亮氨酸与异氰酸化合物混合， 异氰酸化合物的量相对于叔亮氨酸的量为0.9倍摩尔以上1.1倍以下。 根据本发明，可以高效率地容易地制造N-氨基甲酰基 - 叔 - 亮氨酸，同时防止二肽类化合物和尿素化合物等副产物的产生。
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公开(公告)号：US09303062B2
公开(公告)日：2016-04-05
申请号：US14129474
申请日：2012-06-28
申请人： Taku Mouri , Naoaki Taoka , Tadashi Moroshima , Koichi Kinoshita
发明人： Taku Mouri , Naoaki Taoka , Tadashi Moroshima , Koichi Kinoshita
IPC分类号： A61K38/05 , C07K7/02 , A23L1/305 , C07K5/02 , A61K8/64 , A61Q19/00 , C05F11/00 , A23L2/52 , A61K38/00
CPC分类号： C07K7/02 , A23L2/52 , A23L33/17 , A61K8/64 , A61K38/00 , A61Q19/00 , C05F11/00 , C07K5/0215 , Y02E50/343 , Y02W30/47
摘要： A solid oxidized glutathione salt is produced by heating an oxidized glutathione at 30° C. or higher while the oxidized glutathione is brought into contact with an aqueous medium in the presence of a substance for providing a cation, to produce the salt of the oxidized glutathione and the cation as a solid, wherein the aqueous medium is composed of water and/or a water-soluble medium, and the cation is at least one selected from an ammonium cation, a calcium cation and a magnesium cation.
摘要翻译： 通过在30℃或更高温度下加热氧化型谷胱甘肽来产生固体氧化型谷胱甘肽盐，同时在提供阳离子的物质存在下使氧化型谷胱甘肽与水性介质接触，生成氧化型谷胱甘肽盐 阳离子为固体，其中水介质由水和/或水溶性介质组成，阳离子为选自铵阳离子，钙阳离子和镁阳离子中的至少一种。
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公开(公告)号：US08026396B2
公开(公告)日：2011-09-27
申请号：US12854215
申请日：2010-08-11
IPC分类号： C07C233/58
CPC分类号： C07C51/09 , C07B2200/07 , C07C67/343 , C07C209/50 , C07C209/56 , C07C209/58 , C07C233/58 , C07C2601/02 , C07C61/40 , C07C69/753 , C07C211/35 , C07C211/40
摘要： This invention relates to processes for the production of optically active 2-(disubstituted aryl)cyclopropylamine compounds and optically active 2-(disubstituted aryl)cyclopropane carboxamide compounds which are useful intermediates for the preparation of pharmaceutical agents, and in particular the compound [1S-(1α,2α,3β(1S*,2R*),5β)]-3-[7-[2-(3,4-difluorophenyl)-cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)-cyclopentane-1,2-diol.
摘要翻译： 本发明涉及制备光学活性2-（二取代芳基）环丙胺化合物和光学活性2-（二取代芳基）环丙烷甲酰胺化合物的方法，它们是制备药剂的有用中间体，特别是化合物[1S- （1α，2α，3＆bgr;（1S *，2R *），5β]] - 3- [7- [2-（3,4-二氟苯基） - 环丙基]氨基] -5-（丙硫基） ，2,3-三唑并[4,5-d]嘧啶-3-基）-5-（2-羟基乙氧基） - 环戊烷-1,2-二醇。
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8.发明授权Process for preparing pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acids 有权制备N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰氨基酸的药理学可接受盐的方法公开(公告)号：US06335453B1
公开(公告)日：2002-01-01
申请号：US09269107
申请日：1999-03-19
IPC分类号： C07K5062
CPC分类号： C07K5/0222 , C07K5/06026
摘要： There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.N-carboxyanhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.
摘要翻译： 提供了制备N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药学上可接受的盐的方法，其包括将氨基酸和N-（1（S） - 乙氧基羰基 - 3-苯基丙基）-L-丙氨酸N-羧酸酐，在中性和酸性条件下进行脱羧，得到N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸，和 形成其药理学上可接受的盐，其中通过在含水液体中进行一系列操作直到形成药理学上可接受的盐或直到药理学上可接受的盐的分离来抑制副产物（3）的产生。 本发明能够以高产率和经济效益以商业规模制备质量高的N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药理学上可接受的盐。
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公开(公告)号：US20080071114A1
公开(公告)日：2008-03-20
申请号：US11833266
申请日：2007-08-03
IPC分类号： C07C209/00
CPC分类号： C07C51/09 , C07B2200/07 , C07C67/343 , C07C209/50 , C07C209/56 , C07C209/58 , C07C233/58 , C07C2601/02 , C07C61/40 , C07C69/753 , C07C211/35 , C07C211/40
摘要： This invention relates to processes for the production of optically active 2-(disubstituted aryl)cyclopropylamine compounds and optically active 2-(disubstituted aryl)cyclopropane carboxamide compounds which are useful intermediates for the preparation of pharmaceutical agents, and in particular the compound [1S-(1α,2α,3β(1S*,2R*),5β)]-3-[7-[2-(3,4-difluorophenyl)-cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)-cyclopentane-1,2-diol.
摘要翻译： 本发明涉及制备光学活性2-（二取代芳基）环丙胺化合物和光学活性2-（二取代芳基）环丙烷甲酰胺化合物的方法，它们是制备药剂的有用中间体，特别是化合物[1S- （1α，2α，3β（1S *，2R *），5β）] - 3- [7- [2-（3,4-二氟苯基） - 环丙基]氨基] -5-（丙硫基）-3H-1,2 ，3-三唑并[4,5-d]嘧啶-3-基）-5-（2-羟基乙氧基） - 环戊烷-1,2-二醇。
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10.发明授权Process for preparing pharmacologically acceptable salt of n-(1(s)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid 失效制备正（（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药学上可接受的盐的方法公开(公告)号：US06518436B2
公开(公告)日：2003-02-11
申请号：US09989186
申请日：2001-11-21
IPC分类号： C07D20704
CPC分类号： C07K5/0222 , C07K5/06026
摘要： There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S) -ethoxycarbonyl-3-phenylpropyl)-L-alanine N-carboxy-anhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.
摘要翻译： 提供了制备N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药学上可接受的盐的方法，其包括将氨基酸和N-（1（S） - 乙氧基羰基 - 3-苯基丙基）-L-丙氨酸N-羧酸酐，在中性和酸性条件下进行脱羧，得到N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸， 并形成其药学上可接受的盐，其中通过在含水液体中进行一系列操作直至形成药理学上可接受的盐或直到药理学上可接受的盐的分离来抑制副产物（3）的产生。 本发明能够以高产率和经济效益以商业规模制备质量高的N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药理学上可接受的盐。
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