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    METHOD FOR STABILIZING CARBODIIMIDE DERIVATIVE AND STABILIZED COMPOSITION THEREOF
    11.
    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

    申请人： Kunihiko Seno ,  Masao Okuda ,  Hiroaki Kawasaki ,  Tadashi Moroshima ,  Yasuyoshi Ueda

    发明人： Kunihiko Seno ,  Masao Okuda ,  Hiroaki Kawasaki ,  Tadashi Moroshima ,  Yasuyoshi Ueda

    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。

    Process for preparing pharmacologically acceptable salt of n-(1(s)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid
    13.
    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

    申请人： Yasuyoshi Ueda ,  Koichi Kinoshita ,  Tadashi Moroshima ,  Yoshifumi Yanagida ,  Yoshihide Fuse

    发明人： Yasuyoshi Ueda ,  Koichi Kinoshita ,  Tadashi Moroshima ,  Yoshifumi Yanagida ,  Yoshihide Fuse

    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。

    METHOD FOR PRODUCING SURFACTIN AND SALT THEREOF
    14.
    发明申请
    METHOD FOR PRODUCING SURFACTIN AND SALT THEREOF 有权
    生产磺草胺及其盐的方法

    公开(公告)号：US20130197190A1

    公开(公告)日：2013-08-01

    申请号：US13876734

    申请日：2011-09-30

    申请人： Masashi Izumida ,  Hiroaki Kawasaki ,  Tadashi Moroshima

    发明人： Masashi Izumida ,  Hiroaki Kawasaki ,  Tadashi Moroshima

    IPC分类号： C07K1/14 ,  C07K1/36

    CPC分类号： C07K1/145 ,  C07K1/36 ,  C07K7/06

    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。

    Process for producing N2-(1(S)-carboxy-3-phenylpropyl)-L-lysyl-L-proline
    17.
    发明授权
    Process for producing N2-(1(S)-carboxy-3-phenylpropyl)-L-lysyl-L-proline 有权
    制备N2-（1（S） - 羧基-3-苯基丙基）-L-赖氨酰-L-脯氨酸的方法

    公开(公告)号：US06271393B1

    公开(公告)日：2001-08-07

    申请号：US09554827

    申请日：2000-07-17

    申请人： Tadashi Moroshima ,  Yoshifumi Yanagida ,  Yoshihide Fuse ,  Yasuyoshi Ueda

    发明人： Tadashi Moroshima ,  Yoshifumi Yanagida ,  Yoshihide Fuse ,  Yasuyoshi Ueda

    IPC分类号： C07D20706

    CPC分类号： C07K5/0222

    摘要： The process for producing N2-(1(S)-carboxy-3-phenylpropyl)-L-lysyl-L-proline in a simple, efficient and industrially advantageous manner, including the following steps: 1) subjecting N2-(1(S)-alkoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysyl-L-proline (1) to alkali hydrolysis in a mixed solution composed of water and a hydrophilic organic solvent using an inorganic base in an amount of n molar equivalents (n ≧ 3) per mole of the above compound (1), 2) neutralizing the hydrolysis product using an inorganic acid in an amount of (n − 1) to n molar equivalents (n ≧ 3) to form a compound (2) and removing the inorganic salt formed by causing the same to precipitate out from a solvent system suited for decreasing the solubility of the inorganic salt, and 3) causing the compound (2) existing in the mixture after removal of the inorganic salt to crystallize out at the isoelectric point thereof and thereby recovering the compound (2) in the form of crystals while retaining the salts including the trifluoroacetic acid-derived organic acid salt in a state dissolved in the mother liquor.

    摘要翻译： 包括以下步骤制备N2-（1（S） - 羧基-3-苯基丙基）-L-赖氨酰-L-脯氨酸的方法，包括以下步骤：1）使N2-（1（S ） - 烷氧基羰基-3-苯基丙基）-N6-三氟乙酰基-L-赖氨酰-L-脯氨酸（1）在由水和亲水性有机溶剂组成的混合溶液中使用n摩尔当量的无机碱进行碱水解（ n）= 3），2）使用（n-1）〜n摩尔当量（n> = 3）的无机酸中和水解产物，形成化合物（2） ），并且通过使其从适合于降低无机盐的溶解度的溶剂体系中析出而形成的无机盐，以及3）除去无机盐以使其结晶出来，使存在于混合物中的化合物（2）结晶出来 其等电点，从而以晶体的形式回收化合物（2），同时保留盐 将三氟乙酸衍生的有机酸盐以溶解在母液中的状态。

    Process for production of N-carbamoyl-tert-leucine
    18.
    发明授权
    Process for production of N-carbamoyl-tert-leucine 失效
    N-氨基甲酰基 - 叔 - 亮氨酸的制备方法

    公开(公告)号：US08183408B2

    公开(公告)日：2012-05-22

    申请号：US12734661

    申请日：2008-11-07

    申请人： Hiroaki Kawasaki ,  Katsuji Maehara ,  Tadashi Moroshima

    发明人： Hiroaki Kawasaki ,  Katsuji Maehara ,  Tadashi Moroshima

    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。

    Method for obtaining optically active epoxide
    19.
    发明授权
    Method for obtaining optically active epoxide 失效
    获得光学活性环氧化物的方法

    公开(公告)号：US07230126B2

    公开(公告)日：2007-06-12

    申请号：US10475122

    申请日：2002-05-10

    申请人： Tadashi Moroshima ,  Yasuyoshi Ueda

    发明人： Tadashi Moroshima ,  Yasuyoshi Ueda

    IPC分类号： C07D301/02

    CPC分类号： C07D301/36 ,  C07D301/32 ,  C07D303/08

    摘要： The present invention provides a method capable of suppressing a decrease in optical purity due to the exposure to heat during distillation of an optically active epoxide to permit an optically active epoxide of high quality to be simply obtained on an industrial scale. In the method, an optically active epoxide is distilled in the presence of a base to suppress a decrease in optical purity.

    摘要翻译： 本发明提供了一种能够抑制光学活性环氧化物蒸馏期间暴露于热量时光学纯度降低的方法，以便以工业规模简单地获得高质量的光学活性环氧化物。 在该方法中，在碱的存在下蒸发光学活性环氧化物以抑制光学纯度的降低。