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    Method Of Separately Collecting Optically Active Amino Acid Amide And Optically Active Amino Acid
    11.
    发明申请
    Method Of Separately Collecting Optically Active Amino Acid Amide And Optically Active Amino Acid 有权
    分开收集光活性氨基酸酰胺和光活性氨基酸的方法

    公开(公告)号：US20070213559A1

    公开(公告)日：2007-09-13

    申请号：US11587006

    申请日：2005-04-22

    申请人： Atsushi Inoue ,  Akinori Tanaka ,  Satoshi Nanba

    发明人： Atsushi Inoue ,  Akinori Tanaka ,  Satoshi Nanba

    IPC分类号： C07C227/40

    CPC分类号： C07C227/38 ,  C07C231/24 ,  C12P13/04 ,  C07C229/08 ,  C07C237/06

    摘要： The present invention is a method for separately collecting an optically active amino acid amide and an optically active amino acid from an aqueous solution containing the optically active amino acid amide and the optically active amino acid together with at least one member selected from the group consisting of an acid, a base and a salt: comprising a neutralization step of neutralizing an acid or a base when the aqueous solution contains the acid or the base; a desalting step of removing a salt contained in the aqueous solution and/or formed in the neutralization step; and a step of collecting the optically active amino acid amide and the optically active amino acid separately from the aqueous solution which has been desalted in the desalting step, by a process which takes advantage of a difference in solubility between the two components in an organic solvent. The desalting step is preferably performed by an electrodialysis process optionally in the state where ammonia is added to the aqueous solution. According to the present invention, an optically active amino acid amide and an optically active amino acid, which are important as intermediates in the production of pharmaceuticals, agricultural chemicals, and various industrial chemicals, can be separately collected with high efficiency by use of an organic solvent.

    摘要翻译： 本发明是从含有光学活性氨基酸酰胺和光学活性氨基酸的水溶液中分别收集光学活性氨基酸酰胺和光学活性氨基酸的方法，以及选自以下的至少一种： 酸，碱和盐：包含当水溶液含有酸或碱时中和酸或碱的中和步骤; 去除水溶液中含有的盐和/或在中和步骤中形成的脱盐步骤; 以及通过利用有机溶剂中的两种成分之间的溶解度差异的方法，在脱盐步骤中从脱盐的水溶液中分离收集光学活性氨基酸酰胺和光学活性氨基酸的步骤 。 脱盐步骤优选通过电渗析方法进行，任选地在向水溶液中加入氨的状态下进行。 根据本发明，可以通过使用有机物以高效率单独收集作为药物，农药和各种工业化学品生产中的中间体的光学活性氨基酸酰胺和光学活性氨基酸 溶剂。

    Method for producing crystal polymorphs and crystal polymorphs produced thereby
    14.
    发明申请
    Method for producing crystal polymorphs and crystal polymorphs produced thereby 有权
    由此制造晶体多晶型物和晶体多晶型物的方法

    公开(公告)号：US20020137902A1

    公开(公告)日：2002-09-26

    申请号：US10056490

    申请日：2002-01-24

    发明人： Allan S. Myerson ,  Bruce A. Garetz

    IPC分类号： C13K001/00 ,  C07H001/00 ,  C07K001/00

    CPC分类号： C07B61/00 ,  B01D9/0036 ,  C07C227/38 ,  C07K1/306 ,  C07C229/08

    摘要： A method to prepare new or unexpected polymorphs of materials which have not been observed, or to obtain a known polymorph under different conditions than those in which it is usually made, by using a laser to cause nucleation and crystal growth to occur in a supersaturated solution in such a way as to obtain a crystal structure which would not normally appear without the use of the laser.

    摘要翻译： 通过使用激光使得在过饱和溶液中发生成核和晶体生长的方法来制备尚未观察到的材料的新的或意想不到的多晶型物，或者在不同条件下获得已知多晶型物的方法， 以获得在不使用激光的情况下通常不出现的晶体结构的方式。

    Purification process
    15.
    发明授权
    Purification process 失效
    净化过程

    公开(公告)号：US5917086A

    公开(公告)日：1999-06-29

    申请号：US005156

    申请日：1998-01-09

    申请人： James Philip Taylor ,  John Barry Henshall ,  John Whitworth

    发明人： James Philip Taylor ,  John Barry Henshall ,  John Whitworth

    IPC分类号： C07D295/10 ,  C07C227/38 ,  C07C227/40 ,  C07C229/52 ,  C07C229/66 ,  C07D207/08 ,  C07D211/14 ,  C07D307/14 ,  C07D207/04 ,  C07D211/34 ,  C07D295/00

    CPC分类号： C07C227/38

    摘要： A method for the purification of a keto acid having the general formula ##STR1## wherein R1 and R2 independently represent a straight or branched chain alkyl of 1-18 carbon atoms, a cycloalkyl of 4-8 carbon atoms or a phenyl both of which may be substituted by at least one substituent selected from the group consisting of halogen atoms and alkyls having 1-4 carbon atoms, an aralkyl of 7-10 carbon atoms, alkoxyalkyl having 2-20 carbon atoms, tetrahydrofuryl alkyl, alkylcarboxy alkyl, alkyl carboxy benzyl, or R1 and R2 together with the adjacent nitrogen atom may form a heterocyclic ring, or one of R.sub.1 and R.sub.2 is hydrogen, which comprises slurrying the keto acid with an alcohol solvent, maintaining the slurry at elevated temperature in a sealed vessel until the Rhodamine impurity has dissolved, cooling and isolating the pure keto acid by filtration.

    摘要翻译： 一种用于纯化具有以下通式的酮酸的方法：其中R 1和R 2独立地表示1-18个碳原子的直链或支链烷基，4-8个碳原子的环烷基或可以被 选自卤素原子和具有1-4个碳原子的烷基，7-10个碳原子的芳烷基，2-20个碳原子的烷氧基烷基，四氢呋喃基烷基，烷基羧基烷基，烷基羧基苄基或R1的至少一个取代基 并且R 2与相邻的氮原子一起可以形成杂环，或者R 1和R 2中的一个是氢，其包括用醇溶剂将酮酸酸化，将浆液保持在高温下在密封容器中，直到罗丹明杂质溶解 ，通过过滤冷却和分离纯酮酸。

    Method of making 6-aminocaproic acid as active pharmaceutical ingredient
    18.
    发明授权
    Method of making 6-aminocaproic acid as active pharmaceutical ingredient 有权
    制备6-氨基己酸作为活性药物成分的方法

    公开(公告)号：US08809581B2

    公开(公告)日：2014-08-19

    申请号：US13660126

    申请日：2012-10-25

    申请人： Sunny pharmtech Inc.

    发明人： Jien-Heh Tien ,  Chu-yi Pang

    IPC分类号： C07C205/00

    CPC分类号： C07C227/22 ,  C07C227/38

    摘要： The present invention provides a method for making 6-aminocaproic acid as an active pharmaceutical ingredient. The method comprises: performing a hydrolysis procedure to have ε-caprolactam react with acid or base to generate a first reaction mixture, performing a modification procedure to have a solubility regulating agent reacts with 6-aminocaproic acid in the first reaction mixture to form a second reaction mixture including an aminocaproic acid intermediate, performing a separation procedure to have the intermediate separated from the second reaction mixture and performing a hydrogenation procedure to have the aminocaproic acid intermediate hydrogenated to form a 6-aminocaproic acid product.

    摘要翻译： 本发明提供了制备6-氨基己酸作为活性药物成分的方法。 该方法包括：进行水解步骤以使ε-己内酰胺与酸或碱反应以产生第一反应混合物，进行改性步骤以使溶解调节剂与第一反应混合物中的6-氨基己酸反应形成 第二反应混合物，包括氨基己酸中间体，进行分离步骤以使中间体与第二反应混合物分离，并进行氢化方法使氨基己酸中间体氢化形成6-氨基己酸产物。

    Process for the preparation of amino methyl cyclo alkane acetic acids
    19.
    发明授权
    Process for the preparation of amino methyl cyclo alkane acetic acids 有权
    制备氨基甲基环烷烃乙酸的方法

    公开(公告)号：US07635717B2

    公开(公告)日：2009-12-22

    申请号：US10535253

    申请日：2002-11-20

    申请人： Nagarajan Kuppuswamy ,  Sivaramakrishnan Hariharan ,  Arulselvan Mariadas

    发明人： Nagarajan Kuppuswamy ,  Sivaramakrishnan Hariharan ,  Arulselvan Mariadas

    IPC分类号： A61K31/195 ,  C07C229/32

    CPC分类号： C07C227/18 ,  C07C227/38 ,  C07C2601/14 ,  C07C229/28

    摘要： This invention relates to an improved process for the preparation of amino methyl cyclo alkane acetic acids. This invention particularly relates to an improved process for the preparation of gabapentin (which is chemically known as 1-aminomethyl-1-cyclohexaneacetic acid), which is a very well known agent useful for the treatment of epilepsy and other cerebral disorders. In the chemical series of 1-amino methyl cyclo alkane-1-acetic acids, Gabapentin, which is 1-amino methyl cyclo hexane-1-acetic acid has been developed as a drug having anti convulsive properties.

    摘要翻译： 本发明涉及一种制备氨基甲基环烷烃乙酸的改进方法。 本发明特别涉及用于制备加巴喷丁（其化学上称为1-氨基甲基-1-环己烷乙酸）的改进方法，其是用于治疗癫痫和其它脑病的非常熟知的药剂。 在1-氨基甲基环烷-1-乙酸的化学系列中，开发了作为1-氨基甲基环己烷-1-乙酸的加巴喷丁作为具有抗惊厥性质的药物。

    Process suitable for industrial scale production of gabapentin
    20.
    发明授权
    Process suitable for industrial scale production of gabapentin 失效
    工艺适用于加巴喷丁的工业规模生产

    公开(公告)号：US07442834B2

    公开(公告)日：2008-10-28

    申请号：US11457023

    申请日：2006-07-12

    申请人： Tianchun Liu ,  Youming Huang ,  Weirong Fan

    发明人： Tianchun Liu ,  Youming Huang ,  Weirong Fan

    IPC分类号： C07C229/00

    CPC分类号： C07C227/40 ,  C07C227/20 ,  C07C227/38 ,  C07C229/28

    摘要： This invention relates to an improved process for the preparation of substantially pure, stable anhydrous gabapentin. Thus, cyclohexane 1,1-diacetic acid monoamide is first treated with NaOH/NaClO to form 3,3-pentamethylenebutyrolactam, which is treated with aqueous HCl solution under reflux to provide gabapentin HCl salt, which is then neutralized with NaOH followed by a dehydration step to provide substantially pure, storage-stable, pharmaceutical grade gabapentin.

    摘要翻译： 本发明涉及制备基本上纯的，稳定的无水加巴喷丁的改进方法。 因此，首先用NaOH / NaClO处理环己烷1,1-二乙酸单酰胺以形成3,3-五亚甲基丁内酰胺，其在回流下用HCl水溶液处理，得到加巴喷丁HCl盐，然后用NaOH中和脱水 提供基本上纯的储存稳定的药用级加巴喷丁。