专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US08058471B2 Method for producing optically active hydroxycarboxylic acid derivatives or salts thereof 失效
标题翻译：光学活性羟基羧酸衍生物或其盐的制备方法
公开(公告)号：US08058471B2
公开(公告)日：2011-11-15
申请号：US12376803
申请日：2007-08-08
申请人： Susumu Amano , Akio Fujii , Shohei Yamamoto , Masaru Mitsuda
发明人： Susumu Amano , Akio Fujii , Shohei Yamamoto , Masaru Mitsuda
IPC分类号： C07C59/00 , C07C65/21
CPC分类号： C07B53/00 , C07B2200/07 , C07C51/00 , C07C51/367 , C07C201/12 , C07C59/48 , C07C205/56
摘要： The present invention has its object to provide a method for producing an optically active hydroxycarboxylic acid derivative which is an intermediate important for production of medicines, agrochemicals, chemical products, and so on. The production method of the present invention comprises: carrying out a hydrogen-transfer reduction of a ketocarboxylic acid or a salt thereof by the reaction of an optically active diamine complex to produce an optically active hydroxycarboxylic acid derivative. According to the present invention, it is possible to safely and efficiently produce an industrially-useful optically active hydroxycarboxylic acid derivative.
摘要翻译：本发明的目的在于提供一种光学活性羟基羧酸衍生物的制造方法，该方法是制备药物，农药，化学品等的重要中间体。本发明的制造方法包括：通过光学活性二胺配合物的反应进行酮羧酸或其盐的氢转移还原反应，生成光学活性羟基羧酸衍生物。根据本发明，可以安全有效地制备工业上有用的光学活性羟基羧酸衍生物。

2. 发明申请

US20100191011A1 METHOD FOR PRODUCING OPTICALLY ACTIVE HYDROXYCARBOXYLIC ACID DERIVATIVES OR SALTS THEREOF 失效
标题翻译：生产光学活性羟基羧酸衍生物或其盐的方法
公开(公告)号：US20100191011A1
公开(公告)日：2010-07-29
申请号：US12376803
申请日：2007-08-08
申请人： Susumu Amano , Akio Fujii , Shohei Yamamoto , Masaru Mitsuda
发明人： Susumu Amano , Akio Fujii , Shohei Yamamoto , Masaru Mitsuda
IPC分类号： C07C51/347
CPC分类号： C07B53/00 , C07B2200/07 , C07C51/00 , C07C51/367 , C07C201/12 , C07C59/48 , C07C205/56
摘要： The present invention has its object to provide a method for producing an optically active hydroxycarboxylic acid derivative which is an intermediate important for production of medicines, agrochemicals, chemical products, and so on. The production method of the present invention comprises: carrying out a hydrogen-transfer reduction of a ketocarboxylic acid or a salt thereof by the reaction of an optically active diamine complex to produce an optically active hydroxycarboxylic acid derivative. According to the present invention, it is possible to safely and efficiently produce an industrially-useful optically active hydroxycarboxylic acid derivative.
摘要翻译：本发明的目的在于提供一种光学活性羟基羧酸衍生物的制造方法，该方法是制备药物，农药，化学品等的重要中间体。本发明的制造方法包括：通过光学活性二胺配合物的反应进行酮羧酸或其盐的氢转移还原反应，生成光学活性羟基羧酸衍生物。根据本发明，可以安全有效地制备工业上有用的光学活性羟基羧酸衍生物。

3. 发明授权

US07094926B2 Process for producing optically active carboxylic acid substituted in 2-position 失效
公开(公告)号：US07094926B2
公开(公告)日：2006-08-22
申请号：US10182260
申请日：2001-01-25
申请人： Susumu Amano , Masaru Mitsuda , Kenji Inoue , Koichi Kinoshita , Koki Yamashita , Yasuyoshi Ueda
发明人： Susumu Amano , Masaru Mitsuda , Kenji Inoue , Koichi Kinoshita , Koki Yamashita , Yasuyoshi Ueda
IPC分类号： C07C51/58
CPC分类号： C07C327/32 , C07C51/04 , C07C51/367 , C07C51/60 , C07C59/48 , C07C57/58 , C07C57/76
摘要： A nitrous acid salt is added at a temperature of 10 to 80° C. to an aqueous solution which contains an optically active 2-aminocarboxylic acid (4) and a protonic acid, the amount of the latter acid being 1 to 3 equivalents to the former, and which has a proton concentration of 0.5 to 2 mol/kg to conduct a reaction to thereby produce an optically active 2-hydroxycarboxylic acid (1). Thionyl chloride and a basic compound are caused to act on the compound (1) to chlorinate it and simultaneously invert the configuration in the 2-position. Thus, an optically active 2-chlorocarboxylic acid chloride (5) is induced. The compound (5) is hydrolyzed to induce an optically active 2-chlorocarboxylic acid (2). The compound (2) is reacted with a thioacetic acid salt to incorporate an acetylthio group thereinto and simultaneously invert the configuration in the 2-position to thereby produce an optically active 2-acetylthiocarboxylic acid (3).

4. 发明授权

US06515134B1 Substituted acetylpridine derivatives and process for the preparation of intermediates for optically active beta-3 agonist by the use of the same 失效
标题翻译：取代的乙酰嘌呤衍生物和通过使用它们制备光学活性β-3激动剂的中间体的方法
公开(公告)号：US06515134B1
公开(公告)日：2003-02-04
申请号：US09926021
申请日：2001-11-07
申请人： Susumu Amano , Naoaki Taoka , Masaru Mitsuda , Kenji Inoue
发明人： Susumu Amano , Naoaki Taoka , Masaru Mitsuda , Kenji Inoue
IPC分类号： C07D21326
CPC分类号： C07D213/30 , C07D213/50 , C07D213/74 , C07D213/75 , C07D405/04
摘要： It is an objective to produce intermediates of optically active beta-3 adrenaline receptor agonists from readily available raw materials in a safe, efficient and industrially advantageous manner. A substituted acetylpyridine derivative represented by the general formula (9) is reduced by enantioselective reduction to produce an optically active hydroxyethyl derivative represented by the general formula (10) (wherein * represents an asymmetric carbon atom), and it is further derivatized to an intermediate of an optically active beta-3 adrenaline receptor agonist, such as an optically active dihydroxyethylpyridine derivative represented by the general formula (14) or an optically active oxirane derivative represented by the general formula (16).
摘要翻译：目的是以安全，有效和工业上有利的方式从容易获得的原料生产光学活性β-3肾上腺素受体激动剂的中间体。由通式（9）表示的取代的乙酰基吡啶衍生物通过对映选择性还原而被还原，以制备由通式（10）表示的光学活性羟乙基衍生物（其中*表示不对称碳原子），并进一步衍生为中间体的光学活性β-3肾上腺素受体激动剂，例如由通式（14）表示的光学活性二羟基乙基吡啶衍生物或由通式（16）表示的光学活性环氧乙烷衍生物。

5. 发明授权

US07282605B2 Optically active 2-allylcarboxylic acid derivative and process for producing the same 失效
标题翻译：光学活性2-烯丙基羧酸衍生物及其制备方法
公开(公告)号：US07282605B2
公开(公告)日：2007-10-16
申请号：US10553394
申请日：2004-04-16
申请人： Kazumi Okuro , Susumu Amano , Noriyuki Kizaki , Teruaki Takesue , Masaru Mitsuda , Noriyuki Ito , Yoshihiko Yasohara
发明人： Kazumi Okuro , Susumu Amano , Noriyuki Kizaki , Teruaki Takesue , Masaru Mitsuda , Noriyuki Ito , Yoshihiko Yasohara
IPC分类号： C07C291/00 , C07C237/16 , C07C237/18 , C07C237/20
CPC分类号： C07C233/18 , C07B2200/07 , C07C51/06 , C07C67/20 , C07C233/05 , C07C271/64 , C12P7/40 , C12P41/005 , C07C57/03 , C07C69/533
摘要： The present invention provides a process for producing an optically active 2-allylcarboxylic acid derivative, which is useful as a pharmaceutical intermediate, from readily available and inexpensive starting materials by the process which can be practiced on a commercial scale in a simple and easy manner, and certain 2-allylcarboxamide derivatives, which are novel and important intermediates in that process.An N-allylcarboxamide derivative undergoes rearrangement reaction diastereoselectively in the presence of a base to give a 2-allylcarboxamide derivative, the resulting derivative is subjected to a carbamation reaction and solvolysis to give an optically active 2-allylcarboxylic acid ester, and then the ester obtained is stereoselectively hydrolyzed using an enzyme to produce 2-allylcarboxylic acid having a high optical purity. In addition, the present invention provides a 2-allylcarboxamide derivative compound which is a novel intermediate in the process of the present invention.
摘要翻译：本发明提供了一种用于制备可用作药物中间体的光学活性2-烯丙基羧酸衍生物的方法，其由易于获得且廉价的原料通过可以简单和容易的方式在商业规模上实施的方法制备，和某些2-烯丙基羧酰胺衍生物，它们是该方法中新颖且重要的中间体。 N-烯丙基甲酰胺衍生物在碱存在下非对映选择性地进行重排反应，得到2-烯丙基甲酰胺衍生物，所得衍生物进行氨基甲酰化反应和溶剂解，得到光学活性2-烯丙基羧酸酯，然后得到所述酯使用酶进行立体选择性水解以产生具有高光学纯度的2-烯丙基羧酸。此外，本发明提供了在本发明的方法中是新型中间体的2-烯丙基甲酰胺衍生物化合物。

6. 发明申请

US20060247470A1 Process for producing optically active carboxylic acid substituted in 2-position 审中-公开
标题翻译：用于制备2-位取代的光学活性羧酸的方法
公开(公告)号：US20060247470A1
公开(公告)日：2006-11-02
申请号：US11477626
申请日：2006-06-30
申请人： Susumu Amano , Masaru Mitsuda , Kenji Inoue , Koichi Kinoshita , Koki Yamashita , Yasuyoshi Ueda
发明人： Susumu Amano , Masaru Mitsuda , Kenji Inoue , Koichi Kinoshita , Koki Yamashita , Yasuyoshi Ueda
IPC分类号： C07C53/15 , C07C53/16
CPC分类号： C07C327/32 , C07C51/04 , C07C51/367 , C07C51/60 , C07C59/48 , C07C57/58 , C07C57/76
摘要： A nitrous acid salt is added at a temperature of 10 to 80° C. to an aqueous solution which contains an optically active 2-aminocarboxylic acid (4) and a protonic acid, the amount of the latter acid being 1 to 3 equivalents to the former, and which has a proton concentration of 0.5 to 2 mol/kg to conduct a reaction to thereby produce an optically active 2-hydroxycarboxylic acid (1). Thionyl chloride and a basic compound are caused to act on the compound (1) to chlorinate it and simultaneously invert the configuration in the 2-position. Thus, an optically active 2-chlorocarboxylic acid chloride (5) is induced. The compound (5) is hydrolyzed to induce an optically active 2-chlorocarboxylic acid (2). The compound (2) is reacted with a thioacetic acid salt to incorporate an acetylthio group thereinto and simultaneously invert the configuration in the 2-position to thereby produce an optically active 2-acetylthiocarboxylic acid (3).
摘要翻译：在10〜80℃的温度下，向含有光学活性的2-氨基羧酸（4）和质子酸的水溶液中加入亚硝酸盐，后者的酸的量为1〜3当量前者，其质子浓度为0.5〜2mol / kg进行反应，由此制造光学活性的2-羟基羧酸（1）。使亚硫酰氯和碱性化合物作用于化合物（1）以使其氯化，同时反转2-位的构型。因此，引入光学活性的2-氯羧酰氯（5）。将化合物（5）水解以诱导光学活性的2-氯羧酸（2）。使化合物（2）与硫代乙酸盐反应以引入乙酰硫基，同时反转2-位的构型，从而产生光学活性的2-乙酰基硫代羧酸（3）。

7. 发明申请

US20060223152A1 Optically active 2-allylcarboxylic acid derivative and process for producing the same 失效
标题翻译：光学活性2-烯丙基羧酸衍生物及其制备方法
公开(公告)号：US20060223152A1
公开(公告)日：2006-10-05
申请号：US10553394
申请日：2004-04-16
申请人： Kazumi Okuro , Susumu Amano , Noriyuki Kizaki , Teruaki Takesue , Masaru Mitsuda , Noriyuki Ito , Yoshihiko Yasohara
发明人： Kazumi Okuro , Susumu Amano , Noriyuki Kizaki , Teruaki Takesue , Masaru Mitsuda , Noriyuki Ito , Yoshihiko Yasohara
IPC分类号： C12P13/00 , C07F3/02
CPC分类号： C07C233/18 , C07B2200/07 , C07C51/06 , C07C67/20 , C07C233/05 , C07C271/64 , C12P7/40 , C12P41/005 , C07C57/03 , C07C69/533
摘要： The present invention provides a process for producing an optically active 2-allylcarboxylic acid derivative, which is useful as a pharmaceutical intermediate, from readily available and inexpensive starting materials by the process which can be practiced on a commercial scale in a simple and easy manner, and certain 2-allylcarboxamide derivatives, which are novel and important intermediates in that process. An N-allylcarboxamide derivative undergoes rearrangement reaction diastereoselectively in the presence of a base to give a 2-allylcarboxamide derivative, the resulting derivative is subjected to a carbamation reaction and solvolysis to give an optically active 2-allylcarboxylic acid ester, and then the ester obtained is stereoselectively hydrolyzed using an enzyme to produce 2-allylcarboxylic acid having a high optical purity. In addition, the present invention provides a 2-allylcarboxamide derivative compound which is a novel intermediate in the process of the present invention.
摘要翻译：本发明提供了一种用于制备可用作药物中间体的光学活性2-烯丙基羧酸衍生物的方法，其由易于获得且廉价的原料通过可以简单和容易的方式在商业规模上实施的方法制备，和某些2-烯丙基羧酰胺衍生物，它们是该方法中新颖且重要的中间体。 N-烯丙基甲酰胺衍生物在碱存在下非对映选择性地进行重排反应，得到2-烯丙基甲酰胺衍生物，所得衍生物进行氨基甲酰化反应和溶剂解，得到光学活性2-烯丙基羧酸酯，然后得到所述酯使用酶进行立体选择性水解以产生具有高光学纯度的2-烯丙基羧酸。此外，本发明提供了在本发明的方法中是新型中间体的2-烯丙基甲酰胺衍生物化合物。

8. 发明授权

US06642387B2 Substituted acetylpyridine derivatives and process for the preparation of intermediates for optically active &bgr;3 agonist by the use of the same 失效
标题翻译：取代的乙酰基吡啶衍生物及其制备用于光学活性β3激动剂的中间体的方法
公开(公告)号：US06642387B2
公开(公告)日：2003-11-04
申请号：US10305105
申请日：2002-11-27
申请人： Susumu Amano , Naoaki Taoka , Masaru Mitsuda , Kenji Inoue
发明人： Susumu Amano , Naoaki Taoka , Masaru Mitsuda , Kenji Inoue
IPC分类号： C07D21346
CPC分类号： C07D213/30 , C07D213/50 , C07D213/74 , C07D213/75 , C07D405/04
摘要： It is an objective to produce intermediates of optically active beta-3 adrenaline receptor agonists from readily available raw materials in a safe, efficient and industrially advantageous manner. A substituted acetylpyridine derivative represented by the general formula (9) is reduced by enantioselective reduction to produce an optically active hydroxyethylpyridine derivative represented by the general formula (10) (wherein * represents an asymmetric carbon atom), and it is further derivatized to an intermediate of an optically active beta-3 adrenaline receptor agonist, such as an optically active dihydroxyethylpyridine derivative represented by the general formula (14) or an optically active oxirane derivative represented by the general formula (16)
摘要翻译：目的是以安全，有效和工业上有利的方式从容易获得的原料生产光学活性β-3肾上腺素受体激动剂的中间体。由通式（9）表示的取代的乙酰基吡啶衍生物通过对映选择性还原反应来制备由通式（10）表示的光学活性羟乙基吡啶衍生物（其中*表示不对称碳原子），并进一步衍生为中间体的光学活性β-3肾上腺素受体激动剂，例如由通式（14）表示的光学活性二羟基乙基吡啶衍生物或由通式（16）表示的光学活性环氧乙烷衍生物，

9. 发明授权

US4797015A Roller cage assembly for use in a bearing 失效
标题翻译：用于轴承的滚子保持架组件
公开(公告)号：US4797015A
公开(公告)日：1989-01-10
申请号：US124331
申请日：1987-11-20
申请人： Kengo Hidano , Susumu Amano
发明人： Kengo Hidano , Susumu Amano
IPC分类号： F16C33/46
CPC分类号： F16C33/4623 , F16C19/463
摘要： A roller-cage assembly for use in a bearing includes a cylindrical cage provided with a plurality of openings extending axially and spaced apart from one another circumferentially and a plurality of rollers, each of which is received in a corresponding one of the openings. Each opening is defined by a pair of oppositely disposed side guide surfaces and a pair of oppositely disposed end guide surfaces, whereby the distance between the pair of oppositely disposed side guide surfaces is larger than the diameter of the roller and the distance between the pair of opposite end guide surfaces is larger than the length of the roller, so that the roller may rotate freely within the opening. Also provided are at least a pair of oppositely disposed outer projections, which project oppositely from the pair of oppositely disposed side guide surfaces at their outermost locations, and at least a pair of oppositely disposed inner projections, which project oppositely from the pair of oppositely disposed side guide surfaces at their innermost locations, whereby the distance between the tips of each pair of the oppositely disposed inner and outer projections is smaller than the diameter of the roller. Thus, the roller is prevented from being undesirably removed from the cage radially by the inner and outer projections, axially by the pair of end guide surfaces, and circumferentially by the pair of side guide surfaces.
摘要翻译：用于轴承的滚子保持架组件包括：圆柱形保持架，其设置有沿轴向轴向间隔开的多个开口，以及多个辊，每个辊容纳在相应的一个开口中。每个开口由一对相对设置的侧引导表面和一对相对设置的端部引导表面限定，由此一对相对设置的侧引导表面之间的距离大于辊的直径和一对相对端引导表面大于辊的长度，使得辊可以在开口内自由旋转。还设置有至少一对相对设置的外突出部，其在最外侧位置与所述一对相对设置的侧引导表面相对地突出，以及至少一对相对设置的内突出部，所述内突起与所述一对相对布置侧引导表面在其最内部位置处，由此每对相对设置的内部和外部突起的尖端之间的距离小于辊的直径。因此，防止辊被内外凸出部沿轴向地由一对端引导表面沿周向不期望地从保持架中移除，并且被一对侧引导表面周向地移除。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式