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1. 发明授权

US6150567A Process for the reduction of carbonyl compounds 失效
标题翻译：还原羰基化合物的方法
公开(公告)号：US6150567A
公开(公告)日：2000-11-21
申请号：US930011
申请日：1997-12-29
申请人： Tadashi Sugawa , Tadashi Moroshima , Kenji Inoue , Kazunori Kan
发明人： Tadashi Sugawa , Tadashi Moroshima , Kenji Inoue , Kazunori Kan
IPC分类号： C07B41/02 , C07B53/00 , C07C29/143 , C07C213/00 , C07C269/06 , C07C271/16 , C07C271/22 , C07C319/20 , C07C323/43 , C07C27/04
CPC分类号： C07B53/00 , C07B41/02 , C07C213/00 , C07C269/06 , C07C29/143 , C07C319/20
摘要： The present invention provides a process for reducing carbonyl compounds to hydroxy compounds, in particular stereoselectively reducing .alpha.-aminohaloketone derivatives, under mild conditions in an easy and simple manner, which comprises reacting a carbonyl compound of the general formula (1) with an organoaluminum compound of the general formula (4) to provide the corresponding alcohol compound of the general formula (5). ##STR1##
摘要翻译： PCT No.PCT / JP97 / 00189 Sec。 371 1997年12月29日第 102（e）日期1997年12月29日PCT 1997年1月29日PCT PCT。公开号WO97 / 28105 日期：1997年8月7日本发明提供了一种在温和条件下以易于简单的方式将羰基化合物还原成羟基化合物，特别是立体选择性还原α-氨基卤代酮衍生物的方法，其包括使通式（1 ）与通式（4）的有机铝化合物反应，得到相应的通式（5）的醇化合物。

2. 发明授权

US6020518A Process for preparing .beta.-amino-.alpha.-hydroxy acid derivatives 失效
标题翻译：制备β-氨基-α-羟基酸衍生物的方法
公开(公告)号：US6020518A
公开(公告)日：2000-02-01
申请号：US242358
申请日：1999-05-14
申请人： Shingo Matsumoto , Kazuhiko Matsuo , Tadashi Sugawa , Tadashi Moroshima , Kenji Inoue
发明人： Shingo Matsumoto , Kazuhiko Matsuo , Tadashi Sugawa , Tadashi Moroshima , Kenji Inoue
IPC分类号： C07C227/02 , C07C227/42 , C07C229/22 , C07C229/34 , C07C229/36 , C07C269/08 , C07C271/18 , C07C271/22 , C07C303/40 , C07C303/44 , C07C311/19 , C07D209/26 , C07C271/14 , C07C51/16 , C07C229/28 , C07C317/14
CPC分类号： C07C303/44 , C07C227/02 , C07C227/42 , C07C269/08 , C07C271/18 , C07C303/40 , C07D209/26 , Y02P20/55
摘要： An object of the present invention is to provide a process for producing a .beta.-amino-.alpha.-hydroxy acid derivative via efficient and industrially utilizable steps.The present invention provides a process for producing a .beta.-amino-.alpha.-hydroxy acid derivative represented by the general formula (2) given below which comprises hydrolyzing an .alpha.-amino-.alpha.', .alpha.'-dihaloketone derivative of the general formula (1) given below in the presence of a base, followed by protecting the amino group or without protecting the same. ##STR1##
摘要翻译： PCT No.PCT / JP97 / 02844 Sec。 371日期1999年5月14日 102（e）日期1999年5月14日PCT 1997年8月18日PCT公布。公开号WO98 / 07687 日本1998年2月26日本发明的目的是提供一种通过有效和可工业利用的步骤生产β-氨基-α-羟基酸衍生物的方法。本发明提供一种制备由下述通式（2）表示的β-氨基-α-羟基酸衍生物的方法，其包括水解通式（1）的α-氨基-α'，α'-二卤代酮衍生物），然后保护氨基或不保护氨基。

3. 发明授权

US6087530A Process for preparing .beta.-amino-.alpha.-hydroxy acid derivatives 失效
标题翻译：制备β-氨基-α-羟基酸衍生物的方法
公开(公告)号：US6087530A
公开(公告)日：2000-07-11
申请号：US437426
申请日：1999-11-15
申请人： Shingo Matsumoto , Kazuhiko Matsuo , Tadashi Sugawa , Tadashi Moroshima , Kenji Inoue
发明人： Shingo Matsumoto , Kazuhiko Matsuo , Tadashi Sugawa , Tadashi Moroshima , Kenji Inoue
IPC分类号： C07C227/02 , C07C227/42 , C07C229/22 , C07C229/34 , C07C229/36 , C07C269/08 , C07C271/18 , C07C271/22 , C07C303/40 , C07C303/44 , C07C311/19 , C07D209/26 , C07B57/00 , C07C229/06 , C07C229/12 , C07C229/14
CPC分类号： C07C303/44 , C07C227/02 , C07C227/42 , C07C269/08 , C07C271/18 , C07C303/40 , C07D209/26 , Y02P20/55
摘要： An object of the present invention is to provide a process for producing a .beta.-amino-.alpha.-hydroxy acid derivative via efficient and industrially utilizable steps.The present invention provides a process for producing a .beta.-amino-.alpha.-hydroxy acid derivative represented by the general formula (2) given below which comprises hydrolyzing an .alpha.-amino-.alpha.', .alpha.-dihaloketone derivative of the general formula (1) given below in the presence of a base, followed by protecting the amino group or without protecting the same. ##STR1##
摘要翻译：本发明的目的是提供一种通过有效且可工业利用的步骤生产β-氨基-α-羟基酸衍生物的方法。本发明提供一种生产由下述通式（2）表示的β-氨基-α-羟基酸衍生物的方法，其包括水解通式（1）的α-氨基-α'，α-二卤代酮衍生物，在碱的存在下给出，然后保护氨基或不保护氨基。

4. 发明授权

US06720449B2 Process for preparing optically active amino acid derivatives 失效
标题翻译：光学活性氨基酸衍生物的制备方法
公开(公告)号：US06720449B2
公开(公告)日：2004-04-13
申请号：US09926346
申请日：2002-02-05
申请人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07D20308
CPC分类号： C07D203/08 , C07B2200/07 , C07C227/10 , C07C227/32 , C07C227/42 , C07C229/30 , C07C303/36 , C07D203/20 , C07D203/24 , C07C311/19 , C07C229/26
摘要： An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
摘要翻译：光学活性氨基酸衍生物通过N-保护光学活性3-卤代丙氨酸衍生物进行环化生成，或使该衍生物环化，接着进行N-保护，从而得到光学活性N-保护的氮丙啶-2-羧酸衍生物，在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物，或通过N-保护光学活性3-卤代丙氨酸衍生物，由此得到N-保护的氮丙啶 -2-羧酸，其在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物。根据该方法，天然和非天然旋光氨基酸可以是通过简单的程序从便宜的材料生产。

5. 发明授权

US07109352B2 Process for producing optically active amino acid derivatives 失效
标题翻译：光学活性氨基酸衍生物的制备方法
公开(公告)号：US07109352B2
公开(公告)日：2006-09-19
申请号：US10716430
申请日：2003-11-20
申请人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07D203/02 , C07D203/08
CPC分类号： C07D203/08 , C07B2200/07 , C07C227/10 , C07C227/32 , C07C227/42 , C07C229/30 , C07C303/36 , C07D203/20 , C07D203/24 , C07C311/19 , C07C229/26
摘要： An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
摘要翻译：光学活性氨基酸衍生物是通过N-保护光学活性3-卤代丙氨酸衍生物进行环化，或环化该衍生物进行N-保护而得到光学活性N-保护的氮丙啶-2-羧酸衍生物在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物，或通过N-保护光学活性3-卤代丙氨酸衍生物，由此得到N-保护的氮丙啶 -2-羧酸，其在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物。根据该方法，可以通过简单的方法从便宜的材料制备天然和非天然旋光氨基酸。

6. 发明申请

US20050143586A1 Process for producing optically active amino acid derivatives 失效
标题翻译：光学活性氨基酸衍生物的制备方法
公开(公告)号：US20050143586A1
公开(公告)日：2005-06-30
申请号：US10716430
申请日：2003-11-20
申请人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07C227/10 , C07C227/32 , C07C227/42 , C07C229/26 , C07C229/30 , C07C303/36 , C07C311/19 , C07D203/08 , C07D203/20 , C07D203/24 , C07D203/16
CPC分类号： C07D203/08 , C07B2200/07 , C07C227/10 , C07C227/32 , C07C227/42 , C07C229/30 , C07C303/36 , C07D203/20 , C07D203/24 , C07C311/19 , C07C229/26
摘要： An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
摘要翻译：光学活性氨基酸衍生物通过N-保护光学活性3-卤代丙氨酸衍生物进行环化生成，或使该衍生物环化，接着进行N-保护，从而得到光学活性N-保护的氮丙啶-2-羧酸衍生物，在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物，或通过N-保护光学活性3-卤代丙氨酸衍生物，由此得到N-保护的氮丙啶 -2-羧酸，其在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物。根据该方法，可以通过简单的方法从便宜的材料制备天然和非天然旋光氨基酸。

7. 发明授权

US09303062B2 Solid oxidized glutathione salt and method for producing same 有权
标题翻译：固体氧化型谷胱甘肽盐及其制备方法
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。

8. 发明授权

US08026396B2 Processes for the preparation of optically active intermediates 有权
标题翻译：用于制备光学活性中间体的方法
公开(公告)号：US08026396B2
公开(公告)日：2011-09-27
申请号：US12854215
申请日：2010-08-11
申请人： Masaru Mitsuda , Tadashi Moroshima , Kentaro Tsukuya , Kazuhiko Watabe , Masahiko Yamada
发明人： Masaru Mitsuda , Tadashi Moroshima , Kentaro Tsukuya , Kazuhiko Watabe , Masahiko Yamada
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。

9. 发明授权

US06335453B1 Process for preparing pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acids 有权
标题翻译：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
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： 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。

10. 发明授权

US08883968B2 Method for producing surfactin and salt thereof 有权
标题翻译：表面活性素及其盐的制备方法
公开(公告)号：US08883968B2
公开(公告)日：2014-11-11
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 , C07K1/30 , C07K7/06 , 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。

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