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1. 发明授权

US5599954A N-substituted-7-amino-5-hydroxy-3-oxoheptanoic acid derivatives and method for producing the same 失效
标题翻译： N-取代-7-氨基-5-羟基-3-氧代庚酸衍生物及其制备方法
公开(公告)号：US5599954A
公开(公告)日：1997-02-04
申请号：US592494
申请日：1996-01-26
申请人： Sigeru Mitsuhashi , Tsukasa Sotoguchi , Yoshifumi Yuasa , Hidenori Kumobayashi
发明人： Sigeru Mitsuhashi , Tsukasa Sotoguchi , Yoshifumi Yuasa , Hidenori Kumobayashi
IPC分类号： A61K31/21 , A61P3/06 , A61P43/00 , C07C231/12 , C07C233/83 , C07C269/06 , C07C271/16 , C07C271/22 , C07D309/12 , C07D315/00
CPC分类号： C07C233/83 , C07C271/22 , C07D309/12 , Y02P20/55
摘要： Compounds represented by the following general structural formula (1) and methods for producing the compounds: ##STR1## R.sup.1 represents a group such as benzyloxycarbonyl, R.sup.2 represents a lower alkyl group, R.sup.3 represents a hydrogen atom or a protecting group, each of M.sup.1 and M.sup.2 represents a metal atom, and n represents the atomic valence of M.sup.1. Intermediates for HMG-CoA reductase inhibitors can be prepared safely and easily from these compounds.
摘要翻译：由以下一般结构式（1）表示的化合物及其制备方法：R1表示苄氧羰基，R2表示低级烷基，R3表示氢原子或保护基，M1和M2各自表示金属原子，n表示M1的原子价。 HMG-CoA还原酶抑制剂的中间体可以从这些化合物中安全和容易地制备。

2. 发明授权

US5581007A Process for preparing optically active allophenylnorstatin derivatives 失效
标题翻译：制备光学活性异恶唑诺他抑素衍生物的方法
公开(公告)号：US5581007A
公开(公告)日：1996-12-03
申请号：US609619
申请日：1996-03-01
申请人： Noboru Sayo , Tetsuro Yamasaki , Hidenori Kumobayashi , Yoshifumi Yuasa , Tsukasa Sotoguchi
发明人： Noboru Sayo , Tetsuro Yamasaki , Hidenori Kumobayashi , Yoshifumi Yuasa , Tsukasa Sotoguchi
IPC分类号： C07D417/12 , B01J31/24 , C07B53/00 , C07B61/00 , C07C69/732 , C07C227/04 , C07C227/18 , C07C227/32 , C07C229/34 , C07C247/12 , C07C271/22 , C07F7/08 , C07F7/10
CPC分类号： C07C271/22 , C07C227/04 , C07C227/18 , C07C227/32 , C07C247/12 , C07C69/732 , Y02P20/55
摘要： A process for preparing an optically active (2S,3S)-allophenylnorstatin derivative (I) is disclosed, comprising asymmetrically hydrogenating a 4-phenyl-2-halogeno-3-oxobutyric ester (III) in the presence of a ruthenium-phosphine complex to obtain a 4-phenyl-(2S)-halogeno-(3R)-hydroxybutyric ester (IV), epoxidizing the ester (IV) in the presence of a base to obtain a 4-phenyl-(2S,3R)-epoxybutyric ester (V), reacting the ester (V) with a tri(lower alkyl)silylazide or a (lower alkyl)diarylsilylazide in the presence of a Lewis to obtain a (3S)-azido-4-phenyl-(2S)-trisubstituted silyloxybutyric ester (VI), hydrogenolyzing the ester (VI) into a (2S,3S)-allophenylnorstatin derivative (VII), protecting the amino group of the compound (VII), and, if desired, hydrolyzing the compound before or after the amino group protection. Compounds (I) can be obtained at high optical purity safely and in good yield.
摘要翻译：公开了一种制备光学活性（2S，3S） - 萘基异步抑制素衍生物（I）的方法，包括在钌膦络合物存在下不对称氢化4-苯基-2-卤代-3-氧代丁酸酯（III）得到4-苯基 - （2S） - 卤素 - （3R） - 羟基丁酸酯（IV），在碱的存在下使酯（Ⅳ）环氧化，得到4-苯基 - （2S，3R） - 环氧丁酸酯 V），在路易斯存在下使酯（V）与三（低级烷基）甲硅烷基叠氮化物或（低级烷基）二芳基甲硅烷基叠氮化物反应，得到（3S） - 叠氮基-4-苯基 - （2S） - 三取代的甲硅烷氧基丁酸酯（Ⅵ），将酯（Ⅵ）氢解成（2S，3S） - 萘基异步抑制素衍生物（Ⅶ），保护化合物（Ⅶ）的氨基，如果需要，在氨基保护之前或之后水解化合物。化合物（I）可以安全且高收率地获得高光学纯度。

3. 发明授权

US5859249A 2-phenyl-2-(2'-piperidinylidene)acetate derivative, process for manufacturing the same, and process for manufacturing optically active 2-phenyl-2-(2'-piperidinyl)acetate derivative by asymmetrically hydrogenating the same 失效
标题翻译： 2-苯基-2-（2'-亚哌啶基）乙酸酯衍生物，其制备方法，以及通过不对称氢化其制备光学活性2-苯基-2-（2'-哌啶基）乙酸酯衍生物的方法
公开(公告)号：US5859249A
公开(公告)日：1999-01-12
申请号：US895428
申请日：1997-07-16
申请人： Nobuo Seido , Takenobu Nishikawa , Tsukasa Sotoguchi , Yoshifumi Yuasa , Takashi Miura , Hidenori Kumobayashi
发明人： Nobuo Seido , Takenobu Nishikawa , Tsukasa Sotoguchi , Yoshifumi Yuasa , Takashi Miura , Hidenori Kumobayashi
IPC分类号： C07C229/34 , C07C271/22 , C07D211/70 , C07D211/02 , C07D211/32
CPC分类号： C07C229/34 , C07C271/22 , C07D211/70
摘要： Disclosed is a 2-phenyl-2-(2'-piperidinylidene)acetate derivative suitably used for a raw material of a 2-phenyl-2-(2'-piperidinyl)acetate derivative and a process for manufacturing the same. Also disclosed is a process for manufacturing an optically active 2-phenyl-2-(2'-piperidinyl)acetate derivative which is a major intermediate for an antidepressant. The 2-phenyl-2-(2'-piperidinylidene)acetate derivative is manufactured by cyclizing a 7-(N-substituted amino)-3-oxo-2-heptanoate derivative. The optically active 2-phenyl-2-(2'-piperidinyl)acetate derivative is manufactured by asymmetrically hydrogenating the 2-phenyl-2-(2'-piperidinylidene)acetate derivative in the presence of a complex of a Group VIII transition metal or an acid.
摘要翻译：公开了适用于2-苯基-2-（2'-哌啶基）乙酸酯衍生物的原料的2-苯基-2-（2'-亚哌啶基）乙酸酯衍生物及其制造方法。还公开了作为抗抑郁药的主要中间体的光学活性2-苯基-2-（2'-哌啶基）乙酸酯衍生物的制造方法。通过使7-（N-取代的氨基）-3-氧代-2-庚酸酯衍生物环化制备2-苯基-2-（2'-亚哌啶基）乙酸酯衍生物。光学活性的2-苯基-2-（2'-哌啶基）乙酸酯衍生物是通过在第VIII族过渡金属络合物存在下不对称氢化2-苯基-2-（2'-亚哌啶基）乙酸酯衍生物制备的，酸。

4. 发明授权

US5801271A 7-(n-substituted amino)-2-phenylheptanoic acid derivative and process for manufacturing the same 失效
标题翻译： 7-（正取代氨基）-2-苯基庚酸衍生物及其制造方法
公开(公告)号：US5801271A
公开(公告)日：1998-09-01
申请号：US895429
申请日：1997-07-16
申请人： Nobuo Seido , Takenobu Nishikawa , Tsukasa Sotoguchi , Yoshifumi Yuasa , Takashi Miura , Hidenori Kumobayashi
发明人： Nobuo Seido , Takenobu Nishikawa , Tsukasa Sotoguchi , Yoshifumi Yuasa , Takashi Miura , Hidenori Kumobayashi
IPC分类号： B01J31/02 , B01J31/22 , C07B61/00 , C07C229/34 , C07C269/06 , C07C271/18 , C07C271/22 , C07C303/28 , C07C309/73 , C07C271/06
CPC分类号： C07C271/22 , C07C229/34 , Y02P20/55
摘要： Disclosed is a 7-(N-substituted amino)-3-oxo-2-phenylheptanoate derivative, 7-(N-substituted amino)-3-hydroxy-2-phenylheptanoate derivative, and 7-(N-substituted amino)-3-benzenesulfonyloxy-2-phenylheptanoate derivative, which are quite important major intermediates for an antidepressant. The 7-(N-substituted amino)-3-oxo-2-phenylheptanoate derivative can be manufactured by condensing an enolate of phenylacetates with a 5-(N-substituted amino) pentanoate derivative.
摘要翻译：公开了7-（N-取代氨基）-3-氧代-2-苯基庚酸酯衍生物，7-（N-取代氨基）-3-羟基-2-苯基庚酸酯衍生物和7-（N-取代氨基）-3 - 苯磺酰氧基-2-苯基庚酸酯衍生物，它们是抗抑郁药的重要主要中间体。 7-（N-取代氨基）-3-氧代-2-苯基庚酸酯衍生物可以通过将苯乙酸酯的烯醇化物与5-（N-取代的氨基）戊酸酯衍生物缩合来制备。

5. 发明授权

US5942629A Process for producing optically active pyrrolidine derivatives 失效
标题翻译：光学活性吡咯烷衍生物的制备方法
公开(公告)号：US5942629A
公开(公告)日：1999-08-24
申请号：US976491
申请日：1997-11-24
申请人： Yoshifumi Yuasa , Tsukasa Sotoguchi , Nobuo Seido
发明人： Yoshifumi Yuasa , Tsukasa Sotoguchi , Nobuo Seido
IPC分类号： B01J31/24 , C07B61/00 , C07D207/08 , C07D207/09 , C07D207/26
CPC分类号： C07D207/08 , C07D207/09 , C07D207/26
摘要： A production process for obtaining optically active (3R,1'S)-1-benzyl-3-�(1'-N-methylamino)ethyl!pyrrolidine or (3R,1'S)-3-�(1'-N-methylamino)ethyl!pyrrolidine used as an intermediate for the synthesis of pharmaceutical preparations such as anti-fungal agents in high purity and in high yield using a reduced number of processing steps. The process comprises asymmetrically hydrogenating 3-acetyl-1-benzyl-2-pyrrolidinone in the presence of a complex formed from bidentate phosphine and ruthenium as a catalyst to provide (3S,1'R)-1-benzyl-3-�(1'-hydroxy)ethyl!-2-pyrrolidinone, then reducing with a hydride to provide (3R,1'R)-1-benzyl-3-�(1'-hydroxy)ethyl!pyrrolidine, mesylating or tosylating to provide (3R,1'R)-1-benzyl-3-�(1'-methanesulfonyloxy)ethyl!pyrrolidine or (3R,1'R)-1-benzyl-3-�(1'-p-toluenesulfonyloxy)ethyl!pyrrolidine, and reacting with methylamine to obtain (3R,1'S)-1-benzyl-3-�(1'-N-methylamino)ethyl!pyrrolidine. The prcess may further comprise de-benzylating (3R,1'S)-1-benzyl-3-�(1'-N-methylamino)ethyl!pyrrolidine to obtain (3R,1'S)-3-�(1'-N-methylamino)ethyl!pyrrolidine.
摘要翻译：制备光学活性（3R，1'S）-1-苄基-3 - [（1'-N-甲基氨基）乙基]吡咯烷或（3R，1'S）-3 - [（1'-N-甲基氨基）乙基 ]吡咯烷，其用作用于合成药物制剂例如抗真菌剂的中间体，其使用减少数量的加工步骤以高纯度和高产率。该方法包括在二齿膦和钌作为催化剂形成的络合物存在下不对称氢化3-乙酰基-1-苄基-2-吡咯烷酮，得到（3S，1'R）-1-苄基-3 - [（1 然后用氢化物还原得到（3R，1'R）-1-苄基-3 - [（1'-羟基）乙基]吡咯烷，甲磺酰化或甲苯磺酸化，得到（3R ，1'R）-1-苄基-3 - [（1'-甲磺酰氧基）乙基]吡咯烷或（3R，1'R）-1-苄基-3 - [（1'-对甲苯磺酰氧基）乙基] 并与甲胺反应，得到（3R，1'S）-1-苄基-3 - [（1'-N-甲基氨基）乙基]吡咯烷。进一步包括脱苄基化（3R，1'S）-1-苄基-3 - [（1'-N-甲基氨基）乙基]吡咯烷，得到（3R，1'S）-3 - [（1'-N-甲基氨基）乙基]吡咯烷。

6. 发明授权

US5945559A Process for producing 3-oxocarboxylic acid esters 失效
标题翻译： 3-氧代羧酸酯的制备方法
公开(公告)号：US5945559A
公开(公告)日：1999-08-31
申请号：US862263
申请日：1997-05-23
申请人： Tsukasa Sotoguchi , Yoshifumi Yuasa , Akio Tachikawa , Shunichi Harada
发明人： Tsukasa Sotoguchi , Yoshifumi Yuasa , Akio Tachikawa , Shunichi Harada
IPC分类号： B01J23/02 , C07B61/00 , C07C67/343 , C07C69/716 , C07C69/738 , C07C69/66 , C07C69/76
CPC分类号： C07C67/343
摘要： A novel process for producing 3-oxocarboxylic acid esters, which are useful as intermediates in the synthesis of ceramides to be used as a humectant, biodegradable polymers, drugs, etc., at a high purity and a high yield without requiring any troublesome procedure, is disclosed. The process comprises reacting an acetoacetic ester with a calcium compound, a barium compound or a strontium compound in the presence of an organic solvent at a temperature of 10 to 120.degree. C., further reacting the obtained product with a carboxylic acid chloride to thereby acylate it, and then adding thereto an alcohol in an amount 1 to 5 times by mol as much as the calcium compound, barium compound or strontium compound to thereby deacetylate the same.
摘要翻译：一种生产3-氧代羧酸酯的新方法，其可用作合成用作保湿剂的神经酰胺的中间体，可生物降解的聚合物，药物等以高纯度和高产率而不需要任何麻烦的方法，被披露。该方法包括在有机溶剂存在下，在10〜120℃的温度下使乙酰乙酸酯与钙化合物，钡化合物或锶化合物反应，进一步使得到的产物与羧酰氯反应，从而酰化然后向其中加入与钙化合物，钡化合物或锶化合物一样多的1至5倍摩尔量的醇，从而使其脱乙酰化。

7. 发明申请

US20100036149A1 METHOD FOR PRODUCING AN OPTICALLY ACTIVE TETRAHYDROQUINOLINE 有权
标题翻译：生产光学活性四氢喹啉的方法
公开(公告)号：US20100036149A1
公开(公告)日：2010-02-11
申请号：US12550948
申请日：2009-08-31
申请人： Takashi Moroi , Tsukasa Sotoguchi , Kazuhiko Matsumura , Motonobu Takenaka , Wataru Kuriyama , Toshiyuki Murayama , Hideki Nara , Tohru Yokozawa , Kenji Yagi
发明人： Takashi Moroi , Tsukasa Sotoguchi , Kazuhiko Matsumura , Motonobu Takenaka , Wataru Kuriyama , Toshiyuki Murayama , Hideki Nara , Tohru Yokozawa , Kenji Yagi
IPC分类号： C07C227/16
CPC分类号： C07C229/18 , C07C211/49 , C07C229/30 , C07D215/42
摘要： The present invention provides an industrially advantageous production method of optically active tetrahydroquinolines of formula (1), which comprises: 1) a step of reacting a β-ketoester of formula (2) with an amine of formula (3) to produce an enaminoester of formula (4); 2) a step of subjecting the enaminoester of formula (4) above obtained in 1) to asymmetric hydrogenation to produce an optically active β-amino acid derivative of formula (5); 3) a step of amidating the optically active β-amino acid derivative (5) above obtained in 2) to produce an amide of formula (6); 4) a step of alkoxycarbonylating the amide of formula (6) above obtained in 3) to produce a compound of formula (7); and 5) a step of subjecting the compound of formula (7) above to cyclization to produce the optically active tetrahydroquinoline of formula (1).
摘要翻译：本发明提供了一种工业上有利的式（1）的光学活性四氢喹啉的制备方法，其包括：1）使式（2）的β-酮酯与式（3）的胺反应以产生一种公式（4）; 2）使在1）中获得的上述式（4）的烯氨基酯进行不对称氢化以产生式（5）的光学活性β-氨基酸衍生物的步骤; 3）将2）中得到的光学活性β-氨基酸衍生物（5）酰胺化以制备式（6）的酰胺的步骤; 4）在3）中得到的上述式（6）的酰胺进行烷氧基羰基化以制备式（7）化合物的步骤; 和5）使上述式（7）化合物环化以制备式（1）的光学活性四氢喹啉的步骤。

8. 发明授权

US07038087B2 Process for the production of optically active amino alcohols 失效
标题翻译：用于制备光学活性氨基醇的方法
公开(公告)号：US07038087B2
公开(公告)日：2006-05-02
申请号：US10656617
申请日：2003-09-04
申请人： Takahiro Fujiwara , Hideki Nara , Tsukasa Sotoguchi
发明人： Takahiro Fujiwara , Hideki Nara , Tsukasa Sotoguchi
IPC分类号： C07C209/16 , C07C209/46 , C07C209/56
CPC分类号： C07C269/00 , C07B2200/07 , C07C213/02 , C07C2601/08 , C07C2601/14 , Y02P20/55 , C07C215/44 , C07C271/24
摘要： An object of the present invention is to provide a process for the production of an optically active amino alcohol, particularly an optically active amino alcohol of a trans-form, being excellent in economy and efficiency, and suitable for industry using easily available and less expensive materials.The present invention relates to a process for the production of an optically active amino alcohol comprising the steps that an optically active hydroxy ester in a trans-form obtained by an asymmetric hydrogenation of an easily available β-keto ester is reacted with hydrazine, the resulting optically active hydrazinocarbonyl alcohol is subjected to a Curtius rearrangement in the presence of alcohol and protective group of amino group of the resulting optically active alkoxycarbonylamino alcohol is deprotected. As a result of the process for the production in accordance with the present invention, the objected substance is able to be prepared in a high optical purity and in a high yield.
摘要翻译：本发明的目的是提供一种制备光学活性氨基醇，特别是反式形式的光学活性氨基醇的方法，其经济性和效率优异，并且适用于易于获得和较便宜的工业应用材料本发明涉及一种制备光学活性氨基醇的方法，该方法包括以下步骤：通过易于获得的β-酮酯的不对称氢化获得的反式的光学活性羟基酯与肼反应，得到光学活性肼基羰基醇在醇的存在下进行Curtius重排，并将得到的光学活性烷氧基羰基氨基醇的保护基的氨基脱保护。作为根据本发明的生产方法的结果，可以以高光学纯度和高产率制备被
反应物质。

9. 发明授权

US08188307B2 Method for producing an optically active tetrahydroquinoline 有权
标题翻译：光学活性四氢喹啉的制造方法
公开(公告)号：US08188307B2
公开(公告)日：2012-05-29
申请号：US12550948
申请日：2009-08-31
申请人： Takashi Moroi , Tsukasa Sotoguchi , Kazuhiko Matsumura , Motonobu Takenaka , Wataru Kuriyama , Toshiyuki Murayama , Hideki Nara , Tohru Yokozawa , Kenji Yagi
发明人： Takashi Moroi , Tsukasa Sotoguchi , Kazuhiko Matsumura , Motonobu Takenaka , Wataru Kuriyama , Toshiyuki Murayama , Hideki Nara , Tohru Yokozawa , Kenji Yagi
IPC分类号： C07C227/16
CPC分类号： C07C229/18 , C07C211/49 , C07C229/30 , C07D215/42
摘要： Disclosed is an industrially advantageous production method of optically active β-amino acid of formula (5a), which includes subjecting an enaminoester of formula (4a) to an asymmetric hydrogenation: wherein * shows an asymmetric carbon atom.
摘要翻译：公开了一种工业上有利的式（5a）的光学活性的（b） - 氨基酸的制备方法，其包括使式（4a）的烯氨基酯进行不对称氢化反应：其中*表示不对称碳原子。

10. 发明授权

US06608214B2 Process for producing optically active &ggr;-butyrolactone 失效
标题翻译：光学活性γ-丁内酯的制备方法
公开(公告)号：US06608214B2
公开(公告)日：2003-08-19
申请号：US10199136
申请日：2002-07-19
申请人： Tsukasa Sotoguchi , Takaji Matsumoto , Motonobu Takenaka , Takashi Miura
发明人： Tsukasa Sotoguchi , Takaji Matsumoto , Motonobu Takenaka , Takashi Miura
IPC分类号： C07D30733
CPC分类号： C07D307/33 , C07B2200/07 , C07C67/31 , Y02P20/55 , C07C69/734
摘要： This invention provides a novel process for producing optically active 3-hydroxy-&ggr;-butyrolactone in a short step, which is superior economically and in efficiency and industrially suitable by using a starting material which is inexpensive and easily available and reagents easy to handle. This invention relates to a process for producing optically active 3-hydroxy-&ggr;-butyrolactone represented by formula I: wherein the symbol * means an asymmetric carbon atom, which comprises hydrogenating an optically active 4-substituted oxy-3-hydroxybutyrate represented by formula II: wherein R1 represents a C1-4 lower alkyl group, R2 represents a protective group for a hydroxyl group deprotected by hydrogenation with a heterogeneous hydrogenation catalyst, and the symbol * has the same meaning as defined above, in the presence of a heterogeneous hydrogenation catalyst and an acidic substance followed by deprotection and simultaneous ring closure thereof.
摘要翻译：本发明提供了一种在短时间内制备光学活性3-羟基-γ-丁内酯的新方法，其经济性和效率都优异，在工业上适用于便宜且易于获得的试剂和易于处理的试剂。本发明涉及一种由式I表示的光学活性3-羟基-γ-丁内酯的制备方法：其中符号*表示不对称碳原子，其包括将由式II表示的光学活性的4-取代的氧基-3-羟基丁酸：其中R1表示C1-4低级烷基，R2表示通过异相氢化催化剂氢化脱保护的羟基的保护基，符号*具有与上述相同的含义，在非均相加氢催化剂存在下和酸性物质，然后脱保护并同时闭环。

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