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1. 发明授权

US08067640B2 Method for the separation of intermediates which may be used for the preparation of escitalopram 失效
标题翻译：用于分离可用于制备依他普仑的中间体的方法
公开(公告)号：US08067640B2
公开(公告)日：2011-11-29
申请号：US12781026
申请日：2010-05-17
申请人： Naoki Taoka , Takahisa Kato , Shogo Yamamoto , Takashi Yoshida , Toshihiro Takeda , Yasuyoshi Ueda , Hans Petersen , Robert Dancer , Haleh Ahmadian , Lars O. Lyngso
发明人： Naoki Taoka , Takahisa Kato , Shogo Yamamoto , Takashi Yoshida , Toshihiro Takeda , Yasuyoshi Ueda , Hans Petersen , Robert Dancer , Haleh Ahmadian , Lars O. Lyngso
IPC分类号： C07C57/00
CPC分类号： C07B57/00 , C07B2200/07 , C07C253/30 , C07C253/34 , C07C255/34 , C07C255/59 , C07D307/87 , C12P7/22 , C12P13/001 , C12P13/002 , C12P13/008 , C12P13/02 , C12P41/007
摘要： The present invention relates to a novel method for the preparation of diol intermediates having the formula (II) and/or the opposite enantiomer of an acylated diol having the formula (IV) useful for the preparation of escitalopram involving selective enzymatic acylation or deacylation.
摘要翻译：本发明涉及一种制备具有式（II）的二醇中间体和/或具有式（Ⅳ）的酰化二醇的相反对映异构体的新方法，其可用于制备涉及选择性酶酰化或脱酰基化的依他普仑。

2. 发明申请

US20110065937A1 METHOD FOR THE SEPARATION OF INTERMEDIATES WHICH MAY BE USED FOR THE PREPARATION OF ESCITALOPRAM 失效
标题翻译：用于分离可用于制备ESCITALOPRAM的中间体的方法
公开(公告)号：US20110065937A1
公开(公告)日：2011-03-17
申请号：US12781026
申请日：2010-05-17
申请人： Naoki Taoka , Takahisa Kato , Shogo Yamamoto , Takashi Yoshida , Toshihiro Takeda , Yasuyoshi Ueda , Hans Petersen , Robert Dancer , Haleh Ahmadian , Lars O. Lyngso
发明人： Naoki Taoka , Takahisa Kato , Shogo Yamamoto , Takashi Yoshida , Toshihiro Takeda , Yasuyoshi Ueda , Hans Petersen , Robert Dancer , Haleh Ahmadian , Lars O. Lyngso
IPC分类号： C07D307/87
CPC分类号： C07B57/00 , C07B2200/07 , C07C253/30 , C07C253/34 , C07C255/34 , C07C255/59 , C07D307/87 , C12P7/22 , C12P13/001 , C12P13/002 , C12P13/008 , C12P13/02 , C12P41/007
摘要： The present invention relates to a novel method for the preparation of diol intermediates having the formula (II) and/or the opposite enantiomer of an acylated diol having the formula (IV) useful for the preparation of escitalopram involving selective enzymatic acylation or deacylation.
摘要翻译：本发明涉及一种制备具有式（II）的二醇中间体和/或具有式（Ⅳ）的酰化二醇的相反对映异构体的新方法，其可用于制备涉及选择性酶酰化或脱酰基化的依他普仑。

3. 发明申请

US20070129561A1 Method for the separation of intermediates which may be used for the preparation of escitalopram 审中-公开
标题翻译：用于分离可用于制备依他普仑的中间体的方法
公开(公告)号：US20070129561A1
公开(公告)日：2007-06-07
申请号：US10524937
申请日：2003-08-12
申请人： Naoki Taoka , Takahisa Kato , Shogo Yamamoto , Takashi Yoshida , Toshihiro Takeda , Yasuyoshi Ueda , Hans Petersen , Robert Dancer , Haleh Ahmadian , Lars Lyngso
发明人： Naoki Taoka , Takahisa Kato , Shogo Yamamoto , Takashi Yoshida , Toshihiro Takeda , Yasuyoshi Ueda , Hans Petersen , Robert Dancer , Haleh Ahmadian , Lars Lyngso
IPC分类号： C07C323/20 , C07C271/40 , C12P13/00 , C12P7/22
CPC分类号： C07B57/00 , C07B2200/07 , C07C253/30 , C07C253/34 , C07C255/34 , C07C255/59 , C07D307/87 , C12P7/22 , C12P13/001 , C12P13/002 , C12P13/008 , C12P13/02 , C12P41/007
摘要： The present invention relates to a novel method for the preparation of diol intermediates having the formula (II) and/or the opposite enantiomer of an acylated diol having the formula (IV) useful for the preparation of escitalopram involving selective enzymatic acylation or deacylation.
摘要翻译：本发明涉及一种制备具有式（II）的二醇中间体和/或具有式（Ⅳ）的酰化二醇的相反对映异构体的新方法，其可用于制备涉及选择性酶酰化或脱酰基化的依他普仑。

4. 发明申请

US20060247458A1 Process for the production of optically active compounds having substituents at the 2-position 审中-公开
标题翻译：用于制备在2-位具有取代基的光学活性化合物的方法
公开(公告)号：US20060247458A1
公开(公告)日：2006-11-02
申请号：US10546823
申请日：2004-02-25
申请人： Shogo Yamamoto , Toshihiro Takeda , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Shogo Yamamoto , Toshihiro Takeda , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07C319/02
CPC分类号： C07B53/00 , C07B2200/07 , C07C51/363 , C07C319/14 , C07C57/58 , C07C323/56
摘要： The present invention provides a process for producing an optically active compound having a thio group at the 2-position important for manufacturing medicines. An optically active compound having a hydroxyl group at the 2-position is chlorinated with inversion of the configuration at the 2-position, and the resultant optically active compound having a chlorine atom at the 2-position is reacted with a metal thiolate to introduce a thio group with inversion of the configuration at the 2-position. This process is capable of minimizing racemization and producing an optically active compound having a thio group at the 2-position at low cost in high yield. When the optically active compound having a chlorine atom at the 2-position is reacted with the metal thiolate in coexistence with water in the reaction system, the optically active compound having a thio group at the 2-position with higher optical purity can be produced in higher yield. An optically active carboxylic acid having a thio group at the 2-position is crystallized in the presence of an aliphatic hydrocarbon solvent and/or a sulfur-containing solvent to effectively remove coexistent impurities such as an optical isomer and the like, thereby producing crystals of an optically active carboxylic acid having a thio group at the 2-position with higher purity.
摘要翻译：本发明提供了制造药物重要的2位具有硫基的光学活性化合物的方法。在2-位上具有羟基的光学活性化合物用2-位反转形式进行氯化，所得2-位上具有氯原子的光学活性化合物与金属硫醇盐反应，引入硫基与2-位配位反转。该方法能够使外消旋化最小化，并以高产率以低成本制备在2-位具有硫基的光学活性化合物。当反应体系中2-位上具有氯原子的光学活性化合物与金属硫醇盐在水中共存时，具有较高光学纯度的2位具有硫基的光学活性化合物可以在更高的产量。在脂肪族烃溶剂和/或含硫溶剂的存在下，在2-位具有硫基的光学活性羧酸结晶化，以有效除去共同的杂质如旋光异构体等，从而产生在2-位具有较高纯度的具有硫基的光学活性羧酸。

5. 发明授权

US07057066B2 Process for producing 3-amino-2-hydroxypropionic acid derivatives 失效
标题翻译： 3-氨基-2-羟基丙酸衍生物的制备方法
公开(公告)号：US07057066B2
公开(公告)日：2006-06-06
申请号：US10312208
申请日：2001-06-26
申请人： Hiroshi Murao , Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
发明人： Hiroshi Murao , Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
IPC分类号： C07C229/06 , C07C229/34
CPC分类号： C07D263/20 , C07C227/20 , C07C227/32 , C07C227/42 , Y02P20/55 , C07C229/22 , C07C229/34
摘要： The present invention provides a process for preparing 3-amino-2-hydroxypropionic acid derivatives (1) which does not use dangerous reagents, is economically advantageous, and is suitable for an industrial production, which process comprises: treating N-protected-3-amino-2-hydroxypropionic acid derivatives (2) having a steric configuration at 2-position carbon reverse to that of derivatives (1) with a leaving group-introducing agent to convert into N-protected-3-aminopropionic acid derivatives (3), then treating the derivatives with a basic substance to convert into substituted-3-amino-2-hydroxypropionic acid derivatives (4) having an inverted steric configuration at 2-position carbon, and then converting the derivatives into 3-amino-2-hydroxypropionic acid derivatives (1).
摘要翻译：本发明提供了一种制备不使用危险试剂的3-氨基-2-羟基丙酸衍生物（1）的方法，在经济上是有利的，适用于工业生产，该方法包括：将N-保护的3- 具有与衍生物（1）相反的2-位碳位置的氨基-2-羟基丙酸衍生物（2）与离去基团引入剂转化为N-保护的3-氨基丙酸衍生物（3），然后用碱性物质处理衍生物，将其转化成在2-位碳上具有反向立体构型的取代-3-氨基-2-羟基丙酸衍生物（4），然后将其转化为3-氨基-2-羟基丙酸衍生物（1）。

6. 发明申请

US20050153408A1 Process for preparation of 2-aminotetralin derivatives and intermediates thereof 审中-公开
标题翻译： 2-氨基四氢化萘衍生物的制备方法及其中间体
公开(公告)号：US20050153408A1
公开(公告)日：2005-07-14
申请号：US10496639
申请日：2002-11-28
申请人： Tatsuya Honda , Akio Fujii , Kenji Inoue , Yoshihiko Yasohara , Yoshifumi Itagaki , Katsuji Maehara , Toshihiro Takeda , Yasuyoshi Ueda
发明人： Tatsuya Honda , Akio Fujii , Kenji Inoue , Yoshihiko Yasohara , Yoshifumi Itagaki , Katsuji Maehara , Toshihiro Takeda , Yasuyoshi Ueda
IPC分类号： C07C213/02 , C07C217/74 , C07C303/28 , C07C309/66 , C07C309/73 , C12P7/42 , C12P7/62
CPC分类号： C12P7/42 , C07B2200/07 , C07C213/02 , C07C303/28 , C07C309/66 , C07C309/73 , C07C217/74
摘要： The present invention is to efficiently and simply prepare an optically active 7-substituted-2-aminotetralin with industrial advantage. In the process, a 7-substituted-2-tetralone or its bisulfite adduct is reduced with a microorganism to an optically active 7-substituted-2-tetralol. Then, a sulfonyl group is introduced to the hydroxy group to form an optically active 7-substituted-2-sulfonyloxytetralin. Then, with inversion of the configuration, a nitrogen substituent is introduced using a nitrogen nucleophile to form an optically active 2,7-substituted tetralin. Furthermore, if necessary, the nitrogen substituent is converted into a non-substituted amino group. Thus, an optically active 7-substituted-2-aminotetralin or its salt is prepared.
摘要翻译：本发明是有效且简单地制备具有工业优势的光学活性7-取代-2-氨基四氢萘酚。在此过程中，7-取代-2-四氢萘酮或其亚硫酸氢盐加合物与微生物一起还原成光学活性的7-取代-2-四氢萘酚。然后，将磺酰基引入羟基以形成光学活性的7-取代-2-磺酰氧基四氢萘酮。然后，通过配置的倒置，使用氮亲核试剂引入氮取代基以形成光学活性的2,7-取代的四氢化萘。此外，如果需要，氮取代基转化为未取代的氨基。因此，制备光学活性的7-取代-2-氨基四氢萘或其盐。

7. 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。

8. 发明授权

US07307184B2 Processes for preparing oxazolidinone derivatives of β-hydroxyethlamine compounds and for preparing β-hydroxyethlamine compounds 失效
标题翻译：制备β-羟基三甲基胺化合物的恶唑烷酮衍生物和制备β-羟基三甲基胺化合物的方法
公开(公告)号：US07307184B2
公开(公告)日：2007-12-11
申请号：US10478439
申请日：2002-05-23
申请人： Hiroshi Murao , Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
发明人： Hiroshi Murao , Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
IPC分类号： C07C269/00 , C07C269/06
CPC分类号： C07D263/24 , C07D263/22
摘要： The present invention provides a process of starting from N-alkoxycarbonyl-ethylamine compounds having a leaving group at the β-position to prepare oxazolidinone derivatives of β-hydroxyethylamine compounds having an inverted steric configuration at the β-position carbon, which comprises introducing a step of treating in contact with water with heating under acidic to neutral conditions into the process. Also, the present invention provides a process of starting from N-alkoxycarbonyl-ethylamine compounds having a leaving group at the β-position to prepare β-hydroxyethylamine compounds having an inverted steric configuration at the β-position carbon, which comprises subjecting the oxazolidinone derivatives prepared as described above to a step of treating in contact with water under basic conditions.
摘要翻译：本发明提供了从在β-位上具有离去基团的N-烷氧基羰基 - 乙胺化合物开始以制备β-位羟基化合物的恶唑烷酮衍生物的方法，所述β-羟乙基胺化合物在β-位置碳具有反向立体构型，其包括引入步骤在酸性到中性条件下加热处理与水接触。此外，本发明提供了从在β-位上具有离去基团的N-烷氧基羰基 - 乙胺化合物开始以制备在β-位置碳具有反向立体构型的β-羟乙基胺化合物的方法，该方法包括使恶唑烷酮衍生物如上所述制备成在碱性条件下与水接触的步骤。

9. 发明申请

US20060135784A1 PROCESS FOR PRODUCING 3-AMINO-2-HYDROXYPROPIONIC ACID DERIVATIVES 审中-公开
标题翻译：生产3-氨基-2-羟基丙酸衍生物的方法
公开(公告)号：US20060135784A1
公开(公告)日：2006-06-22
申请号：US11276222
申请日：2006-02-17
申请人： Hiroshi MURAO , Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
发明人： Hiroshi MURAO , Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
IPC分类号： C07D263/38 , C07D263/04
CPC分类号： C07D263/20 , C07C227/20 , C07C227/32 , C07C227/42 , Y02P20/55 , C07C229/22 , C07C229/34
摘要： The present invention provides a process for preparing 3-amino-2-hydroxypropionic acid derivatives (1) which does not use dangerous reagents, is economically advantageous, and is suitable for an industrial production, which process comprises: treating N-protected-3-amino-2-hydroxypropionic acid derivatives (2) having a steric configuration at 2-position carbon reverse to that of derivatives (1) with a leaving group-introducing agent to convert into N-protected-3-aminopropionic acid derivatives (3), then treating the derivatives with a basic substance to convert into substituted-3-amino-2-hydroxypropionic acid derivatives (4) having an inverted steric configuration at 2-position carbon, and then converting the derivatives into 3-amino-2-hydroxypropionic acid derivatives (1).
摘要翻译：本发明提供了一种制备不使用危险试剂的3-氨基-2-羟基丙酸衍生物（1）的方法，在经济上是有利的，适用于工业生产，该方法包括：将N-保护的3- 具有与衍生物（1）相反的2-位碳位置的氨基-2-羟基丙酸衍生物（2）与离去基团引入剂转化为N-保护的3-氨基丙酸衍生物（3），然后用碱性物质处理衍生物，将其转化成在2-位碳上具有反向立体构型的取代-3-氨基-2-羟基丙酸衍生物（4），然后将其转化为3-氨基-2-羟基丙酸衍生物（1）。

10. 发明申请

US20050176999A1 Process for production of optically active 2-halogeno-carboxylic acids 失效
标题翻译：光学活性2-卤代羧酸的制备方法
公开(公告)号：US20050176999A1
公开(公告)日：2005-08-11
申请号：US10503264
申请日：2003-02-04
申请人： Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
发明人： Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
IPC分类号： C07C51/363 , C07C51/41 , C07C51/43 , C07C53/15 , C07C53/16
CPC分类号： C07C51/412 , C07C51/363 , C07C51/43 , C07C53/19
摘要： The invention provides processes for producing efficiently optically active 2-halogenocarboxylic acids useful in the preparation of drugs or the like and salts thereof with amines. Specifically an optically active 2-halogenocarboxylic acid is produced by halogenating an optically active amino acid in water in the presence of a hydrophobic organic solvent and nitrous acid with the configuration retained and with the racemization inhibited through the removal of 2-hydroxy-bromocarboxylic acid formed as a by-product; the obtained optically active 2-halogenocarboxylic acid is transferred to an aqueous phase by converting it into a salt thereof with a base, followed by the removal of the organic phase; and the optically active 2-halogenocarboxylic acid is transferred again to an organic solvent phase, followed by the removal of the aqueous phase, whereby an optically active 2-halogenocarboxylic acid is obtained through the removal of a halogen component. Further, a high-quality salt of an optically active 2-halogenocarboxylic acid with an amine can be obtained by a crystallization method wherein the amine is added over the period of ½ hour or longer either continuously or in portions and/or wherein the crystallization solvent consists of a hydrophobic organic solvent and a hydrophilic organic solvent.
摘要翻译：本发明提供了可用于制备药物等的有效光学活性2-卤代羧酸的方法及其与胺的盐。具体地说，光学活性的2-卤代羧酸是通过在疏水性有机溶剂和亚硝酸存在下在水中卤化光学活性氨基酸而形成的，其中保留了结构，并且通过除去形成的2-羟基 - 溴代羧酸来抑制外消旋化作为副产品; 将得到的光学活性2-卤代羧酸通过将其转化为其盐与碱反应，然后除去有机相，转移到水相中。并将光学活性2-卤代羧酸再次转移到有机溶剂相中，然后除去水相，由此通过除去卤素组分获得光学活性的2-卤代羧酸。此外，光学活性2-卤代羧酸与胺的高品质盐可以通过结晶方法获得，其中胺在连续或部分加入0.5小时或更久的时间内和/或其中结晶溶剂由疏水性有机溶剂和亲水性有机溶剂构成。

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