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1. 发明公开

EP1600438A1 PROCESSES FOR THE PRODUCTION OF OPTICALLY ACTIVE COMPOUNDS HAVING SUBSTITUENTS AT THE 2-POSITION 审中-公开
标题翻译： PROCESS FOR在2-位来制备光学活性化合物的取代基
公开(公告)号：EP1600438A1
公开(公告)日：2005-11-30
申请号：EP04714501.6
申请日：2004-02-25
申请人： KANEKA CORPORATION
发明人： YAMAMOTO, Shogo , TAKEDA, Toshihiro , FUSE, Yoshihide , UEDA, Yasuyoshi
IPC分类号： C07C319/14 , C07C51/43 , C07C57/58 , C07C319/28 , C07C323/56
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：本发明提供了用于以2位用于制造药物重要具有硫基光学活性化合物的制造方法。在2-位上的羟基基团的光学活性化合物是氯化与在2-位的构型的反转，将所得具有在2-位上的氯原子的光学活性化合物与金属硫醇盐引入硫基与在2位上的构型反转。这个过程能够最小化的外消旋化，并在光学活性的化合物在生产以高收率低成本在具有2位上含有硫基的。当具有在2-位上的氯原子的光学活性化合物与金属硫醇盐在反应体系中反应。在共存水，可以在产生在具有较高光学纯度的2-位上具有一个硫基的光学活性化合物更高的产量。的诸如旋光异构体和类似物，从而产生结晶：具有在2-位上含有硫基的光学活性羧酸在脂族烃溶剂和/或溶剂来有效地去除共存的杂质的含硫的存在下结晶化的光学具有硫基活性羧酸在具有更高纯度的2-位。

2. 发明公开

EP3124470A1 METHOD FOR PRODUCING TRI-CARBOBENZOXY-ARGININE 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG VON TRI-CARBOBENZOXY-ARGININ
公开(公告)号：EP3124470A1
公开(公告)日：2017-02-01
申请号：EP15769421.7
申请日：2015-03-23
申请人： Kaneka Corporation
发明人： MACHIDA, Koji , MORI, Kohei , KISHIMOTO, Narumi , TAKEDA, Toshihiro
IPC分类号： C07C277/08 , C07C279/24
摘要： A tri-carbobenzoxy-arginine represented by the following formula (2):

is produced by carbobenzoxylating the arginine or arginine derivative (1) represented by the following formula (1), or a salt thereof:

by adding carbobenzoxy chloride and a base in a water/organic solvent bilayer system to an arginine or arginine derivative (1) represented by the formula (1), or a salt thereof.
摘要翻译：由下式（2）表示的三碳代苯甲酰氧基 - 精氨酸：通过对由下式（1）表示的精氨酸或精氨酸衍生物（1）或其盐进行苄氧羰基化生产：通过加入苄氧苯甲酰氯和碱水/有机溶剂双层体系转化为式（1）表示的精氨酸或精氨酸衍生物（1）或其盐。

3. 发明公开

EP1947083A1 PROCESS FOR PRODUCTION OF ARALKYLOXYPYRROLIDINE DERIVATIVE 有权转让
标题翻译：生产脂酰氧基吡咯烷衍生物的方法
公开(公告)号：EP1947083A1
公开(公告)日：2008-07-23
申请号：EP06796649.9
申请日：2006-08-22
申请人： Kaneka Corporation
发明人： TAKEDA, Toshihiro , OHNUKI, Masatoshi , KISHIMOTO, Narumi
IPC分类号： C07D207/12
CPC分类号： C07D207/12 , Y02P20/55
摘要： The present invention provides a process for producing a 3-aralkyloxypyrrolidine derivative which is important for production of pharmaceutical products and the like. In the present invention, a N-protected-3-hydroxypyrrolidine is converted into a N-protected-3-aralkyloxypyrrolidine by allowing an aralkyl halide to act in the presence of a base and at least one of a metal halide and a phase-transfer catalyst followed by deprotecting a N-protecting group to convert it to a 3-aralkyloxypyrrolidine derivative and subsequently treating the derivative in a solvent containing a polar solvent, thereby obtaining the 3-aralkyloxypyrrolidine derivative as a crystal. According to the present invention, a 3-aralkyloxypyrrolidine derivative of high purity can be produced conveniently and efficiently on an industrial scale.
摘要翻译：本发明提供了一种生产药用产品等重要的3-芳烷氧基吡咯烷衍生物的方法。在本发明中，通过使芳烷基卤化物在碱的存在下和至少一种金属卤化物和相转移作用下将N-保护的-3-羟基吡咯烷转化为N-保护的-3-芳烷氧基吡咯烷然后去保护N-保护基团，将其转化为3-芳烷氧基吡咯烷衍生物，随后在含有极性溶剂的溶剂中处理衍生物，由此得到3-芳烷氧基吡咯烷衍生物的晶体。根据本发明，高纯度的3-芳烷氧基吡咯烷衍生物可以在工业规模上方便和有效地生产。

4. 发明公开

EP1179530A1 PROCESSES FOR PREPARING OPTICALLY ACTIVE AMINO ACID DERIVATIVES 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG OPTISCH AKTIVERAMINOSÄUREDERIVATE
公开(公告)号：EP1179530A1
公开(公告)日：2002-02-13
申请号：EP01904517.8
申请日：2001-02-16
申请人： Kaneka Corporation
发明人： SUGAWARA, Masanobu , FUJII, Akio , OKURO, Kazumi , SAKA, Yasuhiro , NAGASHIMA, Nobuo , INOUE, Kenji , TAKEDA, Toshihiro , KINOSHITA, Koichi , MOROSHIMA, Tadashi , FUSE, Yoshihide , UEDA, Yasuyoshi
IPC分类号： C07D203/08 , C07D203/24 , C07C227/04 , C07C227/10 , C07C229/26 , C07C311/19 , C07B53/00
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。

5. 发明公开

EP3489216A1 METHOD FOR PRODUCING CHLOROFORMATE COMPOUND 有权
公开(公告)号：EP3489216A1
公开(公告)日：2019-05-29
申请号：EP17830897.9
申请日：2017-07-11
申请人： Kaneka Corporation
发明人： YASUKOUCHI, Hiroaki , FUNABASHI, Makoto , NISHIYAMA, Akira , TAKEDA, Toshihiro , MITSUDA, Masaru
IPC分类号： C07C68/02 , C07C69/96
摘要： The present invention provides a method for safely producing a large amount of chloroformate compound with high yield. The chloroformate compound can be produced by mixing and reacting a solution of triphosgene ,an amine and an alcohol compound in a flow reactor. The chloroformate compound can also be produced by mixing and reacting a solution of triphosgene with a solution comprising an amine and an alcohol compound in a flow reactor. The amine is preferably tributylamine, and preferably used in an amount of 0.8 to 3 equivalents relative to an amount of the alcohol compound.

6. 发明公开

EP1403257A1 PROCESSES FOR PRODUCING OXAZOLIDINONE DERIVATIVE OF BETA-HYDROXYETHYLAMINE COMPOUND AND FOR PRODUCING BETA-HYDROXYETHYLAMINE COMPOUND 审中-公开
标题翻译：生产β-羟基乙胺化合物的恶唑啉酮衍生物和生产β-羟基乙胺化合物的方法
公开(公告)号：EP1403257A1
公开(公告)日：2004-03-31
申请号：EP02728125.2
申请日：2002-05-23
申请人： KANEKA CORPORATION
发明人： MURAO, Hiroshi , YAMASHITA, Koki , TAKEDA, Toshihiro , UEDA, Yasuyoshi
IPC分类号： C07D263/22 , C07D263/24
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β-位具有离去基团的N-烷氧基羰基 - 乙胺化合物开始，制备在β位碳具有空间立体构型的β-羟基乙胺化合物的恶唑烷酮衍生物的方法，该方法包括将步骤在酸性至中性条件下加热处理与水接触进入该过程。另外，本发明提供了一种从在β-位具有离去基团的N-烷氧基羰基 - 乙胺化合物开始，以制备在β-位碳上具有空间立体构型的β-羟乙胺化合物的方法，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处理的步骤。

7. 发明公开

EP1300391A1 PROCESS FOR PRODUCING 3-AMINO-2-HYDROXYPROPIONIC ACID DERIVATIVES 审中-公开
标题翻译： VERFAHREN ZUR PRODUKTION VON 3-AMINO-2-HYDROXYPROPIONSÄURE-DERIVATEN
公开(公告)号：EP1300391A1
公开(公告)日：2003-04-09
申请号：EP01941242.8
申请日：2001-06-26
申请人： KANEKA CORPORATION
发明人： MURAO, Hiroshi , YAMASHITA, Koki , TAKEDA, Toshihiro , UEDA, Yasuyoshi
IPC分类号： C07C227/30 , C07C227/42 , C07C229/22 , C07D263/24 , C07B53/00
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，将其转化为在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），然后将该衍生物转化为3-氨基-2-羟基丙酸衍生物（1）。

8. 发明授权

EP3124470B1 METHOD FOR PRODUCING TRI-CARBOBENZOXY-ARGININE 有权
公开(公告)号：EP3124470B1
公开(公告)日：2020-01-08
申请号：EP15769421.7
申请日：2015-03-23
申请人： Kaneka Corporation
发明人： MACHIDA, Koji , MORI, Kohei , KISHIMOTO, Narumi , TAKEDA, Toshihiro
IPC分类号： C07C277/08 , C07C279/24

9. 发明授权

EP1947083B1 PROCESS FOR PRODUCTION OF ARALKYLOXYPYRROLIDINE DERIVATIVE 有权转让
标题翻译：生产脂酰氧基吡咯烷衍生物的方法
公开(公告)号：EP1947083B1
公开(公告)日：2010-11-10
申请号：EP06796649.9
申请日：2006-08-22
申请人： Kaneka Corporation
发明人： TAKEDA, Toshihiro , OHNUKI, Masatoshi , KISHIMOTO, Narumi
IPC分类号： C07D207/12
CPC分类号： C07D207/12 , Y02P20/55
摘要： Disclosed is a process for production of an aralkyloxypyrrolidine derivative which is important for the production of a pharmaceutical or the like. A 3-aralkyloxypyrrolidine derivative can be produced in the form of a crystal by a process comprising reacting an N-protected-3-hydroxypyrrolidine with a halogenated aralkyl in the presence of a base and a metal halide and/or a phase transfer catalyst to give an N-protected-3-aralkyloxypyrrolidine, performing the deprotection of the N-protecting group in the product to give a 3-aralkyloxypyrrolidine derivative, and treating the product in a solvent containing a polar solvent. The process can produce a highly pure 3-aralkyloxypyrrolidine derivative in a simple manner, with good efficiency, and in an industrial scale.
摘要翻译：公开了一种生产药物等重要的芳烷氧基吡咯烷衍生物的方法。 3-芳烷氧基吡咯烷衍生物可以通过包括在碱和金属卤化物和/或相转移催化剂存在下使N-保护的-3-羟基吡咯烷与卤代芳烷基反应得到晶体形式，得到 N-保护的-3-芳烷氧基吡咯烷，对产物中的N-保护基进行脱保护得到3-芳烷氧基吡咯烷衍生物，并在含有极性溶剂的溶剂中处理产物。该方法可以以简单的方式高效纯化并以工业规模生产高纯度的3-芳烷氧基吡咯烷衍生物。

10. 发明公开

EP1481960A1 PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE 2-HALOGENO- CARBOXYLIC ACIDS 审中-公开
标题翻译： VERFAHREN ZURHERSTELLUNG OPTISCH AKTIVER 2-HALOGENCARBONSÄUREN
公开(公告)号：EP1481960A1
公开(公告)日：2004-12-01
申请号：EP03737476.6
申请日：2003-02-04
申请人： KANEKA CORPORATION
发明人： YAMASHITA, Koki , TAKEDA, Toshihiro , UEDA, Yasuyoshi
IPC分类号： C07C51/363 , C07C53/19 , C07C51/48 , C07C51/487 , C07C51/43 , C07C51/41
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 1/2 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：光学活性2-卤代羧酸（II）的制备包括在疏水性有机溶剂和亚硝酸的存在下在水中卤化光学活性氨基酸（I），并且通过抑制外消旋化保留配置。式（II）的光学活性2-卤代羧酸的制备包括在疏水性有机溶剂和亚硝酸的存在下在水中卤化式（I）的光学活性氨基酸，并且通过抑制外消旋化保留该构型。 R：任选取代的烷基; X：晕还包括以下独立权利要求：（1）（II）的盐结晶方法包括连续地或部分地和/或通过使用疏水性有机溶剂（优选脂族烃）和亲水有机溶剂添加胺至少30分钟溶剂（优选1-4C醇）作为结晶溶剂; 和（2）（II）的二环己基胺盐。

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