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    METHOD FOR PRODUCING OPTICALLY ACTIVE 2-ARYLPIPERAZINE DERIVATIVE
    1.
    发明申请
    METHOD FOR PRODUCING OPTICALLY ACTIVE 2-ARYLPIPERAZINE DERIVATIVE 失效
    用于生产光学活性2-亚氨基吡啶衍生物的方法

    公开(公告)号：US20100087643A1

    公开(公告)日：2010-04-08

    申请号：US12449460

    申请日：2008-02-05

    申请人： Masatoshi Ohnuki ,  Akira Nishiyama ,  Masaru Mitsuda

    发明人： Masatoshi Ohnuki ,  Akira Nishiyama ,  Masaru Mitsuda

    IPC分类号： C07D241/04

    CPC分类号： C07B53/00 ,  C07D241/04

    摘要： The objective of the present invention is to produce an optically active 2-arylpiperazine derivative useful as a synthetic intermediate for pharmaceutical products and agricultural chemicals from inexpensive and readily available starting material by an industrially practicable method. The objective can be accomplished by treating an optically active substituted aminodiol derivative produced from an optically active styrene oxide derivative with a sulfonating agent in the presence of a base, and then reacting an amine compound to obtain the 2-arylpiperazine derivative. Especially, an optically active 1-unsubstituted-2-arylpiperazine derivative can be produced by treating an optically active 1-allyl-2-arylpiperazine derivative with water in the presence of a transition metal catalyst for deallylation.

    摘要翻译： 本发明的目的是通过工业上可行的方法从便宜且容易获得的原料制备用作药物产品和农药的合成中间体的光学活性2-芳基哌嗪衍生物。 该目的可以通过在碱的存在下用磺化剂处理由光学活性苯乙烯氧化物衍生物产生的光学活性取代的氨基二醇衍生物，然后使胺化合物反应得到2-芳基哌嗪衍生物来实现。 特别地，光学活性的1-未取代-2-芳基哌嗪衍生物可以通过在过渡金属催化剂的存在下用水处理光学活性的1-烯丙基-2-芳基哌嗪衍生物来进行脱气。

    Method for producing optically active 2-arylpiperazine derivative
    2.
    发明授权
    Method for producing optically active 2-arylpiperazine derivative 失效
    光学活性2-芳基哌嗪衍生物的制备方法

    公开(公告)号：US08273883B2

    公开(公告)日：2012-09-25

    申请号：US12449460

    申请日：2008-02-05

    申请人： Masatoshi Ohnuki ,  Akira Nishiyama ,  Masaru Mitsuda

    发明人： Masatoshi Ohnuki ,  Akira Nishiyama ,  Masaru Mitsuda

    IPC分类号： C07D241/04 ,  C07D295/00

    CPC分类号： C07B53/00 ,  C07D241/04

    摘要： The objective of the present invention is to produce an optically active 2-arylpiperazine derivative useful as a synthetic intermediate for pharmaceutical products and agricultural chemicals from inexpensive and readily available starting material by an industrially practicable method. The objective can be accomplished by treating an optically active substituted aminodiol derivative produced from an optically active styrene oxide derivative with a sulfonating agent in the presence of a base, and then reacting an amine compound to obtain the 2-arylpiperazine derivative. Especially, an optically active 1-unsubstituted-2-arylpiperazine derivative can be produced by treating an optically active 1-allyl-2-arylpiperazine derivative with water in the presence of a transition metal catalyst for deallylation.

    摘要翻译： 本发明的目的是通过工业上可行的方法从便宜且容易获得的原料制备用作药物产品和农药的合成中间体的光学活性2-芳基哌嗪衍生物。 该目的可以通过在碱的存在下用磺化剂处理由光学活性苯乙烯氧化物衍生物产生的光学活性取代的氨基二醇衍生物，然后使胺化合物反应得到2-芳基哌嗪衍生物来实现。 特别地，光学活性的1-未取代-2-芳基哌嗪衍生物可以通过在过渡金属催化剂的存在下用水处理光学活性的1-烯丙基-2-芳基哌嗪衍生物来进行脱气。

    Process for the preparation of optically active 2-[6-hydroxymethyl)-1,3-dioxan-4yl]acetic acid derivatives
    3.
    发明授权
    Process for the preparation of optically active 2-[6-hydroxymethyl)-1,3-dioxan-4yl]acetic acid derivatives 有权
    制备光学活性2-Ä6-（羟甲基）-1,3-二恶烷-4-基乙酸衍生物的方法

    公开(公告)号：US06472544B1

    公开(公告)日：2002-10-29

    申请号：US09509998

    申请日：2000-08-16

    申请人： Noriyuki Kizaki ,  Yukio Yamada ,  Yoshihiko Yasohara ,  Akira Nishiyama ,  Makoto Miyazaki ,  Masaru Mitsuda ,  Takeshi Kondo ,  Noboru Ueyama ,  Kenji Inoue

    发明人： Noriyuki Kizaki ,  Yukio Yamada ,  Yoshihiko Yasohara ,  Akira Nishiyama ,  Makoto Miyazaki ,  Masaru Mitsuda ,  Takeshi Kondo ,  Noboru Ueyama ,  Kenji Inoue

    IPC分类号： C07D31906

    CPC分类号： C07D319/06 ,  C07B2200/07 ,  C07C67/343 ,  C07C253/30 ,  C12P7/62 ,  C07C69/716 ,  C07C255/21

    摘要： This invention provides a process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives, which are of value as intermediates of drugs, from inexpensive starting materials without using any special equipment such as that required for super-low temperature reactions. A process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives which comprises reacting an acetic acid derivative at a temperature of not less than −30° C. with an enolate prepared by permitting either a base or a metal having a valency of 0 to act on the derivative to produce a hydroxyoxohexanoic acid derivative, reducing this compound with the aid of a strain of microorganism to provide a halomethyldioxanylacetic acid derivative, treating this compound with an acetalizing agent in the presence of an acid catalyst to provide a halomethyldioxanylacetic acid derivative, reacted with an acyloxylating agent to provide a acyloxymethyldioxanylacetic acid derivative, and subjecting this compound to solvolysis in the presence of a base.

    摘要翻译： 本发明提供了从廉价起始原料生产具有价值作为药物中间体的光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的方法，而不使用任何特殊设备 例如超低温反应所需的方法。一种制备光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的方法，其包括在不是的温度下使乙酸衍生物反应 小于-30℃，通过使碱金属或化合价为0的金属作用于衍生物以制备羟基氧代己酸衍生物而制备的烯醇化物，借助于微生物菌株还原该化合物以提供 卤甲基二恶烷基乙酸衍生物，在酸催化剂存在下用缩醛化剂处理该化合物，得到卤代甲基二恶烷基乙酸衍生物，与酰氧基化剂反应，得到酰氧基甲基二恶烷基乙酸 在碱的存在下，将该化合物施用于溶剂分解。

    Process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives
    4.
    发明授权
    Process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives 有权
    光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的制备方法

    公开(公告)号：US06903225B2

    公开(公告)日：2005-06-07

    申请号：US10242453

    申请日：2002-09-13

    申请人： Noriyuki Kizaki ,  Yukio Yamada ,  Yoshihiko Yasohara ,  Akira Nishiyama ,  Makoto Miyazaki ,  Masaru Mitsuda ,  Takeshi Kondo ,  Noboru Ueyama ,  Kenji Inoue

    发明人： Noriyuki Kizaki ,  Yukio Yamada ,  Yoshihiko Yasohara ,  Akira Nishiyama ,  Makoto Miyazaki ,  Masaru Mitsuda ,  Takeshi Kondo ,  Noboru Ueyama ,  Kenji Inoue

    IPC分类号： C07C67/343 ,  C07C253/30 ,  C07C255/21 ,  C07D319/06 ,  C12P7/62 ,  C12P1/04 ,  C12P17/06

    CPC分类号： C07D319/06 ,  C07B2200/07 ,  C07C67/343 ,  C07C253/30 ,  C12P7/62 ,  C07C69/716 ,  C07C255/21

    摘要： This invention provides a process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives, which are of value as intermediates of drugs, from inexpensive starting materials without using any special equipment such as that required for super-low temperature reactions.A process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives which comprises reacting an acetic acid derivative at a temperature of not less than −30° C. with an enolate prepared by permitting either a base or a metal having a valency of 0 to act on the derivative to produce a hydroxyoxohexanoic acid derivative, reducing this compound with the aid of a strain of microorganism to provide a halomethyldioxanylacetic acid derivative, treating this compound with an acetalizing agent in the presence of an acid catalyst to provide a halomethyl-dioxanylacetic acid derivative, reacted with an acyloxylating agent to provide a acyloxymethyldioxanylacetic acid derivative, and subjecting this compound to solvolysis in the presence of a base.

    摘要翻译： 本发明提供了从廉价起始原料生产具有价值作为药物中间体的光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的方法，而不使用任何特殊设备 例如超低温反应所需的。 一种制备光学活性的2- [6-（羟基甲基）-1,3-二恶烷-4-基]乙酸衍生物的方法，其包括使不饱和-30℃的乙酸衍生物与烯醇化物 通过使碱金属或0价金属作用于衍生物以制备羟基己酸衍生物而制备，借助于微生物菌株还原该化合物以提供卤代甲基二恶烷基乙酸衍生物，用缩醛化处理该化合物 在酸催化剂存在下，提供卤代甲基 - 二恶烷基乙酸衍生物，与酰氧基化剂反应，得到酰氧基甲基二恶烷基乙酸衍生物，并在碱的存在下使其溶解。

    Method for producing optically active hydroxycarboxylic acid derivatives or salts thereof
    6.
    发明授权
    Method for producing optically active hydroxycarboxylic acid derivatives or salts thereof 失效
    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。

    Imidazolidinone derivative, method of producing the same and method of producing optically active amino acid
    7.
    发明授权
    Imidazolidinone derivative, method of producing the same and method of producing optically active amino acid 有权
    咪唑啉酮衍生物，其制备方法和制备光学活性氨基酸的方法

    公开(公告)号：US07947722B2

    公开(公告)日：2011-05-24

    申请号：US12309729

    申请日：2007-05-14

    申请人： Yasuhiro Saka ,  Akio Fujii ,  Kazumi Okuro ,  Masaru Mitsuda

    发明人： Yasuhiro Saka ,  Akio Fujii ,  Kazumi Okuro ,  Masaru Mitsuda

    IPC分类号： A61K31/4166 ,  C07D233/32

    CPC分类号： C07D233/32 ,  C07C227/22 ,  C07C231/10 ,  C07C229/14 ,  C07C229/22 ,  C07C229/36 ,  C07C237/06

    摘要： The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily producing an optically active amino acid by using the derivative. The objective can be achieved by producing an optically active amino acid using a novel optically active imidazolidinone derivative represented by a general formula (3) and the like. According to the method of the present invention, an optically active imidazolidinone derivative can be obtained by preferential crystallization from a mixture of isomers of the imidazolidinone derivative. Therefore, an optically active amino acid can be easily and stereoselectively produced without cumbersome procedures required for the conventional methods, such as resolution of diastereomers, synthesis from an optically active amino acid and resolution of isomers by silica gel column chromatography.

    摘要翻译： 本发明的目的是提供广泛用于合成光学活性氨基酸的光学活性咪唑啉酮衍生物，易于制备衍生物的方法，以及通过使用该衍生物容易地制备光学活性氨基酸的方法。 可以通过使用由通式（3）等表示的新的光学活性咪唑烷酮衍生物制造光学活性氨基酸来实现。 根据本发明的方法，可以通过从咪唑烷酮衍生物的异构体的混合物中优先结晶获得光学活性咪唑烷酮衍生物。 因此，光学活性氨基酸可以容易地和立体选择性地产生，而不需要常规方法所需的繁琐程序，例如拆分非对映异构体，由光学活性氨基酸的合成和通过硅胶柱色谱法拆分异构体。

    Process for industrially producing optically active 1,4- benzodioxane derivative
    9.
    发明申请
    Process for industrially producing optically active 1,4- benzodioxane derivative 审中-公开
    工业生产光学活性1,4-苯并二恶烷衍生物的方法

    公开(公告)号：US20060167282A1

    公开(公告)日：2006-07-27

    申请号：US10522734

    申请日：2003-07-17

    申请人： Tatsuyoshi Tanaka ,  Masaru Mitsuda

    发明人： Tatsuyoshi Tanaka ,  Masaru Mitsuda

    IPC分类号： C07D319/14

    CPC分类号： C07D319/20

    摘要： A simple and safe method for producing optically active 1,4-benzodioxane derivatives useful as intermediates for pharmaceuticals and the like from inexpensive materials is provided. An optically active triol compound (5) produced by reaction of catechol (2) and optically active 3-halogeno-1,2-propanediol (3) is sulfonylated to form optically active trisulfonate (6), followed by cyclization with a base to yield optically active 1,4-benzodioxane (1).

    摘要翻译： 提供了一种用于生产用作药物等的廉价材料的中间体的光学活性1,4-苯并二氧杂环戊烷衍生物的简单和安全的方法。 将由邻苯二酚（2）和光学活性3-卤代-1,2-丙二醇（3）的反应制备的光学活性三醇化合物（5）磺酰化以形成光学活性三磺酸盐（6），随后用碱环化，得到 光学活性1,4-苯并二恶烷（1）。