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55 条记录 (耗时 0.027 秒)

    Process for producing α-substituted ester
    11.
    发明授权
    Process for producing α-substituted ester 有权
    α-取代酯的制备方法

    公开(公告)号：US08278476B2

    公开(公告)日：2012-10-02

    申请号：US13127955

    申请日：2009-10-22

    申请人： Akihiro Ishii ,  Manabu Yasumoto

    发明人： Akihiro Ishii ,  Manabu Yasumoto

    IPC分类号： C07C69/612

    CPC分类号： C07B53/00 ,  C07B55/00 ,  C07B2200/07 ,  C07C67/343 ,  C07C303/24 ,  C07C69/612 ,  C07C305/26

    摘要： There is provided a process for producing an α-substituted ester by reaction of a fluorosulfuric acid ester of α-hydroxyester with a Grignard reagent in the presence of a zinc catalyst. It is newly found that the reaction for production of α-substituted esters, in which the raw reaction substrate is limited to expensive trifluoromethanesulfonic acid esters, can proceed favorably with the use of fluorosulfuric acid esters suitable for mass-production uses. By the use of the fluorosulfuric acid ester high in optical purity, it is possible to obtain the α-substituted ester with high optical purity upon inversion of the asymmetric carbon configuration. The process of the present invention can solve all of the prior art problems and can be applied for industrial uses.

    摘要翻译： 提供了在锌催化剂存在下，通过α-羟基酯的氟代硫酸酯与格氏试剂的反应制备α-取代的酯的方法。 新发现，通过使用适合于批量生产用途的氟代硫酸酯，可以有利地进行生产反应底物被限制为昂贵的三氟甲磺酸酯的α-取代酯的反应。 通过使用光学纯度高的氟代硫酸酯，可以通过不对称碳结构的反转获得具有高光学纯度的α-取代的酯。 本发明的方法可以解决所有现有技术的问题，并且可以应用于工业用途。

    Method for Producing Fluorosulfuric Acid Ester
    13.
    发明申请
    Method for Producing Fluorosulfuric Acid Ester 有权
    生产氟磺酸酯的方法

    公开(公告)号：US20110201825A1

    公开(公告)日：2011-08-18

    申请号：US13125452

    申请日：2009-10-15

    申请人： Akihiro Ishii ,  Manabu Yasumoto

    发明人： Akihiro Ishii ,  Manabu Yasumoto

    IPC分类号： C07D207/16 ,  C07C303/24

    CPC分类号： C07D207/16 ,  C07B53/00 ,  C07C303/24 ,  C07C305/26

    摘要： Fluorosulfuric acid esters can be produced by reacting alcohols with sulfuryl fluoride (SO2F2) in the presence of a base and water. As a substrate thereof, optically active secondary alcohols are preferable, and optically active α-hydroxyesters and optically active 4-hydroxyprolines are particularly preferable. By performing the reaction in a two-phase system in the presence of a reaction solvent immiscible with water, a desired reaction proceeds particularly well. The present invention is a production method solving all the problems involved in conventional techniques while being industrially practicable.

    摘要翻译： 氟代硫酸酯可以通过在碱和水的存在下使醇与硫酰氟（SO 2 F 2）反应来制备。 作为其基材，优选光学活性仲醇，特别优选光学活性的α-羟基酯和光学活性的4-羟基脯氨酸。 通过在与水不混溶的反应溶剂的存在下在两相体系中进行反应，期望的反应进行得特别好。 本发明是在工业上可行的情况下解决常规技术中涉及的所有问题的生产方法。

    Method for Producing 4-Deoxy-4-Fluoro-D-Glucose Derivative
    14.
    发明申请
    Method for Producing 4-Deoxy-4-Fluoro-D-Glucose Derivative 审中-公开
    生产4-脱氧-4-氟-D-葡萄糖衍生物的方法

    公开(公告)号：US20100267940A1

    公开(公告)日：2010-10-21

    申请号：US12747071

    申请日：2008-11-26

    申请人： Akihiro Ishii ,  Manabu Yasumoto ,  Takashi Ootsuka ,  Yasuko Nigorikawa

    发明人： Akihiro Ishii ,  Manabu Yasumoto ,  Takashi Ootsuka ,  Yasuko Nigorikawa

    IPC分类号： C07H15/207 ,  C07H1/00

    CPC分类号： C07H1/00 ,  C07H5/02 ,  C07H15/04

    摘要： There is disclosed a method for producing a 4-deoxy-4-fluoro-D-glucose derivative by reacting a D-galactose derivative with either sulfuryl fluoride (SO2F2), trifluoromethanesulfonyl fluoride (CF3SO2F) or perfluorobutanesulfonyl fluoride (C4F9SO2F) in the presence of an organic base or in the presence of an organic base and a salt or complex of an organic base and hydrogen fluoride.

    摘要翻译： 公开了通过使D-半乳糖衍生物与硫酰氟（SO 2 F 2），三氟甲磺酰氟（CF 3 SO 2 F）或全氟丁磺酰氟（C 4 F 9 SO 2 F）在存在下反应生成4-脱氧-4-氟-D-葡萄糖衍生物的方法 有机碱或有机碱和有机碱和氟化氢的盐或络合物存在下进行。

    Process For Production Of Optically Active Alpha-Fluoro-Carboxylic Ester Derivatives
    15.
    发明申请
    Process For Production Of Optically Active Alpha-Fluoro-Carboxylic Ester Derivatives 失效
    光活性α-氟羧酸酯衍生物的制备方法

    公开(公告)号：US20080103327A1

    公开(公告)日：2008-05-01

    申请号：US11597105

    申请日：2005-08-05

    申请人： Akihiro Ishii ,  Hideyuki Tsuruta ,  Takashi Ootsuka ,  Yokusu Kuriyama ,  Manabu Yasumoto ,  Kenjin Inomiya ,  Koji Ueda

    发明人： Akihiro Ishii ,  Hideyuki Tsuruta ,  Takashi Ootsuka ,  Yokusu Kuriyama ,  Manabu Yasumoto ,  Kenjin Inomiya ,  Koji Ueda

    IPC分类号： C07C69/63 ,  C07C31/38 ,  C07C69/635

    CPC分类号： C07C67/307 ,  C07B2200/07 ,  C07C29/147 ,  C07C69/65 ,  C07C69/63 ,  C07C31/38

    摘要： The present invention relates to a process for producing an optically active α-fluorocarboxylate derivative represented by the formula [2], by reacting an optically active α-hydroxycarboxylate derivative with trifluoromethanesulfonyl fluoride (CF3SO2F) in the presence of an organic base, in the formula [2], R represents a straight-chain or branched-chain alkyl group of a carbon number of 1 to 12; one of or two by any combination of aromatic hydrocarbon groups, unsaturated hydrocarbon groups, straight-chain or branched alkoxy groups of a carbon number of 1 to 6, aryloxy groups, halogen atoms (fluorine, chlorine, bromine and iodine), protected carboxyl groups, protected amino groups or protected hydroxyl group can be substituted on any carbon atoms of the alkyl group; R1 represents a straight-chain or branched-chain alkyl group of a carbon number of 1 to 8; any carbon atoms of the alkyl groups of R and R1 may form a covalent bond; and * represents an asymmetric carbon.

    摘要翻译： 本发明涉及通过使光学活性α-羟基羧酸酯衍生物与三氟甲磺酰氟（CF 3 SO 3）反应制备由式[2]表示的光学活性α-氟代羧酸酯衍生物的方法， 2 F）在有机碱存在下，在式[2]中，R表示碳数为1至12的直链或支链烷基; 碳数为1至6的芳族烃基，不饱和烃基，直链或支链烷氧基，芳氧基，卤素原子（氟，氯，溴和碘）的任意组合中的一个或两个，被保护的羧基 被保护的氨基或被保护的羟基可以在烷基的任何碳原子上被取代; R 1表示碳数为1至8的直链或支链烷基; R和R 1的烷基的任何碳原子可以形成共价键; 和*表示不对称碳。

    Method for Manufacturing Hydroxyl Group Substitution Product
    17.
    发明申请
    Method for Manufacturing Hydroxyl Group Substitution Product 审中-公开
    羟基取代产物的制备方法

    公开(公告)号：US20110251403A1

    公开(公告)日：2011-10-13

    申请号：US13140307

    申请日：2009-12-15

    申请人： Akihiro Ishii ,  Manabu Yasumoto ,  Koji Ueda

    发明人： Akihiro Ishii ,  Manabu Yasumoto ,  Koji Ueda

    IPC分类号： C07D207/16 ,  C07C67/327

    CPC分类号： C07D207/16 ,  C07C67/307 ,  C07C67/31 ,  C07C69/63 ,  C07C69/68

    摘要： In the present invention, a hydroxyl group substitution product is manufactured by reaction of an alcohol with sulfuryl fluoride (SO2F2) in the presence of an organic base and a nucleophile (X−). The present invention is thus effective as an industrial manufacturing method that uses a relatively cheap reagent suitable for large-scale applications and can be accomplished in a simple process with easy purification operation and less waste generation and is suitably applicable for manufacturing of optically active hydroxyl group substitution products, notably optically active α-hydroxyl group substitution ester and optically active 4-hydroxyl group substitution proline. The manufacturing method of the present invention solves all of the prior art problems and can be applied for industrial uses.

    摘要翻译： 在本发明中，通过在有机碱和亲核体（X）的存在下，通过醇与硫酰氟（SO 2 F 2）的反应制备羟基取代产物。 因此，本发明作为工业制造方法是有效的，其使用适合于大规模应用的相对便宜的试剂，并且可以在简单的方法中实现，容易的纯化操作和较少的废物产生，并且适用于制造光学活性羟基 取代产物，特别是光学活性的α-羟基取代酯和光学活性的4-羟基取代脯氨酸。 本发明的制造方法解决了所有现有技术的问题，可以应用于工业用途。

    Process for Producing alpha Substituted Ester
    18.
    发明申请
    Process for Producing alpha Substituted Ester 有权
    生产α取代酯的方法

    公开(公告)号：US20110213176A1

    公开(公告)日：2011-09-01

    申请号：US13127955

    申请日：2009-10-22

    申请人： Akihiro Ishii ,  Manabu Yasumoto

    发明人： Akihiro Ishii ,  Manabu Yasumoto

    IPC分类号： C07C67/343

    CPC分类号： C07B53/00 ,  C07B55/00 ,  C07B2200/07 ,  C07C67/343 ,  C07C303/24 ,  C07C69/612 ,  C07C305/26

    摘要： There is provided a process for producing an α-substituted ester by reaction of a fluorosulfuric acid ester of α-hydroxyester with a Grignard reagent in the presence of a zinc catalyst. It is newly found that the reaction for production of α-substituted esters, in which the raw reaction substrate is limited to expensive trifluoromethanesulfonic acid esters, can proceed favorably with the use of fluorosulfuric acid esters suitable for mass-production uses. By the use of the fluorosulfuric acid ester high in optical purity, it is possible to obtain the α-substituted ester with high optical purity upon inversion of the asymmetric carbon configuration. The process of the present invention can solve all of the prior art problems and can be applied for industrial uses.

    摘要翻译： 提供了在锌催化剂存在下，通过α-羟基酯的氟代硫酸酯与格氏试剂的反应制备α-取代的酯的方法。 新发现，通过使用适合于批量生产用途的氟代硫酸酯，可以有利地进行生产反应底物被限制为昂贵的三氟甲磺酸酯的α-取代酯的反应。 通过使用光学纯度高的氟代硫酸酯，可以通过不对称碳结构的反转获得具有高光学纯度的α-取代的酯。 本发明的方法可以解决所有现有技术的问题，并且可以应用于工业用途。