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    Sphingolipid synthesis inhibitor
    1.
    发明授权
    Sphingolipid synthesis inhibitor 失效
    鞘脂合成抑制剂

    公开(公告)号：US06888015B2

    公开(公告)日：2005-05-03

    申请号：US10472379

    申请日：2002-04-19

    申请人： Shu Kobayashi ,  Kentaro Hanada

    发明人： Shu Kobayashi ,  Kentaro Hanada

    IPC分类号： A61K31/165 ,  A61P43/00 ,  C07C233/18 ,  C07C233/05

    CPC分类号： C07C233/18 ,  A61K31/165

    摘要： A inhibitor of sphingolipids synthesis comprising a compound represented by general formula A. Desirably, a novel inhibitor of sphingolipids synthesis comprising (1R, 3R) N-(3-hydroxy-1-hydroxymethyl-3-phenylpropyl) alkaneamide, wherein carbon number of alkanoyl group is 8-16. (in the formula, X is an aliphatic alkyl group, desirably is an aliphatic alkyl group having 7 to 15 carbon atoms).

    摘要翻译： 含有由通式A表示的化合物的鞘脂合成抑制剂。理想地，包含（1R，3R）N-（3-羟基-1-羟甲基-3-苯基丙基）烷酰胺的新型鞘脂合成抑制剂，其中烷酰基 组是8-16。 （式中，X为脂肪族烷基，优选碳原子数为7〜15的脂肪族烷基）。

    Polysilane-supported transition metal catalyst for liquid phase reaction
    3.
    发明授权
    Polysilane-supported transition metal catalyst for liquid phase reaction 有权
    用于液相反应的聚硅烷负载的过渡金属催化剂

    公开(公告)号：US08318967B2

    公开(公告)日：2012-11-27

    申请号：US12224636

    申请日：2007-02-27

    申请人： Shu Kobayashi ,  Hidekazu Oyamada ,  Ryo Akiyama ,  Takeshi Naito

    发明人： Shu Kobayashi ,  Hidekazu Oyamada ,  Ryo Akiyama ,  Takeshi Naito

    IPC分类号： C07F7/08 ,  C07F7/02 ,  C07F7/00

    CPC分类号： C07C67/303 ,  B01J23/40 ,  B01J23/70 ,  B01J31/124 ,  B01J31/127 ,  B01J31/165 ,  B01J31/26 ,  B01J31/28 ,  B01J35/006 ,  B01J37/0219 ,  B01J2231/4261 ,  B01J2231/641 ,  B01J2531/824 ,  B01J2531/828 ,  C07B2200/11 ,  C07C2/861 ,  C07C5/03 ,  C07C5/08 ,  C07C67/343 ,  C07C205/19 ,  C07C2523/42 ,  C07C2523/44 ,  C07C2523/72 ,  C07F15/0066 ,  C07F15/0086 ,  C07F15/0093 ,  C07C15/54 ,  C07C15/18 ,  C07C69/612 ,  C07C69/618

    摘要： The present invention provides a polysilane-supported transition metal catalysts or a polysilane/inorganic compound-supported transition metal catalysts, wherein various types of transition metals are supported by polysilane compounds, or combination of polysilanes and inorganic compounds. The catalysts of the present invention are hardly soluble in hydrocarbons and alcohols and are useful as catalysts in heterogeneous system for various organic synthetic reactions using the above solvents. Polysilanes supporting transition metals are easily crosslinkable by thermal treatment, microwave irradiation, UV irradiation or chemical methods such as hydrosilylation reaction and are changed to be insoluble in various solvents keeping high catalytic activity. Moreover, the stability and operability of polysilane-supported transition metal catalysts will be improved by the support thereof on inorganic compounds. These polysilane-supported transition metal catalysts show a high catalytic activity in hydrogenation reaction, hydrosilylation reaction, Heck reaction, Suzuki-Miyaura coupling reactions and the like. The catalyst is easily recoverable and reusable and the leakage of metals is extremely few.

    摘要翻译： 本发明提供一种聚硅烷负载的过渡金属催化剂或聚硅烷/无机化合物负载的过渡金属催化剂，其中各种类型的过渡金属由聚硅烷化合物或聚硅烷和无机化合物的组合负载。 本发明的催化剂几乎不溶于烃和醇，并且可用作用于使用上述溶剂的各种有机合成反应的异相体系中的催化剂。 支撑过渡金属的聚硅烷通过热处理，微波照射，UV照射或氢化硅烷化反应等化学方法易于交联，并且改变为不溶于保持高催化活性的各种溶剂。 此外，通过其对无机化合物的支持，聚硅烷负载的过渡金属催化剂的稳定性和可操作性将得到改善。 这些聚硅烷负载的过渡金属催化剂在氢化反应，氢化硅烷化反应，Heck反应，Suzuki-Miyaura偶联反应等中显示出高的催化活性。 催化剂易于回收和再利用，金属的泄漏极少。

    Method of enantioselective nucleophilic addition reaction of enamide to imine and synthesis method of α-amino-γ-keto acid ester
    5.
    发明授权
    Method of enantioselective nucleophilic addition reaction of enamide to imine and synthesis method of α-amino-γ-keto acid ester 失效
    酰胺对亚胺的对映选择性亲核加成反应方法及α-氨基-γ-酮酸酯的合成方法

    公开(公告)号：US07754898B2

    公开(公告)日：2010-07-13

    申请号：US10587075

    申请日：2005-01-24

    申请人： Shu Kobayashi

    发明人： Shu Kobayashi

    IPC分类号： C07D207/14 ,  C07C229/00 ,  C07C237/00

    CPC分类号： C07B53/00 ,  B01J31/1805 ,  B01J2231/341 ,  B01J2531/16 ,  C07B2200/07 ,  C07C231/18 ,  C07D207/273

    摘要： An asymmetric synthesis of amino acid compound that is useful as a starting material or synthetic intermediate for production of medicinal products, agrichemicals, perfumes, functional polymers, etc. There is provided a method of enanthio-selective nucleophilic addition reaction to imine compound being a method of nucleophilic addition reaction of enamide compound accompanied by amino formation to imino group (—CH═N—) of imine compound, characterized in that the reaction is performed in the presence of a chiral copper catalyst. Further, there is provided a novel method of synthesizing an amino acid compound, etc., to which the above is applied.

    摘要翻译： 可用作药物，农药，香料，功能性聚合物等的原料或合成中间体的氨基酸化合物的不对称合成。提供了一种亚胺化合物的富含选择性亲核加成反应的方法， 伴随氨基形成的酰胺化合物与亚胺基的亚氨基（-CH = N-）的亲核加成反应，其特征在于反应在手性铜催化剂存在下进行。 此外，提供了一种合成上述应用的氨基酸化合物等的新方法。

    Process for the allylation of n-acylhydrazones
    6.
    发明授权
    Process for the allylation of n-acylhydrazones 失效
    N-酰基腙的烯丙基化方法

    公开(公告)号：US07659424B2

    公开(公告)日：2010-02-09

    申请号：US10591094

    申请日：2005-02-24

    申请人： Shu Kobayashi ,  Masaharu Sugiura

    发明人： Shu Kobayashi ,  Masaharu Sugiura

    IPC分类号： C07C241/02 ,  C07C227/04 ,  C07C229/08 ,  C07C243/38

    CPC分类号： C07C241/02 ,  C07B53/00 ,  C07C2601/14 ,  C07C243/38

    摘要： [PROBLEMS] To provide a novel method for the allylation of N-acylhydrazones by which enantioselectively allylated N-acylhydrazines can be efficiently obtained.[MEANS FOR SOLVING PROBLEMS] A method for the production of enantioselectively allylated N-acylhydrazines represented by the general formula [3]: [wherein R0 is an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or —COOR1 (wherein R1 is a hydrocarbon group); R2 is acyl; R3 and R4 are each hydrogen, or one of R3 and R4 is hydrogen and the other is a hydrocarbon group; and R5 and R6 are each independently hydrogen or a hydrocarbon group], characterized by reacting an N-acylhydrazone represented by the general formula [1]: [wherein R0 and R2 are as defined above] with an allylating agent such as allyltrichlorosilane or crotyltrichlorosilane in the presence of a chiral phosphine oxide.

    摘要翻译： [问题]提供N-酰腙的烯丙基化的新方法，通过该方法可以有效地获得对映选择性烯丙化的N-酰肼。 用于解决问题的方法制备由通式[3]表示的对映选择性烯丙化N-酰肼的方法：[其中R 0是任选取代的烃基，任选取代的杂环基或-COOR 1（其中R 1是 烃基）; R2是酰基; R3和R4各自为氢，R3和R4中的一个为氢，另一个为烃基; R 5和R 6各自独立地为氢或烃基]，其特征在于使由通式[1]表示的N-酰腙：[其中R 0和R 2如上定义]与烯丙基化试剂如烯丙基三氯硅烷或基环丙基三氯硅烷反应 存在手性氧化膦。

    Polymer-Supported Metal Cluster Composition
    7.
    发明申请
    Polymer-Supported Metal Cluster Composition 有权
    聚合物支持金属簇组合物

    公开(公告)号：US20080058200A1

    公开(公告)日：2008-03-06

    申请号：US10590206

    申请日：2005-03-07

    申请人： Shu Kobayashi ,  Kuniaki Okamoto ,  Ryo Akiyama ,  Keiji Ohno ,  Yoshio Inagaki

    发明人： Shu Kobayashi ,  Kuniaki Okamoto ,  Ryo Akiyama ,  Keiji Ohno ,  Yoshio Inagaki

    IPC分类号： B01J31/06

    CPC分类号： C07C67/31 ,  B01J31/069 ,  B01J31/165 ,  B01J2231/4261 ,  B01J2231/643 ,  B01J2531/824 ,  B01J2531/827 ,  B01J2531/828 ,  C07C17/14 ,  C07C45/68 ,  C07C49/796 ,  C07C67/343 ,  C08F212/08 ,  C08F212/14 ,  C07C22/04 ,  C07C69/732 ,  C07C69/618

    摘要： The objective is to present compositions obtained by supporting by polymers micro clusters of transition metals and the like that are useful as catalysts in various reactions and, once used, are readily recovered and reused.A polymer-supported metal cluster composition is obtained by supporting a transition metal by a cross-linked polymer, and the polymer-supported cluster composition is characterized by the cross-linked polymer obtained by cross-linking of a cross-linkable polymer containing a hydrophilic side chain and a hydrophobic side chain group having a cross-linkable functional group. This polymer-supported metal cluster composition is, for example, preferably formed by first forming a micelle composed of the metal clusters supported by the cross-linkable polymer in a suitable solution and subsequently subjecting the cross-linkable polymer to a cross-linking reaction. The composition is useful as a catalyst and the like in hydrogenation reactions, dehydrogenation reactions, allylic substitution reactions, oxidation reactions, coupling reactions and carbonylation reactions.

    摘要翻译： 目的是提供通过聚合物支撑的组合物，所述过渡金属等的微簇等可用作各种反应中的催化剂，并且一旦使用，就容易回收和重复使用。 聚合物负载的金属簇组合物通过用交联聚合物负载过渡金属而获得，聚合物负载的簇组合物的特征在于通过交联含有亲水性的交联聚合物而获得的交联聚合物 侧链和具有可交联官能团的疏水侧链基团。 该聚合物负载的金属簇组合物例如优选通过首先在合适的溶液中形成由可交联聚合物负载的金属簇构成的胶束，然后使可交联聚合物进行交联反应而形成。 该组合物可用作氢化反应，脱氢反应，烯丙基取代反应，氧化反应，偶联反应和羰基化反应中的催化剂等。

    Process for producing nitrogenous 5-membered cyclic compound
    9.
    发明申请
    Process for producing nitrogenous 5-membered cyclic compound 有权
    生产含氮五元环化合物的方法

    公开(公告)号：US20070191614A1

    公开(公告)日：2007-08-16

    申请号：US10592139

    申请日：2005-02-21

    申请人： Shu Kobayashi ,  Yasuhiro Yamashita

    发明人： Shu Kobayashi ,  Yasuhiro Yamashita

    IPC分类号： C07D231/06

    CPC分类号： C07B53/00 ,  C07D231/04 ,  C07D231/06 ,  C07D401/06

    摘要： A method of the intramolecular and intermolecular cyclization of an N-acylhydrazone for obtaining a pyrazoline skeleton or pyrazolidine skeleton under ordinary conditions with high stereoselectivity and in high yield. An N-acylhydrazone represented by the following formula (I): (wherein R1 and R2 are the same or different and each represents hydrogen or a hydrocarbon group and Ar represents an optionally substituted aromatic hydrocarbon group) is converted to an N-acylpyrazoline derivative with high stereoselectivity in the presence of a Lewis acid catalyst or asymmetric Lewis acid catalyst.

    摘要翻译： 用于获得吡唑啉骨架或吡唑烷骨架的N-酰腙的分子内和分子间环化的方法，在具有高立体选择性和高收率的常规条件下。 由下式（I）表示的N-酰腙：（其中R 1和R 2相同或不同，各自表示氢或烃基，Ar表示任选取代的芳族烃基）转化成N-酰基吡唑啉衍生物， 在路易斯酸催化剂或不对称路易斯酸催化剂存在下具有高立体选择性。