公开(公告)号：US07375244B2

公开(公告)日：2008-05-20

申请号：US10591964

申请日：2005-03-07

Applicant: Shu Kobayashi

Inventor： Shu Kobayashi

IPC: C07F9/02

CPC classification number: B01J31/1805 ,  B01J2531/16 ,  C07B53/00 ,  C07F9/3808 ,  C07F9/3882 ,  C07F9/4006 ,  C07F9/4056

Abstract: To present a reaction system that efficiently catalyzes an enantio selective asymmetric nucleophilic addition reaction of an α-iminophosphonic acid ester. An optically active α-amino-γ-oxophosphonic acid derivative is produced through an asymmetric addition reaction of an α-iminophosphonic acid ester and a nucleophilic agent (for example, a silyl enol ether).

Abstract translation: 提出有效催化α-亚氨基膦酸酯的对映选择性不对称亲核加成反应的反应体系。 通过α-亚氨基膦酸酯和亲核剂（例如甲硅烷基烯醇醚）的不对称加成反应产生光学活性的α-氨基-γ-氧代膦酸衍生物。

公开(公告)号：US20070161804A1

公开(公告)日：2007-07-12

申请号：US10587075

申请日：2004-01-25

Applicant: Shu Kobayashi

Inventor： Shu Kobayashi

IPC: C07D207/14

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

Abstract: 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.

Abstract translation: 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（-CH-N-）亚胺化合物的亲核加成反应，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。

公开(公告)号：US20070073087A1

公开(公告)日：2007-03-29

申请号：US10587078

申请日：2005-01-24

Applicant: Shu Kobayashi

Inventor： Shu Kobayashi

IPC: C07C49/00

CPC classification number: C07D207/18 ,  C07B2200/07 ,  C07C67/343 ,  C07C269/04 ,  C07C69/738 ,  C07C69/716

Abstract: A method of an enantioselective nucleophilic addition reaction to carbonyl, which enables an asymmetric synthesis of an optically active α-hydroxy-γ-keto acid ester, an optically active α-hydroxy-γ-amino acid ester, hydroxydiketone compounds, etc. being useful as a raw material or synthesis intermediate for producing a pharmaceutical preparation, an agricultural chemical, a fragrance, a functional polymer or the like. In this method, the nucleophilic addition reaction of enamide compound accompanied by hydroxyl (—OH) formation to carbonyl is carried out in the presence of a chiral catalyst with copper or nickel.

Abstract translation: 对羰基的对映选择性亲核加成反应的方法，其使得光学活性α-羟基-γ-酮酸酯，光学活性α-羟基-γ-氨基酸酯，羟基二酮化合物等的不对称合成是有用的 作为制备药物制剂，农药，香料，功能聚合物等的原料或合成中间体。 在这种方法中，伴随着羟基（-OH）形成羰基的烯酰胺化合物的亲核加成反应在具有铜或镍的手性催化剂的存在下进行。

公开(公告)号：US20060111590A1

公开(公告)日：2006-05-25

申请号：US10539615

申请日：2003-12-17

Applicant: Shu Kobayashi

Inventor： Shu Kobayashi

IPC: C08F8/30 ,  C07C241/02 ,  C08C19/22 ,  C07C27/18

CPC classification number: C08F8/30 ,  B01J31/0237 ,  B01J31/0247 ,  B01J31/06 ,  B01J31/4007 ,  B01J2231/341 ,  C07C29/38 ,  C07C243/38 ,  C07C2601/16 ,  Y02P20/584 ,  C07C33/20

Abstract: Polymer-immobilized form amides characterized by being represented by the general formula: (wherein R1 is an optionally substituted hydrocarbon chain which may have a cyclic moiety or a heteroatom; R2 is an optionally substituted hydrocarbon group or an optionally substituted hydrocarbon chain which is bonded to R1 to form a ring; and the solid circle represents a polymer); novel organic catalysts containing the same, which catalysts are free from metallic catalyst components and very easy of recovery from reaction mixtures of synthesis and reuse; polymer-immobilized organic compounds useful as intermediates for synthesis; catalysts containing the same as the active ingredient; and a process for the allylation of aldehydes or hydrazones by the use of these catalysts.

Abstract translation: 聚合物固定形式的酰胺，其特征在于由以下通式表示：（其中R 1是可以具有环状部分或杂原子的任选取代的烃链; R 2， 是任选取代的烃基或任选取代的烃链，其与R 1键合以形成环;并且实心圆代表聚合物）; 含有该催化剂的新型有机催化剂，其不含金属催化剂组分，并且非常容易从合成和再利用的反应混合物中回收; 可用作合成中间体的聚合物固定化有机化合物; 含有与活性成分相同的催化剂; 以及通过使用这些催化剂使醛或腙烯丙基化的方法。

公开(公告)号：US06916761B1

公开(公告)日：2005-07-12

申请号：US09889406

申请日：2000-10-23

Applicant: Shu Kobayashi

Inventor： Shu Kobayashi

IPC: C07D263/10 ,  B01J23/10 ,  B01J31/06 ,  B01J31/10 ,  B01J31/12 ,  B01J31/14 ,  B01J31/16 ,  B01J31/22 ,  B01J31/26 ,  B01J31/34 ,  B01J31/36 ,  B01J31/38 ,  B01J31/40 ,  C07B37/00 ,  C07B37/02 ,  C07B61/00 ,  C07C29/40 ,  C07C33/025 ,  C07C33/30 ,  C07C45/64 ,  C07C45/72 ,  C07C49/835 ,  C07C67/31 ,  C07C69/732 ,  C07C253/00 ,  C07C255/42 ,  C07C327/22 ,  B01J23/83 ,  B01J27/02 ,  B01J27/053 ,  C08F4/02

CPC classification number: B01J31/10 ,  B01J31/0227 ,  B01J31/1658 ,  B01J31/2226 ,  B01J31/4015 ,  B01J2231/326 ,  B01J2231/342 ,  B01J2231/343 ,  B01J2231/44 ,  B01J2531/35 ,  B01J2531/37 ,  B01J2531/38 ,  C07B37/02 ,  C07B2200/07 ,  C07C29/38 ,  C07C67/343 ,  C07C227/26 ,  C07C253/00 ,  C07C253/08 ,  C07C327/22 ,  C07C2601/14 ,  C07D263/38 ,  Y02P20/584 ,  C07C69/732 ,  C07C255/42 ,  C07C33/14 ,  C07C33/30

Abstract: In order to provide a novel Lewis acid catalyst, which shows high reaction activity in aqueous medium, is easily recovered, and is excellent in reusability, a Lewis acid group expressed by the general formula (I): MXn  (I) (wherein M represents a polyvalent element, X represents an anionic group, and n is an integer representing the valence of M) is linked and supported on a polymer membrane via an SO3 or SO4 group.

Abstract translation: 为了提供在水性介质中显示高反应活性的新颖的路易斯酸催化剂，易于回收，并且具有优异的可重复使用性，由通式（I）表示的路易斯酸基团：<？在线配方说明书 =“在线公式”end =“lead”？> MX （I）<？in-line-formula description =“In-line Formulas”end =“tail”？>（其中 M表示多价元素，X表示阴离子基团，n表示M价数的整数）通过SO 3或SO 4连接并负载在聚合物膜上， SUB>组。

公开(公告)号：US20050124831A1

公开(公告)日：2005-06-09

申请号：US10507027

申请日：2003-03-07

Applicant: Shu Kobayashi ,  Masaharu Sugiura

Inventor： Shu Kobayashi ,  Masaharu Sugiura

IPC: C07D263/22 ,  B01J27/13 ,  B01J31/30 ,  C07B61/00 ,  C07C269/06 ,  C07C271/18 ,  C07C271/24 ,  C07C29/30

CPC classification number: C07C269/06 ,  B01J27/13 ,  B01J31/30 ,  C07C271/18 ,  C07C271/24

Abstract: A conjugate addition reaction between an α,β-unsaturated ketone compound and a carbamate compound is carried out to synthesize a β-aminoketone, a salt or a hydrate salt of a transition metal of Groups 7 to 11 of the Periodic Table of Elements being present in the reaction system as the catalyst. The novel method and the catalyst are capable of synthesizing the β-aminoketone by the Aza-Michael reaction with high yield and efficiency.

Abstract translation: 进行α，β-不饱和酮化合物和氨基甲酸酯化合物之间的共轭加成反应，以合成出现的元素周期表第7〜11族的过渡金属的β-氨基酮，盐或水合物盐 在反应体系中作为催化剂。 新方法和催化剂能够以高产率和高效率通过Aza-Michael反应合成β-氨基酮。

公开(公告)号：US20050119416A1

公开(公告)日：2005-06-02

申请号：US10507073

申请日：2003-03-11

Applicant: Shu Kobayashi

Inventor： Shu Kobayashi

IPC: B01J31/12 ,  B01J31/16 ,  B01J31/22 ,  B01J31/24 ,  C07C29/143 ,  C07C67/333 ,  C07D207/48 ,  C07D211/96 ,  C07D225/02 ,  C07D307/28 ,  C07D307/92 ,  C07F15/00 ,  C08F8/42 ,  C08F132/00

CPC classification number: C08F8/42 ,  B01J31/1658 ,  B01J31/2295 ,  B01J31/24 ,  B01J2231/324 ,  B01J2231/543 ,  B01J2231/643 ,  B01J2531/821 ,  C07B2200/11 ,  C07C29/143 ,  C07C67/333 ,  C07C2601/10 ,  C07D207/48 ,  C07D211/96 ,  C07D225/02 ,  C07D307/28 ,  C07D307/92 ,  C07F15/0046 ,  C07F15/0053 ,  C07C69/74 ,  C07C33/22

Abstract: A novel polymer-supported arene-ruthenium complex represented by the following formula: wherein A represents an organic polymer with a side chain containing an aromatic ring coordinated to Ru, X1 and X2 represent the same or different halogen atoms, and R represents a hydrocarbon group that may have a substituent is provided for use as a catalyst. This novel polymer-supported arene-ruthenium complex and catalyst thereof can be produced by a simple process, are stable and easy to recover, have a high catalytic activity, and can be used for various organic synthesis reactions. Novel methods for an organic synthesis reaction such as ring-opening metathesis reaction of an olefin compound and reduction of a carbonyl group, using the catalyst are provided.

Abstract translation: 由下式表示的新型聚合物负载的芳烃 - 钌络合物：其中A表示具有侧链的有机聚合物，所述侧链含有与Ru，X 1和X 2配位的芳环， SUB>表示相同或不同的卤素原子，并且R表示可以具有取代基的烃基用作催化剂。 这种新型的聚合物负载的芳烃 - 钌络合物及其催化剂可以通过简单的方法制备，稳定且易于回收，具有高催化活性，可用于各种有机合成反应。 提供了使用催化剂的有机合成反应的新方法，例如烯烃化合物的开环易位反应和羰基还原。

公开(公告)号：US06888015B2

公开(公告)日：2005-05-03

申请号：US10472379

申请日：2002-04-19

Applicant: Shu Kobayashi ,  Kentaro Hanada

Inventor： Shu Kobayashi ,  Kentaro Hanada

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

CPC classification number: C07C233/18 ,  A61K31/165

Abstract: 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).

Abstract translation: 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）。

公开(公告)号：US06844350B2

公开(公告)日：2005-01-18

申请号：US10187895

申请日：2002-07-03

Applicant: Shu Kobayashi ,  Yusuke Wataya ,  Hye-Sook Kim

Inventor： Shu Kobayashi ,  Yusuke Wataya ,  Hye-Sook Kim

IPC: A61K31/00 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/529 ,  A61P33/00 ,  A61P33/06 ,  B01J31/12 ,  B01J31/18 ,  C07B61/00 ,  C07D401/06 ,  C07D491/04 ,  C07D491/048

CPC classification number: C07D401/06 ,  A61K31/517 ,  C07D491/04 ,  Y02A50/411

Abstract: A febrifugine represented by Formula (A): and an isofebrifugine represented by Formula (B): which exhibit extremely strong activities against tropical malarial protozoan are provided, together with a total synthesis route which enables efficient large scale synthesis of the same.

Abstract translation: 提供由式（A）表示的分枝杆菌和由式（B）表示的异苯乙酸：与热带疟原虫相比表现出极强的活性，以及​​能够进行大规模合成的总合成路线。

公开(公告)号：US06838527B2

公开(公告)日：2005-01-04

申请号：US10221372

申请日：2001-03-13

Applicant: Shu Kobayashi

Inventor： Shu Kobayashi

IPC: C07C227/10 ,  C07C213/08 ,  C07C215/08 ,  C07C227/12 ,  C07C229/18 ,  C07C229/24 ,  C07C251/04 ,  C07C251/08 ,  C07D211/86 ,  C07D215/48 ,  C07D221/18 ,  C07D491/04 ,  C07D491/048 ,  C08F8/30 ,  C08F246/00 ,  C08F212/08 ,  C07C227/14 ,  C07C229/00 ,  C07D215/36

CPC classification number: C07D491/04 ,  C07B2200/11 ,  C07C251/08 ,  C07D211/86 ,  C07D215/48 ,  C07D221/18 ,  C08F8/30 ,  C08F246/00

Abstract: As an α-iminoester derivative that is stable under normal conditions and a method of producing various α-aminoester derivatives using them, a polymer-immobilized α-iminoester derivative represented by the following general formula (1): wherein R1 represents an alkyl chain of 1 or more carbons, and R2 represents a hydrogen atom, halogen atom, or an alkyl group, aryl group or alkoxy group that may contain substituents, and a method of producing an α-iminoester derivative using them are provided.

Abstract translation: 作为在正常条件下稳定的α-亚氨基酯衍生物和使用它们生产各种α-氨基酯衍生物的方法，由以下通式（1）表示的聚合物固定的α-亚氨基酯衍生物：其中R 1表示 1个以上的碳原子的烷基链，R 2表示氢原子，卤原子或可以含有取代基的烷基，芳基或烷氧基，提供使用它们的α-亚氨基酯衍生物的制造方法 。