| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 41 | 腙衍生物的制备方法 | CN200680013524.8 | 2006-04-27 | CN101163671A | 2008-04-16 | 吉野博; 小林健太郎; 城祐一 |
| 本发明提供了通式(5)所示腙衍生物的有利于工业化的制备方法，该方法如下反应式所示。 | ||||||
| 42 | 腙化合物的制造方法 | CN200580021542.6 | 2005-06-28 | CN1976896A | 2007-06-06 | 高相圣一; 阿部胜美; 武居厚志 |
| 本发明提供了一种由通式(5)代表的腙化合物的制造方法，其中包括：不将由通式(3)代表的肼化合物从反应器中取出而将所述肼化合物与由通式(4)代表的羰基化合物缩合的步骤。根据本发明，能够以高品质和高收率获得目标腙化合物，而完全不需要将肼化合物从反应器中取出，所述肼化合物是反应中间体，它在结构上不稳定，并且因其毒性(诱变性)而担心威胁到工人的安全。 | ||||||
| 43 | 形成碳－杂原子键的方法 | CN200480016555.X | 2004-05-12 | CN1805924A | 2006-07-19 | C·莫热; G·米格纳尼 |
| 本发明涉及一种通过使带有离去基团的不饱和化合物与亲核性化合物反应而生成碳－杂原子键的方法且优选是生成碳－氮键的方法。具体而言，本发明涉及利用含氮有机衍生物的芳基化而生成碳－氮键的方法。本发明生成碳－杂原子键的方法是，在基于钯的催化剂的存在下，任选地在配体的存在下，通过使带有离去基团的不饱和化合物与引入能够取代离去基团的杂原子的亲核性化合物反应而生成碳－杂原子键。本发明的特征在于，在与醇类溶剂缔合的有效量金属或铵的氢氧化物存在下进行该反应。 | ||||||
| 44 | 通过与重氮酯反应合成一种腙β－酮酯 | CN97198962.1 | 1997-08-29 | CN1109018C | 2003-05-21 | A·S·沙; J·D·克拉克; Y·马; J·C·佩特森; L·帕特里斯 |
| 本发明涉及通过将烷基重氮酯与腙醛在路易斯酸存在下反应以合成腙β-酮酯。在一优选的实施方案中，在碱存在下通过与烷基酰氯反应，将腙β-酮酯然后转变成为哒嗪酮化合物，随后酸化。本发明也涉及制备腙醛的一种连续工艺，它包括将肼与乙二醛相接触，其中肼和乙二醛是以控制的速率同时被加入至反应器。 | ||||||
| 45 | 酮连氮的合成方法 | CN96111654.4 | 1996-08-13 | CN1063433C | 2001-03-21 | 栗山育久; 永田信祐; 吉田净 |
| 这里公开了一种在含有催化剂的工作溶液存在下，从过氧化氢、氨和甲基乙基酮连续和稳定地合成酮连氮的方法，该方法包括通过蒸馏从甲基乙基酮中除去仲丁醇的步骤，其中甲基乙基酮通过循环再利用，以及一种制备水合肼的方法，它包括水解这种酮连氮的步骤。根据本发明，尽管未反应的酮进行循环，杂质在循环酮中的聚集被阻止了，长期将酮连氮的收率和水合肼的收率保持在高水平。 | ||||||
| 46 | 酮连氮的合成方法和水合肼的合成方法 | CN96111654.4 | 1996-08-13 | CN1149049A | 1997-05-07 | 栗山育久; 永田信祐; 吉田净 |
| 这里公开了一种在含有催化剂的工作溶液存在下，从过氧化氢、氨和甲基乙基酮连续和稳定地合成酮连氮的方法，该方法包括通过蒸馏从甲基乙基酮中除去仲丁醇的步骤，其中甲基乙基酮通过循环再利用，以及一种制备水合肼的方法，它包括水解这种酮连氮的步骤。根据本发明，尽管未反应的酮进行循环，杂质在循环酮中的聚集被阻止了，长期将酮连氮的收率和水合肼的收率保持在高水平。 | ||||||
| 47 | PROCESSES AND INTERMEDIATES FOR PREPARING INDOLE PHARMACEUTICALS | US14890514 | 2014-05-13 | US20160107991A1 | 2016-04-21 | James R. MCCARTHY |
| The invention described herein pertains to processes and intermediates for preparing indole containing pharmaceuticals, particularly to processes and intermediates for preparing selective estrogen receptor modulators, such as bazedoxifene. | ||||||
| 48 | Resin, optical material, and optical device | US14003719 | 2012-03-09 | US09221949B2 | 2015-12-29 | Shunsuke Fujii; Shintaro Maekawa; Hitoshi Onishi; Akifumi Kagayama |
| The purpose of the invention is to provide a resin, which has a high refractive index, excellent heat resistance and moldability, and high transparency, and is useful as a material for configuring optical devices, etc. The invention provides a resin comprising acyl hydrazone bonds and having a number average molecular weight of 500-500,000, wherein the acyl hydrazone bond equivalent is 100-4000. | ||||||
| 49 | Method for preparing formamide compounds | US13805899 | 2012-04-04 | US08877971B2 | 2014-11-04 | Thibault Cantat; Christophe Gomes; Olivier Jacquet |
| The present invention relates to a method for preparing formamide compounds using carbon dioxide, and to the use of said method for manufacturing vitamins, pharmaceutical products, adhesives, acrylic fibers, synthetic leathers, pesticides and fertilizers. The invention also relates to a method for manufacturing vitamins, pharmaceutical products, adhesives, acrylic fibers, synthetic leathers, pesticides and fertilizers which includes a step of preparing formamide compounds by the method according to the invention. | ||||||
| 50 | SMALL MOLECULE MALARIAL ALDOLASE-TRAP ENHANCERS AND GLIDEOSOME INHIBITORS | US14353438 | 2012-10-25 | US20140275088A1 | 2014-09-18 | Timothy J. Cardozo; Jürgen Bosch; Sondra Maureen Nemetski |
| In one aspect, the present invention relates to a method of identifying compounds useful in modifying the activity of Aldolase. The method includes providing a first model comprising Aldolase or residues of the amino acid sequence corresponding to SEQ ID NO: 1 said residues being at amino acid positions selected from the group consisting of 10-13, 26, 27, 29, 30, 31, 32, 33, 37, 39, 40, 41, 43, 44, 47, 48, 51, 52, 60, 63, 66, 79, 84, 85, 92, 93, 103, 106-109, 112-117, 138, 142, 146, 148, 151, 153, 179, 182, 183, 185, 186, 194, 196, 197, 198, 199, 208, 226-228, 231-269, 270, 272, 277-283, 285-289, 294, 295, 297-299, 301-304, 306-310 312, 313, 316, 317, 319, 321, 323, 326, 330, 344, 345, and 347, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for modifying the activity of Aldolase. The present invention also discloses compounds and compositions which modify the activity of Aldolase, or a complex between Aldolase and TRAP. Methods of treating or preventing malaria, or an infection by apicomplexan organisms are also disclosed. | ||||||
| 51 | RESIN, OPTICAL MATERIAL, AND OPTICAL DEVICE | US14003719 | 2012-03-09 | US20140001950A1 | 2014-01-02 | Shunsuke Fujii; Shintaro Maekawa; Hitoshi Onishi; Akifumi Kagayama |
| The purpose of the invention is to provide a resin, which has a high refractive index, excellent heat resistance and moldability, and high transparency, and is useful as a material for configuring optical devices, etc. The invention provides a resin comprising acyl hydrazone bonds and having a number average molecular weight of 500-500,000, wherein the acyl hydrazone bond equivalent is 100-4000. | ||||||
| 52 | LIGANDS FOR ESTROGEN RELATED RECEPTORS AND METHODS FOR SYNTHESIS OF SAID LIGANDS | US13237605 | 2011-09-20 | US20130131340A1 | 2013-05-23 | Barry Forman; Donna Yu |
| Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described. | ||||||
| 53 | Ligands for metals and improved metal-catalyzed processes based thereon | US11781651 | 2007-07-23 | US07560582B2 | 2009-07-14 | Stephen L. Buchwald; David W. Old; John P. Wolfe; Michael Palucki; Ken Kamikawa |
| One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency. | ||||||
| 54 | Ligands for Metals and Improved Metal-Catalyzed Processes Based Thereon | US11781651 | 2007-07-23 | US20080033171A1 | 2008-02-07 | Stephen Buchwald; David Old; John Wolfe; Michael Palucki; Ken Kamikawa |
| One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency. | ||||||
| 55 | Ligands for metals and improved metal-catalyzed processes based thereon | US11229043 | 2005-09-16 | US07247731B2 | 2007-07-24 | Stephen L. Buchwald; David W. Old; John P. Wolfe; Michael Palucki; Ken Kamikawa |
| One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency. | ||||||
| 56 | Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds | US11431154 | 2006-05-09 | US20060264673A1 | 2006-11-23 | Stephen Buchwald; Artis Klapars; Jon Antilla; Gabriel Job; Martina Wolter; Fuk Kwong; Gero Nordmann; Edward Hennessy |
| The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-oxygen bond between the oxygen atom of an alcohol and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. The present invention also relates to copper-catalyzed methods of forming a carbon-carbon bond between a reactant comprising a nucleophilic carbon atom, e.g., an enolate or malonate anion, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. Importantly, all the methods of the present invention are relatively inexpensive to practice due to the low cost of the copper comprised by the catalysts. | ||||||
| 57 | Ligands for estrogen related receptors and methods for synthesis of said ligands | US11336515 | 2006-01-20 | US20060189825A1 | 2006-08-24 | Barry Forman; Donna Yu |
| Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described. | ||||||
| 58 | Ligands for metals and improved metal-catalyzed processes based thereon | US10731702 | 2003-12-09 | US20040171833A1 | 2004-09-02 | Stephen L. Buchwald; Xiaohua Huang; Danilo Zim |
| One aspect of the present invention relates to ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency. | ||||||
| 59 | Metal-catalyzed arylations of hydrazines, hydrazones, and related substrates | US09765072 | 2001-01-18 | US20010031894A1 | 2001-10-18 | Stephen L. Buchwald; Seble Wagaw; Oliver Fabian Geis |
| A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols. | ||||||
| 60 | Synthesis of a hydrazone .beta.-keto ester by the reaction with a diazo ester | US254016 | 1999-05-24 | US6025492A | 2000-02-15 | Ajit S. Shah; Jerry D. Clark; Yinong Ma; James C. Peterson; Lefteris Patelis |
| The present invention relates to the synthesis of a hydrazone .beta.-keto ester by the reaction of an alkyl diazoester with a hydrazone aldehyde in the presence of a Lewis acid In a preferred embodiment, the hydrazone .beta.-keto ester is then converted into a pyridazinone compound by the reaction with an alkyl acid chloride in the presence of a base, followed by acidification. A process for the production of a hydrazone aldehyde, which comprises contacting a hydrazine and glyoxal, is also described. | ||||||
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