专利号:US-6051704-A 优先权日:1996-07-22 标题:Synthesis of macrocyclic tetraamido-N ligands 发明人:GORDON-WYLIE SCOTT W; COLLINS TERRENCE J 权利人:UNIV CARNEGIE MELLON 摘要:New synthetic methods for the preparation of macrocyclic amido-N donor ligands are provided. The primary method of the present invention involves in general only two synthetic steps. In the first step, an α or β amino carboxylic acid is allowed to react with an optimal (approximately stoichiometric) amount of an activated malonate or oxalate derivative with mild heating. Upon completion of the double coupling reaction, hydrolysis of the reaction mixture yields a diamide containing intermediate (a macro linker). In the second step, stoichiometric amounts of a diamine, preferably an orthophenylene diamine, are added to the macro linker intermediate in the presence of a coupling agent and heat. This second double coupling reaction, is allowed to proceed for a period of time sufficient to produce a macrocyclic tetraamido compound. The substituent groups on the α or β amino carboxylic acid, the malonate, and the aryl diamine may all be selectively varied so that the resulting tetraamido macrocycle can be tailored to specific desired end uses. The macrocyclic tetraamide ligand may then be complexed with a metal, such as a transition metal, and preferably the middle and later transition metals, to form a robust chelate complex suitable for catalyzing oxidation reactions.
专利号:EP-2665702-A1 优先权日:2011-01-18 标 题 :Process for the preparation of retigabine 发明人:FITZGERALD RUSS N; MILLAR ALAN; TOCZKO JENNIFER FELL 权利人:GLAXO GROUP LTD 摘要:This invention relates to a novel chemical process for the synthesis of 2-ethyoxycarbonylamino-5-(4-fluorobenzylamino)-nitrobenzene and its use in the preparation of 2-amino-4-(4-fluorobenzylamino)-1-ethoxycarbonylaminobenzene (retigabine/ezogabine) and its polymorphic forms thereof.
专利号:US-9102593-B2 优先权日:2011-01-18 标 题 :Process for the preparation of retigabine 发明人:FITZGERALD RUSS N; MILLAR ALAN; TOCZKO JENNIFER FELL 权利人:FITZGERALD RUSS N; MILLAR ALAN; TOCZKO JENNIFER FELL; GLAXO GROUP LTD 摘要:This invention relates to a novel chemical process for the synthesis of 2-ethyoxycarbonylamino-5-(4-fluorobenzylamino)-nitrobenzene and its use in the preparation of 2-amino-4-(4-fluorobenzylamino)-1-ethoxycarbonylaminobenzene (retigabine/ezogabine) and its polymorphic forms thereof.
专利号:US-2013102730-A1 优先权日:2010-04-02 标 题:Polyamine-containing polymers and methods of synthesis and use 发明人:JOST ROBERT W; ULUDAG HASAN; BOLUK MEHMET YAMAN 权利人:JOST ROBERT W; ULUDAG HASAN; BOLUK MEHMET YAMAN; ALBERTA INNOVATES TECHNOLOGY FUTURES 摘要:The present invention relates to polyamine-containing polymers and methods of their synthesis and use. The polymer may be hydroxyethylcellulose, dextran, poly(vinyl alcohol) or poly(methyl acrylate).
专利号:US-2024279231-A1 优先权日:2021-05-20 标题:Map4k4 inhibitors and methods of synthesis and use thereof 发明人:AWASTHI VIBHUDUTTA; EEDA VENKATESWARARAO 权利人:UNIV OKLAHOMA 摘要:The compound DMX-5804, IUPAC name 5-(4-(2-methoxyethoxy)phenyl)-7-phenyl-3,4a,7,7a-tetrahydro-4H-pyrrolo[2,3-d]pyrimidin-4-one, is a potent and selective inhibitor of mitogen-activated protein kinase kinase kinase kinase-4 (MAP4K4). The present disclosure describes a scalable and practical synthesis process for making DMX-5804. The process (1) doesn't rely on transition metals, (2) has reduced duration of reactions, (3) is streamlined with significantly improved yields using low cost raw materials, (4) includes no microwave-assisted reactions, (5) does not require column purification, and (6) generally results in crystalized products having over a 95% purity in each step. The present disclosure also describes DMX-5804 analogs and derivatives for use in inhibiting MAP4K4, and scalable and practical processes for making such DMX-5804 analogs.
专利号:US-8012220-B2 优先权日:2006-04-13 标题 :Specific monocationic monochromophoric compounds of hydrazone type comprising a 2-, 4-pyridinium or 2-, 4-quinolinium unit, synthesis thereof, dye compositions containing them, and method for dyeing keratin fibres 发明人:DAVID HERVE; MURGUET NADEGE; GREAVES ANDREW 权利人:OREAL 摘要:The present disclosure relates to monocationic monochromophoric compounds of formula (I) and (II) and dyeing compositions and multicompartment devices comprising monocationic monochromophoric compounds of formula (I) and (II). The disclosure also relates to methods for preparing monocationic monochromophoric compounds of formula (I) and (II), and also to methods for dyeing comprising applying monocationic monochromophoric compounds of formula (I) and (II) to keratin fibers.
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