邻二氯苯置于镍 硫酸,三氧化硫,氢气,硝酸体系中,用 乙醇 作为反应溶剂,化学反应 6.0H,反应生成 4,5-二氯邻苯二胺 参考文献:Synthesis And Antiviral Evaluation Of 2-Mercapto-5,6-Dichlorobenzimidazole-β-D-Ribofuranonucleoside Derivatives 标题:Synthesis And Antiviral Evaluation Of 2-Mercapto-5,6-Dichlorobenzimidazole-β-D-Ribofuranonucleoside Derivatives 摘要:2-Mercapto-5,6-Dichlorobenzimidazole Beta-D-Ribofuranonucleoside Derivatives 8-10 Have Been Synthesized And Their Antiviral Properties Examined. According To The Glycosylation Procedure Used,The Beta-D-N-1 Isomer (And The N,N-Bis-Riboside) Or The Beta D-S-2-Isomer Have Been Obtained. All The Prepared Compounds Were Tested For Their Activity Against A Variety Of Rna And Dna Viruses,But They Did Not Show Significant Antiviral Activity. DOI:10.1080/15257779408013253
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:US-9951049-B2 优先权日:2014-05-15 标题 :Pyrazole linked benzimidazole conjugates and a process for preparation thereof 发明人:KAMAL AHMED; SHAIK ANVER BASHA; KUMAR GAJJELA BHARATH; REDDY VANGALA SANTHOSH 权利人:COUNCIL OF SCIENT & INDUSTRIAL RESEACH; COUNCIL SCIENT IND RES 摘要:Pyrazole linked benzimidazole conjugates and a method for synthesis of one or more compounds having a pyrazole linked benzimidazole conjugate, particularly pyrazole linked benzimidazole conjugates that are useful as potential antitumor agents against human cancer cell lines, such as leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer. The process comprises the step of oxidative cyclization of o-phenylenediamines and 3-phenyl-1H-pyrazole-5-carbaldehydes with sodium metabisulphite in ethanol/methanol solvent system at a desired temperature for a period of time to obtain the pyrazole linked benzimidazole conjugate.
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-6011152-A 优先权日:1996-07-22 标 题 :Synthesis of macrocyclic tetraamido-N ligands
专利号:CN-115368312-B 优先权日:2021-05-17 标 题 :One-pot synthesis of quinoxaline directly from biomass carbohydrates
[参考文献]: Peter Zllner, Et Al. Derivatization Reaction Of The Mycotoxin Moniliformin With 1,2-Diamino-4,5-Dichlorobenzene: Structure Elucidation Of An Unexpected Reaction Product By Liquid Chromatography/tandem Mass Spectrometry And Liquid Chromatography/nuclear Magnetic Resonance Spectroscopy. J Mass Spectrom. 2003 Jul;38(7):709-14.
合成参考文献
摘要:Irudayanathan, F. M.; Lee, S., Science of Synthesis Knowledge Updates, (2019) 2, 12. 摘要:Irudayanathan, F. M.; Lee, S., Science of Synthesis Knowledge Updates, (2019) 2, 24. 摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 271. 摘要:Tymoshenko, D. O., Science of Synthesis Knowledge Updates, (2012) 3, 355. 摘要:Ambhaikar, N. B., Science of Synthesis Knowledge Updates, (2020) 2, 194.