3-Cyano-7-Hydroxy-2-Iminocoumarin置于盐酸体系中,化学反应 2.0H,反应生成3-氰基-7-羟基香豆素 参考文献:One-Pot Synthesis Of 3-Carboxycoumarins Via Consecutive Knoevenagel And Pinner Reactions In Water 标题:One-Pot Synthesis Of 3-Carboxycoumarins Via Consecutive Knoevenagel And Pinner Reactions In Water 摘要:通过一步法,将适当取代的水杨醛与丙二腈在水中反应,成功制备了氯代,羟基,甲氧基和叔丁基取代的3-羧基香豆素.总体产率较高,且该方法无需使用有机溶剂. Doi:10.1055/s-2003-41061
专利号:US-11091445-B2 优先权日:2016-10-24 标题 :Compounds, process for obtaining the compounds, pharmaceutical composition, use of the compounds and method for treating psychiatric disorders and/or sleep disorders 发明人:RUCH WERNECK GUIMARÃES CRISTIANO; FELYPE ZANETI DE AZEVEDO HATYLAS; MASCARELLO ALESSANDRA; WATANABE DA COSTA RENATA; FREIRE TORRES RUSSO VALTER; MANNOCHIO DE SOUZA RUSSO ELISA 权利人:ACHE LABORATORIOS FARMACEUTICOS SA 摘要:The present disclosure relates to novel and inventive pharmacologically active benzimidazole derivative compounds, which surprisingly have high affinity for melatonin MT1 and MT2 receptors and low affinity for CYP450 complex enzymes, specially CYP1A2. The present invention also relates to novel and inventive routes of synthesis of these compounds, pharmaceutical compositions comprising the compounds and the use of these compounds in the treatment of individuals affected by psychiatric disorders and/or sleep disorders related to these receptors (specially depression, anxiety, circadian cycle disorders), in addition to a process for producing the composition.
专利号:US-7223541-B2 优先权日:2001-08-29 标 题:Terminal-phosphate-labeled nucleotides and methods of use 发明人:FULLER CARL; KUMAR SHIV; SOOD ANUP; NELSON JOHN 权利人:GE HEALTHCARE BIO SCIENCES 摘要:The present invention relates to improved methods of detecting a target using a labeled substrate or substrate analog. The methods comprise reacting the substrate or substrate analog in an enzyme-catalyzed reaction which produces a labeled moiety with independently detectable signal only when such substrate or substrate analog reacts. The present invention, in particular, describes methods of detecting a nucleic acid in a sample, based on the use of terminal-phosphate-labeled nucleotides as substrates for nucleic acid polymerases. The methods provided by this invention utilize a nucleoside polyphosphate, dideoxynucleoside polyphosphate, or deoxynucleoside polyphosphate analogue which has a colorimetric dye, chemiluminescent, or fluorescent moiety, a mass tag or an electrochemical tag attached to the terminal-phosphate. When a nucleic acid polymerase uses this analogue as a substrate, an enzyme-activatable label would be present on the inorganic polyphosphate by-product of phosphoryl transfer. Cleavage of the polyphosphate product of phosphoryl transfer via phosphatase leads to a detectable change in the label attached thereon. When the polymerase assay is performed in the presence of a phosphatase, there is provided a convenient method for real-time monitoring of DNA or RNA synthesis and detection of a target nucleic acid.
专利号:US-7052839-B2 优先权日:2001-08-29 标题 :Terminal-phosphate-labeled nucleotides and methods of use 发明人:NELSON JOHN; FULLER CARL; SOOD ANUP; KUMAR SHIV 权利人:AMERSHAM BIOSCIENCES CORP 摘要:The present invention describes methods of detecting a nucleic acid in a sample, based on the use of terminal-phosphate-labeled nucleotides as substrates for nucleic acid polymerases. The methods provided by this invention utilize a nucleoside polyphosphate, dideoxynucleoside polyphosphate, or deoxynucleoside polyphosphate analogue which has a colorimetric dye, chemiluminescent, or fluorescent moiety, a mass tag or an electrochemical tag attached to the terminal-phosphate. When a nucleic acid polymerase uses this analogue as a substrate, an enzyme-activatable label would be present on the inorganic polyphosphate by-product of phosphoryl transfer. Cleavage of the polyphosphate product of phosphoryl transfer via phosphatase leads to a detectable change in the label attached thereon. When the polymerase assay is performed in the presence of a phosphatase, there is provided a convenient method for real-time monitoring of DNA or RNA synthesis and detection of a target nucleic acid.
专利号:US-7041812-B2 优先权日:2001-08-29 标题 :Labeled nucleoside polyphosphates 发明人:KUMAR SHIV; SOOD ANUP 权利人:AMERSHAM BIOSCIENCES CORP 摘要:The present invention describes new compositions of matter in the form of labeled nucleoside polyphosphates with four or more phosphates. In addition compositions of nucleoside polyphosphates with four or more phosphates that are substrates for nucleic acid polymerases with enhanced substrate properties and methods of using these nucleoside polyphosphates for nucleic acid detection, characterization and quantification are described. The compositions provided by this invention include nucleoside polyphosphate, dideoxynucleoside polyphosphate, or deoxynucleoside polyphosphate analogues which have colorimetric, chemiluminescent, or fluorescent moieties, mass tags or an electrochemical tags attached to the terminal-phosphate. When a nucleic acid polymerase uses this analogue as a substrate, an enzyme-activatable label would be present on the inorganic polyphosphate by-product of phosphoryl transfer. Removal of the polyphosphate product of phosphoryl transfer via phosphate or polyphosphate transferring enzyme leads to a detectable change in the label attached thereon. When the polymerase assay is performed in the presence of a phosphatase, there is provided a convenient method for real-time monitoring of DNA or RNA synthesis and detection of a target nucleic acid.
专利号:CN-109232499-A 优先权日:2018-11-07 标 题:Synthesis and Biochemical Application of Water-Soluble Coumarin-Based Fluorescent Probes
参考标题:Zrcl4/[bmim]Bf4-Catalyzed Condensation Of Salicylaldehydes And Malononitrile: Single-Step Synthesis Of 3-Cyanocoumarin Derivatives 作者:Hassan Valizadeh,Manzar Mahmoodian,Hamid Gholipour |发布日期:2011.7 摘要:A Versatile And Efficient Single‐step Route To 3‐cyanocoumarins Via Knoevenagel Condensation Of Salicylaldehydes And Malononitrile Using Zrcl4 As The Catalyst (15 Mol %) In Ionic Liquid 1‐(N‐butyl)‐3‐methylimidazolium Tetrafluoroborate As Reaction Medium And Catalyst Is Described. The Novel Procedure Features Single Step, Short Reaction Time, Good Yields, And Simple Workup. J. Heterocyclic Chem., (2011)
合成参考文献
参考文献:10.1007/s00228-002-0426-9 摘要:Thapar MM, Ashton M, Lindegårdh N, Bergqvist Y, Nivelius S, Johansson I, Björkman A. Time-dependent pharmacokinetics and drug metabolism of atovaquone plus proguanil (Malarone) when taken as chemoprophylaxis. European Journal of Clinical Pharmacology. 2002 Feb 28;58(1):19–27. doi: 10.1007/s00228-002-0426-9.