(E)-Methyl 2-Cyano-3-(2-Hydroxyphenyl)Propenoate 反应 0.5H,以65%的收率获得香豆素-3腈 参考文献:O'Callaghan,Conor N.; Mcmurry,T. Brian H.; Cardin,Christine J.,Journal Of Chemical Research,Miniprint,1990,# 5,P. 901-922 标题:O'Callaghan,Conor N.; Mcmurry,T. Brian H.; Cardin,Christine J.,Journal Of Chemical Research,Miniprint,1990,# 5,P. 901-922
专利号:US-6303764-B1 优先权日:1998-09-24 标题:Synthesis of 4,7-dialkyl chromogenic glycosides of N-acetylneuraminic acids 发明人:SRIVASTAVA OM; SRIVASTAVA GEETA; DU MINGHUI; HINDSGAUL OLE; BUNDLE DAVID R; LIAV AVRAHAM 权利人:ZYMETX INC; HALIFEX FUND L P 摘要:The present invention provides an improved method of preparing a 4,7-di-O-alkyl chromogenic ketoside of N-acetylneuraminic acid (Neu5Ac) for use in detecting influenza virus types A and B. The ketosides are substrates that are selectively cleaved by a neuraminidase on influenza virus, but not be neuraminidases found on other viruses or on bacteria. The synthesis is efficient and provides large quantities of the ketoside for commercial development. The synthesis includes a step of alkylating the 4- and 7-hydroxyl groups of a protected alkyl ester alkyl ketoside derivative of Neu5Ac by a process that comprises contacting the derivative with a composition comprising an alkyl halide to form a 4,7-di-O-alkyl protected alkyl ester alkyl ketoside derivative of Neu5Ac. The synthesis alternatively includes protecting the 8- and 9-hydroxyl groups of an alkyl ester alkyl ketoside derivative of Neu5Ac by forming an 8,9-epoxide protected alkyl ester alkyl ketoside derivative of Neu5Ac.
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-6420552-B1 优先权日:1999-09-10 标题:Syntheses of 4-alkyl chromogenic glycosides and 7-alkyl chromogenic glycosides of N-acetylneuraminic acids 发明人:SRIVASTAVA OM; SRIVASTAVA GEETA; DU MINGHUI; HINGSGAUL OLE; BUNDLE DAVID R 权利人:ZYMETX INC 摘要:The present invention provides improved method of preparing a 4-O-alkyl chromogenic ketoside of N-acetylneuraminic acid (Neu5Ac) and a 7-O-alkyl chromogenic ketoside of N-acetylneuraminic acid (Neu5Ac) for use in the selective detection of various influenza viruses and parainfluenza viruses. The ketosides are substrates that are selectively cleaved by a neuraminidase on the virus to be detected, but not by neuraminidases found on other viruses or on bacteria, or on the cells of the host. The syntheses are efficient and provide large quantities of the ketosides for commercial development. The synthesis includes a step of alkylating the 4- or 7-hydroxyl groups of a protected alkyl ester alkyl ketoside derivative of Neu5Ac by processes that include contacting the derivative with a composition comprising an alkyl halide to form a 4- or a 7-O-alkyl protected alkyl ester alkyl ketoside derivative of Neu5Ac. The syntheses alternatively include protecting the 8- and 9-hydroxyl groups of an alkyl ester alkyl ketoside derivative of Neu5Ac by forming an 8,9-ketal or an 8,9-epoxide protected alkyl ester alkyl ketoside derivative of Neu5Ac.
专利号:US-7994323-B2 优先权日:2007-05-09 标 题:Chromen-2-one derivatives 发明人:PETERS DAN 权利人:NEUROSEARCH AS 摘要:This invention relates to novel chromen-2-one derivatives useful as starting material for synthesis of pharmaceuticals. On other aspects the invention relates to a method of preparing the chromen-2-one derivatives of the invention.
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.