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4-amino-6-hydroxy-5-(2,2-diethoxyethyl)pyrimidine 6-amino-5-(2,2-diethoxy)-2-mercaptopyrimidine-4-ol 2-thioxo-1,2,3,7-tetrahydro-4H-pyrrolo[2,3-d]pyrimidin-4-one ethyl 2-cyano-4,4-diethoxybutyratepyrimidin-4-thion3,7-Dihydro-4H-pyrrolo2,3-dpyrimidin-4-thion 4-chloro-1H-pyrrolo[2,3-d]pyrimidine 7-deazaxanthine 合成工艺路线路线简述
- 合成目标产物 Pyrrolo[2,3-D]Pyrimidin-4-Ol 主要起始原料 6-Amino-5-(2,2-Diethoxyethyl)Pyrimidin-4-Ol
- (文献来源)合成步骤主要原料 6-Amino-5-(2,2-Diethoxyethyl)Pyrimidin-4-Ol
6-Amino-5-(2,2-Dimethoxyethyl)Pyrimidin-4-Ol置于盐酸体系中,用 水 作为反应溶剂,以64 G的收率获得产物4-羟基吡咯并[2,3-D]嘧啶
参考文献: Method Of Manufacturing 4-Chloro-7H-Pyrrolo[2,3-D]Pyrimidine[fr] Procédé De Fabrication De 4-Chloro-7 H-Pyrrolo [2,3-D] Pyrimidine
标题: Method Of Manufacturing 4-Chloro-7H-Pyrrolo[2,3-D]Pyrimidine[fr] Procédé De Fabrication De 4-Chloro-7 H-Pyrrolo [2,3-D] Pyrimidine
摘要:本发明公开了一种制备4-氯-7H-吡咯并[2,3-D]嘧啶的方法,包括以下步骤:A)通过将乙酸乙酯和2-溴-1,1-二甲氧基乙烷偶联来制备乙基2-氰基-4,4-二甲氧基丁酸酯;b)通过将甲酰胺基加入乙基2-氰基-4,4-二甲氧基丁酸酯来制备6-氨基-5-(2,2-二甲氧基乙基)嘧啶-4-醇;c)将6-氨基-5-(2,2-二甲氧基乙基)嘧啶-4-醇转化为7H-吡咯并[2,3-D]嘧啶-4-醇;和d)将7H-吡咯并[2,3-D]嘧啶-4-醇转化为4-氯-7H-吡咯并[2,3-D]嘧啶.与已知的技术水平相比,该方法提供了更高的产量,更少的副产物和减少废物.
专利信息
专利号:US-5235053-A
优先权日:1992-06-22
标题 :Process for the synthesis of 4-hydroxy-5-halopyrrold[2,3-d]pyrimidine intermediates
发明人:BARNETT CHARLES J; KOBIERSKI MICHAEL E
权利人:LILLY CO ELI
摘要:4-Hydroxypyrrolo[2,3-d]pyrimidines are regiospecifically halogenated at the C-5 position by silylation in the presence of an inert organic solvent and iodination, bromination or chlorination.
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-10233182-B2
优先权日:2014-04-04
标题 :Substituted spirocyclic inhibitors of autotaxin
发明人:BABISS LEE; CLARK MATTHEW; KEEFE ANTHONY D; MULVIHILL MARK J; NI HAIHONG; RENZETTI LOUIS; RUEBSAM FRANK; WANG CE; XIE ZHIFENG; ZHANG YING
权利人:X RX INC
摘要:The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancer, lymphocyte homing, chronic inflammation, neuropathic pain, fibrotic diseases, thrombosis, and cholestatic pruritus, mediated at least in part by ATX.
专利号:US-6855503-B2
优先权日:2002-12-20
标题 :Heterocyclic FRETdye cassettes for labeling biological molecules and their use in DNA sequencing
发明人:NAMPALLI SATYAM; ZHANG WEIHONG; RAO SUDHAKAR; KUMAR SHIV
权利人:AMERSHAM BIOSCIENCES CORP
摘要:Exploitation of suitably functionalized heterocyclic molecules, in the design and synthesis of Fluorescence Resonance Energy Transfer (FRET) cassettes and their corresponding dideoxynucleotide terminators culminated into efficient reagents for DNA sequencing. Additionally, these FRET cassettes/terminators, of the present invention, derived from different classes of heterocyclic systems have high potential to be used for general labelling of biological molecules to generate highly sensitized signals. Their preparation, energy transfer efficiency, and use as labels, specifically, in DNA sequencing reactions is disclosed.
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-9351974-B2
优先权日:2011-11-10
标题 :Substituted pteridinones for the treatment of cancer
发明人:JIN MEIZHONG; KADALBAJOO MRIDULA; LI AN-HU; MULVIHILL MARK J; SIU KAM W; STEINIG ARNO G; WANG JING
权利人:OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula I, as shown below and defined herein: n npharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention.