CAS: 5381-99-7; 2-Chloro-4H-Benzo[d][1,3,2]Dioxaphosphinin-4-One

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1222-87-3 127164-51-6 137372-07-7

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CAS号69-72-7 水杨酸 | CAS号127-09-3 乙酸钠 | CAS号7719-12-2 三氯化磷 | CAS号140383-35-3 2-(diethylamino... | CAS号137073-23-5 2-(2,2,3,3-tetr... | CAS号137073-22-4 2-(2,2,2-triflu... | CAS号16540-40-2 (2-methylpropan... | CAS号117887-30-6 2-methoxy-1,3,2... | CAS号80337-06-0 2-oxo-1,3,2-ben... | CAS号6083-15-4 2-ethoxy-1,3,2-...

水杨酸置于三氯化磷体系中,用 甲苯 作为反应溶剂,化学反应生成 2-氯-1,3,2-苯并二氧磷杂环己烷-4-酮
参考文献:胸腺嘧啶和6-甲基尿嘧啶5'-磷酸化1,2,3-三唑基核苷类似物的合成,抗病毒评价,分子对接研究和细胞毒性
标题:胸腺嘧啶和6-甲基尿嘧啶5'-磷酸化1,2,3-三唑基核苷类似物的合成,抗病毒评价,分子对接研究和细胞毒性
摘要:大系列母体1,2,3-三唑基核苷对流感病毒a/pr/8/34 (H1N1)的体外抗病毒活性(以半最大抑制浓度ic 50 计)的比较分析类似物(以尿嘧啶,胸腺嘧啶,6-甲基尿嘧啶,喹唑啉-2,4-二酮部分作为核碱基)及其带有掩蔽的 5'-磷酸基团(磷酸二乙酯,磷酸二苯酯,氨基磷酸酯)和带负电荷的 H 的前药形式进行了-膦酸酯和单磷酸基团.所获得的结构-活性关系是基于以下假设进行解释的:合成的母体 1,2,3-三唑基核苷类似物及其前药形式,通过与文献数据类比,被细胞激酶代谢为其活性 5'-三磷酸形式,从而抑制病毒rna依赖性rna聚合酶(rdrp)的活性.发现ic 50的实验值与母体1,2,3-三唑基核苷类似物的5'-三磷酸衍生物在rdrp活性位点的结合能的理论值之间存在相关性. 图形概要
DOI:10.1007/s00044-023-03112-Z

专利信息

专利号:US-5204456-A
优先权日:1986-04-08
标题:Derivatives of nucleosides and their use for the synthesis of oligonucleotides
发明人：MOLKO DIDIER; SCHULHOF JEAN-CLAUDE; TEOULE ROBERT
权利人:COMMISSARIAT ENERGIE ATOMIQUE
摘要:The invention relates to derivatives of nucleosides and their use for the synthesis of oligonucleotides. These derivatives are in accordance with the formula: (I) in which B represents a radical derived from guanine, cytosine or adenine, whose exocylic NH group is protected by the group with R1 representing a hydrogen atom or a alkyl radical and R2 a hydrogen atom, and alkyl radical, an alkoxy radical and optionally substituted aryloxy radical, R3 represents a hydrogen atom, the dimethoxytrityl radical or the radical R4 represents a hydrogen atom, the radical of formula: or a radical suitable for the synthesis of polynucelotides and R5 represents a hydrogen atom or the protected or unprotected hydroxyl OH radical.

专利号:US-11059849-B2
优先权日:2014-09-02
标题 :Modified nucleotides for synthesis of nucleic acids, a kit containing such nucleotides and their use for the production of synthetic nucleic acid sequences or genes
发明人：YBERT THOMAS; GARIEL SYLVAIN
权利人:DNA SCRIPT
摘要:A modified nucleotide, intended for the synthesis of long chain nucleic acids by enzymatic processes, comprising a “naturalâ€? nitrogenous base or a natural nitrogenous base analogue, a ribose or deoxyribose carbohydrate, and at least one phosphate group, characterized in that said nucleotide comprises at least one R group, termed the modifier group, carried by said nitrogenous base or analogue and/or by the oxygen in position 3′ of the ribose or deoxyribose molecule, making it possible to block the polymerization of said nucleotide and/or to allow the interaction of said nucleotide with another molecule, such as a protein, during the nucleic acid synthesis, R comprising at least one functional terminal group.

专利号:US-2015376219-A1
优先权日:2014-06-30
标题 :Selective Preparations of Purine Nucleosides and Nucleotides: Reagents and Methods
发明人：ZHONG MINGHONG
权利人:ZHONG MINGHONG
摘要:A process of regiospecific synthesis of N-9 purine nucleoside analogs in either solution or solid phase synthesis is described. The introduction of the sugar moiety or its analogue on to a 6-heteroarylium purine or its mesomeric betaine so that formation of only the N-9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific introduction of the sugar moiety allows the synthesis of purine nucleoside analogs in high yields without formation of the N-7-positional regioisomers, while the 6-heteroaryliums are leaving groups facilitated for nucleophilic displacement. Solid supported 6-heterarylium purine bases can be used for purine based library synthesis and synthesis of nucleotide monophosphates and polyphosphates. Processes for providing novel 6-heteroarylium purines and their corresponding mesomeric betaines for the regiospecific synthesis of N-9 purine nucleoside analogs and nucleotides are described.

专利号:US-2025154546-A1
优先权日:2022-02-11
标题 :Use of 3'-oxymethylene alkyl disulfide protected nucleotides for enzymatic dna and rna synthesis
发明人：MARMA SANO MONG; SOLIMAN SAMEH; GUAN XIAO-PEI; PERBOST MICHEL; PINARD ROBERT
权利人:MILTENYI BIOTEC BV & CO KG
摘要:This invention is about enzymatic synthesis of nucleic acids using 3′-O—(CH2SSR) protected reversible nucleotide terminators. The nucleotide base of the protected nucleotide may consist of natural or non-natural (e.g. 7-de-aza G and 7-de-aza A), or mixture thereof. The base of the nucleotides can be modified with a linker carrying carboxylic acid (—CO2H). amine (—NH2), thiol (—SH). hydroxymethyl (—CH2OH), propargy lamine. alkyne group etc. for subsequent modification and labeling. Such nucleotide substrates can be incorporated into the single strand, template free nucleic acid or into the templated DNA hybrid. And in later step the 3′-O—CH2SSR protecting group can be cleaved off by chemical treatment pre-requisites for enzymatic nucleic acids synthesis. By adding nucleotide in pre-determined fashion and cleave reaction after each step. longer DNA strands can be synthesized in solution or on solid surface starting from a short seeding DNA strands.

专利号:US-5414077-A
优先权日:1990-02-20
标题 :Non-nucleoside linkers for convenient attachment of labels to oligonucleotides using standard synthetic methods
发明人：LIN KUEI-YING; MATTEUCCI MARK
权利人:GILEAD SCIENCES
摘要:Pseudonucleosides and pseudonucleotides are useful in the synthesis of oligomers which contain these components as a means to derivatize the resulting oligonucleotide to useful substituents such as chelators, intercalators, or lipophilic compounds. In general, these pseudonucleotide components are of the formula: (1) wherein each Y is independently O or S; each X is independently H, PO3-2, an activated nucleotide synthesis coupling moiety, a protecting group, a nucleoside, a nucleotide or a nucleotide sequence, or comprises a solid support; F is a functional group capable of linking an additional moiety or said group already reacted to effect the binding of said additional moiety; &squ& is an organic backbone which does not contain additional F or Y-X substituents and which is either achiral even when the Y-X substituents are different, or is a single enantiomer of a chiral compound; with the proviso that at least one X is a nucleoside, nucleotide, nucleotide sequence, an activated nucleotide synthesis coupling moiety, or comprises a solid support, or F represents said functional group already reacted with an additional group. Oligonucleotides having the pseudonucleoside at the 3' terminus are particularly stable in vivo.

专利号:US-2008221303-A1
优先权日:2004-02-18
标 题:Method for the Preparation of Peptide-Oligonucleotide Conjugates
发明人：KATZHENDLER JEHOSHUA; KLAUZNER YAKIR; BEYLIS IRENA; MIZHIRITSKII MICHAEL; SHPERNAT YAACOV; ASHKENAZI BORIS; FRIDLAND DMITRI
权利人:KATZHENDLER JEHOSHUA; KLAUZNER YAKIR; BEYLIS IRENA; MIZHIRITSKII MICHAEL; SHPERNAT YAACOV; ASHKENAZI BORIS; FRIDLAND DMITRI
摘要:The present invention relates to the synthesis of peptide-oligonucleotide conjugates (POC). More specifically, the invention relates to a novel method for the preparation of peptide-oligonucleotide conjugates, which can be conducted under mild conditions on solid support, can be performed manually or by a synthesizer, can be used to synthesize alternating sequences of peptides and oligonucleotides, and is applicable to the synthesis of a wide variety of peptide-oligonucleotide conjugates constructed from alternate peptide and oligonucleotide blocks.