CAS: 69123-94-0; 1-((2R,3S,4R,5R)-3-Fluoro-4-Hydroxy-5-(Hydroxymethyl)Tetrahydrofuran-2-yl)Pyrimidine-2,4(1H,3H)-Dione

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CAS号66-22-8 尿嘧啶 | CAS号122757-52-2 1-[(2R,5S)-3-Fl...

非阿尿苷置于palladium On Activated Charcoal 氢气,三乙胺体系中,用 甲醇,水 作为反应溶剂,化学反应 18.0H,以90.3%的收率获得产物1-(2-脱氧-2-氟-Beta-D-阿拉伯呋喃基)尿嘧啶
参考文献:几种含2'-氟嘧啶核苷的合成及其抗hiv活性.
标题:几种含2'-氟嘧啶核苷的合成及其抗hiv活性.
摘要:报道了几种2'-氟阿拉伯糖-2',3'-二脱氧-和2'-氟-2',3'-不饱和的2',3'-二脱氧嘧啶核苷类似物.饱和的类似物1-(2,3-二脱氧-2-氟-β-D-苏-五氟呋喃糖基)胸腺嘧啶(2'-Threo-Fddt,33),1-(2,3-二脱氧-2-氟-β-胸腺嘧啶通过相应的2'-脱氧-2'-氟阿拉伯糖基核苷类似物,通过3'-Oh的自由基脱氧,可以轻松制备-D-苏-五氟呋喃糖基)尿嘧啶(2'-苏-Fddu,22).不饱和化合物1-(2,3-二脱氧-2-氟-β-D-甘油-戊-2-烯呋喃糖基)胸腺嘧啶(2'-Fd4T,40)和1-[5-O-(单甲氧基三苯甲基)通过o-2,3'-脱水-2'-氟代-的消除反应,合成了-2-氟-2,3-二脱氧-β-D-甘油-Pen T-2--呋喃糖基]尿嘧啶(39). Lyxo衍生物在基本条件下.胞苷类似物28和41是通过氨基化相应的尿苷衍生物制备的;使化合物28和41脱保护,得到1-(2
DOI:10.1021/jm00170A017

专利信息

专利号:US-8912319-B2
优先权日:2010-07-15
标 题 :Synthesis of 2′-deoxy-2′-[18F]fluoro-5-methyl-1-B-D-arabinofuranosyluracil (18F-FMAU)
发明人：LI ZIBO; CAI HANCHENG; CONTI PETER S
权利人:LI ZIBO; CAI HANCHENG; CONTI PETER S; UNIV SOUTHERN CALIFORNIA
摘要:The present invention relates to methods of synthesizing 18 F-FMAU. In particular, 18 F-FMAU is synthesized using one-pot reaction conditions in the presence of Friedel-Crafts catalysts. The one-pot reaction conditions are incorporated into a fully automated cGMP-compliant radiosynthesis module, which results in a reduction in synthesis time and simplifies reaction conditions. The one-pot reaction conditions are also suitable for the production of 5-substituted thymidine or cytidine analogs. The products from the one-pot reaction (e.g. the labeled thymidine or cytidine analogs) can be used as probes for imaging tumor proliferative activity. More specifically, these [ 18 F]-labeled thymidine or cytidine analogs can be used as a PET tracer for certain medical conditions, including, but not limited to, cancer disease, autoimmunity inflammation, and bone marrow transplant.

专利号:US-2023416293-A1
优先权日:2020-11-23
标 题:Synthesis of [18f]-labeled thymidine analogues
发明人：CHEN KAI; CONTI PETER S
权利人:UNIV SOUTHERN CALIFORNIA
摘要:Thymidine analogues, 5-substituted 2′-deoxy-2′-[18F]fluoro-arabinofuranosyluracil derivatives, are promising positron emission tomography (PET) tracers being evaluated for noninvasively imaging cancer cell proliferation and/or reporter gene expression. We report the radiosynthesis of 2′-deoxy-2′-[18F]fluoro-5-methyl-1-β-d-arabinofuranosyluracil ([18F]FMAU) and other 2′-deoxy-2′-[18F]fluoro-5-substituted-1-β-d-arabinofuranosyluracil analogues using 1,4-dioxane to replace the currently used 1,2-dichloroethane. Compared to 1,2-dichloroethane, 1,4-dioxane is analyzed as a better solvent in terms of radiosynthetic yield and toxicity concern. The use of a less toxic solvent allows for the translation of the improved approach to clinical production. The new radiolabeling method can be applied to an extensive range of uses for 18F-labeling of other nucleoside analogues.

专利号:US-9422321-B2
优先权日:2010-09-07
标题 :Pyrimidine nucleoside derivatives, synthesis methods and uses thereof for preparing anti-tumor and anti-virus medicaments
发明人：CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE
权利人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE; HIGH & NEW TECH RES CENTER HENAN ACAD OF SCIENCES; ZHENGZHOU GRANLEN PHARMATECH LTD; UNIV ZHENGZHOU
摘要:The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, particularly compounds of the formula shown below: n nAlso disclosed are methods of preparation and uses for these compounds. The compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.

专利号:WO-2025215034-A1
优先权日:2024-04-10
标 题 :Synthesis and application of magnetic particle conjugates for the extracorporeal removal of antibodies targeting viral vectors to facilitate gene therapy
发明人：LANGENEGGER LUKAS; MORA CARLOS; RIJSBERGEN LAURINE; BENZ SEBASTIAN; KELLER SARAH
权利人:HEMOTUNE AG
摘要:The present invention provides novel conjugates comprising a magnetic particle and a multitude of viral structures covalently bound to said particle. These conjugates are suited for efficient extracorporeal removal of antibodies from blood. In particular, the conjugates are suited as adjuvant treatment in gene therapy.

专利号:US-2009298708-A1
优先权日:2006-08-23
标题 :2'-deoxy-2'-fluoro-beta-d-arabinonucleoside 5'-triphosphates and their use in enzymatic nucleic acid synthesis
发明人：MASAD DAMHA J; GENG PENG CHANG
权利人:MASAD DAMHA J; GENG PENG CHANG
摘要:The invention relates to arabinose modified nucleoside 5′ triphosphates and to the biosynthesis and amplification of oligonucleotides containing and/or from templates containing arabinose modified nucleosides. The invention further relates to methods of generating modified oligonucleotide libraries for use in selection strategies, such as SELEX. The arabinose modified oligonucleotides of the invention are useful for modulating target nucleic acid expression, such as RNA.

专利号:CA-2804823-A1
优先权日:2010-07-15
标题:Synthesis of 2'-deoxy-2'-[18f]fluoro-5-methyl-1-b-d-arabinofuranosyluracil (18f-fmau)