CAS: 92276-38-5; 6-Bromo-3H-[1,2,3]Triazolo[4,5-B]Pyridine

该化合物是具有溴化三氮基核心的七环化合物,是医学化学和有机合成的多用途中间体,其溴替代物可增强反应性,使诸如Suzuki或Buchwald-Hartwig的高效交叉反应对构建复杂的分子结构至关重要.结合的三硝基-丙烯结构具有稳定性和潜在的生物活性,在药物研究中具有价值,特别是对于开发动脉抑制剂或其他生物活性化合物而言.高纯度和定义明确的再活动可确保合成应用中的再生性.这一化合物对于研究人员探索结构-活性关系或修改基于三氮的丁基草药特别有用.

结构式图片

相似化合物

273-34-7 1257554-00-9 408314-14-7

欧盟法规

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上下游产品

5-bromo-pyridine-2,3-diamine 5-bromo-3-nitro-pyridin-2-ylamine 6-bromo-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-[1,2,3]triazolo[4,5-b]pyridine

合成工艺路线路线简述

  • 38875-53-5 = 92276-38-5
    反应条件:1.1 Reagents: Acetic Acid,Sodium Nitrite; 1 H,Rt
    标题:Rational Design Of Original Fused-Cycle Selective Inhibitors Of Tryptophan 2,3-Dioxygenase
    作者:Kozlova,Arina; Thabault,Leopold; Liberelle,Maxime; Klaessens,Simon; Prevost,Julien R. C.; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2021 卷标:64(15) 页码:10967-10980]

    38875-53-5 = 92276-38-5
    反应条件:1.1 Reagents: Sulfuric Acid Solvents: Water; Heated; 0 °C1.2 Reagents: Sodium Nitrite Solvents: Water; Overnight,Rt
    标题:Synthesis,Biological Properties And Structural Study Of New Halogenated Azolo[4,5-B]Pyridines As Inhibitors Of Ck2 Kinase
    作者:Chojnacki,K.; Lindenblatt,D.; Winska,P.; Wielechowska,M.; Toelzer,C.; Et Al
    参考文献:Bioorganic Chemistry 日期:2021 卷标:106
📜2-氨基-5-溴-3-硝基吡啶置于盐酸,硫酸,Tin(Ll) Chloride体系中,用 水 作为反应溶剂,化学反应生成 6-溴-1H-1,2,3-三唑[4,5-B]吡啶
参考文献:新型卤代偶氮[4,5-B]吡啶作为ck2激酶抑制剂的合成,生物学特性和结构研究
标题:新型卤代偶氮[4,5-B]吡啶作为ck2激酶抑制剂的合成,生物学特性和结构研究
摘要:新的卤代 1 H-三唑并[4,5-B]吡啶和 1 H-咪唑并[4,5-B]吡啶作为已知 Ck2 抑制剂的类似物合成:4,5,6,7-四溴-1 H-苯并三唑 (Tbbt) 和 4,5,6,7-四溴-1 H-苯并咪唑 (Tbbi).确定了它们对重组人 Ck2α,Ck2α' 和 Pim1 激酶活性的影响.最有效的抑制剂是二卤代和三卤代 1 H-三唑并[4,5-B]吡啶(4A,5A和10A),Ic为 50Ck2α 的值分别为 2.56,3.82 和 3.26 μm.此外,评估了所有最终化合物对癌细胞系 Mcf-7(人乳腺癌)和 Ccrf-Cem(t 淋巴母细胞白血病)活力的影响.最后,获得了ck2α 1-335与抑制剂4A,5A和10A复合物的三种晶体结构.此外,新方案用于获得与四种抑制剂(4A,5A,5B,10A)复合的 Ck2α' Cys336Ser的高分辨率晶体结构.
DOI:10.1016/j.Bioorg.2020.104502

海关参考信息

专利信息


专利号:WO-2024233563-A1
优先权日:2023-05-09
标 题:6,6-fused bicyclic amides and compositions for use as 15-prostaglandin dehydrogenase modulators
发明人:GREENMAN KEVIN LLOYD; WANG HUI-LING; WEIRES NICHOLAS ANTHONY; ALLEN JOHN G; AMEGADZIE ALBERT K; BOURBEAU MATTHEW P; LI KEXUE
权利人:AMGEN INC
摘要:The present disclosure provides novel 15-hydroxy-prostaglandin dehydrogenase inhibitors, pharmaceutical compositions comprising such compounds, and methods of using such compounds and compositions in treating 15-hydroxy-prostaglandin dehydrogenase-mediated disease. Also provided are methods of making such compounds and intermediates thereof. The compounds have a structure of Formula (I): or a pharmaceutically acceptable salt thereof; wherein is Formula (i) or Formula (ii) Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).

专利号:US-2024409557-A1
优先权日:2023-05-09
标 题 :5,6-fused and 6,6-fused bicyclic alcohols and ethers and compositions for use as 15-prostaglandin dehydrogenase modulators
发明人:GREENMAN KEVIN LLOYD; PICKRELL ALEXANDER J; LI KEXUE; AMEGADZIE ALBERT K; WANG HUI-LING; WEIRES NICHOLAS ANTHONY; ALLEN JOHN G; BOURBEAU MATTHEW P
权利人:AMGEN INC
摘要:The present disclosure provides novel 15-hydroxy-prostaglandin dehydrogenase inhibitors, pharmaceutical compositions comprising such compounds, and methods of using such compounds and compositions in treating 15-hydroxy-prostaglandin dehydrogenase-mediated disease. Also provided are methods of making such compounds and intermediates thereof. The compounds have a general Formula (A).Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (A).

专利号:US-9751874-B2
优先权日:2014-12-17
标题:Hydroxy containing FXR (NR1H4) modulating compounds
发明人:GEGE CHRISTIAN; KINZEL OLAF; KREMOSER CLAUS; SCHMITT AARON C
权利人:GILEAD SCIENCES INC
摘要:The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

供应商参考报价(招募中)

品牌试剂参考报价(招募中)

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

主要参考文献

参考标题: Hydroxy Containing Fxr (Nr1H4) Modulating Compounds Composés Modulateurs De Fxr (Nr1H4) Contenant Des Grouhydroxy
摘要:The Present Invention Relates To Compounds (1) Which Bind To The Nr1 H4 Receptor (Fxr) And Act As Agonists Of Fxr. The Invention Further Relates To The Use Of The Compounds (1) For The Preparation Of A Medicament For The Treatment Of Diseases And/or Conditions Through Binding Of Said Nuclear Receptor By Said Compounds And To A Process For The Synthesis Of Said Compounds.

合成参考文献


参考文献:10.1021/acs.jmedchem.2c00951
摘要:Dammann M, Stahlecker J, Zimmermann MO, Klett T, Rotzinger K, Kramer M, Coles M, Stehle T, Boeckler FM. Screening of a Halogen-Enriched Fragment Library Leads to Unconventional Binding Modes. J Med Chem. 2022 Nov 10;65(21):14539–52. doi: 10.1021/acs.jmedchem.2c00951.
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