CAS: 824-24-8; 4-Methyl-1H-Pyrrolo[2,3-B]Pyridine

该化合物是一种杂交有机化合物,其特点是结合了铁环系统中氮原子的内溶胶和结构,在铁环系统中含有氮原子,在球球球运动4位置上有一个甲基组,影响其化学反应和特性,该化合物一般在室内温度下是固体,在有机溶剂中表现出中等溶解性,其分子结构有助于其在药用化学中的潜在应用,特别是在制药方面,因为它能够与生物目标相互作用. 环状中的氮原子加强了其基本性,能够影响其电子特性,使其成为各种化学研究领域感兴趣的对象.此外,4-M乙基-7-azaintole可能参与各种化学反应,包括电药替代和核毒攻击,这在热循环化学中很常见.处理和储存任何化学物质时,都应参考安全数据.

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5654-93-3 344327-11-3 728034-12-6

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合成工艺路线路线简述

  • 14069-74-0 = 824-24-8
    反应条件:1.1 Reagents: Sodium Solvents: Methanol,Toluene
    标题:Synthesis Of Precursors And Fragments Of Antibiotics. Xii. The Condensation Of Organosilicon Compounds With Thioglycolic Acid And Its Ethyl Ester
    作者:Voronkina,T. M.; Et Al
    参考文献:Zhurnal Obshchei Khimii 日期:1964 卷标:34(5) 页码:1464-7]

    55052-28-3 = 824-24-8
    反应条件:1.1 Solvents: Diethyl Ether,Toluene; 30 °C; 3 H,80 °C; 80 °C -> 30 °C; Overnight,30 °C -> 0 °C
    标题:Discovery Of 3-Cyano-N-(3-(1-Isobutyrylpiperidin-4-Yl)-1-Methyl-4-(Trifluoromethyl)-1H-Pyrrolo[2,3-B]Pyridin-5-Yl)Benzamide: A Potent,Selective,And Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist
    作者:Schnute,Mark E.; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2018 卷标:61(23) 页码:10415-10439
📜甲基溴化镁,4-氯-7-氮杂吲哚置于(1,1'-Bis(Diphenylphosphino)Ferrocene)Palladium(II) Dichloride体系中,用 乙醚,甲苯 作为反应溶剂,化学反应 3.0H,以89%的收率获得产物4-甲基-7-氮杂吲哚
参考文献:3-氰基-N-(3-(1-异丁酰基哌啶-4-基)-1-甲基-4-(三氟甲基)-1 H-吡咯并[2,3-B]吡啶-5-基)苯甲酰胺的发现:有力,选择性和口服生物可用的视黄酸受体相关的孤儿受体c2反激动剂.
标题:3-氰基-N-(3-(1-异丁酰基哌啶-4-基)-1-甲基-4-(三氟甲基)-1 H-吡咯并[2,3-B]吡啶-5-基)苯甲酰胺的发现:有力,选择性和口服生物可用的视黄酸受体相关的孤儿受体c2反激动剂.
摘要:核激素受体视黄酸受体相关的孤儿c2(rorc2,也称为rorγt)是治疗自身免疫性疾病的有希望的靶标.预期该受体的小分子反向激动剂会减少关键的促炎细胞因子il-17的产生.通过高通量筛选方法,我们鉴定了一种分子,该分子显示出对rorc2的有希望的结合亲和力,抑制th17细胞中il-17的产生以及对相关rora和rorb受体同工型的选择性.铅优化以提高这种命中的效力和代谢稳定性为重点,主要集中在两个关键设计策略上,即,通过提高亲脂性效率和结构指导的构象限制驱动的迭代优化,以实现最佳的基态能量学和最大化受体停留时间.n-(3-(1-异丁酰基哌啶-4-基)-1-甲基-4-(三氟甲基)-1 H-吡咯并[2,3-B]吡啶-5-基)苯甲酰胺为强效且选择性的rorc2逆激动剂,在临床前体内动物模型中,口服给药后表现出非常好的代谢稳定性,口服生物利用度以及降低il-17水平和皮肤炎症的能力.
DOI:10.1021/acs.Jmedchem.8B00392

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专利信息


专利号:US-10000487-B2
优先权日:2015-11-20
标 题 :Heterocyclic compounds that inhibit the kinase activity of Mnk useful for treating various cancers
发明人：SPRENGELER PAUL A; REICH SEIGFRIED H; WEBBER STEPHEN E; ERNST JUSTIN T
权利人:EFFECTOR THERAPEUTICS INC
摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula IA or Formula IB, as well as stereoisomers, tautomers or pharmaceutically acceptable salts thereof. n nFor Formula IA and Formula IB compounds A 1 , A 2 , A 3 , A 4 , W 1 , W 2 , Y, X, R 1 , R 2 , R 3 , R 4a , R 4b , R 5a , R 5b , R 6 , R 7 , R 8 , R 9 , R 9a , R 9b , R 10 and subscript n are as defined in the specification. The inventive Formula IA and Formula IB compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.

专利号:US-12415804-B2
优先权日:2023-06-28
标题 :Compounds for activating a serotonin receptor
发明人：BANISTER SAMUEL; JORGENSEN WILLIAM; TAN JINLONG; WHISH LACHLAN
权利人:Psylo Pty Ltd
摘要:The present disclosure relates generally to compounds, their methods of synthesis, and their use in the treatment of mental illness or central nervous system disorders.

专利号:US-2025163044-A1
优先权日:2021-12-24
标 题:Compounds
发明人：BANISTER SAMUEL; JORGENSEN WILLAM; TAN JINLONG
权利人:Psylo Pty Ltd
摘要:The present disclosure relates generally to compounds, their methods of synthesis, and their use in the treatment of mental illness or central nervous system disorders.

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合成参考文献


摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 203.
摘要:A. Albert and R.E. Willette. J. Chem. Soc. 1964, 4063.
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