2-叠氮喹啉 | 75275-88-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 2-叠氮喹啉
• 英文名称: 2-azidoquinoline
• 英文别名: Azidoquinoline
• CAS: 75275-88-6
• 化学式: C₉H₆N₄
• 分子量: 170.173
• InChiKey: KXQOKGMTRJVFJL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  27.2
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-叠氮喹啉 生成 4-氰基吲哚
  参考文献：
  名称：

  Isolation of diazacycloheptatetraenes from thermal nitrene-nitrene rearrangements

  摘要：

  DOI：

  10.1021/ja00539a039
• 作为产物：
  描述：

  2-氯喹啉 在 1-butyl-3-methylimidazolium azide 作用下， 以 1,4-二氧六环 为溶剂， 反应 72.0h， 以51.8%的产率得到2-叠氮喹啉
  参考文献：
  名称：

  Ionic Liquids/[bmim][N₃] Mixtures: Promising Media for the Synthesis of Aryl Azides by S_NAr

  摘要：

  The nucleophilic aromatic substitution of some activated aryl or heteroaryl halides has been performed in ionic liquid solution, using the 1-butyl-3-methylimidazolium azide as a nucleophile. The reaction course was studied varying the structures of both substrates and ionic liquids. In particular, in the latter case, the reaction of 2-bromo-5-nitrothiophene was carried out in five different ionic liquids ([bmim][BF4], [bmim] [PF6], [bmim] [NTf2], [bm(2)im] [NTf2], and [bmpyrr] [NTf2]). Finally, for all the substrates considered, a comparison with data obtained in MeOH solution in the presence of NaN3 was also performed. Data collected indicate that in some cases it is possible to obtain aromatic or heteroaromatic azide derivatives in satisfactory yield by means of a SNAr reaction using [bmim][N-3] as the nucleophile.

  DOI：

  10.1021/jo800676d

文献信息

• Discovery of novel 1,4-disubstituted 1,2,3-triazole phenylalanine derivatives as HIV-1 capsid inhibitors
  作者：Xiangyi Jiang、Gaochan Wu、Waleed A. Zalloum、Megan E. Meuser、Alexej Dick、Lin Sun、Chin-Ho Chen、Dongwei Kang、Lanlan Jing、Ruifang Jia、Simon Cocklin、Kuo-Hsiung Lee、Xinyong Liu、Peng Zhan

  DOI：10.1039/c9ra05869a

  日期：——

  drugs. Accordingly, in this research, we report the design, synthesis and biological evaluation of a series of novel phenylalanine derivatives as HIV-1 CA protein inhibitors using the Cu(I)-catalyzed azide and alkyne 1,3-dipolar cycloaddition (CuAAC) reaction. Among this series of inhibitors, compound II-10c displayed a remarkable anti-HIV activity (EC50 = 2.13 μM, CC50 > 35.49 μM). Furthermore, surface

  HIV-1 衣壳 (CA) 蛋白在病毒生命周期的早期和晚期都发挥着至关重要的作用，这引起了研究人员的兴趣，将其作为开发抗 HIV 药物的目标。因此，在这项研究中，我们报告了一系列新型苯丙氨酸衍生物作为 HIV-1 CA 蛋白抑制剂的设计、合成和生物学评估，这些衍生物使用 Cu(I) 催化的叠氮化物和炔烃 1,3-偶极环加成 (CuAAC) 反应. 在这一系列抑制剂中，化合物 II-10c 表现出显着的抗 HIV 活性（EC50 = 2.13 μM，CC50 > 35.49 μM）。此外，表面等离子共振 (SPR) 结合试验表明化合物 II-10c 和 PF-74（先导化合物）与 HIV-1 CA 单体具有相似的亲和力。进一步研究表明，代表性化合物的弱渗透性和水溶性可能是限制其细胞活性的重要因素。根据这些化合物的活性及其已知结构推断出初步的构效关系 (SAR)。通过分子动力学模拟 (MD)
• [EN] METHODS OF MODULATING CFTR ACTIVITY<br/>[FR] PROCÉDÉS DE MODULATION DE L'ACTIVITÉ DE CFTR
  申请人：PROTEOSTASIS THERAPEUTICS INC

  公开号：WO2014210159A1

  公开（公告）日：2014-12-31

  The invention encompasses methods of modulating CFTR activity in a subject in need thereof comprising administering an effective amount of a compound of Formula (I). The invention also encompasses methods of treating a condition associated with CFTR activity or condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a compound of Formula (I).

  这项发明涵盖了在需要的受试者中调节CFTR活性的方法，包括向受试者施用化合物Formula (I)的有效量。该发明还涵盖了治疗与CFTR活性相关的疾病或与蛋白质稳态功能障碍相关的疾病的方法，包括向受试者施用化合物Formula (I)的有效量。
• Alkylsulphonamide Quinolines
  申请人：Albert Jeffrey

  公开号：US20080293765A1

  公开（公告）日：2008-11-27

  Compounds of Formula I wherein R 1 , A, R 2 , R 3 , R 4 , R 5 , R 8 , n, m, q and r are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

  式I中的化合物，其中R1、A、R2、R3、R4、R5、R8、n、m、q和r如规范中所述，药用盐，制备方法，含有该化合物的药物组合物，以及使用该化合物的方法。
• METHODS OF MODULATING CFTR ACTIVITY
  申请人：PROTEOSTASIS THERAPEUTICS, INC.

  公开号：US20160151335A1

  公开（公告）日：2016-06-02

  The invention encompasses methods of modulating CFTR activity in a subject in need thereof comprising administering an effective amount of a compound of Formula (I). The invention also encompasses methods of treating a condition associated with CFTR activity or condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a compound of Formula (I).

  本发明涵盖了调节需要的受体内CFTR活性的方法，包括给予公式（I）化合物的有效量。本发明还涵盖了治疗与CFTR活性相关的病症或与蛋白质稳态失调相关的病症的方法，包括给予受体公式（I）化合物的有效量。
• Positive type photoresist composition
  申请人：NIPPON OIL COMPANY, LIMITED

  公开号：EP0471326A1

  公开（公告）日：1992-02-19

  A positive type photoresist composition contains (a) 100 parts by weight of a resin which is a polymer compound (A) including carbon-carbon double bonds and having a molecular weight of 300 to 30,000 and an iodine value of 50 to 500. To at least a part of the double bonds of the polymer compound (A), a group represented by the formula (I) is introduced wherein R¹ denotes a hydrogen atom, a halogen atom or an alkyl group having 1 to 3 carbon atoms and R² denotes an alkyl group having 1 to 10 carbon atoms, a cycloalkyl group or an aryl group. The composition further contains (b) 25 to 100 parts by weight of a compound containing a quinone diazide unit.

  一种正型光刻胶组合物含有 (a) 100 重量份的树脂，它是一种聚合物化合物 (A)，包括碳碳双键，分子量为 300 至 30000，碘值为 50 至 500。在聚合物化合物 (A) 的至少部分双键上引入由式 (I) 代表的基团 其中 R¹ 表示氢原子、卤素原子或具有 1 至 3 个碳原子的烷基，R² 表示具有 1 至 10 个碳原子的烷基、环烷基或芳基。该组合物还含有(b) 25 至 100 重量份的含有重氮化醌单元的化合物。