4-(4-azidophenyl)morpholine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 4-(4-azidophenyl)morpholine
• 英文别名: 4-morpholinophenyl azide；4-(4-azido-phenyl)-morpholine；4-Morpholino-phenyl-azid
• 化学式: C₁₀H₁₂N₄O
• 分子量: 204.231
• InChiKey: DOXPTTBJQKIAQV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  26.8
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-氯-4-(2-丙炔-1-基氧基)苯 、 4-(4-azidophenyl)morpholine 在 copper(ll) sulfate pentahydrate 、 sodium ascorbate 作用下， 以 水 、 叔丁醇 为溶剂， 以87%的产率得到4-(4-(4-((4-chlorophenoxy)methyl)-1H-1,2,3-triazol-1-yl)phenyl)morpholine
  参考文献：
  名称：

  Prasad, Davinder; Aggarwal, Nisha; Kumar, Rajesh, Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 2012, vol. 51, # 5, p. 731 - 738

  摘要：

  DOI：
• 作为产物：
  描述：

  4-(4-硝基苯基)吗啉 在 盐酸 、 tin(II) chloride dihdyrate 、 sodium nitrite 作用下， 以 水 为溶剂， 反应 0.33h， 生成 4-(4-azidophenyl)morpholine
  参考文献：
  名称：

  Prasad, Davinder; Aggarwal, Nisha; Kumar, Rajesh, Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 2012, vol. 51, # 5, p. 731 - 738

  摘要：

  DOI：

文献信息

• Syntheses and biological evaluation of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib
  作者：Yong-Tao Li、Jing-Han Wang、Cheng-Wen Pan、Fan-Fei Meng、Xiao-Qian Chu、Ya-hui Ding、Wen-Zheng Qu、Hui-ying Li、Cheng Yang、Quan Zhang、Cui-Gai Bai、Yue Chen

  DOI：10.1016/j.bmcl.2016.01.068

  日期：2016.3

  Three novel series of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib were prepared and evaluated in vitro for their cytostatic effects against a human chronic myeloid leukemia (K562), acute myeloid leukemia (HL60), and human leukemia stem-like cell line (KG1a). The structure–activity relationship was analyzed by determining the inhibitory rate of each imatinib analog. Benzene and piperazine

  制备了伊马替尼的三个新系列的1,2,3-三唑和1,3,4-恶二唑衍生物，并在体外评估了它们对人慢性髓性白血病（K562），急性髓性白血病（HL60）和人白血病干样细胞系（KG1a）。通过确定每种伊马替尼类似物的抑制率来分析结构与活性之间的关系。苯和哌嗪环是这些化合物中维持对K562和HL60细胞系抑制活性所必需的基团。引入三氟甲基基团显着增强了化合物对这两种细胞系的效力。出人意料的是，某些化合物对KG1a细胞显示出显着的抑制活性，而没有抑制常见的白血病细胞系（K562和HL60）。
• Identification of a novel NAMPT inhibitor by combinatorial click chemistry and chemical refinement
  作者：S. Theeramunkong、U. Galli、A. A. Grolla、A. Caldarelli、C. Travelli、A. Massarotti、M. P. Troiani、M. A. Alisi、G. Orsomando、A. A. Genazzani、G. C. Tron

  DOI：10.1039/c5md00261c

  日期：——

  The identification of compounds able to inhibit the NAD salvage pathway is experiencing a growing popularity as it has been proposed to be a novel target for antitumoral and anti-inflammatory drugs.

  化合物的鉴定能够抑制NAD回收途径，正变得越来越受欢迎，因为它被提议作为抗肿瘤和抗炎药物的新靶点。
• [EN] QUINOLIN-2-ONE DERIVATIVES<br/>[FR] DÉRIVÉS DE QUINOLIN-2-ONE
  申请人：MERCK PATENT GMBH

  公开号：WO2017121444A1

  公开（公告）日：2017-07-20

  Compounds of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, Q and Y have the meanings indicated in Claim 1, are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.

  式(I)中X1、X2、X3、X4、R1、R2、R3、Q和Y的含义如权利要求书中所示，是c-Kit激酶的抑制剂，可用于癌症的治疗。
• Aryl Azides as Forgotten Electrophiles in the Van Leusen Reaction: A Multicomponent Transformation Affording 4-Tosyl-1-arylimidazoles
  作者：Cristiana Necardo、Antonella Ilenia Alfano、Erika Del Grosso、Sveva Pelliccia、Ubaldina Galli、Ettore Novellino、Fiorella Meneghetti、Mariateresa Giustiniano、Gian Cesare Tron

  DOI：10.1021/acs.joc.9b02546

  日期：2019.12.20

  Considering aryl azides as electrophilic partners for the TosMIC mediated Van Leusen reaction, a novel multicomponent synthesis of 4-tosyl-1-arylimidazoles is reported. In this transformation, two molecules of TosMIC participate in the reaction mechanism in two different ways, with the second molecule undergoing a novel type of fragmentation resulting in the incorporation of a C-H into the final product

  考虑到芳基叠氮化物是TosMIC介导的Van Leusen反应的亲电分子，据报道，有一种新颖的多组分合成4-tosyl-1-arylimidazoles的方法。在此转化中，两个TosMIC分子以两种不同的方式参与反应机理，第二个分子经历了新型的断裂，导致CH结合到最终产物中。
• Further enhancement of the clickability of doubly sterically-hindered aryl azides by <i>para</i>-amino substitution
  作者：Suguru Yoshida、Junko Tanaka、Yoshitake Nishiyama、Yuki Hazama、Takeshi Matsushita、Takamitsu Hosoya

  DOI：10.1039/c8cc05791e

  日期：——

  Introduction of an amino group at the para position of doubly sterically-hindered aryl azides significantly enhances the reactivity with cyclooctynes. The distortability of the azido group is synergistically enhanced by the para-electron-donating group and two bulky ortho substituents, which increases the HOMO energy level and provoke the steric inhibition of resonance, respectively.

  在双空间受阻的芳基叠氮化物的对位引入氨基显着增强了与环辛炔的反应性。对位给电子基团和两个庞大的邻位取代基协同增强叠氮基团的可扭曲性，这分别增加了HOMO的能级并引起了共振的空间抑制。