1,2-Dibenzyloxy-4-nitrobenzol | 28387-13-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1,2-Dibenzyloxy-4-nitrobenzol
• 英文别名: 1,2-Bis(benzyloxy)-4-nitrobenzene；4-nitro-1,2-bis(phenylmethoxy)benzene
• CAS: 28387-13-5
• 化学式: C₂₀H₁₇NO₄
• 分子量: 335.359
• InChiKey: ZWEVOPCBFNUSMD-UHFFFAOYSA-N

物化性质

• 熔点：
  97 °C
• 沸点：
  512.1±40.0 °C(Predicted)
• 密度：
  1.238±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  25
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  64.3
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1,2-Dibenzyloxy-4-nitrobenzol 在 盐酸 、 溶剂黄146 作用下， 生成 4-硝基儿茶酚
  参考文献：
  名称：

  437. 1：2：3：4-四羟基苯的衍生物。第二部分

  摘要：

  DOI：

  10.1039/jr9320002876
• 作为产物：
  描述：

  4-硝基儿茶酚 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 1,2-Dibenzyloxy-4-nitrobenzol
  参考文献：
  名称：

  New non peptidic C5a receptor antagonists

  摘要：

  A series of phenylguanidines which bind to the C5a receptor has been developed. The lead compound 1 (IC50=30 mu M), discovered through random screening, has been modified to provide 32 (RPR121154) with submicromolar activity. This compound was shown to further elicit functional antagonism in a human neutrophil C5a stimulated respiratory burst assay. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0960-894x(97)00124-8

文献信息

• [EN] SUBSTITUTED N-ARYL BENZAMIDES AND RELATED COMPOUNDS FOR TREATMENT OF AMYLOID DISEASES AND SYNUCLEINOPATHIES<br/>[FR] N-BENZAMIDES D'ARYLE SUBSTITUÉS ET COMPOSÉS LIÉS POUR TRAITEMENT DES MALADIES AMYLOÏDES ET DES SYNUCLÉINOPATHIES
  申请人：PROTEOTECH INC

  公开号：WO2005113489A1

  公开（公告）日：2005-12-01

  Substituted diaryl compounds of the Formulae (I, II, III), where the variables are as defined in the claims, and their pharmaceutically acceptable derivatives, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including Aß amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment are provided.

  根据权利要求中定义的变量，提供了公式（I，II，III）的取代二芳基化合物及其药学上可接受的衍生物，它们的合成，含有它们的药物组合物，以及它们在治疗淀粉样疾病中的用途，包括阿尔茨海默病中观察到的Aß淀粉样病变，如2型糖尿病中观察到的IAPP淀粉样病变，以及在帕金森病中观察到的α-突触核病变，并提供了用于制造这种治疗药物的方法。
• Synthesis and evaluation of azalamellarin N and its A-ring-modified analogues as non-covalent inhibitors of the EGFR T790M/L858R mutant
  作者：Tsutomu Fukuda、Mizuho Anzai、Akane Nakahara、Kentaro Yamashita、Kazuaki Matsukura、Fumito Ishibashi、Yusuke Oku、Naoyuki Nishiya、Yoshimasa Uehara、Masatomo Iwao

  DOI：10.1016/j.bmc.2021.116039

  日期：2021.3

  Azalamellarin N, a synthetic lactam congener of the marine natural product lamellarin N, and its A-ring-modified analogues were synthesized and evaluated as potent and non-covalent inhibitors of the drug-resistant epidermal growth factor receptor T790M/L858R mutant. An in vitro tyrosine kinase assay indicated that the inhibitory activities of the synthetic azalamellarin analogues were higher than those

  Azalamellarin N，一种海洋天然产物 lamellarin N 的合成内酰胺同源物，及其 A 环修饰的类似物被合成并评估为耐药表皮生长因子受体 T790M/L858R 突变体的有效和非共价抑制剂。体外酪氨酸激酶试验表明，合成的氮杂紫杉醇类似物的抑制活性高于相应的紫胨。在 C20 和 C21 位带有两个 3-（二甲氨基）丙氧基的氮杂紫杉醇类似物对突变激酶表现出最高的活性和选择性 [IC 50 (T790M/L858R) = 1.7 nM；集成电路50(WT) = 4.6 nM]。抑制活性归因于B环的内酰胺NH基团和甲硫氨酸残基的羰基之间的氢键相互作用。
• Substituted N-aryl benzamides and related compounds for treatment of amyloid diseases and synucleinopathies
  申请人：Snow D. Alan

  公开号：US20060199838A1

  公开（公告）日：2006-09-07

  Substituted n-aryl benzamides, related compounds and their pharmaceutically acceptable derivatives, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment are provided.

  本发明提供了取代的n-芳基苯甲酰胺，相关化合物及其药学上可接受的衍生物，它们的合成方法，含有它们的制药组合物，以及它们在治疗淀粉样疾病中的应用，包括Aβ淀粉样蛋白病，如阿尔茨海默病中观察到的IAPP淀粉样蛋白病，如2型糖尿病中观察到的以及突触核蛋白病，如帕金森病中观察到的，以及制造用于这种治疗的药物。
• c-MET MODULATORS AND METHOD OF USE
  申请人：BANNEN CANNE LYNNE

  公开号：US20070244116A1

  公开（公告）日：2007-10-18

  The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

  本发明提供了用于调节蛋白激酶酶活性，以调节细胞活动，如增殖、分化、程序性细胞死亡、迁移和化学侵袭的化合物。更具体地，本发明提供了喹唑啉和喹啉，这些化合物抑制、调节和/或调节激酶受体，特别是c-Met、KDF、c-Kit、flt-3和flt-4，与上述细胞活动变化相关的信号转导途径，包含这些化合物的组合物，以及使用它们治疗激酶依赖性疾病和病况的方法。本发明还提供制备上述化合物的方法和包含这些化合物的组合物。
• C-MET MODULATORS AND METHOD OF USE
  申请人：Bannen Canne Lynne

  公开号：US20070225307A1

  公开（公告）日：2007-09-27

  The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

  本发明提供了用于调节蛋白激酶酶活性以调节细胞活动（如增殖、分化、程序性细胞死亡、迁移和化学入侵）的化合物。更具体地，该发明提供了喹唑啉和喹啉，它们能够抑制、调节和/或调节激酶受体，特别是c-Met、KDF、c-Kit、flt-3和flt-4，与上述细胞活动变化相关的信号转导途径，包含这些化合物的组合物，以及使用它们治疗激酶依赖性疾病和病况的方法。本发明还提供了制备上述化合物和包含这些化合物的组合物的方法。