2-甲氧基-4,5-二硝基苯酚 | 105780-30-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 酚类
• 中文名称: 2-甲氧基-4,5-二硝基苯酚
• 英文名称: 1,2-Dinitro-4-hydroxy-5-methoxybenzene
• 英文别名: 2-methoxy-4,5-dinitrophenol；2-methoxy-4,5-dinitro phenol；4.5-dinitro-2-hydroxy-1-methoxy-benzene；Methyl-(4.5-dinitro-2-hydroxy-phenyl)-aether；4.5-Dinitro-2-hydroxy-1-methoxy-benzol；4.5-Dinitro-brenzcatechin-1-methylaether；Phenol, 2-methoxy-4,5-dinitro-
• CAS: 105780-30-1
• 化学式: C₇H₆N₂O₆
• 分子量: 214.134
• InChiKey: FFOSGJSASFGRSA-UHFFFAOYSA-N

物化性质

• 熔点：
  172 °C
• 沸点：
  456.7±45.0 °C(Predicted)
• 密度：
  1.579±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  121
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-甲氧基-4,5-二硝基苯酚 在 氨 、 formamide 作用下， 以 水 为溶剂， 生成 5-amino-2-methoxy-4-nitrophenol
  参考文献：
  名称：

  3-amino-4-nitrophenols, the process for preparation thereof and their

  摘要：

  新的3-氨基-4-硝基苯酚，其制备方法及其在染色角蛋白质纤维中的应用，以及新的中间体4,5-二硝基苯酚。本发明涉及一种式为：##STR1##其中Z表示--CH.sub.2 --W，W表示氢，C.sub.1-C.sub.6烷基，C.sub.1-C.sub.6羟基烷基，C.sub.2-C.sub.6多羟基烷基，（C.sub.1-C.sub.3）烷氧基（C.sub.1-C.sub.6）烷基或（C.sub.1-C.sub.3）羟基氧基（C.sub.1-C.sub.6）烷基，R表示氢，C.sub.1-C.sub.6烷基，C.sub.1-C.sub.6羟基烷基，C.sub.2-C.sub.6多羟基烷基或（C.sub.1-C.sub.3）烷氧基（C.sub.1-C.sub.6）烷基的3-氨基-4-硝基苯酚的制备方法以及式为：##STR2##其中Z'表示CH.sub.2 --W，W表示C.sub.1-C.sub.6羟基烷基，C.sub.2-C.sub.6多羟基烷基，（C.sub.1-C.sub.3）烷氧基（C.sub.1-C.sub.6）烷基或（C.sub.1-C.sub.3）羟基氧基（C.sub.1-C.sub.6）烷基的中间化合物。染料（I）在直接染色角蛋白质纤维，特别是人发中有用。

  公开号：

  US04740622A1
• 作为产物：
  描述：

  胡椒环 在 硝酸 、 三乙胺 作用下， 以 乙醇 为溶剂， 反应 8.0h， 生成 2-甲氧基-4,5-二硝基苯酚
  参考文献：
  名称：

  喹喔啉-2(1H)-酮类化合物及其制备方法和应 用

  摘要：

  本发明涉及式(I)表示的1-取代-6-甲氧基-7-(3-吗啡啉丙氧基)喹喔啉-2(1H)-酮类化合物及其制备方法和应用。式(I)中R表示不同取代的芳基烷基。本发明方法是以胡椒环为原料，进行两次硝化反应生成二硝化产物5,6-二硝基苯并[d][1,3]二氧杂环戊烷，然后在强碱条件下得到开环产物2-甲氧基-4,5-二硝基苯酚，再和4-(3-氯丙基)吗啡啉发生亲核取代反应，得到的产物4-(3-(2-甲氧基-4,5-二硝基苯氧基)丙基)吗啡啉被还原后再与乙醛酸乙酯发生关环反应，生成化合物6-甲氧基-7-(3-吗啡啉丙氧基)喹喔啉-2(1H)-酮，最后在碱性条件下与含有取代基R的卤代烃反应得到本发明化合物。本发明化合物对EGFR激酶具有抑制作用。

  公开号：

  CN103787993B

文献信息

• Treatment of platelet derived growth factor related disorders such as cancers
  申请人：University of California

  公开号：US06331555B1

  公开（公告）日：2001-12-18

  The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.

  本发明涉及能够抑制血小板源性生长因子受体（PDGF-R）活性的化合物，最好这些化合物还能抑制PDGF-R超家族的其他成员的活性，并且对PDGF-R超家族的成员具有选择性。PDGF-R超家族包括PDGF-R和PDGF-R相关激酶Flt和KDR。这些特色化合物在细胞培养中对降低PDGF-R活性以及最好地对一种或多种PDGF-R相关激酶具有活性。下面描述了一种特色化合物A10（见图1a）及其抑制体内肿瘤细胞生长的能力。利用本申请作为指南，可以获得其他能够抑制PDGF-R、最好是Flt和/或KDR的化合物。这些化合物最好用于治疗患有由不适当PDGF-R活性特征的细胞增殖紊乱症状的患者。
• Treatment of platelet derived growth factor related disorders such as
  申请人：Sugen Inc.

  公开号：US05990141A1

  公开（公告）日：1999-11-23

  The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.

  本发明涉及一类可以抑制血小板源性生长因子受体（PDGF-R）活性的化合物，最好这些化合物还可以抑制PDGF-R超家族的其他成员的活性，并且对PDGF-R超家族的成员具有选择性。PDGF-R超家族包括PDGF-R和PDGF-R相关激酶Flt和KDR。这些特色化合物在细胞培养中对降低PDGF-R活性以及最好是一个或多个PDGF-R相关激酶的活性方面是活跃的。下面描述了一个特色化合物A10（见图1a）及其在体内抑制肿瘤细胞生长的能力。通过本申请作为指南，可以获得其他能够抑制PDGF-R，最好是Flt和/或KDR的化合物。这些化合物最好用于治疗患有细胞增殖异常的患者，其特征是PDGF-R活性异常。
• [EN] QUINOLINE AND QUINOXALINE COMPOUNDS AS PDGF-RECEPTOR AND/OR LCK TYROSINE KINASE INHIBITORS<br/>[FR] COMPOSES DE QUINOLEINE ET QUINOXALINE UTILISES COMME INHIBITEURS DU RECEPTEUR PDGF ET/OU DE LA TYROSINE KINASE LCK
  申请人：AVENTIS PHARM PROD INC

  公开号：WO2000031051A1

  公开（公告）日：2000-06-02

  This invention is directed to quinoline/quinoxaline compounds of formula (I), which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising theses compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.

  本发明涉及公式（I）的喹啉/喹噁啉化合物，其抑制血小板来源性生长因子或p56lck酪氨酸激酶活性，以及包含这些化合物的制药组合物，并且用于治疗患有或受到涉及细胞分化、增殖、细胞外基质产生或介质释放和/或T细胞激活和增殖的疾病/症状的患者。
• [EN] QUINOLINE AND QUINOXALINE COMPOUNDS AS PDGF-R AND/OR LCK TYROSINE KINASE INHIBITORS<br/>[FR] COMPOSES DE QUINOLINE ET DE QUINOXALINE AGISSANT COMME INHIBITEURS DU PDGG-R ET/OU DE LCK TYROSINE KINASE
  申请人：AVENTIS PHARM PROD INC

  公开号：WO2000031049A1

  公开（公告）日：2000-06-02

  This invention is directed to quinoline/quinoxaline compounds of formula (I) wherein X is L1OH or L2Z2; L1 is (CR3aR3b)r or (CR3aR3b)m-Z3-(CR3'aR3'b)n; L2 is (CR3aR3b)p-Z4-(CR3'aR3'b)q or ethenyl; Z1 is CH or N; Z2 is optionally substituted hydroxycycloalkyl, optionally substituted hydroxycycloalkenyl, optionally substituted hydroxyheterocyclyl or optionally substituted hydroxyheterocyclenyl; Z3 is O, NR4, S, SO or SO2; Z4 is O, NR4, S, SO, SO2 or a bond; m is 0 or 1; n is 2 or 3, and n + m = 2 or 3; p and q are independently 0, 1, 2, 3 or 4, and p + q = 0, 1, 2, 3 or 4 when Z4 is a bond, and p + q = 0, 1, 2 or 3 when Z4 is other than a bond; r is 2, 3 or 4; which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.

  本发明涉及公式（I）的喹啉/喹噁啉化合物，其中X为L1OH或L2Z2; L1为（CR3aR3b）r或（CR3aR3b）m-Z3-（CR3'aR3'b）n; L2为（CR3aR3b）p-Z4-（CR3'aR3'b）q或乙烯基; Z1为CH或N; Z2为可选择取代的羟基环烷基，可选择取代的羟基环烯基，可选择取代的羟基杂环基或可选择取代的羟基杂环烷基; Z3为O，NR4，S，SO或SO2; Z4为O，NR4，S，SO，SO2或键; m为0或1; n为2或3，且n + m = 2或3; p和q独立地为0、1、2、3或4，当Z4为键时，p + q = 0、1、2、3或4，当Z4不是键时，p + q = 0、1、2或3; r为2、3或4; 这些化合物抑制血小板来源生长因子或p56lck酪氨酸激酶活性，本发明还涉及包含这些化合物的制药组合物，以及使用这些化合物治疗患有或患有涉及细胞分化、增殖、细胞外基质产生或介质释放和/或T细胞激活和增殖的疾病/症状的患者的用途。
• Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases
  申请人：——

  公开号：US20010023250A1

  公开（公告）日：2001-09-20

  This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56 lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.

  本发明涉及抑制血小板源性生长因子或p56lck酪氨酸激酶活性的喹啉/喹噁啉化合物，以及包含这些化合物的制药组合物，以及使用这些化合物治疗患有或受到涉及细胞分化，增殖，细胞外基质产生或介质释放和/或T细胞激活和增殖的疾病/病症的患者。