(4-methoxy-phenyl)-methyl-pyridin-2-yl-amine | 1383232-09-4

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (4-methoxy-phenyl)-methyl-pyridin-2-yl-amine
• 英文别名: N-(4-methoxyphenyl)-N-methylpyridin-2-amine；N-(4-methoxyphenyl)-N-methyl-2-aminopyridine；(4-Methoxy-phenyl)-methyl-pyridin-2-yl-amine
• CAS: 1383232-09-4
• 化学式: C₁₃H₁₄N₂O
• 分子量: 214.267
• InChiKey: AXFWVCRSCVJZMW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  25.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (4-methoxy-phenyl)-methyl-pyridin-2-yl-amine 在 copper(l) iodide 、 三溴化硼 、 caesium carbonate 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 0.5h， 生成 2-[4-(methyl-pyridin-2-yl-amino)-phenoxy]-pyrido[3,4-d]pyrimidin-4-ol
  参考文献：
  名称：

  [EN] HISTONE DEMETHYLASE INHIBITORS
  [FR] INHIBITEURS DE L'HISTONE DÉMÉTHYLASE

  摘要：

  本发明通常涉及治疗癌症和肿瘤性疾病的组合物和方法。本文提供了替代的吡啶并[3,4-d]嘧啶-4-酮衍生物化合物和包含该化合物的药物组合物。所述化合物和组合物对组蛋白去甲基化酶的抑制有用。此外，所述化合物和组合物对于治疗癌症，如前列腺癌、乳腺癌、膀胱癌、肺癌和/或黑色素瘤等方面是有用的。

  公开号：

  WO2016044429A1
• 作为产物：
  描述：

  N-methyl-N-(4-methoxyphenyl)pyridine-2-sulfonamide 在 bis(1,5-cyclooctadiene)nickel (0) 、 三苯基硼烷 、 3,4-bis(dicyclohexylphosphino)thiophene 、 sodium t-butanolate 作用下， 以 5,5-dimethyl-1,3-cyclohexadiene 为溶剂， 反应 16.0h， 以52%的产率得到(4-methoxy-phenyl)-methyl-pyridin-2-yl-amine
  参考文献：
  名称：

  镍催化的分子内脱硫CN偶联：芳香胺的合成

  摘要：

  提出了通过SO 2挤出的镍催化的分子内CN偶联反应。与以前报道的通过CO或CO 2挤出进行的CN偶联反应（160-180°C）相比，使用催化量的BPh 3可使转化在较温和的条件下（60 °C）进行。另外，该方法显示出良好的官能团耐受性和多功能性，因为它可用于合成二烷基芳基胺，烷基二芳基胺和三芳基胺。通过三个高产量的克级反应证明了脱硫CN偶联的稳健性。

  DOI：

  10.1021/acs.joc.0c00009

文献信息

• Palladium-catalyzed oxidative alkynylation of arene C–H bond using the chelation-assisted strategy
  作者：Seok Hwan Kim、Sae Hume Park、Sukbok Chang

  DOI：10.1016/j.tet.2012.04.003

  日期：2012.7

  Palladium-catalyzed alkynylation of arene C–H bonds with (triisopropylsilyl)acetylene was developed for the first time under oxidative conditions in the present study. Among various type of directing groups examined, the N-phenyl-2-aminopyridine skeleton was shown to be most effective and selective for the Pd-catalyzed direct alkynylation reaction, and the desired alkynylated products were obtained

  本研究首次在氧化条件下开发了钯催化的芳烃CH键与（三异丙基甲硅烷基）乙炔的炔基化反应。在所考察的各种类型的导向基团中，N-苯基-2-氨基吡啶骨架显示出对Pd催化的直接炔基化反应最有效和最具选择性，并且以中等至良好的收率获得了所需的炔基化产物。
• HISTONE DEMETHYLASE INHIBITORS
  申请人：Celgene Quanticel Research, Inc.

  公开号：US20160194323A1

  公开（公告）日：2016-07-07

  The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer, melanoma, and the like.

  本发明涉及治疗癌症和肿瘤疾病的组合物和方法。本文提供了取代的吡啶并[3,4-d]嘧啶-4-酮衍生物化合物及包含该化合物的制药组合物。所述化合物和组合物对组蛋白去甲基化酶的抑制具有用途。此外，所述化合物和组合物对治疗癌症，如前列腺癌，乳腺癌，膀胱癌，肺癌，黑色素瘤等具有用途。
• Histone demethylase inhibitors
  申请人：Celgene Quanticel Research, Inc.

  公开号：US10030017B2

  公开（公告）日：2018-07-24

  The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer, melanoma, and the like.

  本发明一般涉及治疗癌症和肿瘤性疾病的组合物和方法。本发明提供了取代的吡啶并[3,4-d]嘧啶-4-酮衍生物化合物和包含所述化合物的药物组合物。所述化合物和组合物可用于抑制组蛋白去甲基化酶。此外，所述化合物和组合物还可用于治疗癌症，如前列腺癌、乳腺癌、膀胱癌、肺癌、黑色素瘤等。
• Novel organic electroluminescent compounds and organic electroluminescent device using the same
  申请人：Kim Young Gil

  公开号：US20100108997A1

  公开（公告）日：2010-05-06

  Provided are novel organic electroluminescent compounds, and organic electroluminescent devices comprising the same as electroluminescent material. Specifically, the organic electroluminescent compounds according to the present invention are represented by Chemical Formula (1): wherein, at least one substituent(s) among Ar 1 , Ar 2 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 14 and R 15 represent(s) The organic electroluminescent compounds according to the present invention exhibit high luminous efficiency and excellent life property of material, so that an OLED having very good operation life can be manufactured therefrom. Further, the organic electroluminescent compound according to the present invention, when it is contained in an electroluminescent layer or a hole transport layer, lowers the operation voltage to result in noticeable decrease in power consumption, with exhibiting at least comparable luminous efficiency as compared to conventional OLED's.
• US9643965B2
  申请人：——

  公开号：US9643965B2

  公开（公告）日：2017-05-09