N-(4-methoxy-3-nitrophenyl) acrylamide

• 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: N-(4-methoxy-3-nitrophenyl) acrylamide
• 英文别名: 1-methoxy-2-nitro-4-acrylamidobenzene；N-(4-methoxy-3-nitrophenyl)prop-2-enamide
• 化学式: C₁₀H₁₀N₂O₄
• 分子量: 222.2
• InChiKey: JZKOXTWCDRVZBU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  84.2
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N-(4-methoxy-3-nitrophenyl) acrylamide 在 ammonium sulfide 、 溴 、 铁粉 、 溶剂黄146 作用下， 以 异丙醇 为溶剂， 生成 N-[2-[[2-(二甲基氨基)乙基]甲基氨基]-4-甲氧基-5-[[4-(1-甲基-1H-吲哚-3-基)-2-嘧啶基]氨基]苯基]-2-丙烯酰胺
  参考文献：
  名称：

  甲磺酸奥斯替尼的制备方法

  摘要：

  本发明公开了甲磺酸奥斯替尼的制备方法，所述甲磺酸奥斯替尼化学名称为N‑(2‑((2‑(二甲基氨基)乙基)(甲基)氨基)‑4‑甲氧基‑5‑((4‑(1‑甲基‑1H‑吲哚‑3‑基)嘧啶‑2‑基)氨基)苯基)丙烯酰胺甲磺酸盐(AZD9291)，其化学式为C28H33N7O2.CH4O3S；本发明制备工艺过程简洁，原料易得，经济环保，有利于实现工业化，可促进奥斯替尼原料药的经济技术发展，降低了生产成本，适于大批量生产。

  公开号：

  CN107915724A
• 作为产物：
  描述：

  p-methoxyanilinium nitrate 在 硫酸 、 三乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 6.0h， 生成 N-(4-methoxy-3-nitrophenyl) acrylamide
  参考文献：
  名称：

  2,4-二取代的嘧啶类化合物

  摘要：

  本发明属于医药化学领域，涉及2,4‑二取代的嘧啶类化合物，具体涉及如式(I)所示的化合物或其药学上可接受的盐、其药物组合物、及其在治疗EGFR或/和ALK介导的疾病中的用途。

  公开号：

  CN106905245B

文献信息

• [EN] PROTEIN TYROSINE KINASE MODULATORS AND METHODS OF USE<br/>[FR] MODULATEURS DE LA PROTÉINE TYROSINE KINASE ET MÉTHODES D'UTILISATION
  申请人：BETTA PHARMACEUTICALS CO LTD

  公开号：WO2015003658A1

  公开（公告）日：2015-01-15

  Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative,and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed.

  揭示了调节突变选择性表皮生长因子受体（EGFR）和ALK激酶活性的杂环嘧啶化合物。更具体地，该发明提供了抑制、调节和/或调节激酶受体的嘧啶类化合物，特别是在选择性调节各种EGFR突变活性和ALK激酶活性方面已经被揭示。揭示了包括嘧啶衍生物的药物组合物，以及用于治疗与蛋白激酶酶活性相关的疾病的方法，特别是包括非小细胞肺癌的EGFR或ALK激酶活性，其中包括给予嘧啶衍生物的治疗。
• 布鲁顿酪氨酸激酶抑制剂
  申请人：正大天晴药业集团股份有限公司

  公开号：CN108329274B

  公开（公告）日：2021-09-03

  本申请属于药物化学领域，具体涉及式(I)化合物或其药物上可接受的盐、其制备方法、含有该化合物的药物组合物。本申请还涉及这些化合物或其药物上可接受的盐及包含这些化合物的药物组合物在治疗布鲁顿酪氨酸激酶相关疾病中的用途。
• Discovery of 4‐(4‐aminophenyl)‐6‐phenylisoxazolo[3,4‐ <i>b</i> ]pyridine‐3‐amine derivatives as novel FLT3 covalent inhibitors for the intervention of acute myeloid leukemia
  作者：Qing‐Xin Wang、Yi‐Bo Wang、Jiu‐Kai Sha、Hai Zhou、Jia‐Chuan Liu、Jia‐Zhen Wu、Zhen‐Jiang Tong、Jiao Cai、Zi‐Jun Chen、Chen‐Qian Zhang、Xin‐Rui Zheng、Jing‐Jing Wang、Xiao‐Long Wang、Xin Xue、Yan‐Cheng Yu、Ning Ding、Xue‐Jiao Leng、Wei‐Chen Dai、Shan‐Liang Sun、Liang Chang、Nian‐Guang Li、Zhi‐Hao Shi

  DOI：10.1002/ddr.22032

  日期：——

  AbstractSmall molecule covalent drugs have proved to be desirable therapies especially on drug resistance related to point mutations. Secondary mutations of FLT3 have become the main mechanism of FLT3 inhibitors resistance which further causes the failure of treatment. Herein, a series of 4‐(4‐aminophenyl)‐6‐phenylisoxazolo[3,4‐b]pyridine‐3‐amine covalent derivatives were synthesized and optimized to overcome the common secondary resistance mutations of FLT3. Among these derivatives, compound F15 displayed potent inhibition activities against FLT3 (IC50 = 123 nM) and FLT3‐internal tandem duplication (ITD) by 80% and 26.06%, respectively, at the concentration of 1 μM. Besides, F15 exhibited potent activity against FLT3‐dependent human acute myeloid leukemia (AML) cell lines MOLM‐13 (IC50 = 253 nM) and MV4‐11 (IC50 = 91 nM), as well as BaF3 cells with variety of secondary mutations. Furthermore, cellular mechanism assays indicated that F15 inhibited phosphorylation of FLT3 and its downstream signaling factors. Notably, F15 could be considered for further development as potential drug candidate to treat AML.
• PROTEIN TYROSINE KINASE MODULATORS AND METHODS OF USE
  申请人：BETTA PHARMACEUTICALS CO., LTD

  公开号：US20160145237A1

  公开（公告）日：2016-05-26

  Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative, and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed.
• US4076706A
  申请人：——

  公开号：US4076706A

  公开（公告）日：1978-02-28