(E)-3-(4-isopropylphenyl)-N-methylacrylamide | 1448684-87-4

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂酸及其衍生物
• 英文名称: (E)-3-(4-isopropylphenyl)-N-methylacrylamide
• 英文别名: N-methyl-3-[4-(propan-2-yl)phenyl]prop-2-enamide；(E)-N-methyl-3-(4-propan-2-ylphenyl)prop-2-enamide
• CAS: 1448684-87-4
• 化学式: C₁₃H₁₇NO
• 分子量: 203.284
• InChiKey: UKNOVUXVOUMUSW-RMKNXTFCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  N-甲基甲酰胺 、 4-异丙基肉桂酸 在 二叔丁基过氧化物 、 copper(II) sulfate 作用下， 反应 48.0h， 以19%的产率得到(E)-3-(4-isopropylphenyl)-N-methylacrylamide
  参考文献：
  名称：

  肉桂酸和N-取代甲酰胺的直接酰胺化反应在铜催化下合成α，β-不饱和酰基酰胺

  摘要：

  首次报道了在容易获得的肉桂酸和N-取代的甲酰胺之间通过铜催化的直接酰胺化反应，高效合成α，β-不饱和酰基酰胺。该协议易于访问且实用。

  DOI：

  10.1016/j.tet.2013.06.078

文献信息

• HISTONE DEACETYLASE INHIBITORS
  申请人：Bradner James Elliot

  公开号：US20100056588A1

  公开（公告）日：2010-03-04

  In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.

  为了开发新型治疗剂，本发明提供了新型组蛋白去乙酰化酶抑制剂。这些化合物包括酯键，使它们对酯酶的失活敏感。因此，这些化合物在治疗皮肤疾病方面特别有用。当这些化合物进入血液循环时，酯酶或具有酯酶活性的酶将其裂解成生物学上不活性的碎片或具有大大降低活性的碎片。理想情况下，这些降解产物表现出短的血清和/或系统半衰期，并迅速被排出体外。这些化合物及其制剂在治疗切除性T细胞淋巴瘤、神经纤维瘤、银屑病、脱发、皮肤色素沉着和皮炎等方面特别有用。本发明还提供了制备本发明化合物及其中间体的方法。
• Histone Deacetylase and Tubulin Deacetylase Inhibitors
  申请人：Mazitschek Ralph

  公开号：US20090209590A1

  公开（公告）日：2009-08-20

  In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel inhibitors of histone deacetylases, tubulin deacetylases, and/or aggresome inhibitors, and pharmaceutically acceptable salts and derivatives thereof. The inventive compounds fall into two classes—“isotubacin” class and “isoisotubacin” class—all of which include a 1,3-dioxane core. The present invention further provides methods for treating disorders regulated by histone deacetylase activity, tubulin deacetylase activity, and/or the aggresome (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, protein degradation disorders, protein deposition disorders, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
• BIFUNCTIONAL HISTONE DEACETYLASE INHIBITORS
  申请人：Bradner James Elliot

  公开号：US20090312363A1

  公开（公告）日：2009-12-17

  In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
• US8222423B2
  申请人：——

  公开号：US8222423B2

  公开（公告）日：2012-07-17
• US8304451B2
  申请人：——

  公开号：US8304451B2

  公开（公告）日：2012-11-06