4-(1-phenylpropyl)morpholine | 92196-08-2

• 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: 4-(1-phenylpropyl)morpholine
• 英文别名: 4-(1-phenyl-propyl)-morpholine；1-Morpholino-1-phenyl-propan
• CAS: 92196-08-2
• 化学式: C₁₃H₁₉NO
• 分子量: 205.3
• InChiKey: LSTVSNRAJKBTNW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  正丙基苯 在 四溴化碳 、 (4,4'-di-tert-butyl-2,2'-dipyridyl)-bis-(2-phenylpyridine(-1H))-iridium(III) hexafluorophosphate 作用下， 以 二氯甲烷 为溶剂， 生成 4-(1-phenylpropyl)morpholine
  参考文献：
  名称：

  Visible-light-mediated benzylic sp3 C–H bond functionalization to C–Br or C–N bond

  摘要：

  A visible-light-promoted functionalization of unactivated benzylic sp(3) C-H bonds was developed. Ethylbenzene derivatives were converted to the corresponding benzyl bromides or afforded benzylamine derivatives in a one-pot manner under visible light photoredox conditions. (C) 2016 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2016.04.036

文献信息

• Copper-Catalyzed Intermolecular Regioselective Hydroamination of Styrenes with Polymethylhydrosiloxane and Hydroxylamines
  作者：Yuya Miki、Koji Hirano、Tetsuya Satoh、Masahiro Miura

  DOI：10.1002/anie.201304365

  日期：2013.10.4

  Playing Reversi with H and N: A copper‐catalyzed intermolecular regioselective hydroamination of styrenes with polymethylhydrosiloxane and hydroxylamine derivatives has been developed. The catalysis accommodates challenging β‐substituted substrates. Moreover, the chiral biphosphine‐ligated copper complex successfully forms benzylamines with good enantiomeric ratios.

  与H和N进行逆反应：已经开发了铜催化的苯乙烯与聚甲基氢硅氧烷和羟胺衍生物的分子间区域选择性加氢胺化反应。催化作用可适应具有挑战性的β-取代的底物。此外，手性双膦连接的铜络合物可成功形成具有良好对映体比率的苄胺。
• Achieving Aliphatic Amine Addition to Arylalkynes via the Lewis Acid Assisted Triazole-Gold (TA-Au) Catalyst System
  作者：Teng Jia、Shengyu Fan、Fengmian Li、Xiaohan Ye、Wenke Zhang、Zhiguang Song、Xiaodong Shi

  DOI：10.1021/acs.orglett.1c02098

  日期：2021.8.6

  Transition metal catalyzed intermolecular hydroamination of the arylalkynes with aliphatic amine is generally problematic due to the good coordination between amine and metal cation. With the combination of 1,2,3-triazole coordinated gold(I) catalyst (TA-Au) and Zn(OTf)2 cocatalyst, this challenging transformation was achieved with good to excellent yields and regioselectivity. Compared to previously

  由于胺和金属阳离子之间的良好配位，过渡金属催化的芳基炔与脂肪胺的分子间加氢胺化通常存在问题。通过结合 1,2,3-三唑配位金 (I) 催化剂 (TA-Au) 和 Zn(OTf) 2助催化剂，实现了这一具有挑战性的转化，并具有良好至优异的产率和区域选择性。与之前报道的方法相比，该方法提供了一种替代催化剂系统，以高效率和实用条件实现这一基本化学转化。
• 2,4,6-TRIAMINO-1,3,5-TRIAZINE DERIVATIVE
  申请人：Kubota Hideki

  公开号：US20080227785A1

  公开（公告）日：2008-09-18

  This invention relates to an anti-dementia agent which uses a BEC 1 potassium channel inhibitor as the active ingredient. It was proved that the BEC 1 potassium channel inhibitor has an action to improve learning disorder and is useful as a preventive or therapeutic agent for diseases, preferably dementia, in which the BEC 1 potassium channel is considered to be concerned. Illustratively, it was confirmed by an in vivo test that the BEC 1 potassium channel inhibitor has an action to improve learning disorder. Also, it was found that a compound having 2,4,6-triamino-1,3,5-triazine has a BEC 1 potassium channel inhibitory action.

  本发明涉及一种以BEC 1钾离子通道抑制剂作为活性成分的抗痴呆剂。已经证明，BEC 1钾离子通道抑制剂具有改善学习障碍的作用，并且作为预防或治疗剂是有用的，尤其是对于BEC 1钾离子通道与之相关的疾病，如痴呆症。例如，通过体内试验证实，BEC 1钾离子通道抑制剂具有改善学习障碍的作用。此外，还发现具有2,4,6-三氨基-1,3,5-三嗪的化合物具有BEC 1钾离子通道抑制作用。
• AMIDE DERIVATIVE OR SALT THEREOF
  申请人：Kaku Hidetaka

  公开号：US20090062363A1

  公开（公告）日：2009-03-05

  [Problem] To provide a compound which can be used for the prevention and/or treatment of diseases in which 5-HT 2B receptor and 5-HT 7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that an amide derivative characterized by the possession of a nitrogen-containing bicyclic hetero ring (e.g., an indole or the like), or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT 2B receptor and 5-HT 7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT 2B receptor and 5-HT 7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).

  [问题] 提供一种可用于预防和/或治疗与5-HT2B受体和5-HT7受体有关的疾病的化合物，特别是用于治疗肠易激综合征（IBS）。 [解决方法] 发现一种具有含氮双环杂环（例如吲哚或类似物）的酰胺衍生物或其药学上可接受的盐具有强烈的5-HT2B受体和5-HT7受体的拮抗作用。此外，本发明的化合物具有对两种受体的拮抗活性，与仅使用选择性拮抗剂相比，表现出良好的药理作用。基于上述，本发明的化合物可用于预防和/或治疗与5-HT2B受体和5-HT7受体有关的疾病，特别是用于治疗肠易激综合征（IBS）。
• Pyridine and Pyrazine derivative for the Treatment of CF
  申请人：BAETTIG Urs

  公开号：US20150045364A1

  公开（公告）日：2015-02-12

  The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.

  本发明提供了吡啶和吡嗪衍生物，能够恢复或增强突变型和/或野生型CFTR的功能，以治疗囊性纤维化、原发性纤毛运动障碍、慢性支气管炎、慢性阻塞性肺疾病、哮喘、呼吸道感染、肺癌、口干症和角膜结膜炎，或便秘（IBS、IBD、阿片类药物引起的）。还包括含有这些衍生物的药物组合物。