4-(2-methyloctyl)morpholine | 145060-20-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 4-(2-methyloctyl)morpholine
• CAS: 145060-20-4
• 化学式: C₁₃H₂₇NO
• 分子量: 213.363
• InChiKey: BZZWTIJQIIHRPN-UHFFFAOYSA-N

物化性质

• 沸点：
  278.9±15.0 °C(Predicted)
• 密度：
  0.881±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  15
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 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：

  吗啉 、 辛烯 、 一氧化碳 在 chloro(1,5-cyclooctadiene)rhodium(I) dimer 氢气 作用下， 以 1,4-二氧六环 为溶剂， 80.0 ℃ 、11.0 MPa 条件下， 反应 24.0h， 生成 4-(2-methyloctyl)morpholine 、 4-nonylmorpholine
  参考文献：
  名称：

  One-Pot Synthesis of Secondary and Tertiary Amines by Carbonylative Hydroaminomethylation of Alkenes Catalyzed by Di(μ-chloro)bis(η4-1,5-cyclooctadiene)dirhodium

  摘要：

  次级和三级胺通过在[Rh(cod)Cl]2催化剂存在下，烯烃与一级或二级胺、一氧化碳和氢气反应，经一步法羰基合成-胺缩合-还原序列高效选择性制备。

  DOI：

  10.1055/s-1997-1338

文献信息

• Glycerol Boosted Rh‐Catalyzed Hydroaminomethylation Reaction: A Mechanistic Insight
  作者：Alejandro Serrano‐Maldonado、Trung Dang‐Bao、Isabelle Favier、Itzel Guerrero‐Ríos、Daniel Pla、Montserrat Gómez

  DOI：10.1002/chem.202001978

  日期：2020.10

  We report a Rh‐catalyzed hydroaminomethylation reaction of terminal alkenes in glycerol that proceeds efficiently under mild conditions to produce the corresponding amines in relatively high selectivity towards linear amines, moderate to excellent yields by using a low catalyst loading (1 mol % [Rh], 2 mol % phosphine) and relative low pressure (H2/CO, 1:1, total pressure 10 bar). This work sheds light

  我们报道了甘油中末端烯烃的Rh催化加氢氨基甲基化反应，该反应在温和条件下有效地进行，以相对高的线性胺选择性生成相应的胺，通过使用低催化剂负载量（1 mol％[Rh]， 2摩尔％的膦）和相对低压（H 2/ CO，1：1，总压力10 bar）。这项工作揭示了甘油在通过氢转移使烯胺还原中的重要性。而且，通过排除有害的醛醇缩合反应，首次在加氢氨基甲基化反应的框架中获得了Rh在缩合步骤中作为化学选择性催化剂的关键作用的证据。氢氨基甲基化是在分子机制下进行的。催化活性物质进入金属基纳米颗粒的结果使催化体系失去活性。
• One-pot synthesis of amines by aminomethylation of alkenes catalysed by dinuclear rhodium complexes under mild conditions
  作者：Thierry Baig、Philippe Kalck

  DOI：10.1039/c39920001373

  日期：——

  The complex [Rh2(µ-S-But)2(CO)2(PPh3)2] with a slight excess of PPh3 catalyses the aminomethylation reaction of terminal alkenes under low pressures of carbon monoxide and hydrogen.

  含有少量过量 PPh3 的[Rh2(µ-S-But)2(CO)2(PPh3)2]复合物可在低压一氧化碳和氢气条件下催化末端烯的氨基甲基化反应。
• Epoxyketone compounds for enzyme inhibition
  申请人：CENTRAX INTERNATIONAL, INC.

  公开号：US10640533B2

  公开（公告）日：2020-05-05

  The present disclosure relates to novel compounds and pharmaceutical compositions thereof which are useful as inhibitors of proteasomes. The compounds provided herein have improved proteasome potency and selectivity, and increased aqueous solubility, and are useful in treating various conditions or diseases associated with proteasomes.

  本公开涉及可用作蛋白酶体抑制剂的新型化合物及其药物组合物。本文所提供的化合物具有更好的蛋白酶体效力和选择性，以及更高的水溶性，可用于治疗与蛋白酶体相关的各种病症或疾病。
• Urea derivatives and uses thereof
  申请人：Kala Pharmaceuticals, Inc.

  公开号：US10723719B2

  公开（公告）日：2020-07-28

  The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.

  本发明提供了式(I)-(III)中任一项的新型化合物及其药物组合物。本发明还提供了由式（I）-（III）化合物及其药物组合物组成的具有粘液渗透性的颗粒（如纳米颗粒）。本发明还提供了使用本发明化合物及其药物组合物治疗和/或预防与异常或病理性血管生成和/或生长因子（如血管内皮生长因子 (VEGF)）异常信号转导相关疾病的方法和试剂盒，如增殖性疾病（如、如癌症、良性肿瘤、炎症性疾病、自身免疫性疾病）和眼部疾病（如黄斑变性、青光眼、糖尿病视网膜病变、视网膜母细胞瘤、水肿、葡萄膜炎、干眼症、睑缘炎和手术后炎症）。
• Efficient and Regioselective Ruthenium-catalyzed Hydro-aminomethylation of Olefins
  作者：Lipeng Wu、Ivana Fleischer、Ralf Jackstell、Matthias Beller

  DOI：10.1021/ja312271c

  日期：2013.3.13

  An efficient and regioselective ruthenium-catalyzed hydroaminomethlyation of olefins is reported. Key to success is the use of specific 2-phosphino-substituted imidazole ligands and triruthenium dodecacarbonyl as catalyst. Both industrially important aliphatic as well as various functionalized olefins react with primary and secondary amines to give the corresponding secondary and tertiary amines generally in high yields (up to 96%) and excellent regioselectivities (n/iso up to 99:1).