4-(2-phenylpropyl)morpholine

• 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-(2-phenylpropyl)morpholine
• 化学式: C₁₃H₁₉NO
• 分子量: 205.3
• InChiKey: WRENTAXEJRYOTE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 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：

  2-苯基丙酸 在 bis(1,5-cyclooctadiene)diiridium(I) dichloride 、 苯硅烷 作用下， 以 甲苯 为溶剂， 反应 18.0h， 生成 4-(2-phenylpropyl)morpholine
  参考文献：
  名称：

  使用羧酸催化胺的还原性N-烷基化

  摘要：

  我们报告了伯胺或仲胺与羧酸的催化还原烷基化反应。两阶段过程涉及硅烷介导的直接酰胺化，然后进行催化还原。

  DOI：

  10.1039/c5cc08881j

文献信息

• Hydrogen-free reductive amination using iron pentacarbonyl as a reducing agent
  作者：Oleg I. Afanasyev、Dmitry L. Usanov、Denis Chusov

  DOI：10.1039/c7ob02795h

  日期：——

  We developed solvent-free reductive amination without an external hydrogen source using iron pentacarbonyl as a reducing agent. Neither a catalyst nor any other additives were employed. Various types of substrates are suitable for the reaction, including those with low reactivity, e.g. benzophenone. Among others, the protocol tolerates bromo-, cyano-, benzyloxy-, pyrimidyl and styryl moieties.

  我们使用五羰基铁作为还原剂，开发了无溶剂的无需外部氢源的还原胺化方法。既未使用催化剂也未使用任何其他添加剂。各种类型的底物都适合该反应，包括低反应性的底物，例如二苯甲酮。其中，该方案耐受溴，氰基，苄氧基，嘧啶基和苯乙烯基部分。
• Carbon monoxide-driven osmium catalyzed reductive amination harvesting WGSR power
  作者：Klim O. Biriukov、Mikhail M. Vinogradov、Oleg I. Afanasyev、Dmitry V. Vasilyev、Alexey A. Tsygankov、Maria Godovikova、Yulia V. Nelyubina、Dmitry A. Loginov、Denis Chusov

  DOI：10.1039/d1cy00695a

  日期：——

  First osmium-catalyzed reductive amination under the water gas–shift reaction conditions was developed. Proposed catalytic system demonstrates high performance even at the catalyst loading as low as 0.0625 mol%.

  首次在水煤气转移反应条件下开发了铂催化的还原胺化反应。提出的催化体系表现出高性能，即使在催化剂负载量仅为0.0625 mol% 时也是如此。
• NOVEL BENZAMIDE DERIVATIVE AND USE THEREOF
  申请人：VIVOZON, INC.

  公开号：US20140336378A1

  公开（公告）日：2014-11-13

  Disclosed are a novel benzamide derivative and pharmaceutical use thereof, and more particularly, a novel benzamide derivative having a structure of Formula 1 or pharmaceutically acceptable salts thereof, and a composition for prevention or treatment of pain or itching including the above material. The novel benzamide derivative and pharmaceutically acceptable salt thereof according to the present invention exhibit excellent pain-suppressive effect and, in particular, pain-suppressive effect in not only a neuropathic animal model but also other models such as a formalin model, and therefore, may be used in suppression of different pains such as nociceptive pain, chronic pain, etc. Further, since it was demonstrated that the present invention displays anti-pruritic efficacy even in an itching model, to which a mechanism and treatment concept established with respect to pain is applied, the present invention may also be effectively used in radical treatment of atopic dermatitis by applying the inventive product to an anti-pruritic composition in order to suppress an initial itching stage and treat symptoms thereof, thus preventing skin damage or inflammation after the scratching stage.

  揭示了一种新的苯甲酰胺衍生物及其药用，更具体地说，一种具有化学式1结构或其药用盐的新苯甲酰胺衍生物，以及包括上述材料的用于预防或治疗疼痛或瘙痒的组合物。根据本发明，所述新的苯甲酰胺衍生物及其药用盐表现出优异的镇痛效果，特别是在不仅神经病理动物模型中而且其他模型如福尔马林模型中表现出的镇痛效果，因此，可用于抑制不同类型的疼痛，如伤害性疼痛、慢性疼痛等。此外，由于证明了本发明在瘙痒模型中显示出抗瘙痒功效，应用于疼痛方面建立的机制和治疗概念，因此，本发明还可通过将创新产品应用于抗瘙痒组合物中，以抑制初始瘙痒阶段并治疗其症状，从而预防刮痒阶段后的皮肤损伤或炎症。
• Base-catalyzed amination of olefins: an example of an environmentally friendly synthesis of amines
  作者：Matthias Beller、C Breindl

  DOI：10.1016/s0045-6535(00)00319-2

  日期：2001.4

  The base-catalyzed amination of aromatic olefins is described as an environmentally friendly synthesis of various beta-arylethylamines. Primary and secondary aliphatic amines as well as aromatic amines react with styrene derivatives to give the corresponding beta-arylethylamines in high yield up to 99%. While aliphatic amines react with styrenes in the presence of n-BuLi as the pre-catalyst, anilines

  芳族烯烃的碱催化胺化反应被描述为各种β-芳基乙胺的环保合成方法。伯和仲脂族胺以及芳族胺与苯乙烯衍生物反应生成相应的β-芳基乙胺，产率高达99％。尽管脂族胺在正丁基锂存在下作为催化剂与苯乙烯反应，但苯胺可以使用KOtBu作为催化剂进行烯化。
• One-Pot Synthesis of Secondary and Tertiary Amines by Carbonylative Hydroaminomethylation of Alkenes Catalyzed by Di(μ-chloro)bis(η4-1,5-cyclooctadiene)dirhodium
  作者：Thorsten Rische、Peter Eilbracht

  DOI：10.1055/s-1997-1338

  日期：1997.11

  Secondary and tertiary amines are selectively prepared with high yields by the reaction of alkenes with primary or secondary amines, carbon monoxide and hydrogen in the presence of [Rh(cod)Cl]2 as catalyst via a one-pot hydroformylation - amine condensation - reduction sequence.

  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。