N-(2-Iod-ethyl)-anilin | 115151-90-1

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N-(2-Iod-ethyl)-anilin
• 英文别名: N-(2-iodoethyl)aniline
• CAS: 115151-90-1
• 化学式: C₈H₁₀IN
• 分子量: 247.079
• InChiKey: MQFWRHQNJYVOEX-UHFFFAOYSA-N

物化性质

• 沸点：
  299.0±23.0 °C(Predicted)
• 密度：
  1.713±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  10
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  N-苯基乙醇胺 在 四丁基碘化铵 、 三苯基膦 、 2,3-二氯-5,6-二氰基-1,4-苯醌 作用下， 以 二氯甲烷 为溶剂， 以92%的产率得到N-(2-Iod-ethyl)-anilin
  参考文献：
  名称：

  三苯基膦/ 2,3-二氯-5,6-二氰基苯并醌是一种新的，选择性的中性体系，可在卤离子存在下将醇，硫醇和硒醇轻松转化为卤代烷

  摘要：

  在CH 2 Cl 2中的三苯膦（Ph 3 P）和2,3-二氯-5,6-二氰基苯并醌的混合物提供了一种络合物，该络合物在R 4 NX（X = Cl，Br，I）存在下转化为醇，硫醇在室温下以高收率将硒醇和硒醇转化为其相应的烷基卤。该方法对于在2°的醇存在下1°醇的转化以及在3°的醇，硫醇，环氧化物，三甲基甲硅烷基和四氢吡喃基醚，1,3二噻烷，二硫化物和酰胺。

  DOI：

  10.1016/s0040-4020(02)01089-x

文献信息

• Synergetic activation of CO₂ by the DBU-organocatalyst and amine substrates towards stable carbamate salts for synthesis of oxazolidinones
  作者：Xiao-Chao Chen、Kai-Chun Zhao、Yin-Qing Yao、Yong Lu、Ye Liu

  DOI：10.1039/d1cy01298c

  日期：——

  under mild conditions (80–100 °C, 12 h, 1.0 MPa CO2). Control experiments demonstrated that the formation of an ion-pair carbamate salt intermediate IS-B derived from the reaction of CO2, DBU (catalyst) and an amine (substrate) was the key step for this three-component reaction. The available DBU–amine–CO2 adduct intermediate (like IS-B-2) with fair stability will evolve into the thermodynamically stable

  将CO 2转化为有价值的化学品的有效方法的开发引起了关于CO 2利用的挑战性问题的越来越多的关注。在此，DBU 有机超强碱催化CO 2、伯（脂肪族/芳香族）胺和 1,2-二氯乙烷（或其衍生物）制备恶唑烷酮的有效方法在温和条件下获得了 47-97% 的产率(80–100 °C, 12 h, 1.0 MPa CO 2 )。对照实验表明，由 CO 2反应生成的离子对氨基甲酸盐中间体IS-B、DBU（催化剂）和胺（底物）是这种三组分反应的关键步骤。可用的 DBU-胺-CO 2加合物中间体（如IS-B-2）在 1,2-二氯乙烷（或其衍生物）的攻击下，随着 DBU 的再生，将演变成热力学稳定的产物恶唑烷酮催化剂。或者，稳定性相对较差的 DBU-芳胺-CO 2加合物（如IS-B-1）的分解也可能导致 1,2-二氯乙烷（或其衍生物）与芳胺的竞争性取代反应。这项工作提供了对 DBU 催化剂和亲核胺底物协同 CO
• Use of GAL 3 receptor antagonists for the treatment of depression and /or anxiety and compounds useful in such methods
  申请人：H. Lundbeck A/S

  公开号：EP2140862A2

  公开（公告）日：2010-01-06

  This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

  本发明涉及嘧啶和吲哚酮衍生物，它们是 GAL3 受体的选择性拮抗剂。本发明提供了一种药物组合物，它包含治疗有效量的本发明化合物和药学上可接受的载体。本发明还提供了一种由治疗有效量的本发明化合物和药学上可接受的载体组合而成的药物组合物。本发明进一步提供了一种药物组合物的制造工艺，该工艺包括将治疗有效量的本发明化合物与药学上可接受的载体相结合。本发明还提供了一种治疗抑郁症和/或焦虑症患者的方法，该方法包括向患者施用有效量的本发明化合物，以治疗患者的抑郁症和/或焦虑症。本发明还提供了一种治疗受试者抑郁症和/或焦虑症的方法，该方法包括向受试者施用一种组合物，该组合物包含药学上可接受的载体和治疗有效量的GAL3受体拮抗剂。
• COMBINATION PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
  申请人：Intellikine, LLC

  公开号：EP2705181B1

  公开（公告）日：2016-12-21
• [EN] KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE<br/>[FR] COMPOSÉS INHIBITEURS DE KINASE, COMPOSITIONS ET PROCÉDÉS D'UTILISATION
  申请人：ICAHN SCHOOL MED MOUNT SINAI

  公开号：WO2020142485A1

  公开（公告）日：2020-07-09

  Disclosed herein are kinase inhibitor compounds having structure (I), or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R1, R2, R3, R4, R5, R6, R7, X, Y, Z, and (AA) are as defined herein. Also disclosed are compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.
• Triphenylphosphine/2,3-dichloro-5,6-dicyanobenzoquinone as a new, selective and neutral system for the facile conversion of alcohols, thiols and selenols to alkyl halides in the presence of halide ions
  作者：N Iranpoor、H Firouzabadi、Gh Aghapour、A.R Vaez zadeh

  DOI：10.1016/s0040-4020(02)01089-x

  日期：2002.10

  6-dicyanobenzoquinone in CH2Cl2 affords a complex which in the presence of R4NX (X=Cl, Br, I) converts alcohols, thiols and selenols into their corresponding alkyl halides in high yields at room temperature. The method is highly selective for the conversion of 1° alcohols in the presence of 2° ones and also 1° and 2° alcohols in the presence of 3° alcohols, thiols, epoxides, trimethylsilyl- and tetrahydropyranyl

  在CH 2 Cl 2中的三苯膦（Ph 3 P）和2,3-二氯-5,6-二氰基苯并醌的混合物提供了一种络合物，该络合物在R 4 NX（X = Cl，Br，I）存在下转化为醇，硫醇在室温下以高收率将硒醇和硒醇转化为其相应的烷基卤。该方法对于在2°的醇存在下1°醇的转化以及在3°的醇，硫醇，环氧化物，三甲基甲硅烷基和四氢吡喃基醚，1,3二噻烷，二硫化物和酰胺。