2',4'-dichlorobiphenyl-4-amine | 939757-52-5

• 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: 2',4'-dichlorobiphenyl-4-amine
• 英文别名: 2',4'-Dichloro-[1,1'-biphenyl]-4-amine；4-(2,4-dichlorophenyl)aniline
• CAS: 939757-52-5
• 化学式: C₁₂H₉Cl₂N
• 分子量: 238.116
• InChiKey: JOEYVWJDOFQLJM-UHFFFAOYSA-N

物化性质

• 沸点：
  348.6±27.0 °C(Predicted)
• 密度：
  1.316±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2',4'-dichlorobiphenyl-4-amine 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 三乙酰氧基硼氢化钠 、 potassium carbonate 、 溶剂黄146 作用下， 以 1,4-二氧六环 、 水 、 1,2-二氯乙烷 为溶剂， 反应 32.0h， 生成 ethyl 3-(5-(2-(((2',4'-dichloro-[1,1'-biphenyl]-4-yl)amino)methyl)-5-(trifluoromethyl)phenyl)picolinamido)propanoate
  参考文献：
  名称：

  PICOLINAMIDO-PROPANOIC ACID DERIVATIVES USEFUL AS GLUCAGON RECEPTOR ANTAGONISTS

  摘要：

  本发明涉及吡咯烷酰基丙酸衍生物，含有它们的药物组合物以及它们在治疗和/或预防通过拮抗一个或多个胰高血糖素受体而改善的疾病和症状中的用途，包括例如代谢性疾病，如2型糖尿病和肥胖症。

  公开号：

  US20120302610A1
• 作为产物：
  描述：

  2,4-二氯苯硼酸 、 对碘苯胺 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride potassium carbonate 作用下， 以 1,4-二氧六环 、 水 为溶剂， 反应 16.0h， 生成 2',4'-dichlorobiphenyl-4-amine
  参考文献：
  名称：

  PICOLINAMIDO-PROPANOIC ACID DERIVATIVES USEFUL AS GLUCAGON RECEPTOR ANTAGONISTS

  摘要：

  本发明涉及吡咯烷酰基丙酸衍生物，含有它们的药物组合物以及它们在治疗和/或预防通过拮抗一个或多个胰高血糖素受体而改善的疾病和症状中的用途，包括例如代谢性疾病，如2型糖尿病和肥胖症。

  公开号：

  US20120302610A1

文献信息

• Biphenyl derivatives useful as glucagon receptor antagonists
  申请人：Chakravarty Devraj

  公开号：US09045389B2

  公开（公告）日：2015-06-02

  The present invention is directed to biphenyl derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.

  本发明涉及二苯基衍生物、含有它们的制药组合物及其在治疗和/或预防通过拮抗一个或多个胰高血糖素受体改善的疾病和病况中的应用，包括代谢性疾病，如II型糖尿病和肥胖症。
• Picolinamido-propanoic acid derivatives useful as glucagon receptor antagonists
  申请人：Chakravarty Devraj

  公开号：US08748624B2

  公开（公告）日：2014-06-10

  The present invention is directed to picolanmido-propanoic acid derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.

  本发明涉及吡可酰胺丙酸衍生物、含有它们的药物组合物以及它们在治疗和/或预防通过拮抗一个或多个胰高血糖素受体改善的疾病和状况中的应用，包括代谢性疾病，如2型糖尿病和肥胖症。
• N-substituted oligomers and methods for their synthesis, e.g. polyglycine bearing nucleic acid bases
  申请人：CHIRON CORPORATION

  公开号：EP1258492A1

  公开（公告）日：2002-11-20

  Poly N-substituted Glycines (poly NSGs), wherein the substituents bear purine or pyrimidine bases (R9) every second glycine: In addition, a solid phase method for the synthesis of N-substituted oligomers of more general structures is disclosed.The poly NSGs obtainable by this method can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two "sub-monomers" directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound α-haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using the automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.

  聚 N-取代甘氨酸（poly NSGs），其中每第二个甘氨酸的取代基都带有嘌呤或嘧啶碱（R9）： 此外，还公开了一种用于合成更一般结构的 N-取代低聚物的固相方法。通过这种方法获得的聚 NSG 可以具有多种侧链取代基。每个 N-取代甘氨酸单体由两个 "子单体 "直接在固体支持物上组装而成。每个单体加成循环包括两个步骤：(1) 用包含能被 -NH2 亲核置换的离去基团（如卤乙酸）的酰化剂将与载体结合的仲胺酰化，以及 (2) 通过离去基团的亲核置换引入侧链、(2) 通过亲核置换离去基团，如卤素（作为与树脂结合的 α-卤代乙酰胺）和足量的包含 -NH2 基团的第二亚单体，如伯胺、烷氧基胺、半肼、酰肼、肼基脲或类似物，引入侧链。重复酰化和置换两步循环，即可得到所需的低聚物。利用本方法的自动合成技术可高效合成多种低聚 NSG，这使得这些低聚物在生成和快速筛选各种肽模拟库方面具有吸引力。本发明公开的低聚物，如 N-取代甘氨酸（即多 NSG），提供了一类新的肽类化合物，这类化合物在自然界中并不存在，但可以通过合成获得，而且已被证明具有显著的生物活性和蛋白水解稳定性。
• NOVEL HYDRAZONE DERIVATIVE WITH ARYL OR HETEROARYL GROUP SUBSTITUTED AT TERMINAL AMINE GROUP THEREOF AND USE THEREOF
  申请人：Korea Institute of Science and Technology

  公开号：EP3901139A1

  公开（公告）日：2021-10-27

  The present invention relates to novel hydrazone derivatives in which a terminal amine group is substituted with an aryl group or a heteroaryl group, and uses thereof.

  本发明涉及末端胺基被芳基或杂芳基取代的新型腙衍生物及其用途。
• Selective inducible microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors derived from an oxicam template
  作者：Jane Wang、David Limburg、Jeff Carter、Gabriel Mbalaviele、James Gierse、Michael Vazquez

  DOI：10.1016/j.bmcl.2010.01.060

  日期：2010.3

  Here we describe the SAR of a series of potent and selective mPGES-1 inhibitors based on an oxicam template. Compound 13j demonstrated low nanomolar mPGES-1 inhibition in an enzyme assay. In addition, it displayed PGE(2) inhibition in a cell-based assay (0.42 mu M) and had over 238-fold selectivity for mPGES-1 over COX-2 and over 200-fold selectivity for mPGES-1 over 6-keto PGF(1 alpha). (C) 2010 Elsevier Ltd. All rights reserved.