1-(2-pyrazinyl)-(1H)-imidazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 1-(2-pyrazinyl)-(1H)-imidazole
• 英文别名: Pyrazine, 2-(1H-imidazol-1-yl)-；2-imidazol-1-ylpyrazine
• 化学式: C₇H₆N₄
• 分子量: 146.151
• InChiKey: WIVMRJUXSGKZRU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  11
• 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：
  43.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-(2-pyrazinyl)-(1H)-imidazole 、 2-溴乙酰胺 在 ammonium hexafluorophosphate 作用下， 生成 1-acetamido-3-(2-pyrazinyl)-imidazolium bromide
  参考文献：
  名称：

  A triple helical structure supported solely by C–H?O hydrogen bonding

  摘要：

  报告了一种由阳离子分子--1-乙酰氨基-3-(2-吡嗪基)-咪唑鎓--自组装的新型三重螺旋结构。计算分析表明，三重螺旋的形成是由 CâH?

  DOI：

  10.1039/c1cc15656j
• 作为产物：
  描述：

  咪唑 、 2-氯吡嗪 在 2-唑烷酮 、 copper(l) iodide 、 sodium methylate 作用下， 以 二甲基亚砜 为溶剂， 反应 16.0h， 以67%的产率得到1-(2-pyrazinyl)-(1H)-imidazole
  参考文献：
  名称：

  Oxazolidin-2-one as Efficient Ligand for the Copper-Catalyzed N-arylation of Pyrrole, Imidazole and Indole

  摘要：

  发现氧杂环丁烷-2-酮是一种便捷的配体，可用于通过应用碘化铜（CuI）催化对吡咯、吲哚和咪唑进行芳基和杂芳基的N-取代反应。该催化体系的易制备性、商业可获得性、较低的分子量以及广泛的底物适用性和取代基兼容性，使得氧杂环丁烷-2-酮在已经被应用于多种反应的铜催化方法中具有明显的优势。

  DOI：

  10.2174/157017810791112496

文献信息

• <i>N</i>,<i>N</i>′-(Phenylmethylene)diacetamide Analogues as Economical and Efficient Ligands in Copper-Catalyzed Arylation of Aromatic Nitrogen-Containing Heterocycles
  作者：Yuan-Jiang Pan、Jie-Ping Wan、Yun-Feng Chai、Jian-Mei Wu

  DOI：10.1055/s-0028-1087350

  日期：2008.12

  N,N′-(Phenylmethylene)diacetamide analogues which were simply prepared from the condensation reaction of an aldehyde with an amide or urea were found to be efficient ligands in copper-catalyzed coupling reaction of aryl halides with various azole nucleophiles. The newly developed ligand showed broad application scope in this conversion. Compounds including imidazoles, benzoimidazoles, pyrrole, indole, and benzotriazole were successfully arylated with diversified aromatic halides to give corresponding products in moderate to excellent yields.

  N,N′-(苯亚甲基)二乙酰胺类似物是通过醛与酰胺或尿素的缩合反应简单制备而成的，发现其在铜催化的芳基卤化物与各种杂环核苷酸的偶联反应中是有效的配体。新开发的配体在该转化过程中显示了广泛的应用范围。包括咪唑、苯并咪唑、呋喃、吲哚和苯并三唑等化合物成功地与多样化的芳香卤化物发生芳基化反应，得到相应的产物，产率中等到优秀。
• PROCESS FOR PREPARING ORTHO-METALLATED METAL COMPOUNDS
  申请人：Merck Patent GmbH

  公开号：US20200048289A1

  公开（公告）日：2020-02-13

  The present invention describes a process for producing tris-orthometalated metal compounds which can be used as coloring components as functional materials in a number of diverse applications that can be broadly attributed to the electronics industry.

  本发明描述了一种生产三正交金属化合物的过程，这些化合物可用作功能材料中的着色组分，在许多不同的应用中被广泛归因于电子工业。
• TREATMENT OF CANCERS USING PI3 KINASE ISOFORM MODULATORS
  申请人：Infinity Pharmaceuticals, Inc.

  公开号：EP3811974A1

  公开（公告）日：2021-04-28

  Provided herein is a PI3K inhibitor, alone or in combination with one or more other therapeutic agents, for use in treating or managing indolent non-Hodgkin's lymphoma (iNHL) in a subject that is, or is identified as, relapsed or refractory to a prior treatment with rituximab and the iNHL is refractory to chemotherapy or radioimmunotherapy (RIP), wherein the PI3K inhibitor is Compound 292 or a pharmaceutically acceptable salt, a hydrate or a solvate thereof. Furthermore the application relates to a PI3K inhibitor, alone or in combination with one or more other therapeutic agents, for use in treating or managing cancer or hematologic malignancy in a subject who developed resistance to a prior treatment, wherein the PI3K inhibitor is Compound 292, or a pharmaceutically acceptable salt, a hydrate or a solvate thereof, and wherein the prior treatment is a treatment with one or more BTK inhibitors, anti-CD20 antibodies, proteasome inhibitors, or alkylating agents.

  本发明提供了一种PI3K抑制剂，单独或与一种或多种其它治疗剂联合，用于治疗或控制对先前利妥昔单抗治疗复发或难治，且iNHL对化疗或放射免疫治疗（RIP）难治的受试者中的懒惰性非霍奇金淋巴瘤（iNHL），其中PI3K抑制剂是化合物292或其药学上可接受的盐、水合物或溶液。此外，本申请还涉及一种PI3K抑制剂，单独或与一种或多种其它治疗剂联合使用，用于治疗或控制对先前治疗产生耐药性的受试者的癌症或血液恶性肿瘤，其中PI3K抑制剂是化合物292或其药学上可接受的盐、水合物或溶液，而先前的治疗是一种或多种BTK抑制剂、抗CD20抗体、蛋白酶体抑制剂或烷化剂的治疗。
• <i>N</i>-Hydroxyimides as Efficient Ligands for the Copper-Catalyzed N-Arylation of Pyrrole, Imidazole, and Indole
  作者：Heng-Chang Ma、Xuan-Zhen Jiang

  DOI：10.1021/jo7015983

  日期：2007.11.1

  [GRAPHICS]An experimentally simple, efficient, and inexpensive catalyst system was developed for the N-arylation of pyrroles, indoles, and imidazole with aryl and heteroaryl iodides, bromides, and chlorides by applying CuI as catalyst, N-hydroxy-succinimide (L-1), N-hydroxymaleimide (L-2), or N-hydroxyphthalimide (L-3) as ligand, CH3ONa as base, and DMSO as solvent. A variety of functional groups are tolerated in the reaction, including those that are not compatible with Pd-catalyzed amidation methodology.
• LUMINESCENT PIGMENTS AND THEIR USE IN SECURITY APPLICATIONS
  申请人：Fábrica Nacional de Moneda Y Timbre - Real Casa de la Moneda

  公开号：EP2673335A1

  公开（公告）日：2013-12-18