N-(4-甲基-1H-咪唑-2-基)乙酰胺 | 160041-61-2

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: N-(4-甲基-1H-咪唑-2-基)乙酰胺
• 中文别名: N-(4-甲基-1H-咪唑基-2-基)乙酰胺
• 英文名称: N-(5-methyl-1H-imidazol-2-yl)acetamide
• 英文别名: imidazole, 2-acetamino-5-methyl-；2-acetamino-5-methyl imidazole；2-acetamino-5-methyl-imidazole；N-(4-methyl-1(3)H-imidazol-2-yl)-acetamide；2-Acetamido-4(5)-methylimidazol；N-(4-Methyl-1H-imidazol-2-yl)acetamide
• CAS: 160041-61-2
• 化学式: C₆H₉N₃O
• mdl: MFCD15474890
• 分子量: 139.157
• InChiKey: AIEWKBISOOGENG-UHFFFAOYSA-N

物化性质

• 密度：
  1.261±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.333
• 拓扑面积：
  57.8
• 氢给体数：
  2
• 氢受体数：
  2

安全信息

• 海关编码：
  2933290090

反应信息

• 作为反应物：
  描述：

  N-(4-甲基-1H-咪唑-2-基)乙酰胺 在 硫酸 作用下， 以 甲醇 、 水 为溶剂， 反应 24.0h， 以82%的产率得到5-甲基-1H-咪唑-2-胺
  参考文献：
  名称：

  A Simple and Practical Synthesis of 2-Aminoimidazoles

  摘要：

  A new and simple two-step procedure to synthesize 2-aminoimidazoles (2-AI's) from readily available materials has been developed. The cyclization reaction of alpha-halo ketones and N-acetylguanidine in acetonitrile (MeCN) at reflux, or in dimethylformamide (DMF) at ambient temperature, gives 4(5)-substituted and 4,5-disubstituted N-(1H-imidazol-2-yl)acetamides, which are then hydrolyzed to their respective 2-AI's. In general, the purified products were isolated in good yields. We have prepared several examples and have demonstrated the usefulness of this method by its application in the total synthesis of 8, an interesting histamine analog, and oroidin, 15, a marine natural product isolated from various sponges.

  DOI：

  10.1021/jo00103a021
• 作为产物：
  描述：

  N-乙酰基胍 、 一氯丙酮 在 氩 、 水 作用下， 以 乙腈 为溶剂， 反应 12.0h， 以to give 0.324 g N-(4-methyl-1H-imidazol-2-yl)acetamide的产率得到N-(4-甲基-1H-咪唑-2-基)乙酰胺
  参考文献：
  名称：

  JAK-2 modulators and methods of use

  摘要：

  本发明涉及蛋白酪氨酸激酶及其抑制剂领域。具体来说，本发明涉及JAK-2的抑制剂、用于抑制JAK-2的化合物的制药组合物、在细胞中抑制JAK-2的方法，包括将需要抑制JAK-2的细胞与本发明的化合物或制药组合物中含有的化合物接触。本发明还包括治疗涉及JAK-2的疾病或病症的方法，包括向患者投与本发明的化合物组成的制药组合物。

  公开号：

  US08088767B2

文献信息

• JAK-2 Modulators and Methods of Use
  申请人：Galan Adam Antoni

  公开号：US20100136136A1

  公开（公告）日：2010-06-03

  This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that involves JAK-2 comprising administering to a patient a pharmaceutical composition comprising a compound according to the invention.

  本发明涉及蛋白酪氨酸激酶及其抑制剂领域。具体而言，本发明涉及JAK-2的抑制剂，以及用于抑制JAK-2的化合物的制药组合物，包括通过将含有本发明化合物的化合物或制药组合物与需要抑制JAK-2的细胞接触来抑制JAK-2的细胞方法。本发明还包括治疗涉及JAK-2的疾病或病状的方法，包括向患者施用包含本发明化合物的制药组合物。
• COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS
  申请人：Charmot Dominique

  公开号：US20120263670A1

  公开（公告）日：2012-10-18

  The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.

  本公开涉及化合物和方法，用于治疗与液体潴留或盐过载相关的疾病，如心力衰竭（特别是充血性心力衰竭）、慢性肾脏病、终末期肾脏病、肝病和过氧化物酶体增殖物激活受体（PPAR）γ激动剂引起的液体潴留。本公开还涉及化合物和方法，用于治疗高血压。本公开还涉及化合物和方法，用于治疗胃肠道疾病，包括治疗或减轻与胃肠道疾病相关的疼痛。
• COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDER
  申请人：Ardelyx, Inc.

  公开号：US20150190389A1

  公开（公告）日：2015-07-09

  The present disclosure is directed to compounds of the structure (X): CoreL-NHE) n (X) wherein: n is 2 or 3; NHE has the structure wherein: R 1 is H or —SO 2 —NR 7 R 8 —; R 2 is selected from H, —NR 7 (CO)R 8 , —SO 2 —NR 7 R 8 — and —NR 7 R 8 ; R 3 is hydrogen; R 7 is hydrogen; R 8 is a bond linking to L; L is a polyalkylene glycol linker; and Core has the following structure: wherein: X is selected from the group consisting of a bond, —O—, —NH—, NHC(═O)—, —NHC(═O)NH— and —NHSO 2 —; and Y is selected from the group consisting of a bond, optionally substituted C 1-6 alkylene, optionally substituted benzene, pyridinyl, a polyethylene glycol linker and —(CH 2 ) 1-6 O(CH 2 ) 1-6 —, and methods of using such compounds for the treatment of irritable bowel syndrome, chronic kidney disease and end-stage renal disease.

  本公开涉及结构为（X）：CoreL-NHE)n（X）的化合物，其中：n为2或3；NHE具有以下结构：其中：R1为H或—SO2—NR7R8—；R2选自H，—NR7（CO）R8，—SO2—NR7R8—和—NR7R8；R3为氢；R7为氢；R8为连接到L的键；L为多聚乙二醇连接剂；Core具有以下结构：其中：X选自由键，—O—，—NH—，NHC（═O）—，—NHC（═O）NH—和—NHSO2—；Y选自键，可选择性地取代的C1-6烷基，可选择性地取代的苯，吡啶基，聚乙二醇连接剂和—（CH2）1-6O（ ）1-6—，以及使用这种化合物治疗肠易激综合征、慢性肾脏病和终末期肾脏疾病的方法。
• Diphenyl Substituted Alkanes
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2546232A1

  公开（公告）日：2013-01-16

  The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors: Compounds of Formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.

  本发明提供的式 I 化合物是 5-脂氧合酶活化蛋白抑制剂： 式 I 化合物可用作抗动脉粥样硬化、抗哮喘、抗过敏、抗炎和细胞保护剂。
• Methods and materials for reducing amyloid beta levels within a mammal
  申请人：THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORK

  公开号：US10639322B2

  公开（公告）日：2020-05-05

  This document provides methods and materials for reducing amyloid beta levels within a mammal (e.g. a mammal having Alzheimer's disease). For example, this document provides methods for using compositions containing a potato polysaccharide preparation to reduce one or more symptoms of Alzheimer's disease. In some cases, a composition containing a potato polysaccharide preparation provided herein can be used to increase binding, sequestration, and/or degradation of CNS-derived amyloid beta polypeptides, thereby inhibiting the formation of neurofibrillary plaques.

  本文提供了降低哺乳动物（如患有阿尔茨海默病的哺乳动物）体内淀粉样β水平的方法和材料。例如，本文提供了使用含有马铃薯多糖制剂的组合物减轻阿尔茨海默病的一种或多种症状的方法。在某些情况下，本文提供的含有马铃薯多糖制剂的组合物可用于增加中枢神经系统衍生的淀粉样β多肽的结合、螯合和/或降解，从而抑制神经纤维斑的形成。