1-甲基-1-吡啶-4-基肼 | 76890-04-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 1-甲基-1-吡啶-4-基肼
• 英文名称: 4-(N-methyl-hydrazino)-pyridine
• 英文别名: 1-methyl-1-(4-pyridinyl)hydrazine；4-(1-Methylhydrazin-1-yl)pyridine；1-methyl-1-pyridin-4-ylhydrazine
• CAS: 76890-04-5
• 化学式: C₆H₉N₃
• mdl: MFCD13175363
• 分子量: 123.158
• InChiKey: XWEFKJNJSVXMOD-UHFFFAOYSA-N

物化性质

• 沸点：
  235.4±13.0 °C(Predicted)
• 密度：
  1.142±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.166
• 拓扑面积：
  42.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-甲基-1-吡啶-4-基肼 在 lithium aluminium tetrahydride 、 magnesium sulfate 作用下， 以 四氢呋喃 、 乙醇 为溶剂， 生成 2-[3-(3-Methoxyphenyl)propyl]-1-methyl-1-pyridin-4-ylhydrazine
  参考文献：
  名称：

  Merriman, Gregory H.; Fink, David M.; Freed, Brian S., Synlett, 2000, # 1, p. 137 - 139

  摘要：

  DOI：
• 作为产物：
  描述：

  4-氯吡啶盐酸盐 、 甲基肼 以 乙醇 为溶剂， 以73%的产率得到1-甲基-1-吡啶-4-基肼
  参考文献：
  名称：

  Synthetic nanoparticles for selective hydrolysis of bacterial autoinducers in quorum sensing

  摘要：

  N-acyl homoserine lactones (AHLs) are signal molecules used by a large number of gram-negative bacteria in quorum sensing and their hydrolysis is known to inhibit biofilm formation. Micellar imprinting of AHL-like templates with catalytic functional monomers yielded water-soluble nanoparticles with AHL-shaped active site and nearby catalytic groups. Either Lewis acidic zinc ions or nucleophilic pyridyl ligands could be introduced through this strategy, yielding artificial enzymes for the hydrolysis of AHLs in a substrate-selective fashion.

  DOI：

  10.1016/j.bmcl.2019.02.016

文献信息

• 3-PYRIDINE CARBOXYLIC ACID HYDRAZIDES
  申请人：Grether Uwe

  公开号：US20130065876A1

  公开（公告）日：2013-03-14

  The present invention relates to compounds of formula I, wherein R 1 to R 5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof. The present invention relates also to the manufacture of said compounds, pharmaceutical compositions containing them and methods for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.

  本发明涉及公式I的化合物，其中R1至R5在描述和权利要求中定义，并且其药学上可接受的盐。本发明还涉及所述化合物的制备，含有它们的药物组合物以及用于治疗和/或预防可以用HDL-胆固醇升高剂治疗的疾病的方法，例如脂质代谢异常、动脉粥样硬化和心血管疾病。
• Tri-substituted acylhydrazines as tertiary amide bioisosteres: HCV NS5B polymerase inhibitors
  作者：Eda Canales、Joseph S. Carlson、Todd Appleby、Martijn Fenaux、Johnny Lee、Yang Tian、Neeraj Tirunagari、Melanie Wong、William J. Watkins

  DOI：10.1016/j.bmcl.2012.05.025

  日期：2012.7

  The use of a tri-substituted acylhydrazine as an isostere of a tertiary amide was explored in a series of HCV NS5B thumb site II inhibitors. Direct replacement generated an analog with similar conformational and physicochemical properties. The series was extended to produce compounds with potent binding affinities and encouraging levels of cellular potency.

  在一系列 HCV NS5B 拇指位点 II 抑制剂中探索了使用三取代的酰基肼作为叔酰胺的等排体。直接替换产生具有相似构象和物理化学性质的类似物。该系列被扩展为生产具有有效结合亲和力和令人鼓舞的细胞效力水平的化合物。
• [EN] 3 -PYRIDINE CARBOXYLIC ACID HYDRAZIDES AS HDL-CHOLESTEROL RAISING AGENTS<br/>[FR] HYDRAZIDES D'ACIDE 3-PYRIDINE-CARBOXYLIQUE EN TANT QU'AGENTS D'ÉLÉVATION DU CHOLESTÉROL HDL
  申请人：HOFFMANN LA ROCHE

  公开号：WO2013037703A1

  公开（公告）日：2013-03-21

  The present invention relates to compounds of the formula wherein R1 to R5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.

  本发明涉及以下式中R1至R5在描述和权利要求中定义的化合物，以及其药学上可接受的盐，它们的制备，含有它们的药物组合物以及它们作为治疗和/或预防可用高密度脂蛋白胆固醇升高剂治疗的疾病的药物的用途，例如特别是脂质代谢异常，动脉粥样硬化和心血管疾病。
• N-(pyridinylamino) isoindolines and related compounds
  申请人：Hoechst Marion Roussel, Inc.

  公开号：US06004977A1

  公开（公告）日：1999-12-21

  Novel N-(pyridinylamino)isoindolines and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the N-(pyridinylamino)isoindolines and related compounds, the intermediates or compositions thereof are disclosed.

  小说N-(吡啶基氨基)异吲哚和相关化合物，其制备的中间体和方法，以及利用N-(吡啶基氨基)异吲哚和相关化合物、中间体或其组合物缓解记忆功能障碍和治疗抑郁症的方法被披露。
• [EN] PROTEASE INHIBITORS<br/>[FR] INHIBITEURS DE PROTEASES
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2000038687A1

  公开（公告）日：2000-07-06

  The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

  本发明提供了4-氨基-氮杂丙烷-3-酮蛋白酶抑制剂及其药学上可接受的盐、水合物和溶剂化物，其能够抑制蛋白酶，包括卡他普西蛋白酶K，还提供了这些化合物的制药组合物、这些化合物的新中间体以及用于治疗过度骨质流失或软骨或基质降解等疾病的方法，包括骨质疏松症；牙龈疾病，包括牙龈炎和牙周炎；关节炎，更具体地说是骨关节炎和类风湿性关节炎；帕吉特病；恶性高钙血症；以及代谢性骨病，通过向需要的患者施用本发明化合物来抑制骨质流失或过度软骨或基质降解。