1-Nitro-2-piperidino-ethan | 702-01-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 1-Nitro-2-piperidino-ethan
• 英文别名: N-<2-Nitro-aethyl>-piperidin；1-(2-nitro-ethyl)-piperidine；1-(2-Nitroethyl)piperidine
• CAS: 702-01-2
• 化学式: C₇H₁₄N₂O₂
• 分子量: 158.2
• InChiKey: MRVVARZYSLLFKK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  49.1
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  哌啶 、 2-(Benzoyloxy)-1-Nitroethane 以 乙醇 为溶剂， 反应 7.0h， 以94%的产率得到1-Nitro-2-piperidino-ethan
  参考文献：
  名称：

  An Improved Procedure for the Preparation of β-Nitroethylamines

  摘要：

  硝基乙烯和δ-硝基苯乙烯分别由 2-苯甲酰氧基-1-硝基乙烷和 2-苯甲酰氧基-1-硝基-1-苯基乙烷原位生成，它们与脂肪族胺反应生成相应的迈克尔加合物，产率接近定量。

  DOI：

  10.1055/s-1991-26499

文献信息

• HETEROCYCLIC AMIDE COMPOUNDS AS PROTEIN KINASE INHIBITORS
  申请人：Reddy Panduranga Adulla P.

  公开号：US20120208826A1

  公开（公告）日：2012-08-16

  The present invention relates to heterocyclic amide derivatives of Formula (I): Formula (I) wherein the variables are as defined in the specification. The present invention further relates to compositions comprising said heterocyclic amide derivatives of formula (I) and methods for using said heterocyclic amide derivatives of formula (I) for treating or preventing a disease or disorder related to the activity of a protein kinase, in particular, a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal infection.

  本发明涉及式(I)的杂环酰胺衍生物：式(I)其中变量如规范中所定义。本发明还涉及包含式(I)的上述杂环酰胺衍生物的组合物以及使用式(I)的上述杂环酰胺衍生物治疗或预防与蛋白激酶活性相关的疾病或障碍的方法，特别是增生性疾病、抗增生性障碍、炎症、关节炎、神经系统或神经退行性疾病、心血管疾病、脱发、神经疾病、缺血性损伤、病毒性疾病或真菌感染。
• METHOD FOR SYNTHESIS OF ELIGLUSTAT AND INTERMEDIATE COMPOUNDS THEREOF
  申请人：Zhejiang Ausun Pharmaceutical Co., Ltd.

  公开号：EP3611171A1

  公开（公告）日：2020-02-19

  The present invention relates to a process for synthesis of Eliglustat and intermediate compounds thereof. In particular, the present invention belongs to the field of synthesis of organic compounds, relates to a process for synthesis of Eliglustat and pharmaceutically acceptable salts thereof, and relates to the intermediate compounds used in the process and a process for preparation of the intermediate compounds. Compared with the existing synthetic processes, the process for preparing Eliglustat according to the present invention utilizes novel intermediates and steps for synthesis, has advantages of convenient operations, high yield, good purity of intermediates and desired product, and it is easy to apply the process in the industrial production..

  本发明涉及一种艾格司他及其中间体化合物的合成工艺。具体而言，本发明属于有机化合物合成领域，涉及一种艾格司他及其药学上可接受的盐的合成工艺，并涉及该工艺中使用的中间体化合物以及中间体化合物的制备工艺。与现有的合成工艺相比，根据本发明制备依格司他的工艺利用了新颖的中间体和合成步骤，具有操作方便、收率高、中间体和所需产物纯度好、易于应用于工业生产等优点。
• US5750802A
  申请人：——

  公开号：US5750802A

  公开（公告）日：1998-05-12
• US8669259B2
  申请人：——

  公开号：US8669259B2

  公开（公告）日：2014-03-11
• An Improved Procedure for the Preparation of β-Nitroethylamines
  作者：Achille Barco、Simonetta Benetti、Gian Piero Pollini、Giampiero Spalluto

  DOI：10.1055/s-1991-26499

  日期：——

  Nitroethylene and α-nitrostyrene, generated in situ from 2-benzoyloxy-1-nitroethane and 2-benzoyloxy-1-nitro-1-phenyl-ethane respectively, reacted with aliphatic amines to give the corresponding Michael adducts in near quantitative yield.

  硝基乙烯和δ-硝基苯乙烯分别由 2-苯甲酰氧基-1-硝基乙烷和 2-苯甲酰氧基-1-硝基-1-苯基乙烷原位生成，它们与脂肪族胺反应生成相应的迈克尔加合物，产率接近定量。