isopropyl 2-morpholinoacetate | 121777-38-6

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: isopropyl 2-morpholinoacetate
• 英文别名: Isopropyl-2-morpholinoacetate；propan-2-yl 2-morpholin-4-ylacetate
• CAS: 121777-38-6
• 化学式: C₉H₁₇NO₃
• mdl: MFCD16041161
• 分子量: 187.239
• InChiKey: GQWWHLUNKDBIGM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.888
• 拓扑面积：
  38.8
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  吗啉-4-基苯甲酸酯 、 醋酸异丙酯 在 Zn(TMP)₂ 、 2,2'-联吡啶 、 copper dichloride 作用下， 以 甲苯 、 四氢呋喃 为溶剂， 反应 1.0h， 以94%的产率得到isopropyl 2-morpholinoacetate
  参考文献：
  名称：

  通过O-酰基羟胺对烯醇锌的双重反应，对酯和酰胺进行选择性α-氨基化和α-酰化。

  摘要：

  酯和酰胺的选择性α-胺化和α-酰化已经开发出来，采用O-酰基羟胺作为双反应性胺化和酰化试剂。用O-酰基羟胺处理烯醇锌可以在温和的条件下仅提供1,3-二羰基化合物。将铜催化剂引入系统会完全改变反应性，仅产生α-胺化产物。

  DOI：

  10.1039/c3cc49296f

文献信息

• Fluorene Derivative or Pharmaceutically Acceptable Salt Thereof, Preparation Method Therefor, and Pharmaceutical Composition Comprising Same as Effective Ingredient for Preventing or Treating HCV-Related Disease
  申请人：Seoul National University R&DB Foundation

  公开号：US20200231573A1

  公开（公告）日：2020-07-23

  The present invention relates to a fluorene derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition comprising the same as an effective ingredient for preventing or treating HCV-related disease. A fluorene derivative according to the present invention is identified to exhibit an antiviral performance against not only HCV, but also highly against HCV mutants, particularly double mutants and thus can be used in a pharmaceutical composition for prevention or treatment of HCV-caused liver disease, such as acute hepatitis C, chronic hepatitis C, liver cirrhosis, hepatocellular cancer, etc., particularly, liver disease caused by mutants of HCV. The derivative can be useful in a pharmaceutical composition for prevention or treatment of HCV-related liver disease by which the problem of resistant mutation against conventional therapeutic agents is solved.

  本发明涉及一种芴衍生物或其药用可接受的盐，其制备方法以及包含其作为有效成分的用于预防或治疗HCV相关疾病的药物组合物。根据本发明，所述芴衍生物被确定为不仅对HCV表现出抗病毒性能，而且对HCV突变体表现出很高的抗性，尤其是双重突变体，因此可以用于制备预防或治疗HCV引起的肝病的药物组合物，如急性丙型肝炎、慢性丙型肝炎、肝硬化、肝细胞癌等，特别是由HCV突变体引起的肝病。该衍生物可用于制备预防或治疗HCV相关肝病的药物组合物，从而解决了对传统治疗药物的抗性突变问题。
• Epoxyketone compounds for enzyme inhibition
  申请人：CENTRAX INTERNATIONAL, INC.

  公开号：US10640533B2

  公开（公告）日：2020-05-05

  The present disclosure relates to novel compounds and pharmaceutical compositions thereof which are useful as inhibitors of proteasomes. The compounds provided herein have improved proteasome potency and selectivity, and increased aqueous solubility, and are useful in treating various conditions or diseases associated with proteasomes.

  本公开涉及可用作蛋白酶体抑制剂的新型化合物及其药物组合物。本文所提供的化合物具有更好的蛋白酶体效力和选择性，以及更高的水溶性，可用于治疗与蛋白酶体相关的各种病症或疾病。
• EPOXYKETONE COMPOUNDS FOR ENZYME INHIBITION
  申请人：CENTRAX INTERNATIONAL, INC.

  公开号：US20170158734A1

  公开（公告）日：2017-06-08

  The present disclosure relates to novel compounds and pharmaceutical compositions thereof which are useful as inhibitors of proteasomes. The compounds provided herein have improved proteasome potency and selectivity, and increased aqueous solubility, and are useful in treating various conditions or diseases associated with proteasomes.