octahydro-5,5-dimethylindolizin | 1258963-09-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚里西啶
• 英文名称: octahydro-5,5-dimethylindolizin
• 英文别名: 5,5-dimethyl-2,3,6,7,8,8a-hexahydro-1H-indolizine
• CAS: 1258963-09-5
• 化学式: C₁₀H₁₉N
• 分子量: 153.268
• InChiKey: VAQVHNRNGLQNKG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  5,5-Dimethyl-6,7-dihydroindolizin-8-one 在 5% Pd(II)/C(eggshell) 、 氢气 作用下， 以 溶剂黄146 为溶剂， 20.0 ℃ 、1.0 MPa 条件下， 反应 24.0h， 以41%的产率得到octahydro-5,5-dimethylindolizin
  参考文献：
  名称：

  Straightforward synthesis of indolizidine alkaloid 167B

  摘要：

  The synthetic access to indolizidines, substituted in C-5 position, was reported with good diastereoselectivity. The strategy developed was based on a key step of Michael addition associated with a Clauson-Kaas condensation. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2010.09.105

文献信息

• Protein kinase C inhibitors and uses thereof
  申请人：Rigel Pharmaceuticals, Inc.

  公开号：US10005777B2

  公开（公告）日：2018-06-26

  This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

  本公开涉及的化合物可作为蛋白激酶 C (PKC) 的抑制剂，因此可用于治疗通过 PKC 的活性介导或维持的各种疾病和失调。本公开还涉及包含这些化合物的药物组合物、使用这些化合物治疗各种疾病和失调的方法、制备这些化合物的工艺以及在这些工艺中有用的中间体。
• PROTEIN KINASE C INHIBITORS AND USES THEREOF
  申请人：Rigel Pharmaceuticals, Inc.

  公开号：EP2833889B1

  公开（公告）日：2017-11-01
• Protein Kinase C Inhibitors and Uses Thereof
  申请人：Rigel Pharmaceuticals, Inc.

  公开号：US20170360786A1

  公开（公告）日：2017-12-21

  This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
• US4526969A
  申请人：——

  公开号：US4526969A

  公开（公告）日：1985-07-02
• US4599343A
  申请人：——

  公开号：US4599343A

  公开（公告）日：1986-07-08