<(2S)-piperidin-2-yl>-N-methylmethanamine

• 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: <(2S)-piperidin-2-yl>-N-methylmethanamine
• 英文别名: Methyl({[(2S)-piperidin-2-yl]methyl})amine；N-methyl-1-[(2S)-piperidin-2-yl]methanamine
• 化学式: C₇H₁₆N₂
• 分子量: 128.217
• InChiKey: MGOVUZGBXAFMCY-ZETCQYMHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  9
• 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：
  24.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  (-)-2-氰-6-苯基恶唑哌啶 在 palladium on activated charcoal sodium hydroxide 、 lithium aluminium tetrahydride 、 氢气 作用下， 以 甲醇 、 乙醚 、 氯仿 为溶剂， 反应 8.0h， 生成 <(2S)-piperidin-2-yl>-N-methylmethanamine
  参考文献：
  名称：

  Asymmetric Synthesis. 39.¹ Synthesis of 2-(1-Aminoalkyl)piperidines via 2-Cyano-6-phenyl Oxazolopiperidine

  摘要：

  The asymmetric synthesis of a series of 2-(1-aminoalkyl) piperidines using (-)-2-cyano-6-phenyloxazolopiperidine 1 is described. LiAlH4 reduction of 1 followed by hydrogenolysis led to the diamine 3. The same strategy applied to C-2-methylated compound 7 afforded [(2S)-2-methylpiperidin-2-yl]methanamine (9). Addition of lithium derivatives to the cyano group of 1 resulted in the formation of an intermediate imino bicyclic system (11a-c) which could be diastereoselectively reduced to substituted diamino alcohols 13a-c. The addition of an excess of PhLi to 1 in the presence of LiBr furnished disubstituted amine 19, the precursor of diphenyl[(2S)-piperidin-2-yl]methanamine (22).

  DOI：

  10.1021/jo960910s

文献信息

• [EN] AMINO-BENZOISOTHIAZOLE AND AMINO-BENZOISOTHIADIAZOLE AMIDE COMPOUNDS<br/>[FR] COMPOSÉS D'AMIDE D'AMINO-BENZOISOTHIAZOLE ET D'AMINO-BENZOISOTHIADIAZOLE
  申请人：AERIE PHARMACEUTICALS INC

  公开号：WO2019178324A1

  公开（公告）日：2019-09-19

  Provided herein are amino-benzoisothiazole and benzoisothiadiazole amide compounds. In particular, provided herein are compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds provided herein are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, retinal diseases such as acute macular degeneration (AMD) and diabetic macular edema (DME), diseases and conditions characterized by inflammatory processes, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. Also provided are compositions (e.g., pharmaceutical compositions) comprising the compounds provided herein.

  本文提供了氨基苯并异噻唑和苯并异噻二唑酰胺化合物。具体来说，本文提供了影响细胞激酶功能并可用作治疗剂或与治疗剂一起使用的化合物。本文提供的化合物在治疗各种疾病和病况方面具有用途，包括眼部疾病如青光眼，视网膜疾病如急性黄斑变性（AMD）和糖尿病黄斑水肿（DME），以及以炎症过程为特征的疾病和病况、心血管疾病，以及以异常生长为特征的疾病，如癌症。还提供了含有本文提供的化合物的组合物（例如，制药组合物）。
• 2, 6-NAPHTHRIDINE DERIVATIVES
  申请人：van Eis Maurice

  公开号：US20100130469A1

  公开（公告）日：2010-05-27

  The present invention relates to novel organic compounds comprising a naphthyridine which may be mediators of a selective subset of kinases belonging to the AGC kinase family, such as for example PKC, PKD, PKN-1/2, CDK-9, MRCK-beat, PASK, PRKX, ROCK-I/II or mediators of other kinases, the selectivity of which would be depending on the structural variation thereof.

  本发明涉及一种新的有机化合物，包括一种萘啶，它可能是AGC激酶家族的一种选择性亚组的介质，例如PKC，PKD，PKN-1/2，CDK-9，MRCK-beat，PASK，PRKX，ROCK-I/II或其他激酶的介质，其选择性取决于其结构变化。
• Diazaborolidines, a new class of enantioselective organoboron catalytic agents.
  作者：Olivier Froelich、Martine Bonin、Jean-Charles Quirion、Henri-Philippe Husson

  DOI：10.1016/s0957-4166(00)80097-x

  日期：1993.11

  Diazaborolidines 6 and 9, derived from 2-aminomethyl-piperidine, have been prepared in an optically pure form from 2-cyano-6-phenyl oxazolopiperidine 3. The best results for the asymmetric reduction of acetophenone (yield>95%, 72% ee) have been obtained with BH3.Me2S in the presence of 9a as a chiral catalyst.
• Asymmetric Synthesis. 39.¹ Synthesis of 2-(1-Aminoalkyl)piperidines <i>via</i> 2-Cyano-6-phenyl Oxazolopiperidine
  作者：Olivier Froelich、Patrice Desos、Martine Bonin、Jean-Charles Quirion、Henri-Philippe Husson、Jieping Zhu

  DOI：10.1021/jo960910s

  日期：1996.1.1

  The asymmetric synthesis of a series of 2-(1-aminoalkyl) piperidines using (-)-2-cyano-6-phenyloxazolopiperidine 1 is described. LiAlH4 reduction of 1 followed by hydrogenolysis led to the diamine 3. The same strategy applied to C-2-methylated compound 7 afforded [(2S)-2-methylpiperidin-2-yl]methanamine (9). Addition of lithium derivatives to the cyano group of 1 resulted in the formation of an intermediate imino bicyclic system (11a-c) which could be diastereoselectively reduced to substituted diamino alcohols 13a-c. The addition of an excess of PhLi to 1 in the presence of LiBr furnished disubstituted amine 19, the precursor of diphenyl[(2S)-piperidin-2-yl]methanamine (22).