trans-3-Hydroxy-6-methyl-piperidin | 150197-75-4

• 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: trans-3-Hydroxy-6-methyl-piperidin
• 英文别名: (3S,6S)-6-Methylpiperidin-3-OL
• CAS: 150197-75-4
• 化学式: C₆H₁₃NO
• mdl: MFCD19238013
• 分子量: 115.175
• InChiKey: UAZCJMVDJHUBIA-WDSKDSINSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  8
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  trans-3-Hydroxy-6-methyl-piperidin 在 吡啶 、 4-二甲氨基吡啶 、 三乙基硼氢化锂 作用下， 以 四氢呋喃 为溶剂， 反应 26.0h， 生成 (S)-(+)-2-methyl-1-(4-toluenesulfonyl)piperidine
  参考文献：
  名称：

  2-（penta-1,3-dienyl）oxazolidines：通过立体选择性狄尔斯-阿尔德反应合成羟基化的哌啶

  摘要：

  与（-）-麻黄碱缩合的2,4-己二烯六酸酯主要生成恶唑烷4，恶唑烷4与亚硝基甲酸苄酯进行立体选择性Diels-Alder反应，以约5：2的比例生成环加合物9和10。还已经进行了9的进一步转化以给出光学活性的单和三羟基哌啶衍生物11和15。

  DOI：

  10.1016/s0040-4020(01)86312-2
• 作为产物：
  描述：

  (E,E,2S,4S,5R)-3,4-dimethyl-2-(penta-1,3-dien-1-yl)-5-phenyloxazolidine 在 palladium on activated charcoal 4 A molecular sieve 、 氢气 、 四丁基高碘酸铵 作用下， 以 乙醇 为溶剂， -65.0~25.0 ℃ 、200.0 kPa 条件下， 反应 98.0h， 生成 trans-3-Hydroxy-6-methyl-piperidin
  参考文献：
  名称：

  2-（penta-1,3-dienyl）oxazolidines：通过立体选择性狄尔斯-阿尔德反应合成羟基化的哌啶

  摘要：

  与（-）-麻黄碱缩合的2,4-己二烯六酸酯主要生成恶唑烷4，恶唑烷4与亚硝基甲酸苄酯进行立体选择性Diels-Alder反应，以约5：2的比例生成环加合物9和10。还已经进行了9的进一步转化以给出光学活性的单和三羟基哌啶衍生物11和15。

  DOI：

  10.1016/s0040-4020(01)86312-2

文献信息

• Novel diazepan derivatives
  申请人：Aebi Johannes

  公开号：US20070249589A1

  公开（公告）日：2007-10-25

  The invention is concerned with novel diazepan derivatives of formula (I) wherein A, X, R 3 , R 4 , R 5 , R 6 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.

  这项发明涉及式（I）的新型二氮杂环己烷衍生物，其中A、X、R3、R4、R5、R6、R8、R9、R10、R11、R12、R13、m和n的定义如描述和索赔中所述，以及其生理上可接受的盐。这些化合物是CCR-2受体、CCR-5受体和/或CCR-3受体的拮抗剂，可用作药物。
• [EN] 2-PYRIDYLOXY-3-ESTER-4-ETHER OREXIN RECEPTOR ANTAGONISTS<br/>[FR] COMPOSÉS 2-PYRIDYLOXY-3-ESTER-4-ÉTHER ANTAGONISTES DES RÉCEPTEURS DE L'OREXINE
  申请人：MERCK SHARP & DOHME

  公开号：WO2015088864A1

  公开（公告）日：2015-06-18

  The present invention is directed to 2-pyridyloxy-3-ester-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

  本发明涉及对促醒素受体的拮抗剂2-吡啶氧基-3-酯基-4-醚化合物。本发明还涉及在潜在的治疗或预防神经和精神疾病中使用本文所述的2-吡啶氧基-4-醚化合物。本发明还涉及包含这些化合物的药物组合物。本发明还涉及在预防或治疗促醒素受体参与的这类疾病中使用这些药物组合物。
• [EN] PIPERIDINYLOXY LACTONE OREXIN RECEPTOR ANTAGONISTS<br/>[FR] COMPOSÉS PIPÉRIDINYLOXY LACTONE SERVANT D'ANTAGONISTES DES RÉCEPTEURS DE L'OREXINE
  申请人：MERCK SHARP & DOHME

  公开号：WO2015095442A1

  公开（公告）日：2015-06-25

  The present invention is directed to piperidinyloxy lactone compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyloxy lactone compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

  本发明涉及对奥雷克星受体的拮抗剂-哌啶氧代内酯化合物。本发明还涉及所述哌啶氧代内酯化合物在潜在的涉及奥雷克星受体的神经和精神障碍和疾病的治疗或预防中的用途。本发明还涉及包含这些化合物的药物组合物。本发明还涉及这些药物组合物在预防或治疗涉及奥雷克星受体的疾病中的用途。
• 2,5-Disubstituted Piperidine Orexin Rceptor Antagonists
  申请人：Breslin Michael J.

  公开号：US20110201632A1

  公开（公告）日：2011-08-18

  The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

  本发明涉及2,5-二取代哌啶酰胺化合物，它们是促进睡眠荷尔蒙受体的拮抗剂，并且在治疗或预防神经和精神障碍以及其中促进睡眠荷尔蒙受体的疾病方面非常有用。该发明还涉及包含这些化合物的制药组合物，以及在预防或治疗其中促进睡眠荷尔蒙受体相关疾病方面使用这些化合物和组合物。
• DIAZEPAN DERIVATIVES MODULATORS OF CHEMOKINE RECEPTORS
  申请人：F. Hoffmann-La Roche AG

  公开号：EP2010506A1

  公开（公告）日：2009-01-07