(R)-5-氨基-2-哌啶酮盐酸盐 | 1003021-01-9

• 物质功能分类: 医药中间体
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: (R)-5-氨基-2-哌啶酮盐酸盐
• 中文别名: (5R)-5-氨基哌啶-2-一盐酸盐；(R)-5-氨基-哌啶-2-酮盐酸盐
• 英文名称: (5R)-5-aminopiperidin-2-one hydrochloride
• 英文别名: (R)-5-Aminopiperidin-2-one hydrochloride；(5R)-5-aminopiperidin-2-one;hydrochloride
• CAS: 1003021-01-9
• 化学式: C₅H₁₀N₂O*ClH
• 分子量: 150.608
• InChiKey: KFJLLOJCPFYWRV-PGMHMLKASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.35
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  55.1
• 氢给体数：
  3
• 氢受体数：
  2

制备方法与用途

(R)-5-氨基-哌啶-2-酮盐酸盐是一种哌啶类衍生物，可用于制备医药中间体。

反应信息

• 作为反应物：
  描述：

  2-(1-{6-chloro-1-[3-(trifluoromethyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl}piperidin-4-yl)propan-2-ol 、 (R)-5-氨基-2-哌啶酮盐酸盐 在 N,N-二异丙基乙胺 作用下， 以 N-甲基吡咯烷酮 为溶剂， 反应 72.0h， 以15 mg的产率得到(5R)-5-({4-[4-(2-hydroxypropan-2-yl)piperidin-1-yl]-1-[3-(trifluoromethyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl}amino)piperidin-2-one
  参考文献：
  名称：

  SUBSTITUTED PYRAZOLOPYRIMIDINES AS IRAK4 INHIBITORS

  摘要：

  本申请涉及用于治疗和/或预防疾病的新的吡唑并嘧啶衍生物，以及将它们用于生产用于治疗和/或预防人类和动物疾病的药物，尤其是增殖性疾病、自身免疫性疾病、代谢和炎症性疾病，这些疾病的特点是免疫系统过度反应，特别是风湿性疾病、炎症性皮肤病、心血管疾病、肺部疾病、眼病、神经系统疾病、疼痛疾病和癌症，在人类中，以及动物的过敏性/或炎症性疾病，特别是异位性皮炎和/或跳蚤过敏性皮炎，尤其是在家养动物中，特别是在狗中。

  公开号：

  EP3800188A1

文献信息

• Dihydrothienopyrimidines for the Treatment of Inflammatory Diseases
  申请人：Pouzet Pascale

  公开号：US20080096882A1

  公开（公告）日：2008-04-24

  The invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO 2 , but preferably SO, and wherein R 1 , R 2 and R 3 have the meanings given in the description, and which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.

  该发明涉及公式1的新二氢噻吡嘧啶，以及其药理学上可接受的盐、对映体、旋光异构体、消旋体、水合物或溶剂合物，其中X为SO或SO2，但最好为SO，R1、R2和R3在描述中给出的含义，并且适用于治疗呼吸道或胃肠道疾病、关节、皮肤或眼睛的炎症性疾病、外周或中枢神经系统疾病或癌症，以及含有这些化合物的药物组合物。
• Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith
  申请人：Albers J. Ronald

  公开号：US20060287344A1

  公开（公告）日：2006-12-21

  Provided herein are Aminopurine Compounds having the following structure: wherein R 1 , R 2 and and R 3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.

  本文提供的是具有以下结构的氨基嘌呤化合物：其中R1、R2和R3的定义如本文所述，以及包含有效量氨基嘌呤化合物的组合物和用于治疗或预防癌症、心血管疾病、肾脏疾病、自身免疫疾病、炎症性疾病、黄斑变性、缺血再灌注损伤、疼痛和相关综合征、与疾病相关的消耗、石棉相关疾病、肺动脉高压或可通过抑制JNK通路治疗或预防的疾病的方法，包括向需要治疗的患者施用有效量的氨基嘌呤化合物。
• Dihydrothienopyrimidines for the treatment of inflammatory Diseases
  申请人：POUZET Pascale

  公开号：US20120108534A1

  公开（公告）日：2012-05-03

  The invention relates to new dihydrothienopyrimidine of formula 1 , as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO 2 , but preferably SO, and wherein R 1 , R 2 and R 3 have the meanings given in the description, and which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.

  本发明涉及一种新的二氢噻唑嘧啶化合物，其化学式为1，以及其药物学上可接受的盐、对映异构体、对映体、外消旋体、水合物或溶剂化物，其中X为SO或SO2，但优选为SO，R1、R2和R3在说明中给出了其含义，该化合物适用于治疗呼吸或胃肠道不适或疾病、关节、皮肤或眼睛的炎症性疾病、周围或中枢神经系统疾病或癌症，以及含有这些化合物的制药组合物。
• 6,7-Dihydrothieno[3,2-d]pyrimidine for the Treatment of Inflammatory Diseases
  申请人：POUZET Pascale

  公开号：US20140005154A1

  公开（公告）日：2014-01-02

  The invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO 2 , but preferably SO, and wherein R 1 , R 2 and R 3 have the meanings given in the description, and which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.

  本发明涉及式1的新的二氢噻唑嘧啶，以及其药学上可接受的盐、对映异构体、对映体混合物、水合物或溶剂化物，其中X为SO或SO2，但优选为SO，R1、R2和R3具有所述描述中给出的含义，适用于治疗呼吸或消化不适或疾病、关节、皮肤或眼睛的炎症性疾病、外周或中枢神经系统疾病或癌症，以及含有这些化合物的制药组合物。
• HALOARYL SUBSTITUTED AMINOPURINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
  申请人：Signal Pharmaceuticals LLC

  公开号：EP2010186B1

  公开（公告）日：2012-12-26