(R)-1-amino-3-methoxypropan-2-ol | 1174289-21-4

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (R)-1-amino-3-methoxypropan-2-ol
• 英文别名: (2R)-1-amino-3-methoxypropan-2-ol
• CAS: 1174289-21-4
• 化学式: C₄H₁₁NO₂
• mdl: MFCD09260573
• 分子量: 105.137
• InChiKey: IDSWHVZEQHESIJ-SCSAIBSYSA-N

物化性质

• 沸点：
  197.0±20.0 °C(Predicted)
• 密度：
  1.025±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.5
• 重原子数：
  7
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  55.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (R)-1-amino-3-methoxypropan-2-ol 、 4-(溴甲基)-3-溴苯甲酸甲酯 在 potassium carbonate 作用下， 以 乙腈 为溶剂， 反应 16.0h， 以39%的产率得到methyl (R)-3-bromo-4-(((2-hydroxy-3-methoxypropyl)amino)methyl)benzoate
  参考文献：
  名称：

  3-ALKYL-4-AMIDO-BICYCLIC [4,5,0] HYDROXAMIC ACIDS AS HDAC INHIBITORS

  摘要：

  本公开涉及抑制锌依赖性组蛋白去乙酰化酶（HDACs）的抑制剂，用于治疗与HDAC（例如HDAC6）相关的疾病或疾病，其具有以下式I： 其中R、L、X1、X2、X3、X4、Y1、Y2、Y3和Y4如本文所述。

  公开号：

  US20160222028A1
• 作为产物：
  描述：

  (R)-(-)-环氧丙基甲基醚 在 氨 作用下， 以 甲醇 为溶剂， 反应 18.0h， 以84%的产率得到(R)-1-amino-3-methoxypropan-2-ol
  参考文献：
  名称：

  [EN] 1-HETEROARYL-INDOLINE-4-CARBOXAMIDES AS MODULATORS OF GPR52 USEFUL FOR THE TREATMENT OR PREVENTION OF DISORDERS RELATED THERETO
  [FR] 1-HÉTÉROARYL-INDOLINE-4-CARBOXAMIDES EN TANT QUE MODULATEURS DE GPR52 UTILES DANS LE TRAITEMENT OU LA PRÉVENTION DE TROUBLES ASSOCIÉS À CEUX-CI

  摘要：

  本发明涉及式（la）的化合物及其药物组合物，其调节GPR52的活性。本发明的化合物及其药物组合物适用于治疗GPR52介导的疾病（例如亨廷顿病、精神分裂症、躁郁症、注意力缺陷多动障碍（ADHD）或抽动症候群）；锥体外或运动障碍；运动障碍；过动运动障碍；精神障碍；痴呆症；情绪障碍；抑郁障碍；焦虑障碍；强迫症；自闭症谱系障碍；垂体泌乳素相关障碍（例如高泌乳素血症）；神经认知障碍；创伤或应激相关障碍（例如创伤后应激障碍（PTSD））；破坏性、冲动控制或行为障碍；睡眠-觉醒障碍；物质相关障碍；成瘾障碍；行为障碍；前额叶功能减退；下丘脑-边缘系统、中脑边缘系统、中前额叶或黑质纹状体通路异常；纹状体活动降低；皮层功能障碍；神经认知功能障碍；以及相关疾病。

  公开号：

  WO2016176571A1

文献信息

• [EN] SUBSTITUTED PYRIDINES AND METHOD OF USE<br/>[FR] PYRIDINES SUBSTITUÉES ET MÉTHODE D'UTILISATION
  申请人：ABBVIE SARL

  公开号：WO2016193812A1

  公开（公告）日：2016-12-08

  The invention discloses compounds of Formula (I) wherein X, R1, R2, and R3 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.

  该发明公开了式（I）化合物，其中X、R1、R2和R3如本文所定义。本发明涉及化合物及其在囊性纤维化治疗中的应用，其生产方法，包含相同化合物的药物组合物，以及通过给予该发明的化合物来治疗囊性纤维化的方法。
• 3-ALKYL BICYCLIC [4,5,0] HYDROXAMIC ACIDS AS HDAC INHIBITORS
  申请人：Forma Therapeutics, Inc.

  公开号：US20160221972A1

  公开（公告）日：2016-08-04

  The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , and Y 4 are described herein.

  本公开涉及抑制锌依赖性组蛋白去乙酰化酶（HDACs）的抑制剂，用于治疗与HDAC相关的疾病或障碍，例如HDAC6，其具有公式I：其中R，L，X1，X2，X3，X4，Y1，Y2，Y3和Y4如本文所述。
• Novel amino linkers enabling efficient labeling and convenient purification of amino-modified oligonucleotides
  作者：Yasuo Komatsu、Naoshi Kojima、Maiko Sugino、Akiko Mikami、Ken Nonaka、Yumi Fujinawa、Takashi Sugimoto、Kousuke Sato、Kenichi Matsubara、Eiko Ohtsuka

  DOI：10.1016/j.bmc.2007.10.011

  日期：2008.1

  We developed new amino linker reagents for an oligonucleotide (ONT) terminus. These reagents consist of an aminoethyl carbamate main linkage and a side-chain residue, which was a naphthylmethoxymethyl, methoxymethyl, or methyl group or a hydrogen atom. The primary amine was protected with a monomethoxytrityl (MMT) group. The chemical properties of ONTs containing these amino-modifications were investigated. The MMT group of these amino-modifications could be quite rapidly removed from the amine under very mild acidic conditions, which are not strong enough for the deprotection of a conventional aliphatic amine. This significant feature enabled the amino-modified ONTs to be conveniently purified with a reverse phase column. Furthermore, the amino-modifications efficiently reacted to active esters, as compared with other amino-modifications. We also found that the pK(a), values of the amino-modifications were lower than that of the aliphatic amine. All of the experimental results showed that these chemical properties are closely related to their structures. We report here the chemical properties and the availability of the new amino linker reagents. (C) 2007 Elsevier Ltd. All rights reserved.
• 3-ALKYL-4-AMIDO-BICYCLIC [4,5,0] HYDROXAMIC ACIDS AS HDAC INHIBITORS
  申请人：Forma Therapeutics, Inc.

  公开号：US20160222028A1

  公开（公告）日：2016-08-04

  The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , and Y 4 are described herein.

  本公开涉及抑制锌依赖性组蛋白去乙酰化酶（HDACs）的抑制剂，用于治疗与HDAC（例如HDAC6）相关的疾病或疾病，其具有以下式I： 其中R、L、X1、X2、X3、X4、Y1、Y2、Y3和Y4如本文所述。
• [EN] 1-HETEROARYL-INDOLINE-4-CARBOXAMIDES AS MODULATORS OF GPR52 USEFUL FOR THE TREATMENT OR PREVENTION OF DISORDERS RELATED THERETO<br/>[FR] 1-HÉTÉROARYL-INDOLINE-4-CARBOXAMIDES EN TANT QUE MODULATEURS DE GPR52 UTILES DANS LE TRAITEMENT OU LA PRÉVENTION DE TROUBLES ASSOCIÉS À CEUX-CI
  申请人：ARENA PHARM INC

  公开号：WO2016176571A1

  公开（公告）日：2016-11-03

  The present invention relates to compounds of Formula (la) and pharmaceutical compositions thereof that modulate the activity of GPR52. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a GPR52-mediated disorder (e.g., Huntington's disease, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder (ADHD), or Tourette's syndrome); an extrapyramidal or movement disorder; a motor disorder; a hyperkinetic movement disorder; a psychotic disorder; catatonia; a mood disorder; a depressive disorder; an anxiety disorder; obsessive-compulsive disorder (OCD); an autism spectrum disorder; a prolactin-related disorder (e.g., hyperprolactinemia); a neurocognitive disorder; a trauma- or stressor-related disorder (e.g., posttraumatic stress disorder (PTSD)); a disruptive, impulse-control, or conduct disorder; a sleep-wake disorder; a substance-related disorder; an addictive disorder; a behavioral disorder; hypofrontality; an abnormality in the tuberoinfundibular, mesolimbic, mesocortical, or nigrostriatal pathway; decreased activity in the striatum; cortical dysfunction; neurocognitive dysfunction; and conditions related thereto.

  本发明涉及式（la）的化合物及其药物组合物，其调节GPR52的活性。本发明的化合物及其药物组合物适用于治疗GPR52介导的疾病（例如亨廷顿病、精神分裂症、躁郁症、注意力缺陷多动障碍（ADHD）或抽动症候群）；锥体外或运动障碍；运动障碍；过动运动障碍；精神障碍；痴呆症；情绪障碍；抑郁障碍；焦虑障碍；强迫症；自闭症谱系障碍；垂体泌乳素相关障碍（例如高泌乳素血症）；神经认知障碍；创伤或应激相关障碍（例如创伤后应激障碍（PTSD））；破坏性、冲动控制或行为障碍；睡眠-觉醒障碍；物质相关障碍；成瘾障碍；行为障碍；前额叶功能减退；下丘脑-边缘系统、中脑边缘系统、中前额叶或黑质纹状体通路异常；纹状体活动降低；皮层功能障碍；神经认知功能障碍；以及相关疾病。