(2R)-1-(benzyloxy)propan-2-amine | 181495-37-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (2R)-1-(benzyloxy)propan-2-amine
• 英文别名: (2R)-1-phenylmethoxypropan-2-amine
• CAS: 181495-37-4
• 化学式: C₁₀H₁₅NO
• 分子量: 165.235
• InChiKey: HYUZZQIAJWNRAQ-SECBINFHSA-N

物化性质

• 沸点：
  251.8±15.0 °C(Predicted)
• 密度：
  0.997±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (2R)-1-(benzyloxy)propan-2-amine 在 氨 、 potassium carbonate 、 sodium amide 作用下， 以 四氢呋喃 、 乙醚 为溶剂， 反应 48.5h， 生成 (R)-1-[2-(1-phenylmethoxy)propyl]-2-methyleneaziridine
  参考文献：
  名称：

  Synthesis of chiral, nonracemic methyleneaziridines derived from β-amino alcohols

  摘要：

  An efficient three step process for the synthesis of chiral, nonracemic methyleneaziridines derived from homochiral beta-amino alcohols is described, Methyleneaziridines 4a-e produced using this chemistry have been shown to possess high enantiomeric purities (greater than or equal to 95% ee). Copyright (C) 1996 Elsevier Science Ltd

  DOI：

  10.1016/s0957-4166(96)00447-8
• 作为产物：
  描述：

  (-)-(R)-3-benzyloxy-2-methylpropionic acid 在 ammonium hydroxide 、 三乙胺 、 [双(三氟乙酰氧基)碘]苯 作用下， 以 四氢呋喃 、 水 、 乙腈 为溶剂， 反应 4.5h， 生成 (2R)-1-(benzyloxy)propan-2-amine
  参考文献：
  名称：

  Synthesis of chiral α-amino acids

  摘要：

  A novel method for the synthesis of chiral alpha-amino acids has been developed where the acid functionality was constructed by oxidizing a hydroxymethyl group introduced by Evans' method in the alpha-position of an appropriate acid substrate and the amino part came from the amide of the original carboxyl group following a modified Hofmann rearrangement reaction. (C) 2002 Published by Elsevier Science Ltd.

  DOI：

  10.1016/s0040-4039(02)02433-4

文献信息

• [EN] HETEROARYL COMPOUNDS AND THEIR USE AS THERAPEUTIC DRUGS<br/>[FR] COMPOSÉS HÉTÉROARYLE ET LEUR UTILISATION COMME MÉDICAMENTS THÉRAPEUTIQUES
  申请人：DONG-A SOCIO HOLDINGS CO LTD

  公开号：WO2017039331A1

  公开（公告）日：2017-03-09

  The present invention provides heterocyclic compounds, the stereoisomer thereof, the enantiomer thereof, or the pharmaceutically acceptable salt, which are capable of modulating the activity of Mer receptor tyrosine kinase (MERTK). This invention also provides pharmaceutical compositions thereof, methods to prepare the said compounds, and the use of such compounds as a medicament. The present invention is directed to MERTK inhibitory compounds with marked potency, thereby having an outstanding potential for a pharmaceutical intervention of cancer and any other diseases related to MERTK dysregulation.

  本发明提供了一种杂环化合物、其立体异构体、对映异构体或药用可接受的盐，这些化合物能够调节Mer受体酪氨酸激酶（MERTK）的活性。本发明还提供了这些化合物的药物组合物、制备所述化合物的方法以及将这些化合物用作药物的应用。本发明针对的是具有显著活性的MERTK抑制性化合物，因此具有在癌症和任何与MERTK调控失调相关的疾病中进行药物干预的卓越潜力。
• <i>O</i>-(1-Phenylbutyl)benzyloxyacetaldoxime, a Versatile Reagent for the Asymmetric Synthesis of Protected 1,2-Aminoalcohols and 2-Hydroxymethyl Nitrogen Heterocycles
  作者：Christopher J. Moody、Tracey S. Cooper、Alexander S. Larigo、Pierre Laurent、Andrew K. Takle

  DOI：10.1055/s-2002-34235

  日期：——

  Addition of organometallic reagents to O-(1-phenylbutyl)benzyloxyacetaldoxime in the presence of boron trifluoride diethyl etherate is highly diastereoselective; the resulting hydroxylamines are readily converted into protected 1,2-aminoalcohols and 2-hydroxymethyl nitrogen heterocycles, including the iminosugar 1,4-dideoxy-1,4-imino-d-ribitol, in high enantiomeric excess.

  在硼氟酸二乙醚存在下，有机金属试剂与O-(1-苯基丁基)苄氧基乙醛肟的加成具有高度的非对映选择性；生成的羟胺可方便地转化为受到保护的1,2-氨基醇和2-羟甲基氮杂环化合物，其中包括高对映体纯度的1,4-二脱氧1,4-亚氨基-d-核糖醇。
• [EN] 6-SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-BENZO[D]AZEPINES AS 5-HT2C RECEPTOR AGONISTS<br/>[FR] 2,3,4,5-TETRAHYDRO-1H-BENZO[D]AZEPINES SUBSTITUES EN POSITION 6 EN TANT QU'AGONISTES DE RECEPTEUR 5-HT2C
  申请人：LILLY CO ELI

  公开号：WO2005082859A1

  公开（公告）日：2005-09-09

  The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: I where: R6 is -C=C-R10, -O-R12, -S-R14, or -NR24R25; and other substituents are as defined in the specification.

  本发明提供了公式I中的6-取代的2,3,4,5-四氢-1H-苯并[d]氮杂环庚烯作为选择性5-HT2C受体激动剂，用于治疗与5-HT2C相关的疾病，包括肥胖症、强迫症/强迫性障碍、抑郁症和焦虑症：I其中：R6为-C=C-R10，-O-R12，-S-R14或-NR24R25；其他取代基如规范中所定义。
• Diaminopropionic acid derivatives
  申请人：Fotouhi Nader

  公开号：US20070155671A1

  公开（公告）日：2007-07-05

  A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.

  化合物1a的公式，对于治疗再灌注损伤是有用的，包括盐类、前药和相关化合物。
• 6-SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-BENZO[D]AZEPINES AS 5-HT2C RECEPTOR AGONISTS
  申请人：Allen John Gordon

  公开号：US20090099155A1

  公开（公告）日：2009-04-16

  The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzoazepines of Formula I as selective 5-HT 2C receptor agonists for the treatment of 5-HT 2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R 6 is -C≡C-R 10 , -O-R 12 , -S-R 14 , or -NR 24 R 25 ; and other substituents are as defined in the specification.

  本发明提供了式I的6-取代的2,3,4,5-四氢-1H-苯并氮烯作为选择性5-HT2C受体激动剂，用于治疗5-HT2C相关疾病，包括肥胖症、强迫症、抑郁症和焦虑症：其中：R6为-C≡C-R10，-O-R12，-S-R14或-NR24R25；其他取代基如规范中所定义。