(1R)-1-(2-吡啶基)-1-丙胺 | 249920-06-7

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: (1R)-1-(2-吡啶基)-1-丙胺
• 英文名称: (R)-1-(pyridin-2-yl)propan-1-amine
• 英文别名: (R)-(2-pyridyl)propylamine；(1R)-1-(pyridin-2-yl)propan-1-amine；[R]-1-pyridin-2-yl-propylamine；(1R)-1-pyridin-2-ylpropan-1-amine
• CAS: 249920-06-7
• 化学式: C₈H₁₂N₂
• 分子量: 136.197
• InChiKey: ARIBPNACTHQUIK-SSDOTTSWSA-N

物化性质

• 沸点：
  214.1±15.0 °C(Predicted)
• 密度：
  0.998±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  38.9
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 包装等级：
  III
• 危险类别：
  8
• 危险性防范说明：
  P301+P330+P331,P303+P361+P353,P363,P304+P340,P310,P321,P260,P264,P280,P305+P351+P338,P405,P501
• 危险品运输编号：
  2735
• 危险性描述：
  H314
• 储存条件：
  存储条件为：2-8℃，避光，惰性气体环境。

反应信息

• 作为反应物：
  描述：

  3-[(2-乙氧基-3,4-二氧代-1-环丁基-1-氨基]-2-羟基-N,N-二甲基-苄胺 、 (1R)-1-(2-吡啶基)-1-丙胺 以 乙醇 为溶剂， 生成 (R)-3-(3,4-dioxo-2-(1-(pyridin-2-yl)propylamino)cyclobut-1-enylamino)-2-hydroxy-N,N-dimethylbenzamide
  参考文献：
  名称：

  Synthesis and structure–activity relationships of heteroaryl substituted-3,4-diamino-3-cyclobut-3-ene-1,2-dione CXCR2/CXCR1 receptor antagonists

  摘要：

  Comprehensive SAR studies were undertaken in the 3,4-diaminocyclobut-3-ene-1,2-dione class of CXCR2/CXCR1 receptor antagonists to explore the role of the heterocycle on chemokine receptor binding affinities, functional activity, as well as oral exposure in rat. The nature of the heterocycle as well as the requisite substitution pattern around the heterocycle was shown to have a dramatic effect on the overall biological pro. le of this class of compounds. The furyl class, particularly the 4-halo adducts, was found to possess superior binding affinities for both the CXCR2 and CXCR1 receptors, functional activity, as well as oral exposure in rat versus other heterocyclic derivatives. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.01.024
• 作为产物：
  描述：

  (S)-3-methyl-2-((R)-1-(pyridin-2-yl)propylamino)butan-1-ol 在 水 、 甲胺 作用下， 以 甲醇 为溶剂， 生成 (1R)-1-(2-吡啶基)-1-丙胺
  参考文献：
  名称：

  ORGANIC COMPOUNDS

  摘要：

  本发明涉及以下式（I）的化合物 其中X，R1，R2，R3，R4和R5如本文所定义，这些化合物对于治疗对CXCR2受体介质有响应的疾病是有用的。还描述了含有这些化合物的药物组合物以及制备这些化合物的方法。

  公开号：

  US20100029670A1

文献信息

• 7[4′-trifluoromethyl-biphenyl-2-carbonyl)amino]-quinoline-3-carboxylic acid amides, and method of inhibiting the secretion of apolipoprotein B
  申请人：Pfizer, Inc.

  公开号：US06369075B1

  公开（公告）日：2002-04-09

  This invention relates to compounds of Formula I that inhibit the secretion of apolipoprotein B, to pharmaceutical compositions comprising the compounds, and to methods of treating and/or preventing atherosclerosis, obesity, diabetes, hyperlipidemia, hyperliproproteinemia, hypercholesterolemia, hypertriglyceridemia, hypoalphalipoproteinemia, pancreatitis, myocardial infarction, stroke, restenosis, or Syndrome X. This invention also relates to methods of reducing the secretion of apolipoprotein B and/or inhibiting microsomal triglyceride transfer protein.

  这项发明涉及抑制载脂蛋白B分泌的I号公式化合物的制备，包括含有该化合物的药物组合物，以及治疗和/或预防动脉粥样硬化、肥胖、糖尿病、高脂血症、高脂蛋白血症、高胆固醇血症、高甘油三酯血症、低α脂蛋白血症、胰腺炎、心肌梗死、中风、再狭窄或X综合症的方法。该发明还涉及减少载脂蛋白B分泌和/或抑制微粒体甘油三酯转移蛋白的方法。
• Conformational control of propeller-like chirality in Zn(II) complexes: Tightly balanced steric bias
  作者：Yu-Hung Chiu、Osvaldo dos Santos、James W Canary

  DOI：10.1016/s0040-4020(99)00713-9

  日期：1999.10

  The conformational behavior of a series of chiral tripodal ligand-Zn(II) complexes was examined. The ligands adopt propeller-like conformations upon complexation of trigonal bipyramidal metal ions such as Zn(II), with the chirality of the propeller determined by the absolute configuration of a single chiral center in one of the tripod arms. Surprisingly, increasing the size of the substituent in the

  检查了一系列手性三脚架配体-Zn（II）配合物的构象行为。配体在与三角双锥体金属离子（例如Zn（II））络合时采用螺旋桨状构象，螺旋桨的手性由三脚架臂之一中单个手性中心的绝对构型决定。出人意料的是，增加手性臂中取代基的尺寸并不能改善复合物的几何定义，如复合物的圆二色性光谱所示。
• [EN] FUSED PYRROLEDICARBOXAMIDES AND THEIR USE AS PHARMACEUTICALS<br/>[FR] PYRROLEDICARBOXAMIDES FUSIONNÉS ET LEUR UTILISATION EN TANT QUE PRODUITS PHARMACEUTIQUES
  申请人：SANOFI SA

  公开号：WO2013113860A1

  公开（公告）日：2013-08-08

  The present invention relates to fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in the claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.

  本发明涉及公式（I）中的融合吡咯二羧酰胺，其中R1至R9、X、m和n如权利要求中所定义。公式（I）化合物是酸敏感钾通道TASK-1的抑制剂，适用于治疗TASK-1通道介导的疾病，如心律失常，特别是心房心律失常，如心房颤动或心房扑动，以及呼吸系统疾病，特别是与睡眠相关的呼吸系统疾病，如睡眠呼吸暂停症等。
• Direct Asymmetric Reductive Amination of Alkyl (Hetero)Aryl Ketones by an Engineered Amine Dehydrogenase
  作者：Weixi Kong、Yunting Liu、Chen Huang、Liya Zhou、Jing Gao、Nicholas J. Turner、Yanjun Jiang

  DOI：10.1002/anie.202202264

  日期：2022.5.16

  A novel amine dehydrogenase (Ja-AmDH) has been developed by a directed evolution approach for the direct asymmetric reductive amination of alkyl (hetero)aryl ketones. The engineered enzyme provided access to a series of chiral α-(hetero)aryl primary amines in high yields with excellent enantioselectivity.

  已经通过定向进化方法开发了一种新型胺脱氢酶 ( J a-AmDH)，用于烷基（杂）芳基酮的直接不对称还原胺化。该工程酶以高产率和优异的对映选择性提供了一系列手性α-（杂）芳基伯胺。
• 7-[(4'-trifluoromethyl-biphenyl-2-carbonyl)amino]-quinoline-3-carboxylic acid amides, and methods of inhibiting the secretion of apolipoprotein B
  申请人：——

  公开号：US20020132806A1

  公开（公告）日：2002-09-19

  This invention relates to compounds of Formula I 1 that inhibit the secretion of apolipoprotein B, to pharmaceutical compositions comprising the compounds, and to methods of treating and/or preventing atherosclerosis, obesity, diabetes, hyperlipidemia, hyperliproproteinemia, hypercholesterolemia, hypertriglyceridemia, hypoalphalipoproteinemia, pancreatitis, myocardial infarction, stroke, restenosis, or Syndrome X. This invention also relates to methods of reducing the secretion of apolipoprotein B and/or inhibiting microsomal triglyceride transfer protein.

  本发明涉及一种公式I1的化合物，其抑制载脂蛋白B的分泌，以及包含该化合物的制药组合物，以及治疗和/或预防动脉硬化、肥胖症、糖尿病、高脂血症、高脂蛋白血症、高胆固醇血症、高三酰甘油血症、低α-脂蛋白血症、胰腺炎、心肌梗死、中风、再狭窄或X综合症的方法。本发明还涉及减少载脂蛋白B的分泌和/或抑制微粒体三酰甘油转移蛋白的方法。