1-(3-pyridinyl)-2-phenylethylamine | 118385-85-6

• 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: 1-(3-pyridinyl)-2-phenylethylamine
• 英文别名: 2-phenyl-1-(pyridin-3-yl)ethan-1-amine；benzylpyridin-3-ylmethylamine；2-phenyl-1-[3]pyridyl-ethylamine；2-Phenyl-1-[3]pyridyl-aethylamin；2-Phenyl-1-pyridin-3-YL-ethylamine；2-phenyl-1-pyridin-3-ylethanamine
• CAS: 118385-85-6
• 化学式: C₁₃H₁₄N₂
• 分子量: 198.268
• InChiKey: XZAJERQRTFFKNB-UHFFFAOYSA-N

物化性质

• 沸点：
  329.2±27.0 °C(Predicted)
• 密度：
  1.097±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  38.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(3-pyridinyl)-2-phenylethylamine 生成 2-amino-N-[1-(3-pyridinyl)-2-phenylethyl]acetamide dihydrochloride
  参考文献：
  名称：

  2-aminoacetamide pyridinyl derivatives

  摘要：

  提供以下一般结构的化合物：##STR1## 其中R.sub.1、R.sub.2和R.sub.3独立地选择氢或甲基；A是氨基、C.sub.1-C.sub.4单烷基氨基、C.sub.2-C.sub.8双烷基氨基、1-吡咯烷基、1-哌啶基、4-吗啉基或环丙基氨基；并且W和Q独立地选择2-吡啶基、3-吡啶基或4-吡啶基或苯基，但W和Q不能同时为苯基。

  公开号：

  US04769466A1
• 作为产物：
  描述：

  烟酸乙酯 在 水 、 氢溴酸 、 sodium ethanolate 作用下， 生成 1-(3-pyridinyl)-2-phenylethylamine
  参考文献：
  名称：

  Some α-Substituted β-Pyridylethylamines

  摘要：

  DOI：

  10.1021/ja01161a031

文献信息

• Substituted (1,2-Diarylethyl)amide Acyl-CoA:Cholesterol Acyltransferase Inhibitors: Effect of Polar Groups on in Vitro and in Vivo Activity
  作者：John W. Clader、Joel G. Berger、Robert E. Burrier、Harry R. Davis、Martin Domalski、Sundeep Dugar、Timothy P. Kogan、Brian Salisbury、Wayne Vaccaro

  DOI：10.1021/jm00010a004

  日期：1995.5

  Substituted (1,2-diarylethyl)amides have been prepared and evaluated for their ability to inhibit microsomal acyl-CoA:cholesterol acyltransferase activity in vitro and to lower hepatic cholesteryl ester content in vivo in a cholesterol-fed hamster. Simple unsubstituted (diarylethyl)amides were potent inhibitors in vitro but showed poor activity in vivo. Introduction of polar groups at specific locations

  已经制备了取代的（1,2-二芳基乙基）酰胺，并评估了它们在体外抑制微粒体酰基辅酶A：胆固醇酰基转移酶活性并降低体内胆固醇喂养的仓鼠体内肝胆固醇酯含量的能力。简单的未取代的（二芳基乙基）酰胺在体外是有效的抑制剂，但在体内却显示出较差的活性。在二芳基乙胺部分的特定位置引入极性基团会降低体外活性，但会增加体内活性。两种作用都高度依赖于结构，表明在每种模型中介导活性的特定相互作用。这些相反作用的优化导致化合物在两种模型中均有效。
• Alkaline-Metal-Catalyzed One-Pot Aminobenzylation of Aldehydes with Toluenes
  作者：Guoqing Liu、Patrick J. Walsh、Jianyou Mao

  DOI：10.1021/acs.orglett.9b02737

  日期：2019.11.1

  A novel and easily accessible MN(SiMe3)2 (M = Li or Na)/Cs2CO3 co-catalyzed benzylation of in situ generated N-(trimethylsilyl) aldimines with toluene derivatives has been successfully developed. The catalyst exhibits high chemoselectivity for deprotonation of toluenes at the benzylic position. The utility of this system is exemplified by the one-pot synthesis of a diverse array of bioactive 1,2-diarylethylamines

  已成功开发了一种新颖且易于使用的MN（SiMe 3）2（M = Li或Na）/ Cs 2 CO 3催化原位生成的N-（三甲基甲硅烷基）亚胺与甲苯衍生物的苄基化反应。该催化剂对苄基位置的甲苯去质子表现出高化学选择性。一锅合成具有优异效率和宽泛的官能团耐受性的各种生物活性1,2-二芳基乙胺的例子说明了该系统的实用性。
• Anthranilamides and methods of their use
  申请人：——

  公开号：US20030187033A1

  公开（公告）日：2003-10-02

  The present invention is related to anthranilamides of formula I, 1 in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).

  本发明涉及具有式I的蒽酰胺，其中R(1)至R(7)具有本文中指示的含义，其制备方法，它们作为药物的用途，以及含有它们的药物制剂。这些化合物作用于Kv1.5钾通道，抑制一种被称为人类心房中超快速激活延迟整流器的钾电流。因此，这些化合物适用于作为新型抗心律失常药物，用于治疗和预防心房心律失常（例如心房颤动（AF）或心房扑动）。
• Anthranilamides with heteroarylsulfonyl side chain, process of preparation, and use
  申请人：——

  公开号：US20030114499A1

  公开（公告）日：2003-06-19

  This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them. Compounds of formula I, 1 in which R1 to R7 have the meanings stated in the claims, act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. They are therefore suitable as novel antiarrhythmic ingredients, such as for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutter.

  这项发明涵盖了具有杂环磺酰基侧链的蒽酰胺，其制备方法，它们作为药物或诊断辅助剂的用途，以及含有它们的制药制剂。具有式I的化合物，在其中R1至R7具有权利要求中所述的含义，作用于Kv1.5钾通道，并抑制被称为人类心房中超快速激活延迟整流器的钾电流。因此，它们适用作为新型抗心律失常成分，例如用于治疗和预防心房心律失常，如心房颤动（AF）或心房扑动。
• ANTHRANILAMIDES AND METHODS OF THEIR USE
  申请人：Brendel Joachim

  公开号：US20070117807A1

  公开（公告）日：2007-05-24

  The present invention is related to a process for preparing anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).

  本发明涉及一种制备式I的蒽酰胺的方法，其中R（1）至R（7）具有本文中所示的含义，其制备方法，作为药物的使用以及含有它们的制药制剂。该化合物对Kv1.5钾通道产生作用，并抑制被称为人类心房中超快速激活延迟整流器的钾电流。因此，该化合物适用于作为新型抗心律失常剂用于治疗和预防心房心律失常（例如心房颤动（AF）或心房扑动）。