2-[Methyl(2-pyrazinyl)amino]-1-ethanol | 866156-88-9

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 2-[Methyl(2-pyrazinyl)amino]-1-ethanol
• 英文别名: 2-[methyl(pyrazin-2-yl)amino]ethanol
• CAS: 866156-88-9
• 化学式: C₇H₁₁N₃O
• mdl: MFCD05669919
• 分子量: 153.184
• InChiKey: YMYFEMWFUHHFCL-UHFFFAOYSA-N

物化性质

• 沸点：
  290.6±30.0 °C(Predicted)
• 密度：
  1?+-.0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  11
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.428
• 拓扑面积：
  49.2
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-[Methyl(2-pyrazinyl)amino]-1-ethanol 在 甲醇 、 碘 、 哌啶乙酸盐 、 sodium hydride 、 magnesium 作用下， 以 甲苯 为溶剂， 反应 22.0h， 生成 5-{4-[2-(Methyl-pyrazin-2-yl-amino)-ethoxy]-benzyl}-thiazolidine-2,4-dione
  参考文献：
  名称：

  [[.omega.-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents

  摘要：

  A series of [(ureidoethoxy)benzyl]-2,4-thiazolidinediones and [[(heterocyclylamino)alkoxy]-benzyl]-2,4-thiazolidinediones was synthesized from the corresponding aldehydes. Compounds from the urea series, exemplified by 16, showed antihyperglycemic potency comparable with known agents of the type such as pioglitazone and troglitazone (CS-045). The benzoxazole 49, a cyclic analogue of 16, was a very potent enhancer of insulin sensitivity, and by modification of the aromatic heterocycle, an aminopyridine, 37, was identified as a lead compound from SAR studies. Evaluation of antihyperglycemic activity together with effects on blood hemoglobin content, to determine the therapeutic index, was performed in 8-day repeat administration studies in genetically obese C57 Bl/6 ob/ob mice. From these studies, BRL 49653 (37) has been selected, on the basis of antihyperglycemic potency combined with enhanced selectivity against reductions in blood hemoglobin content, for further evaluation.

  DOI：

  10.1021/jm00049a017
• 作为产物：
  描述：

  2-氯吡嗪 、 N-甲基-2-羟基乙胺 反应 15.0h， 生成 2-[Methyl(2-pyrazinyl)amino]-1-ethanol
  参考文献：
  名称：

  [[.omega.-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents

  摘要：

  A series of [(ureidoethoxy)benzyl]-2,4-thiazolidinediones and [[(heterocyclylamino)alkoxy]-benzyl]-2,4-thiazolidinediones was synthesized from the corresponding aldehydes. Compounds from the urea series, exemplified by 16, showed antihyperglycemic potency comparable with known agents of the type such as pioglitazone and troglitazone (CS-045). The benzoxazole 49, a cyclic analogue of 16, was a very potent enhancer of insulin sensitivity, and by modification of the aromatic heterocycle, an aminopyridine, 37, was identified as a lead compound from SAR studies. Evaluation of antihyperglycemic activity together with effects on blood hemoglobin content, to determine the therapeutic index, was performed in 8-day repeat administration studies in genetically obese C57 Bl/6 ob/ob mice. From these studies, BRL 49653 (37) has been selected, on the basis of antihyperglycemic potency combined with enhanced selectivity against reductions in blood hemoglobin content, for further evaluation.

  DOI：

  10.1021/jm00049a017

文献信息

• Heterocyclische Verbindungen
  申请人：NIHON BAYER AGROCHEM K.K.

  公开号：EP0192060A1

  公开（公告）日：1986-08-27

  Die vorliegende Erfindung betrifft neue heterocyclische Verbindungen der Formel (I) worin N 0 oder 1, R1, R2, R5 und R6 unabhängig voneinander ein Wasserstoffatom oder eine Alkylgruppe bedeuten, R3 und R4 unabhängig voneinander ein Wasserstoffatom, eine Hydroxygruppe oder eine Alkylgruppe bezeichnen, wenn n 1 bezeichnet, R2 eine Einfachbindung zusammen mit R5 zu bilden vermag, X ein Schwefelatom, ein Sauerstoffatom oder die folgenden Gruppen bedeutet: worin R7 und R8 die im Anmeldetext angegebene Bedeutung haben, R ein Wasserstoffatom oder eine Alkylgruppe bedeutet, Y ein Stickstoffatom oder die Gruppe bedeutet, worin R9 die im Anmeldungstext angegebene Bedeutung hat und Z die im Anmeldungstext angegebene Bedeutung hat.

  本发明涉及式 (I) 的新型杂环化合物 其中 N 是 0 或 1、 R1、R2、R5 和 R6 独立地表示氢原子或烷基、 R3 和 R4 独立地表示氢原子、羟基或烷基，当 n 表示 1 时，R2 能与 R5 形成单键、 X 表示硫原子、氧原子或以下基团： 其中 R7 和 R8 具有应用文本中给出的含义、 R 代表氢原子或烷基，Y 代表氮原子或以下基团 其中 R9 具有本申请文本中给出的含义，以及 Z 具有本申请文本中给出的含义。
• Inhibitors of the Notch transcriptional activation complex and methods for use of the same
  申请人：UNIVERSITY OF MIAMI

  公开号：US10501413B2

  公开（公告）日：2019-12-10

  Disclosed herein are inhibitors of the Notch transcriptional activation complex, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: Formula (I), wherein the substituents are as described.

  本文公开了 Notch 转录激活复合物的抑制剂，以及将其用于治疗或预防癌症等疾病的方法。本文所述的抑制剂可包括式（I）化合物及其药学上可接受的盐类：式 (I)，其中取代基如所述。
• INHIBITORS OF THE NOTCH TRANSCRIPTIONAL ACTIVATION COMPLEX AND METHODS FOR USE OF THE SAME
  申请人：SPYVEE Mark

  公开号：US20180086700A1

  公开（公告）日：2018-03-29

  Disclosed herein are inhibitors of the Notch transcriptional activation complex, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: Formula (I), wherein the substituents are as described.
• US4742060A
  申请人：——

  公开号：US4742060A

  公开（公告）日：1988-05-03
• US4845106A
  申请人：——

  公开号：US4845106A

  公开（公告）日：1989-07-04