2-amino-1-benzyloxy-3-methylbutane | 116774-42-6

• 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: 2-amino-1-benzyloxy-3-methylbutane
• 英文别名: 3-Methyl-1-phenylmethoxybutan-2-amine
• CAS: 116774-42-6
• 化学式: C₁₂H₁₉NO
• 分子量: 193.289
• InChiKey: BTNSRWZJXQKKKS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  14
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 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：

  2-amino-1-benzyloxy-3-methylbutane 、 溴乙酰溴 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 4.0h， 以76%的产率得到
  参考文献：
  名称：

  An Air/Water-Stable Tridentate N-Heterocyclic Carbene- Palladium(II) Complex: Catalytic CH Activation of HydrocarbonsviaHydrogen/Deuterium Exchange Process in Deuterium Oxide

  摘要：

  Abstractmagnified imageWhile developing novel catalysts for carbon‐carbon or carbon‐heteroatom coupling (nitrogen, oxygen, or fluorine), we were able to introduce tridentate N‐heterocyclic carbene (NHC)‐amidate‐alkoxide palladium(II) complexes. In aqueous solution, these NHC‐Pd(II) complexes showed high ability for CH activation of various hydrocarbons (cyclohexane, cyclopentane, dimethyl ether, tetrahydrofuran, acetone, and toluene) under mild conditions.

  DOI：

  10.1002/adsc.200800698
• 作为产物：
  描述：

  tert-butyl N-(3-methyl-1-phenylmethoxybutan-2-yl)carbamate 在 甲酸 作用下， 生成 2-amino-1-benzyloxy-3-methylbutane
  参考文献：
  名称：

  An Air/Water-Stable Tridentate N-Heterocyclic Carbene- Palladium(II) Complex: Catalytic CH Activation of HydrocarbonsviaHydrogen/Deuterium Exchange Process in Deuterium Oxide

  摘要：

  Abstractmagnified imageWhile developing novel catalysts for carbon‐carbon or carbon‐heteroatom coupling (nitrogen, oxygen, or fluorine), we were able to introduce tridentate N‐heterocyclic carbene (NHC)‐amidate‐alkoxide palladium(II) complexes. In aqueous solution, these NHC‐Pd(II) complexes showed high ability for CH activation of various hydrocarbons (cyclohexane, cyclopentane, dimethyl ether, tetrahydrofuran, acetone, and toluene) under mild conditions.

  DOI：

  10.1002/adsc.200800698

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。
• Mitomycin derivatives
  申请人：KYOWA HAKKO KOGYO KABUSHIKI KAISHA

  公开号：EP0272063A1

  公开（公告）日：1988-06-22

  Mitomycin derivatives having potent anti-tumour activity having the formula: wherein A is selected from the following (i) to (v):- wherein R1 is selected from unsubstituted or substituted alkyl (wherein the substituent is one or more members independently selected from lower alkoxycarbonyl, benzyloxy, benzyloxycarbonyl, carboxy, halogen, hydroxy, lower alkoxy, lower alkanoyloxy, trilower alkylsilyloxy, amino, lower alkylamino, dilower alkylamino and benzyloxycarbonylamino), unsubstituted or substituted cycloalkyl (wherein the substituent is one or more members independently selected from lower alkyl, lower alkoxycarbonyl, benzyloxycarbonyl, carboxy, halogen, hydroxy, lower alkoxy, lower alkanoyloxy, trilower alkylsilyloxy, amino, lower alkylamino, dilower alkylamino and benzyloxycarbonylamino), unsubstituted or substituted aralkyl (wherein the benzene nucleus is substituted by one or more members independently selected from lower alkoxy, halogen, lower alkyl, nitro, hydroxy, amino, cyano and carboxy), 2-benzyloxycarbonyl-1-phenylethyl and (wherein R3 is selected from hydrogen, benzyl, lower alkyl, lower alkanoyl and benzyloxycarbonyl; and p is 0 or 1) and R2 represents hydrogen; or R1 and R2 each independently represents alkyl; (ii) morpholino; wherein R4 is selected from hydrogen, hydroxy, lower alkoxy, lower alkanoyloxy, lower alkylamino, dilower alkylamino, benzyloxycarbonylamino and benzyl; and q is 0 or 1; wherein R5 represents hydrogen or hydroxy; Y represents hydroxy, lower alkoxy, benzyloxy, lower alkanoyloxymethoxy, amino, lower alkylamino, dilower alkylamino, benzylamino or (wherein Re represents hydrogen or hydroxy); and wherein R7 is selected from hydrogen, lower alkanoyl, trifluoroacetyl, benzoyl, benzyloxycarbonyl, lower alkoxycarbonyl, lower alkyl and benzyl; and R8 represents hydrogen or lower alkyl; . n is 0 or 1, provided that when n is 0, X represents oxygen or sulphur and when n is 1, X is oxygen; m is an integer of from 2 to 8; and Ra and Rb each independently represents hydrogen or methyl provided that Ra and Rb do not both represent hydrogen, and carboxylic acid salts thereof.

  具有强效抗肿瘤活性的丝裂霉素衍生物，其式如下 其中 A 选自以下(i)至(v)项：- 其中 R1 选自未取代或取代的烷基（其中取代基是一个或多个成员，独立选自低 级烷氧基羰基、苄氧基、苄氧羰基、羧基、卤素、羟基、低级烷氧基、低级烷酰氧基、 三低级烷基硅氧基、氨基、低级烷基氨基、稀低级烷基氨基和苄氧羰基氨基）、未取代或取代 的环烷基（其中取代基是一个或多个成员，独立选自低级烷基、未取代或取代的芳烷基（其中苯核被一个或多个独立选自下烷氧基、卤素、下烷基、硝基、羟基、氨基、氰基和羧基的成员取代）、2-苄氧羰基-1-苯乙基和 2-苄氧羰基-1-苯乙基（其中 R3 独立选自下烷氧基、卤素、下烷基、硝基、羟基、氨基、氰基和羧基）。 (其中 R3 选自氢、苄基、低级烷基、低级烷酰基和苄氧羰基；p 为 0 或 1），R2 代表氢；或 R1 和 R2 各自独立地代表烷基； (ii) 吗啉基； 其中 R4 选自氢、羟基、低级烷氧基、低级烷酰氧基、低级烷基氨基、稀释烷基 氨基、苄氧羰基氨基和苄基；且 q 为 0 或 1； 其中 R5 代表氢或羟基；Y 代表羟基、低级烷氧基、苄氧基、低级烷酰氧基甲氧基、氨基、低级烷基氨基、稀释烷基氨基、苄基氨基或苄基。 (其中 Re 代表氢或羟基）；以及 其中 R7 选自氢、低级烷酰基、三氟乙酰基、苯甲酰基、苄氧羰基、低级烷氧羰基、低级烷基和苄基；R8 代表氢或低级烷基；.n 为 0 或 1，条件是当 n 为 0 时，X 代表氧或硫，而当 n 为 1 时，X 代表氧；m 为 2 至 8 的整数；Ra 和 Rb 各自独立地代表氢或甲基，条件是 Ra 和 Rb 不同时代表氢，以及它们的羧酸盐。
• Heteroaryl compounds and their use as therapeutic drugs
  申请人：Dong-A Socio Holdings Co., Ltd.

  公开号：US10125118B2

  公开（公告）日：2018-11-13

  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.

  本发明提供了能够调节Mer受体酪氨酸激酶（MERTK）活性的杂环化合物、其立体异构体、对映体或药学上可接受的盐。本发明还提供了其药物组合物、制备上述化合物的方法以及此类化合物作为药物的用途。 本发明涉及具有显著效力的 MERTK 抑制性化合物，因此在对癌症和任何其他与 MERTK 失调有关的疾病进行药物干预方面具有突出的潜力。
• HETEROARYL COMPOUNDS AND THEIR USE AS THERAPEUTIC DRUGS
  申请人：Dong-A Socio Holdings Co., Ltd.

  公开号：EP3344613A1

  公开（公告）日：2018-07-11
• US4863935A
  申请人：——

  公开号：US4863935A

  公开（公告）日：1989-09-05