2-(2-溴苄氧基)苯胺 | 3434-04-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 中文名称: 2-(2-溴苄氧基)苯胺
• 英文名称: 2-(2-bromobenzyloxy)aniline
• 英文别名: o-(o-bromobenzyloxy)aniline；2-(2-bromo-benzyloxy)-aniline；o--anilin；2-(o-Brom-benzyloxy)-anilin；2-(o-Bromobenzyloxy)-anilin；2-(o-Bromobenzyloxy) aniline；2-[(2-bromophenyl)methoxy]aniline
• CAS: 3434-04-6
• 化学式: C₁₃H₁₂BrNO
• mdl: MFCD09803660
• 分子量: 278.148
• InChiKey: QYJYHEDTIDXBLJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.076
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2922299090

反应信息

• 作为反应物：
  描述：

  2-(2-溴苄氧基)苯胺 在 copper(l) iodide 、 potassium tert-butylate 、 sodium hydride 、 L-脯氨酸 作用下， 以 乙醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 37.0h， 生成 6-(dibenzo[b,e][1,4]oxazepin-5(11H)-yl)-1-(piperidin-1-yl)hexan-2-ol
  参考文献：
  名称：

  Tricyclic dihydrobenzoxazepine and tetracyclic indole derivatives can specifically target bacterial DNA ligases and can distinguish them from human DNA ligase I

  摘要：

  DNA连接酶是所有生物体中DNA代谢的关键组成部分。

  DOI：

  10.1039/c5ob00439j
• 作为产物：
  描述：

  硝苯酚 在 盐酸 、 铁粉 、 potassium carbonate 作用下， 以 乙醇 、 丙酮 为溶剂， 反应 3.0h， 生成 2-(2-溴苄氧基)苯胺
  参考文献：
  名称：

  Tricyclic dihydrobenzoxazepine and tetracyclic indole derivatives can specifically target bacterial DNA ligases and can distinguish them from human DNA ligase I

  摘要：

  DNA连接酶是所有生物体中DNA代谢的关键组成部分。

  DOI：

  10.1039/c5ob00439j

文献信息

• Elaboration of the Oxazepine Ring System via CuI/<scp>l</scp>-Proline-Catalyzed Intramolecular Aryl Amination
  作者：Dawei Ma、Lei Guo、Ben Li、Wenlong Huang、Gang Pei

  DOI：10.1055/s-2008-1078506

  日期：——

  A two-step approach for assembling oxazepines is described, which started from 2-aminophenols and substituted 2-bromobenzyl bromides and used CuI/l-proline-catalyzed coupling reaction as the key step.

  该方法以 2-氨基苯酚和取代的 2-溴苄溴为起点，以 CuI/l 脯氨酸催化的偶联反应为关键步骤，分两步合成了草氮平。
• Process for producing new oxazepine derivatives
  申请人：AJINOMOTO CO. INC

  公开号：US20020133004A1

  公开（公告）日：2002-09-19

  A process for producing a 5-substituted-5,11-dihydro-debenzo [b,e] [1,4] oxazepine compound, wherein a [2-(2-bromobenzyloxy)phenyl]amide derivative having a substituent introduced through amido bond, the substituent locating at the 5-position of the final compound, as the starting material, is subjected to the intramolecular arylation and then the obtained product is reduced. In particular, (R)-1-[(4-methoxyphenyl)acetyl]pyrrolidine-2-carboxylic acid [2-(2-bromo benzyloxy)phenyl]amide is subjected to the intramolecular arylation to obtain (R)-[[2-(5,11-dihydro-dibenzo[b,e][1,4]oxazepine-5-carbonyl)pyrrolidin]-1-yl]-2-(4-methoxyphenyl)ethanone and then this product is reduced.

  一种制备5-取代-5，11-二氢-二苯并[b，e][1,4]噁唑啉化合物的方法，其中以[R]-1-[(4-甲氧基苯基)乙酰基]吡咯烷-2-羧酸[2-(2-溴苄氧基)苯基]酰胺作为起始物质，通过分子内芳基化反应，然后还原所得产物。具体来说，将[R]-[2-(2-溴苄氧基)苯基]酰胺-[1-[(4-甲氧基苯基)乙酰基]吡咯烷-2-羧酸]经过分子内芳基化反应，得到(R)-[[2-(5,11-二氢-二苯并[b,e][1,4]噁唑啉-5-羰基)吡咯烷-1-基]-2-(4-甲氧基苯基)乙酮，然后还原该产物。
• Dihydrodiaryloxazepine derivative and pharmaceutical composition containing the same
  申请人：Ajinomoto Co., Inc.

  公开号：US20040110742A1

  公开（公告）日：2004-06-10

  The present invention provides dihydrodiaryloxazepine derivative represented by the following formula [1], analogs thereof and pharmaceutical compositions containing them. Those compounds have an excellent effect of improving functional diseases of gastrointestinal tracts. 1

  本发明提供了以下公式（1）所表示的二氢二苯并噁唑啉衍生物，其类似物以及含有它们的制药组合物。这些化合物具有改善胃肠道功能性疾病的优异效果。
• Method for producing alkoxy arylamine compounds
  申请人：Honeywell International Inc.

  公开号：US06420606B1

  公开（公告）日：2002-07-16

  Disclosed are methods of producing of alkoxy arylamine compounds which find particular use in the syntheses of pharmaceutical drug. The alkoxy arylamine compounds generally have the formula: H2N—Ar—OR wherein Ar is an unsubstituted or substituted aromatic group, and R is an unsubstituted or substituted alkyl or aryl group. The methods comprise generally, the steps of (a) alkylating a protected-amino arylalcohol to form a protected-amino arylether; and (b) deprotecting said protected-amino arylether to form an alkoxy arylamine compound.

  本发明涉及一种制备烷氧基芳胺化合物的方法，该方法在制备药物中具有特殊用途。烷氧基芳胺化合物通常具有以下式子：H2N—Ar—OR，其中Ar是未取代或取代的芳香族基，R是未取代或取代的烷基或芳基。该方法通常包括以下步骤：(a)烷基化保护氨基芳基醇以形成保护氨基芳基醚；(b)去保护所述保护氨基芳基醚以形成烷氧基芳胺化合物。
• 3-PIPERIDYL-4-OXOQUINAZOLINE DERIVATIVES AND MEDICINCAL COMPOSITIONS CONTAINING THE SAME
  申请人：Japan Tobacco Inc.

  公开号：EP0970954A1

  公开（公告）日：2000-01-12

  3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 4, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases. Furthermore, they can be used as therapeutic or preventive agents for pancreatitis, obesity, hypercholesterolemia, and hypertriglyceridemia.

  提供了3-哌啶基-4-氧代喹唑啉衍生物，由式(I)表示： 其中 R 代表氨基或环状氨基，如二苯并氮杂卓，它们各自被取代或未被取代的芳基、取代或未被取代的杂芳基或类似基团取代，n 是 1 至 4 的整数，R3 和 R4 独立地代表氢原子、低级烷基或类似基团，或其药学上可接受的盐。本发明的化合物（I）具有优异的 MTP 抑制活性。因此，这些化合物不仅能抑制导致动脉硬化疾病的低密度脂蛋白的形成，还能调节血液中的总胆固醇、胆固醇和脂蛋白（如低密度脂蛋白），并通过调节 MTP 活性来调节细胞脂质。它们还可用作高脂血症或动脉硬化疾病的新型预防或治疗药物。此外，它们还可用作胰腺炎、肥胖症、高胆固醇血症和高甘油三酯血症的治疗或预防药物。