Butyl 2-(4-bromophenyl)acetate | 133017-10-4

• 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: Butyl 2-(4-bromophenyl)acetate
• 英文别名: n-Butyl 2-(4-bromophenyl)acetate
• CAS: 133017-10-4
• 化学式: C₁₂H₁₅BrO₂
• 分子量: 271.154
• InChiKey: MMLFPGZTRUZTEV-UHFFFAOYSA-N

物化性质

• 沸点：
  317.4±17.0 °C(Predicted)
• 密度：
  1.303±0.06 g/cm3(Predicted)
• 保留指数：
  1781

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  15
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  Butyl 2-(4-bromophenyl)acetate 在 叠氮磷酸二苯酯 、 水 、 三乙胺 、 sodium hydroxide 、 lithium hexamethyldisilazane 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 反应 48.0h， 生成 [1-(4-溴苯基)-环丙基]氨基甲酸叔丁酯
  参考文献：
  名称：

  1-杂芳基/芳基环烷基胺的通用且经济有效的合成方法及其广泛应用

  摘要：

  已经开发了一种通用且成本有效的途径，以容易的产率从易得的杂芳基乙酸酯合成1-杂芳基取代的环烷基胺。该合成具有LHMDS促进环化和一锅水解/柯式重排的特点。该途径可以容易地以克为单位进行，并且还可以用于制备1-芳基取代的环烷基/环杂烷基胺。1-杂芳基/芳基取代的环烷基/环杂烷基胺是通用的构建基块，它们在有机和药物化学中的应用已在吗啉和N-甲基哌嗪类似物以及已知的Rho激酶抑制剂化合物9的合成中得到证明。

  DOI：

  10.1016/j.tet.2016.02.060

文献信息

• Copper on charcoal: Cu⁰ nanoparticle catalysed aerobic oxidation of α-diazo esters
  作者：Rong Zhao、Jiangge Teng、Zhiwei Wang、Wenwen Dong、Jia Lin、Changhu Chu

  DOI：10.1039/d1ob00811k

  日期：——

  By using a charcoal supported nano Cu0 catalyst (Cu/C), a highly efficient oxidation of α-diazo esters to α-ketoesters with molecular oxygen as the sole oxidant has been developed. In the presence of the Cu/C catalyst, 2-aryl-α-diazo esters with both electron-donating and electron-withdrawing groups can be oxidized to the corresponding α-ketoesters efficiently. Furthermore, this Cu/C catalyst can catalyse

  通过使用木炭负载纳米Cu 0催化剂（Cu / C），已开发出一种以分子氧为唯一氧化剂将α-重氮酯高效氧化为α-酮酯的方法。在Cu/C催化剂存在下，具有给电子基团和吸电子基团的2-芳基-α-重氮酯可以有效地氧化成相应的α-酮酯。此外，该Cu/C催化剂可以催化芳基α-重氮酯与水反应生成芳基酮酯、2-芳基-2-羟基乙酸酯和2-芳基乙酸酯。在这种情况下，水被α-重氮酯分解，重氮基团被水中的氧或氢原子取代。机理研究表明，α-重氮酯与氧的反应通过自由基途径进行。在 2,2,6,6-四甲基哌啶氮氧化物存在下，α-重氮酯与氧的反应被显着抑制。此外，通过同位素示踪法研究了α-重氮酯与水的反应，GCMS检测表明α-重氮酯与水发生了歧化反应。
• Novel Antagonists of the Glucagon Receptor
  申请人：Gomez-Galeno Jorge E.

  公开号：US20120214769A1

  公开（公告）日：2012-08-23

  The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

  本发明提供了式（I）的新化合物及其药学上可接受的盐和共晶体，具有胰高血糖素受体拮抗剂或反向激动剂活性。本发明还提供了包含该化合物的制药组合物，以及治疗、预防、延迟发病时间或降低一种或多种需要胰高血糖素受体拮抗剂的疾病或症状的发展或进展的方法，包括1型和2型糖尿病、胰岛素抵抗和高血糖。本发明还提供了制备式I的化合物，包括其盐和共晶体的方法，以及包含该化合物的制药组合物。
• NOVEL ANTAGONISTS OF THE GLUCAGON RECEPTOR
  申请人：Metabasis Therapeutics, Inc.

  公开号：US20140135400A1

  公开（公告）日：2014-05-15

  The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

  本发明提供了一种新型化合物Formula (I)及其药学上可接受的盐和共晶体，具有胰高血糖素受体拮抗剂或反向激动剂活性。本发明还提供了包含这些化合物的药物组合物，以及用于治疗、预防、延迟发病时间或降低一种或多种胰高血糖素受体拮抗剂适用的疾病或病症的风险，包括I型和II型糖尿病、胰岛素抵抗和高血糖的方法。本发明还提供了制备Formula (I)化合物，包括其盐和共晶体，以及包含它们的药物组合物的方法。
• Antagonists of the glucagon receptor
  申请人：Metabasis Therapeutics, Inc.

  公开号：EP2786985A2

  公开（公告）日：2014-10-08

  The present invention provides for novel compounds of Formula I and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as their use in methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistence and hyperglycemia.

  本发明提供了具有胰高血糖素受体拮抗剂或反向激动剂活性的新型式 I 化合物及其药学上可接受的盐和共晶体。本发明进一步提供了包含这些化合物的药物组合物，以及它们在治疗、预防、推迟发病时间或降低疾病或病情发展或恶化风险的方法中的用途，这些疾病或病情适用于一种或多种胰高血糖素受体拮抗剂，包括 I 型和 II 型糖尿病、胰岛素抵抗和高血糖症。
• Aromatic heterocyclic compound
  申请人：MITSUBISHI TANABE PHARMA CORPORATION

  公开号：US10308636B2

  公开（公告）日：2019-06-04

  The compound represented by the general formula: wherein ring A is benzene which may be substituted and the like; ring B is benzene which may be substituted and the like; X is a single bond and the like; Y is alkyl which may be substituted and the like; Z is CR1 or nitrogen atom; R1 is hydrogen and the like; R2 is alkyl which may be substituted and the like or a pharmaceutically acceptable salt thereof is useful as a prevention/treatment agent of obesity, diabetes, and the like.

  由通式表示的化合物：其中环 A 是苯，可被取代等；环 B 是苯，可被取代等；X 是单键等；Y 是烷基，可被取代等；Z 是 CR1 或氮原子；R1 是氢等；R2 是烷基，可被取代等或其药学上可接受的盐，可用作肥胖症、糖尿病等的预防/治疗剂。