4-[(1S)-1-肼基乙基]-苯甲酸 | 924887-08-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 4-[(1S)-1-肼基乙基]-苯甲酸
• 英文名称: 4-[(1S)-1-hydrazinylethyl]benzoic acid
• CAS: 924887-08-1
• 化学式: C₉H₁₂N₂O₂
• 分子量: 180.206
• InChiKey: ZIKOQDHMWSGDEP-LURJTMIESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.8
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  75.4
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  (S)-1-p-carboethoxyphenyl-1-(2-benzoylhydrazino)ethane 在 盐酸 、 水 作用下， 反应 24.0h， 生成 4-[(1S)-1-肼基乙基]-苯甲酸
  参考文献：
  名称：

  Catalytic Enantioselective Hydrogenation of N-Alkoxycarbonyl Hydrazones: A Practical Synthesis of Chiral Hydrazines

  摘要：

  An enantioselective hydrogenation of hydrazones catalyzed by Rh complexes (Rh-Josiphos or Rh-Taniaphos) has been developed. The protocol can be applied to hydrazones with three different protective groups (Boc, Cbz, and methoxycarbonyl), allowing for selective deprotection and further elaboration of the hydrazine products in the presence of other functional groups.

  DOI：

  10.1021/ol902602c

文献信息

• [EN] PROCESS FOR THE PRODUCTION OF A CRYSTALLINE GLUCAGON RECEPTOR ANTAGONIST COMPOUND<br/>[FR] PROCÉDÉ POUR LA PRODUCTION D'UN COMPOSÉ CRISTALLIN ANTAGONISTE DU RÉCEPTEUR DU GLUCAGON
  申请人：MERCK & CO INC

  公开号：WO2009035558A1

  公开（公告）日：2009-03-19

  The present invention relates to a process for the production of crystalline particles of a glucagon receptor antagonist compound. The process includes the steps of generating microseeds and subjecting the microseeds to a crystallization process. The resulting crystalline particles have a mean particle size of less than about 100 mm. The present invention also provides for a pharmaceutical composition which includes the crystalline particles produced by the method described herein and a pharmaceutically acceptable carrier.

  本发明涉及一种制备葡萄糖高升素受体拮抗剂化合物的晶体颗粒的方法。该方法包括生成微晶种并将微晶种暴露于结晶过程中。所得到的晶体颗粒的平均粒径小于约100毫米。本发明还提供了一种制药组合物，其中包括通过本文所述方法制备的晶体颗粒和药用可接受载体。
• PROCESS FOR THE PRODUCTION OF A CRYSTALLINE GLUCAGON RECEPTOR ANTAGONIST COMPOUND
  申请人：Cohen Benjamin M.

  公开号：US20100184995A1

  公开（公告）日：2010-07-22

  The present invention relates to a process for the production of crystalline particles of a glucagon receptor antagonist compound. The process includes the steps of generating microseeds and subjecting the microseeds to a crystallization process. The resulting crystalline particles have a mean particle size of less than about 100 mm. The present invention also provides for a pharmaceutical composition which includes the crystalline particles produced by the method described herein and a pharmaceutically acceptable carrier.
• US8232413B2
  申请人：——

  公开号：US8232413B2

  公开（公告）日：2012-07-31
• Catalytic Enantioselective Hydrogenation of <i>N</i>-Alkoxycarbonyl Hydrazones: A Practical Synthesis of Chiral Hydrazines
  作者：Naoki Yoshikawa、Lushi Tan、J. Christopher McWilliams、Deepa Ramasamy、Ruth Sheppard

  DOI：10.1021/ol902602c

  日期：2010.1.15

  An enantioselective hydrogenation of hydrazones catalyzed by Rh complexes (Rh-Josiphos or Rh-Taniaphos) has been developed. The protocol can be applied to hydrazones with three different protective groups (Boc, Cbz, and methoxycarbonyl), allowing for selective deprotection and further elaboration of the hydrazine products in the presence of other functional groups.