1-[4-chloro-2-benzoylphenyl]-3-phthalimidopropan-1-one | 76049-60-0

• 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: 1-[4-chloro-2-benzoylphenyl]-3-phthalimidopropan-1-one
• 英文别名: 2-[3-(2-benzoyl-4-chlorophenyl)-3-oxopropyl]isoindole-1,3-dione
• CAS: 76049-60-0
• 化学式: C₂₄H₁₆ClNO₄
• 分子量: 417.848
• InChiKey: TUFXCBHXGAMBBE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  71.5
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-[4-chloro-2-benzoylphenyl]-3-phthalimidopropan-1-one 在 copper(ll) bromide 作用下， 以 四氢呋喃 、 乙醇 、 氯仿 、 乙酸乙酯 为溶剂， 反应 1.5h， 生成 2-<<2-amino-4-(2-benzoyl-4-chlorophenyl)-5-thiazolyl>methyl>-1H-isoindole-1,3(2H)-dione
  参考文献：
  名称：

  2-Benzazepines. 2. Thiazolo[5,4-d][2]benzazepines

  摘要：

  As part of a program in the area of annelated 2-benzazepines, several thiazolo[5,4-d))[2]benzazepines were prepared. Treatment of the bromo ketones 7-9 with various thio amides gave the thiazoles 10-15, which when treated with methylamine gave the title compounds. The preliminary pharmacology of these compounds showed that they had central nervous system activity similar to the 1,4-benzodiazepines, such as diazepam. The thiazolo[5,4-d][2]benzazepines were also found to bind to the benzodiazepine-receptor complex, indicating that their pharmacological actions are probably related to the 1,4-benzodiazepines.

  DOI：

  10.1021/jm00355a020
• 作为产物：
  描述：

  1-[4-chloro-2-benzoylphenyl]-3-phthalimidopropyne 在 甲酸 、 水 、 mercury(II) sulfate 作用下， 以 二氯甲烷 为溶剂， 反应 0.67h， 以65%的产率得到1-[4-chloro-2-benzoylphenyl]-3-phthalimidopropan-1-one
  参考文献：
  名称：

  2-Benzazepines. 2. Thiazolo[5,4-d][2]benzazepines

  摘要：

  As part of a program in the area of annelated 2-benzazepines, several thiazolo[5,4-d))[2]benzazepines were prepared. Treatment of the bromo ketones 7-9 with various thio amides gave the thiazoles 10-15, which when treated with methylamine gave the title compounds. The preliminary pharmacology of these compounds showed that they had central nervous system activity similar to the 1,4-benzodiazepines, such as diazepam. The thiazolo[5,4-d][2]benzazepines were also found to bind to the benzodiazepine-receptor complex, indicating that their pharmacological actions are probably related to the 1,4-benzodiazepines.

  DOI：

  10.1021/jm00355a020

文献信息

• N-oxides of 5-oxo-1-phenyl-2-benzazepines
  申请人：Hoffmann-La Roche Inc.

  公开号：US04469633A1

  公开（公告）日：1984-09-04

  Compounds of the formula ##STR1## wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl, are disclosed. The compounds are useful as intermediates in the production of 2-benzazepines, compounds of pharmacological activity. Also disclosed are other intermediates and processes for their production.

  公式为##STR1##的化合物被揭示，其中X和Y选自氢，卤素和三氟甲基。这些化合物可用作2-苯并氮杂环化合物的中间体，这些化合物具有药理活性。还揭示了其他中间体和它们的制备方法。
• Intermediates in the production of 2-benzazepines
  申请人：Hoffmann-La Roche Inc.

  公开号：US04318854A1

  公开（公告）日：1982-03-09

  Compounds of the formula ##STR1## wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl, are disclosed. The compounds are useful as intermediates in the production of 2-benzazepines, compounds of pharmacological activity. Also disclosed are other intermediates and processes for their production.

  公式为##STR1##的化合物揭示了其中X和Y选择自氢、卤素和三氟甲基的群组。这些化合物在生产具有药理活性的2-苯并氮杂环化合物的中间体中是有用的。还揭示了其他中间体和它们的生产过程。
• Production of 1-halophenyl and
  申请人：Hoffmann-La Roche Inc.

  公开号：US04388239A1

  公开（公告）日：1983-06-14

  Compounds of the formula ##STR1## wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl, are disclosed. The compounds are useful as intermediates in the production of 2-benzazepines, compounds of pharmacological activity. Also disclosed are other intermediates and processes for their production.

  公式为##STR1##的化合物被披露，其中X和Y选自氢，卤素和三氟甲基。这些化合物在2-苯并氮杂环类化合物的生产中作为中间体是有用的，这些化合物具有药理活性。还披露了其他中间体和它们的生产过程。
• Production of 2-benzazepines
  申请人：Hoffmann-La Roche Inc.

  公开号：US04394311A1

  公开（公告）日：1983-07-19

  Compounds of the formula ##STR1## wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl, are disclosed. The compounds are useful as intermediates in the production of 2-benzazepines, compounds of pharmacological activity. Also disclosed are other intermediates and processes for their production.

  公式为##STR1##的化合物被披露，其中X和Y选择自氢，卤素和三氟甲基的组。这些化合物可用作生产具有药理活性的2-苯并氮杂环化合物的中间体。还披露了其他中间体和它们的生产过程。
• Process for the preparation of 1-(phenyl and
  申请人：Hoffmann-La Roche Inc.

  公开号：US04379090A1

  公开（公告）日：1983-04-05

  Compounds of the formula ##STR1## wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl, are disclosed. The compounds are useful as intermediates in the production of 2-benzazepines, compounds of pharmacological activity. Also disclosed are other intermediates and processes for their production.

  公式为##STR1##的化合物被揭示，其中X和Y选自氢，卤素和三氟甲基。这些化合物在2-苯并氮杂环的生产中作为中间体是有用的，这些化合物具有药理活性。还揭示了其他中间体和它们的生产过程。