N-(triphenylmethyl)succinimide | 66365-49-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: N-(triphenylmethyl)succinimide
• 英文别名: N-tritylsuccinimide；N-Triphenylmethyl-succinimid；N-Trityl-succinimid；1-Trityl-2,5-pyrrolidinedione；1-tritylpyrrolidine-2,5-dione
• CAS: 66365-49-9
• 化学式: C₂₃H₁₉NO₂
• 分子量: 341.409
• InChiKey: AHENCLFHHZTCCL-UHFFFAOYSA-N

物化性质

• 熔点：
  203-204 °C
• 沸点：
  578.5±49.0 °C(Predicted)
• 密度：
  1.227±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  26
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  37.4
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-(triphenylmethyl)succinimide 在 硼烷四氢呋喃络合物 作用下， 以 四氢呋喃 为溶剂， 反应 6.0h， 以81%的产率得到N-tritylpyrrolidine
  参考文献：
  名称：

  PREPARATION OFN-TRITYLPYRROLIDINE ANDN-TRITYLPIPERIDINE

  摘要：

  DOI：

  10.1080/00304949909355715
• 作为产物：
  描述：

  丁二酰亚胺 、 三苯基氯甲烷 在 potassium carbonate 作用下， 以 乙腈 为溶剂， 以26%的产率得到N-(triphenylmethyl)succinimide
  参考文献：
  名称：

  具有增强活性的烟酰胺N-甲基转移酶（NNMT）的双底物抑制剂。

  摘要：

  烟酰胺N-甲基转移酶（NNMT）催化烟酰胺的甲基化以形成N-甲基烟酰胺。NNMT的过度表达与多种疾病（包括许多癌症和代谢紊乱）有关，这表明NNMT作为潜在的治疗靶标具有重要作用。通过对先前在我们小组中开发的NNMT抑制剂的结构进行修饰，我们制备了多种抑制剂库来探测酶活性位点的不同区域。这项研究表明，旨在通过π-π堆积相互作用结合疏水烟酰胺结合口袋的萘部分的引入显着提高了双底物样NNMT抑制剂的活性（半数最大抑制浓度为1.41μM）。这些发现得到了等温滴定量热结合试验和模型研究的进一步支持。在本研究中鉴定出的最具活性的NNMT抑制剂对HSC-2人口腔癌细胞系的细胞增殖表现出剂量依赖性抑制作用。

  DOI：

  10.1021/acs.jmedchem.9b00413

文献信息

• MELANIN PRODUCTION INHIBITOR
  申请人：Yokoyama Kouji

  公开号：US20110243865A1

  公开（公告）日：2011-10-06

  Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor comprises a compound represented by general formula (1) (excluding clotrimazole), and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent, wherein at least one of A1, A2 and A3 is selected from the aryl group and the aromatic heterocyclic group, the total number of carbon atoms contained in A1, A2 and A3 is 6 to 50 and, when at least two of A1, A2 and A3 represent the aryl groups or the aromatic heterocyclic groups, the adjacent two aryl or aromatic heterocyclic groups may be bound to each other via an alkyl chain or an alkenyl chain to form a ring; m represents an integer of 0 to 2; X represents a hetero atom, a hydrogen atom, or a carbon atom; R1 and R2 are independently selected from a hydrogen atom and an oxo group, wherein when one of R1 and R2 is an oxo group, the other is not present; and R3 is selected from a hydrogen atom, and a C 1-8 hydrocarbon group in which one or some of hydrogen atoms or carbon atoms may be substituted by a hetero atom or hetero atoms, wherein the number of R3's present in the compound corresponds to the number of X's and, when two or more R3's are present, the R3's are independently present and the adjacent two R3's may be bound to each other to form, together with X, a ring, and the terminal of R3 may be bound to a carbon atom to which A1, A2 and A3 are bound, thereby forming a ring.

  披露了一种黑色素生产抑制剂，它对黑色素的生产具有出色的抑制活性且高度安全。该黑色素生产抑制剂包括由通用公式（1）表示的化合物（不包括克霉唑）和/或其药理上可接受的盐。在公式中，A1、A2和A3独立地选自氢原子、可能带有取代基的芳基团和可能带有取代基的芳香杂环团，其中至少A1、A2和A3之一选自芳基团和芳香杂环团，A1、A2和A3中包含的碳原子总数为6至50，并且当至少两个A1、A2和A3表示芳基团或芳香杂环团时，相邻的两个芳基或芳香杂环团可以通过烷基链或烯基链相互连接形成环；m代表0至2的整数；X代表异原子、氢原子或碳原子；R1和R2独立地选自氢原子和氧代基，其中当R1和R2之一是氧代基时，另一个不出现；R3选自氢原子和C 1-8 碳氢化合物组，其中一些或所有的氢原子或碳原子可能被异原子或异原子取代，其中化合物中存在的R3的数量对应于X的数量，并且当存在两个或更多R3时，R3独立地存在，并且相邻的两个R3可以相互连接以与X一起形成环，并且R3的末端可以与A1、A2和A3连接的碳原子结合，从而形成环。
• Melanin production inhibitor
  申请人：Pola Chemical Industries Inc.

  公开号：EP2845587A2

  公开（公告）日：2015-03-11

  Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor comprises a compound represented by general formula (1) (excluding clotrimazole) and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent, wherein at least one of A1, A2 andA3 is selected from the aryl group and the aromatic heterocyclic group, the total number of carbon atoms contained in A1, A2 and A3 is 6 to 50 and, when at least two of A1, A2 and A3 represent the aryl groups or the aromatic heterocyclic groups, the adjacent two aryl or aromatic heterocyclic groups may be bound to each other via an alkyl chain or an alkenyl chain to form a ring; m represents an integer of 0 to 2; X represents a hetero atom, a hydrogen atom, or a carbon atom; R1 and R2 are independently selected from a hydrogen atom and an oxo group, wherein when one of R1 and R2 is an oxo group, the other is not present; and R3 is selected from a hydrogen atom, and a C1-8 hydrocarbon group in which one or some of hydrogen atoms or carbon atoms may be substituted by a hetero atom or hetero atoms, wherein the number of R3's present in the compound corresponds to X and, when two or more R3' s are present, the R3' s are independently present and the adjacent two R3's may be bound to each other to form, together with X, a ring, and the terminal of R3 may be bound to a carbon atom to which A1, A2 and A3 are bound, thereby forming a ring.

  本发明公开了一种黑色素生成抑制剂，它对黑色素的生成具有极佳的抑制活性，且安全性高。黑色素生成抑制剂包括通式（1）代表的化合物（不包括克霉唑）和/或其药理上可接受的盐。式中，A1、A2 和 A3 独立选自氢原子、可具有取代基的芳基和可具有取代基的芳香杂环基团，其中 A1、A2 和 A3 中至少有一个选自芳基和芳香杂环基团、A1、A2 和 A3 所含的碳原子总数为 6 至 50，当 A1、A2 和 A3 中至少有两个代表芳基或芳香杂环基团时，相邻的两个芳基或芳香杂环基团可通过烷基链或烯基链相互结合形成一个环；m 代表 0 至 2 的整数； X 代表杂原子、氢原子或碳原子；R1 和 R2 分别独立地选自氢原子和氧代基团，其中当 R1 和 R2 中的一个是氧代基团时，另一个不存在；R3选自氢原子和C1-8烃基，其中一个或部分氢原子或碳原子可被一个或多个杂原子取代，其中化合物中存在的R3的数目与X相对应，当存在两个或多个R3's时，R3's独立存在，相邻的两个R3's可相互结合，与X一起形成一个环，R3的末端可与A1、A2和A3所结合的碳原子结合，从而形成一个环。
• The Lithium Aluminum Hydride Reduction of Some N-Substituted Succinimides¹
  作者：KURT C. SCHREIBER、VINCENT P. FERNANDEZ

  DOI：10.1021/jo01065a012

  日期：1961.6
• Eberson, Lennart; Finkelstein, Manuel; Hart, Shirly A., Acta Chemica Scandinavica, 1989, vol. 43, # 10, p. 1000 - 1003
  作者：Eberson, Lennart、Finkelstein, Manuel、Hart, Shirly A.、Ross, Sidney D.

  DOI：——

  日期：——
• A REVERSIBLE STOICHIOMETRIC PROCESS FOR CONJUGATING BIOMOLECULES
  申请人：KÖSTER, Hubert

  公开号：EP1000081A2

  公开（公告）日：2000-05-17