1-(Triphenylmethyl)piperazine | 32422-96-1

• 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: 1-(Triphenylmethyl)piperazine
• 英文别名: 1-tritylpiperazine
• CAS: 32422-96-1
• 化学式: C₂₃H₂₄N₂
• 分子量: 328.457
• InChiKey: LAZQWLMVJAIYFE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  15.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(Triphenylmethyl)piperazine 在 碳酸氢钠 、 三乙胺 作用下， 以 乙醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 40.0h， 生成 1-(7H-purin-6-ylsulfanyl)-3-(4-tritylpiperazin-1-yl)propan-2-ol
  参考文献：
  名称：

  Synthesis and structure-activity relationship of 6-substituted purine derivatives as novel selective positive inotropes

  摘要：

  A series of purine derivatives was prepared and examined for selective inotropic activity in vitro and in vivo. Thioether-linked derivatives were superior to their oxygen and nitrogen isosteres. Substitution of electron-withdrawing groups on the benzhydryl moiety of these agents increased potency. The best compound of the study, 17 (carsatrin), was examined further and demonstrated selective oral activity as a positive inotrope. These compounds are presumed to act by affecting the kinetics of the cardiac sodium channel by analogy to the prototypic agent DPI 201106 (1). Their high selectivity for increasing contractile force and dP/dt without affecting blood pressure or heart rate is consistent with this mechanism. Carsatrin (17) was selected as a potential development candidate.

  DOI：

  10.1021/jm00102a001
• 作为产物：
  描述：

  溴苯 在 magnesium 、 三乙胺 、 乙酰氯 作用下， 以 乙醚 、 二氯甲烷 、 苯 为溶剂， 反应 44.0h， 生成 1-(Triphenylmethyl)piperazine
  参考文献：
  名称：

  设计，合成和鉴定作为载脂蛋白E生产抑制剂的新型三芳基甲胺化合物

  摘要：

  我们已经确定了可以抑制载脂蛋白E（apoE）产生的一类新的三芳基甲胺化合物。ApoE是一种胆固醇和脂质载体蛋白，与衰老，动脉粥样硬化，阿尔茨海默氏病（AD）以及其他神经系统疾病和脂质相关疾病有关。apoE产生的减弱通常被认为具有治疗价值。大脑中的大部分apoE是由星形胶质细胞产生的。在这里，我们描述了一个小的化合物文库的设计，合成和生物学筛选，该文库导致了四种三芳基甲胺的鉴定，它们是CCF-STTG1星形细胞瘤细胞中apoE产生的有效抑制剂。

  DOI：

  10.1016/j.bmcl.2012.08.009

文献信息

• SYNTHESIS OF MORPHOLINO OLIGOMERS USING DOUBLY PROTECTED GUANINE MORPHOLINO SUBUNITS
  申请人：REEVES MATTHEW DALE

  公开号：US20090131624A1

  公开（公告）日：2009-05-21

  Morpholino compounds are provided having the structure: where R 1 is selected from the group consisting of lower alkyl, di(lower alkyl)amino, and phenyl; R 2 is selected from the group consisting of lower alkyl, monocyclic arylmethyl, and monocyclic (aryloxy)methyl; R 3 is selected from the group consisting of triarylmethyl and hydrogen; and Y is selected from the group consisting of: a protected or unprotected hydroxyl or amino group; a chlorophosphoramidate group; and a phosphorodiamidate linkage to the ring nitrogen of a further morpholino compound or a morpholino oligomer. Such compounds include doubly protected morpholino guanine (MoG) monomers. Also described is their use in synthesis of morpholino oligomers.

  Morpholino化合物具有以下结构： 其中 R1选自由较低烷基、二(较低烷基)氨基和苯基组成的群体； R2选自由较低烷基、单环芳基甲基和单环(芳氧基)甲基组成的群体； R3选自由三芳基甲基和氢原子组成的群体；以及 Y选自由受保护或未受保护的羟基或氨基团；氯磷酰胺基团；以及与另一种morpholino化合物或morpholino寡聚体的环氮原子形成磷酰二胺酸酯键的群体。这类化合物包括双保护的morpholino鸟嘌呤（MoG）单体。还描述了它们在morpholino寡聚体合成中的用途。
• EXON SKIPPING COMPOSITIONS FOR TREATING MUSCULAR DYSTROPHY
  申请人：SAREPTA THERAPEUTICS, INC.

  公开号：US20160040162A1

  公开（公告）日：2016-02-11

  Antisense molecules capable of binding to a selected target site in the human dystrophin gene to induce exon 53 skipping are described.

  抗义RNA分子能够结合到人类肌营养不良蛋白基因中的特定靶位点，诱导外显子53跳跃。
• [EN] EXON SKIPPING OLIGOMER CONJUGATES FOR MUSCULAR DYSTROPHY<br/>[FR] CONJUGUÉS OLIGOMÈRES DE SAUTS D'EXONS POUR LA DYSTROPHIE MUSCULAIRE
  申请人：SAREPTA THERAPEUTICS INC

  公开号：WO2018118662A1

  公开（公告）日：2018-06-28

  Antisense oligomer conjugates complementary to a selected target site in the human dystrophin gene to induce exon 53 skipping are described.

  与人类肌营养不良基因中选择的靶位点互补的反义寡核苷酸共轭物用于诱导外显子53跳跃。
• [EN] PROCESSES FOR PREPARING OLIGOMERS<br/>[FR] PROCÉDÉS DE PRÉPARATION D'OLIGOMÈRES
  申请人：SAREPTA THERAPEUTICS INC

  公开号：WO2017205496A1

  公开（公告）日：2017-11-30

  Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to scaling up oligomersynthesis while maintaining overall yield and purity of a synthesized oligomer.

  本文提供了制备寡聚物（例如吗啉基寡聚物）的过程。本文描述的合成过程可能有利于扩大寡聚物合成规模，同时保持合成寡聚物的总产量和纯度。
• 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。