N-tritylpyrrolidine | 18265-12-8

• 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-tritylpyrrolidine
• 英文别名: 1-(triphenylmethyl)pyrrolidine；1-Tritylpyrrolidine
• CAS: 18265-12-8
• 化学式: C₂₃H₂₃N
• 分子量: 313.442
• InChiKey: DVFDHIZVAQOEMX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  24
• 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：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  三苯基氯甲烷 在 5-(3-methoxy-3-methylbut-1-yn-1-yl)-1,3-bis(1-(3,5-bis(trifluoromethyl)-phenyl)-1H-1,2,3-triazol-4-yl)benzene 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 72.0h， 生成 N-tritylpyrrolidine
  参考文献：
  名称：

  “单击”双三唑为中性C吗？H⋅⋅⋅阴离子受体有机催化剂

  摘要：

  球场上的新球员！“点击”双-三唑已被引入作为高效率的新型类中性的C  H⋅⋅⋅anion结合有机催化剂（参见方案）。DFT和NMR研究用于确认这种活化方式并确定最佳催化剂。

  DOI：

  10.1002/chem.201203360

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。
• Pyrrole-Based Anion-Responsive π-Electronic Molecules as Hydrogen-Bonding Catalysts
  作者：Goki Hirata、Hiromitsu Maeda

  DOI：10.1021/acs.orglett.8b00855

  日期：2018.5.18

  boron complexes as hydrogen-bonding donor organocatalysts were examined by the Mannich-type reaction of N-acyl heteroarenium chlorides with 1-methoxy-2-methyl-1-trimethylsiloxy-1-propene, as well as by the classical N-alkylation of amines with trityl chloride under base-free conditions. 1H NMR examinations of the hydrogen-bonding interaction between the pyrrole NH of the catalyst and the Cl– in the

  N-酰基杂芳基氯化物与1-甲氧基-2-甲基-1-三甲基甲硅烷氧基-1-丙烯的曼尼希型反应以及经典的N检验了二吡咯基二酮硼配合物作为氢键供体有机催化剂的能力。在无碱条件下用三苯甲基氯对胺进行烷基化。1个催化剂的吡咯NH和氯之间的氢键相互作用的1 H NMR检查-在Ñ酰基heteroarenium盐建议的激活Ñ酰基heteroarenium氯化物阴离子通过由催化剂发生结合。
• Design, synthesis and identification of a new class of triarylmethyl amine compounds as inhibitors of apolipoprotein E production
  作者：Mandeep Singh、Jason T. Schott、Martin A. Leon、Robert T. Granata、Harkiran K. Dhah、Jason A. Welles、Michelle A. Boyce、Hafeez S. Oseni-Olalemi、Charles E. Mordaunt、Anthony J. Vargas、Nilay V. Patel、Santanu Maitra

  DOI：10.1016/j.bmcl.2012.08.009

  日期：2012.10

  We have identified a new class of triarylmethyl amine compounds that can inhibit apolipoprotein E (apoE) production. ApoE is a cholesterol- and lipid-carrier protein implicated in aging, atherosclerosis, Alzheimer’s Disease (AD), and other neurological and lipid-related disorders. Attenuation of apoE production is generally considered to be of therapeutic value. A majority of the apoE in the brain

  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。
• Temporal control in tritylation reactions through light-driven variation in chloride ion binding catalysis – a proof of concept
  作者：Surbhi Grewal、Saonli Roy、Himanshu Kumar、Mayank Saraswat、Naimat K. Bari、Sharmistha Sinha、Sugumar Venkataramani

  DOI：10.1039/d0cy01090a

  日期：——

  photoswitchable catalysts T1–5 have been designed, synthesized and optimized for the tritylation reaction of benzylamine (BzNH2). The tritylation reaction rates/yields achieved by light induced isomerization are compared between the native and photoswitched states of the catalyst T1. This concept of controlling the tritylation reaction rates with light has also been extended to additional substrates. The

  三脚架三唑连接的偶氮（杂）芳烃基光可催化剂T1 - 5已经被设计，合成和苄胺三苯甲基化反应（BzNH优化2）。在催化剂T1的自然状态和光开关状态之间比较通过光诱导的异构化获得的三苯甲基化反应速率/产率。用光控制三苯甲基反应速率的这一概念也已经扩展到另外的底物上。三唑C-H⋯氯的关键作用-光谱，量热和计算研究相结合已证实相互作用。而且，已经证明了在催化剂的时间控制中，在室温下催化剂的天然和光开关状态之间的结合亲和力变化的影响。
• Non-peptide inhibition of T-lymphocyte activation and therapies related thereto
  申请人：The Regents of the University of California

  公开号：US07235577B1

  公开（公告）日：2007-06-26

  Compounds, preparations and methods for immunosuppressive treatment of autoimmune disorders, graft rejection and/or graft/host disease. Therapeutically effective amounts of certain substituted triarylmethane compounds, such as 1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole, are administered to mammalian patients to selectively inhibit the calcium-activated K+ channel (IKCa1) in lymphocytes, monocytes, macrophages, platelets or endothelial cells without concomitant inhibition of P450-dependent enzyme systems, resulting in reduction of antigen-, cytokine-, or mitogen-induced calcium entry through store operated calcium channels in these cells, suppression of cytokine production by these cells, and inhibition of activation of these cells. Such inhibition of the Ca++ activated K+ channel (IKCa1) prevents the pre-Ca++ stage of cell activation and thus causes immunosuppression and an anti-inflammatory response.

  化合物、制剂和方法用于免疫抑制治疗自身免疫性疾病、移植排斥和/或移植/宿主病。通过给哺乳动物患者投予一定量的某些取代的三芳基甲烷化合物，例如1-[(2-氯苯基)二苯甲基]-1H-吡唑，选择性地抑制淋巴细胞、单核细胞、巨噬细胞、血小板或内皮细胞中的钙激活的K+通道（IKCa1），不会同时抑制P450依赖的酶系统，从而减少这些细胞通过储存激活钙通道的抗原、细胞因子或促进剂诱导的钙进入，抑制这些细胞的细胞因子产生，抑制这些细胞的激活。这种对Ca++激活的K+通道（IKCa1）的抑制防止了细胞激活的前Ca++阶段，从而引起免疫抑制和抗炎反应。