吡啶-4-基(1-三苯甲游基-1H-咪唑-4-基)甲醇 | 224168-75-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 中文名称: 吡啶-4-基(1-三苯甲游基-1H-咪唑-4-基)甲醇
• 英文名称: pyridin-4-yl-(1-trityl-1H-imidazol-4-yl)methanol
• 英文别名: Pyridin-4-YL(1-trityl-1H-imidazol-4-YL)methanol；pyridin-4-yl-(1-tritylimidazol-4-yl)methanol
• CAS: 224168-75-6
• 化学式: C₂₈H₂₃N₃O
• 分子量: 417.51
• InChiKey: WKIHEQYNXPKUBJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  50.9
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  吡啶-4-基(1-三苯甲游基-1H-咪唑-4-基)甲醇 在 platinum(IV) oxide 4-二甲氨基吡啶 、 lithium aluminium tetrahydride 、 三丁基膦 、 氢气 、 溶剂黄146 、 1,1'-azodicarbonyl-dipiperidine 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 为溶剂， 生成 4-{3-[4-(1-Trityl-1H-imidazol-4-ylmethyl)-piperidin-1-yl]-propoxy}-benzaldehyde
  参考文献：
  名称：

  基于4-[（（1H-咪唑-4-基）甲基]哌啶骨架的新型组胺H3受体拮抗剂。

  摘要：

  我们报告基于4-[（（1H-咪唑-4-基）甲基]哌啶的新型组胺H（3）受体拮抗剂的发现。该系列中最有效的化合物（例如7种）是由取代的苯胺酰胺通过二亚甲基连接基连接到主要药效基团哌啶上的结果。

  DOI：

  10.1016/j.bmcl.2005.09.076
• 作为产物：
  描述：

  4-吡啶甲醛 、 1-三苯甲基-4-碘咪唑 在 乙基溴化镁 作用下， 以 乙醚 、 二氯甲烷 为溶剂， 反应 1.5h， 生成 吡啶-4-基(1-三苯甲游基-1H-咪唑-4-基)甲醇
  参考文献：
  名称：

  [EN] NOVEL PHARMACEUTICALLY ACCEPTABLE SALTS OF 4-(1H-IMIDAZOL-4-YLMETHYL)PYRIDINE AND THEIR THERAPEUTICAL USES
  [FR] NOUVEAUX SELS PHARMACEUTIQUEMENT ACCEPTABLES DE 4-(1H-IMIDAZOL-4-YLMÉTHYL)PYRIDINE ET LEURS UTILISATIONS THÉRAPEUTIQUES

  摘要：

  本发明涉及新型的immethridine药物组成物，特别是其新型的药用可接受盐，例如immethridine的dioxalate盐，以及其治疗用途和新型制备方法。

  公开号：

  WO2010133598A1

文献信息

• [EN] NOVEL PHARMACEUTICALLY ACCEPTABLE SALTS OF 4-(1H-IMIDAZOL-4-YLMETHYL)PYRIDINE AND THEIR THERAPEUTICAL USES<br/>[FR] NOUVEAUX SELS PHARMACEUTIQUEMENT ACCEPTABLES DE 4-(1H-IMIDAZOL-4-YLMÉTHYL)PYRIDINE ET LEURS UTILISATIONS THÉRAPEUTIQUES
  申请人：BIOPROJET SOC CIV

  公开号：WO2010133598A1

  公开（公告）日：2010-11-25

  The present invention concerns novel pharmaceutical compositions of immethridine, in particular of novel pharmaceutically acceptable salts thereof, such as the dioxalate salt of immethridine, as well as its therapeutical uses and novel process of preparation.

  本发明涉及新型的immethridine药物组成物，特别是其新型的药用可接受盐，例如immethridine的dioxalate盐，以及其治疗用途和新型制备方法。
• NOVEL PHARMACEUTICALLY ACCEPTABLE SALTS OF 4-(1H-IMIDAZOL-4-YLMETHYL)PYRIDINE AND THEIR THERAPEUTICAL USES
  申请人：Capet Marc

  公开号：US20120129892A1

  公开（公告）日：2012-05-24

  The present invention concerns novel pharmaceutical compositions of immethridine, in particular of novel pharmaceutically acceptable salts thereof, such as the dioxalate salt of immethridine, as well as its therapeutical uses and novel process of preparation.

  本发明涉及新型的imethridine制药组合物，特别是其新型药用可接受的盐，如imethridine的二草酸盐，以及其治疗用途和新型制备方法。
• Novel pharmaceutically acceptable salts of 4-(1H-imidazol-4-ylmethyl)pyridine and their therapeutical uses
  申请人：BIOPROJET

  公开号：EP2263672A1

  公开（公告）日：2010-12-22

  The present invention concerns novel pharmaceutical compositions of immethridine, in particular of novel pharmaceutically acceptable salts thereof, such as the dioxalate salt of immethridine, as well as its therapeutical uses and novel process of preparation.

  本发明涉及氨甲蝶呤的新型药物组合物，特别是其新型药学上可接受的盐类，例如氨甲蝶呤的二噁盐，以及其治疗用途和新型制备工艺。
• Synthesis and Structure−Activity Relationships of Conformationally Constrained Histamine H₃ Receptor Agonists
  作者：Ruengwit Kitbunnadaj、Obbe P. Zuiderveld、Iwan J. P. De Esch、Roeland C. Vollinga、Remko Bakker、Martin Lutz、Anthony L. Spek、Emile Cavoy、Marie-France Deltent、Wiro M. P. B. Menge、Henk Timmerman、Rob Leurs

  DOI：10.1021/jm030905y

  日期：2003.12.1

  Immepip, a conformationally constrained analogue of the histamine congener imbutamine, shows high affinity and functional activity on the human H-3 receptor. Using histamine and its homologues as prototypes, other rigid analogues containing either a piperidine or pyrrolidine ring in the side chain were synthesized and tested for their activities at the human H-3 receptor and the closely related H-4 receptor. In the series of piperidine containing analogues, immepip was found to be the most potent H-3 receptor agonist, whereas its propylene analogue 13a was identified as a high-affinity neutral antagonist for the human H-3 receptor. Moreover, replacement of the piperidine ring of immepip by a pyrrolidine ring led to a pair of enantiomers that show a distinct stereoselectivity at the human H-3 and H-4 receptor.
• Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold
  作者：Wayne D. Vaccaro、Rosy Sher、Michael Berlin、Neng-Yang Shih、Robert Aslanian、John H. Schwerdt、Kevin D. McCormick、John J. Piwinski、Robert E. West、John C. Anthes、Shirley M. Williams、Ren-Long Wu、H. Susan She、Maria A. Rivelli、Jennifer C. Mutter、Michel R. Corboz、John A. Hey、Leonard Favreau

  DOI：10.1016/j.bmcl.2005.09.076

  日期：2006.1

  We report the discovery of novel histamine H(3) receptor antagonists based on 4-[(1H-imidazol-4-yl)methyl]piperidine. The most potent compounds in the series (e.g., 7) result from the attachment of a substituted aniline amide to the main pharmacophore piperidine via a two-methylene linker.

  我们报告基于4-[（（1H-咪唑-4-基）甲基]哌啶的新型组胺H（3）受体拮抗剂的发现。该系列中最有效的化合物（例如7种）是由取代的苯胺酰胺通过二亚甲基连接基连接到主要药效基团哌啶上的结果。