(R,S)-1-(4-fluoronaphthalen-1-yl)ethanamine | 1260486-39-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: (R,S)-1-(4-fluoronaphthalen-1-yl)ethanamine
• 英文别名: 1-(4-Fluoronaphthalen-1-yl)ethanamine
• CAS: 1260486-39-2
• 化学式: C₁₂H₁₂FN
• mdl: MFCD18706828
• 分子量: 189.232
• InChiKey: MVNSJXXBMVYRCM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.166
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (R,S)-1-(4-fluoronaphthalen-1-yl)ethanamine 在 盐酸 、 aluminum (III) chloride 、 lithium aluminium tetrahydride 、 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 、 水 为溶剂， 反应 20.0h， 生成 1-(4-fluoro-1-naphthyl)-N-(1H-indol-2-ylmethyl)ethanamine hydrochloride
  参考文献：
  名称：

  Design and synthesis of calindol derivatives as potent and selective calcium sensing receptor agonists

  摘要：

  We report the first comprehensive structure-activity study of calindol (4, (R)-N-[(1H-indol-2-yl) methyl]1-(1-naphthyl) ethanamine), a positive allosteric modulator, or calcimimetic, of the calcium sensing receptor (CaSR). While replacement of the naphthyl moiety of calindol by other aromatic groups (phenyl, biphenyl) was largely detrimental to calcimimetic activity, incorporation of substituents on the 4, 5 or 7 position of the indole portion of calindol was found to provide either equipotent derivatives compared to calindol (e.g., 4-phenyl, 4-hydroxy, 5-hydroxycalindol 44, 52, 53) or, in the case of 7-nitrocalindol (51), a 6-fold more active calcimimetic displaying an EC50 of 20 nM. Unlike calindol, the more active CaSR calcimimetics were shown not to act as antagonists of the closely related GPRC6A receptor, suggesting a more selective profile for these new analogues. (c) 2015 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2015.12.019
• 作为产物：
  描述：

  4-氟-1-萘乙酮 在 titanium(IV) isopropylate 、 palladium on activated charcoal 、 氢气 作用下， 以 甲醇 为溶剂， 生成 (R,S)-1-(4-fluoronaphthalen-1-yl)ethanamine
  参考文献：
  名称：

  [EN] LABELED COMPOUNDS AND CALCIUM SENSING RECEPTOR LIGANDS FOR IMAGING AND USES THEREOF
  [FR] COMPOSÉS MARQUÉS ET LIGANDS DE RÉCEPTEUR DE DÉTECTION DE CALCIUM POUR IMAGERIE ET LEURS UTILISATIONS

  摘要：

  The present invention relates to labeled compounds suitable for positron emission tomography (PET) imaging and/or fluorescence imaging such as near-infrared fluorescence imaging (NIRF). The invention further relates to the use of these compounds for carrying out PET scans, imaging calcium sensing receptor (CSR)-positive organs, excising parathyroid tissue, protecting parathyroid tissue during thyroid surgery, and treating disorder(s) of a CSR- positive tissue in a subject.

  公开号：

  WO2023287686A1

文献信息

• [EN] HETEROCYCLIC COMPOUNDS, METHODS OF MAKING THEM AND THEIR USE IN THERAPY<br/>[FR] COMPOSES HETEROCYCLIQUES, PROCEDES DE PRODUCTION DE CEUX-CI ET UTILISATION DE CEUX-CI DANS UN TRAITEMENT
  申请人：AFFINIUM PHARM INC

  公开号：WO2004052890A1

  公开（公告）日：2004-06-24

  In part, the present invention is directed to antibacterial compounds of formula (I) wherein A is a bicyclic heteroaryl ring or a tricyclic ring and R2 is an heterocyclic residue; L is a bond, or L is alkyl, alkenyl or cycloalkyl.

  在某种程度上，本发明涉及公式（I）的抗菌化合物，其中A是一个双环杂芳基环或三环环，R2是一个杂环残基；L是一个键，或者L是烷基，烯基或环烷基。
• [EN] SULFONAMIDE DERIVATIVES AND PHARMACEUTICAL APPLICATIONS THEREOF<br/>[FR] DÉRIVÉS DE SULFONAMIDE ET LEURS APPLICATIONS PHARMACEUTIQUES
  申请人：SUNSHINE LAKE PHARMA CO LTD

  公开号：WO2015158313A1

  公开（公告）日：2015-10-22

  Provided herein are sulfonamide derivatives or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and their uses for treating Alzheimer's disease. Also provided herein are pharmaceutical compositions containing such compounds, and use of such compounds or pharmaceutical compositions thereof for managing or treating 5-HT6 receptor-mediated diseases, especially in the manufacture of a medicament for managing or treating Alzheimer's disease.

  本文提供了磺胺衍生物或其立体异构体、几何异构体、互变异构体、N-氧化物、水合物、溶剂合物、代谢物、药用可接受的盐或其前药，以及它们用于治疗阿尔茨海默病的用途。本文还提供了含有这些化合物的药物组合物，并使用这些化合物或其药物组合物来管理或治疗5-HT6受体介导的疾病，特别是用于制造治疗或管理阿尔茨海默病的药物。
• Compositions comprising multiple bioactive agents, and methods of using the same
  申请人：Berman M. Judd

  公开号：US20060142265A1

  公开（公告）日：2006-06-29

  In part, the present invention is directed to compositions comprising a FabI inhibitor and at least one other bioactive agent. In another part, the present invention is directed to antibacterial compositions comprising a compound of formulas I-III and at least one other antibacterial agent.

  本发明的一部分涉及含有FabI抑制剂和至少一种其他生物活性剂的组合物。另一部分，本发明涉及含有I-III式化合物和至少一种其他抗菌剂的抗菌组合物。
• Heterocyclic compounds, methods of making them and their use in therapy
  申请人：Berman Judd

  公开号：US20060183908A1

  公开（公告）日：2006-08-17

  In part, the present invention is directed to antibacterial compounds of formula (I) wherein A is a bicyclic heteroaryl ring or a tricyclic ring and R 2 is an heterocyclic residue; L is a bond, or L is alkyl, alkenyl or cycloalkyl.

  部分地，本发明涉及公式（I）中的抗菌化合物，其中A是双环杂芳基环或三环环，并且R2是杂环残基; L是键合或L是烷基，烯基或环烷基。
• Heterocyclic Compounds, Methods of Making Them and Their Use in Therapy
  申请人：Berman Judd

  公开号：US20110124633A1

  公开（公告）日：2011-05-26

  In part, the present invention is directed to antibacterial compounds.

  部分地，本发明涉及抗菌化合物。