1-bromo-4-[(2-methoxyethyl)thio]benzene | 73655-43-3

• 分子结构分类: 有机化合物 - 有机硫化合物 - 硫醚类
• 英文名称: 1-bromo-4-[(2-methoxyethyl)thio]benzene
• 英文别名: (4-bromophenyl)(2-methoxyethyl)sulfane；1-bromo-4-(2-methoxyethylsulfanyl)benzene
• CAS: 73655-43-3
• 化学式: C₉H₁₁BrOS
• 分子量: 247.156
• InChiKey: XEPIBIXPXFUJQF-UHFFFAOYSA-N

物化性质

• 沸点：
  292.7±25.0 °C(Predicted)
• 密度：
  1.43±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  34.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-bromo-4-[(2-methoxyethyl)thio]benzene 在 间氯过氧苯甲酸 作用下， 以 二氯甲烷 为溶剂， 生成 1-(2-methoxyethylsulfonyl)-4-bromobenzene
  参考文献：
  名称：

  [EN] AXL COMPOUNDS
  [FR] COMPOSÉS AXL

  摘要：

  Compounds of Formula I that inhibit AXL, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by AXL.

  公开号：

  WO2022246177A1
• 作为产物：
  描述：

  4-溴苯硫酚 、 2-溴乙基甲基醚 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 反应 18.0h， 以83%的产率得到1-bromo-4-[(2-methoxyethyl)thio]benzene
  参考文献：
  名称：

  Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: Discovery of (R)-1-(2-(4′-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916)

  摘要：

  The design of a new clinical candidate histamine-H-3 receptor antagonist for the potential treatment of excessive daytime sleepiness (EDS) is described. Phenethyl-R-2-methylpyrrolidine containing biphenylsulfonamide compounds were modified by replacement of the sulfonamide linkage with a sulfone. One compound from this series, 2j (APD916) increased wakefulness in rodents as measured by polysomnography with a duration of effect consistent with its pharmacokinetic properties. The identification of a suitable salt form of 2j allowed it to be selected for further development. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.11.075

文献信息

• [EN] N-LINKED HYDROXAMIC ACID DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS<br/>[FR] DÉRIVÉS D'ACIDE HYDROXAMIQUE À LIAISON N, UTILES COMME AGENTS ANTIBACTÉRIENS
  申请人：PFIZER

  公开号：WO2011073845A1

  公开（公告）日：2011-06-23

  The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections. Formula (I).

  本发明涉及一类新的羟肟酸衍生物，它们作为LpxC抑制剂的用途，更具体地用于治疗细菌感染。公式（I）。
• N-Linked Hydroxamic Acid Derivatives Useful As Antibacterial Agents
  申请人：Brown Matthew Frank

  公开号：US20120258948A1

  公开（公告）日：2012-10-11

  The present invention is directed to a new class of hydroxamic acid derivatives of formula I, wherein the variables G, T, D, L, R 1 , R 2 , R 3 are as described herein, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections in a patient in need thereof.

  本发明涉及一种新的羟肟酸衍生物类别，其化学式为I，其中变量G，T，D，L，R1，R2，R3如本文所述，其用作LpxC抑制剂，更具体地用于治疗有需要的患者的细菌感染。
• BIPHENYL SULFONYL AND PHENYL-HETEROARYL SULFONYL MODULATORS OF THE HISTAMINE H3-RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
  申请人：Santora Vincent J.

  公开号：US20100240653A1

  公开（公告）日：2010-09-23

  The present invention relates to certain biphenyl sulfonamide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3-receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease and the like.

  本发明涉及公式（Ia）的某些联苯磺酰胺衍生物及其制药组合物，其调节组织胺H3受体的活性。本发明的化合物和制药组合物适用于治疗组织胺H3相关疾病的方法，例如认知障碍，癫痫，脑外伤，抑郁症，肥胖症，睡眠和清醒障碍，如嗜睡症，倒班综合征，药物副作用引起的嗜睡，维持警觉以帮助完成任务等，猝倒症，过度睡眠症，嗜睡综合征，时差反应，睡眠呼吸暂停等，注意力缺陷多动障碍（ADHD），精神分裂症，过敏症，上呼吸道过敏反应，过敏性鼻炎，鼻塞，痴呆，阿尔茨海默病等。
• N-Link Hydroxamic Acid Derivatives Useful As Antibacterial Agents
  申请人：Pfizer Inc.

  公开号：US20140128363A1

  公开（公告）日：2014-05-08

  The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.

  本发明涉及一种新的羟肟酸衍生物类，其用作LpxC抑制剂，更具体地用于治疗细菌感染。
• 5-PHENYLAZAINDOLE DERIVATIVE HAVING AMPK ACTIVATING EFFECT
  申请人：Shionogi & Co., Ltd

  公开号：EP3421467A1

  公开（公告）日：2019-01-02

  Provided is a compound which is useful as an AMPK activator. A compound represented by formula: wherein X is substituted or unsubstituted monocyclic heterocyclyl or the like; ring A is substituted aryl, substituted heteroaryl, substituted cycloalkyl, substituted cycloalkenyl, or substituted heterocyclyl, wherein the ring A may further have a substituent(s) other than Y; Y is halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like; R4, R5, R6 and R7 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkyloxy, substituted or unsubstituted alkylthio, substituted or unsubstituted alkylsulfonyl, substituted or unsubstituted acyl, substituted or unsubstituted carbamoyl, substituted or unsubstituted sulfamoyl, or substituted or unsubstituted amino; R8 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like; and R9 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like, or its pharmaceutically acceptable salt.

  本文提供了一种可用作 AMPK 激活剂的化合物。一种由式表示的化合物： 其中 X 是取代或未取代的单环杂环基或类似物； 环 A 是取代的芳基、取代的杂芳基、取代的环烷基、取代的环烯基或取代的杂环烯基，其中环 A 可进一步具有除 Y 以外的取代基； Y 是卤素、羟基、氰基、硝基、羧基、取代或未取代的烷基、取代或未取代的烯基、取代或未取代的炔基或类似物； R4、R5、R6 和 R7 各自独立地是氢、卤素、羟基、氰基、硝基、羧基、取代或未取代的烷基、取代或未取代的烯基、取代或未取代的炔基、取代或未取代的烷氧基、取代或未取代的烷硫基、取代或未取代的烷磺酰基、取代或未取代的酰基、取代或未取代的氨基甲酰基、取代或未取代的氨基磺酰基或取代或未取代的氨基； R8 是氢、卤素、羟基、氰基、硝基、羧基、取代或未取代的烷基、取代或未 取代的烯基、取代或未取代的炔基或类似物；以及 R9 是氢、卤素、羟基、氰基、硝基、羧基、取代或未取代的烷基、取代或未取代的烯基、取代或未取代的炔基或类似物、 或其药学上可接受的盐。