4-hydroxy-3-nitro diphenylsulphone | 2493-66-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 酚类
• 英文名称: 4-hydroxy-3-nitro diphenylsulphone
• 英文别名: 4-Hydroxy-3-nitrophenyl phenyl sulfone；4-phenylsulfonyl-2-nitrophenol；4-(benzenesulfonyl)-2-nitrophenol；2-Nitro-4-hydroxyphenyl-phenyl-sulfon；Phenyl-(3-nitro-4-hydroxy-phenyl)-sulfon；3-Nitro-4-hydroxy-diphenyl-sulfon；4-Benzolsulfonyl-2-nitro-phenol；2-nitro-4-phenylsulfonylphenol；2-Nitro-4-phenylsulfon-phenol；3-Nitro-4-hydroxy-1-phenylsulfon-benzol
• CAS: 2493-66-5
• 化学式: C₁₂H₉NO₅S
• 分子量: 279.273
• InChiKey: KATRASQPUDIQOV-UHFFFAOYSA-N

物化性质

• 熔点：
  137 °C
• 沸点：
  465.5±35.0 °C(Predicted)
• 密度：
  1.484±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  109
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-hydroxy-3-nitro diphenylsulphone 在 aluminum nickel 作用下， 以 乙醇 、 氢气 为溶剂， 生成 2-amino-4-phenylsulfonylphenol
  参考文献：
  名称：

  3,4-dihydro-2H-1,4-benzoxazine derivatives and pharmaceutical

  摘要：

  提供了一种新颖的苯并恶唑衍生物，其化学公式为(I): ##STR1##，以及它们的药用可接受盐和一种方法，用于将它们用作激活钾通道的剂2-(3,4-二氢-2,2-二甲基-6-苯磺酰基-2H-1,4-苯并恶唑-4-基)吡啶N-氧化物是公式(I)的苯并恶唑衍生物的示例。还提供了诸如公式(II)的中间化合物:##STR2##

  公开号：

  US05420126A1
• 作为产物：
  描述：

  4-(苯基磺酰基)苯胺 在 吡啶 、 sodium hydroxide 、 硫酸 、 水 、 硝酸 、 溶剂黄146 作用下， 生成 4-hydroxy-3-nitro diphenylsulphone
  参考文献：
  名称：

  48.亚磺酸盐对2：4-二硝基二苯基砜的作用

  摘要：

  DOI：

  10.1039/jr9360000218

文献信息

• A Convenient Synthesis of 2-Nitrophenols from 1,2-Dichlorobenzenes
  作者：Joseph Zilberman、David Ioffe、Igal Gozlan

  DOI：10.1055/s-1992-26192

  日期：——

  Aromatic nucleophilic substitution of 1,2-dichlorobenzenes 1 possessing a strong electron-withdrawing group in the 4-position with a nitrite ion give the corresponding 2-nitrophenols 5.

  具有强吸电子基团的4-位1,2-二氯苯1与亚硝酸根离子进行亲核芳香取代反应，得到相应的2-硝基酚5。
• [EN] FLUOROPIPERIDINE COMPOUNDS AS PURE 5-HT6 RECEPTOR ANTAGONISTS<br/>[FR] COMPOSÉS DE FLUOROPIPÉRIDINE UTILISÉS EN TANT QU'ANTAGONISTES PURS DU RÉCEPTEUR 5-HT 6
  申请人：SUVEN LIFE SCIENCES LTD

  公开号：WO2019030641A1

  公开（公告）日：2019-02-14

  The present invention relates to fluoropiperidine compounds of formula (I), their stereoisomers, isotopic forms or pharmaceutically acceptable salts thereof as 5-HT6 receptor antagonists. In particular the present invention discloses the methods of preparation, pharmaceutical composition, combinations and use of fluoropiperidine compounds, their stereoisomers, isotopic forms or pharmaceutically acceptable salts thereof. In formula (I), R1 represents phenyl or pyridyl; wherein the phenyl or pyridyl is optionally substituted with one or more groups selected from halogen, (C1-6)-alkyl or halo(C1-6 )-alkyl; R2 represents hydrogen or (C1-6)-alkyl; R3 represents hydrogen or (C1-6)-alkyl; or R2 and R3 can combine together to form (C3-6)- cycloalkyl; R4 represents hydrogen, (C1-6)-alkyl or halo(C1-6)-alkyl; R5 represents hydrogen, (C1-6)-alkyl, halo(C1-6)-alkyl or -(CH2)0-3- (C3-6)-cycloalkyl. The compounds can be used in the treatment of cognitive disorder mediated by the 5-Hydroxytryptamine 6 receptor, wherein said cognitive disorder is selected from the group consisting of dementia in Alzheimer's disease, dementia in Parkinson's disease, dementia in Huntington's disease, dementia associated with Down syndrome, dementia associated with Tourette's syndrome, dementia associated with post menopause, frontotemporal dementia, Lewy body dementia, Vascular dementia, dementia in HIV, dementia in Creutzfeldt-Jakob disease, substance-induced persisting dementia, dementia in Pick's disease, dementia in schizophrenia, dementia in general medical conditions and senile dementia.

  本发明涉及式(I)的氟哌啶化合物，其立体异构体、同位素形式或药学上可接受的盐作为5-HT6受体拮抗剂。特别是，本发明公开了氟哌啶化合物、其立体异构体、同位素形式或药学上可接受的盐的制备方法、药物组合物、组合及其用途。在式(I)中，R1代表苯基或吡啶基；其中苯基或吡啶基任选地被一个或多个选自卤素、(C1-6)-烷基或卤代(C1-6)-烷基的基团取代；R2代表氢或(C1-6)-烷基；R3代表氢或(C1-6)-烷基；或者R2和R3可以结合在一起形成(C3-6)-环烷基；R4代表氢、(C1-6)-烷基或卤代(C1-6)-烷基；R5代表氢、(C1-6)-烷基、卤代(C1-6)-烷基或-(CH2)0-3-(C3-6)-环烷基。这些化合物可用于治疗由5-羟色胺6受体介导的认知障碍，其中所述认知障碍选自阿尔茨海默病中的痴呆、帕金森病中的痴呆、亨廷顿病中的痴呆、唐氏综合症相关的痴呆、图雷特综合症相关的痴呆、绝经后痴呆、额颞叶痴呆、路易体痴呆、血管性痴呆、HIV中的痴呆、克雅氏病中的痴呆、物质诱发的持续性痴呆、皮克病中的痴呆、精神分裂症中的痴呆、一般医疗条件下的痴呆和老年性痴呆。
• Benzoxazine and quinoxaline derivatives and uses thereof
  申请人：Sethofer Steven

  公开号：US20060106012A1

  公开（公告）日：2006-05-18

  Compounds of the formula I: or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein k, m, n, p, q, X, Y, Z, Ar, R 1 , R 2 , R 3 and R 4 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

  公式I的化合物：或其药学上可接受的盐、溶剂化合物或前药，其中k、m、n、p、q、X、Y、Z、Ar、R1、R2、R3和R4的定义如本文所述。同时提供了制备公式I化合物的方法，包括含有该化合物的组合物的方法和使用该化合物的方法。
• Benzoxazine derivatives, their preparation and pharmaceutical compositions containing them
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP0432893A2

  公开（公告）日：1991-06-19

  A novel benzoxazine derivative of the formula (I): and a pharmaceutically acceptable salt thereof which are useful as potassium channel activating agents are disclosed.

  本研究公开了一种新型的式 (I) 苯并恶嗪衍生物： 及其药学上可接受的盐，可用作钾通道激活剂。
• Vicarious Nucleophilic Hydroxylation of aromatic nitro compounds with organic hydroperoxides
  作者：Thomas Brose、Felix Holzscheiter、Gunter Mattersteig、Wilhelm Pritzkow、Volkmar Voerckel

  DOI：10.1002/prac.19923340609

  日期：——

  Nitrobenzene, alpha-nitronaphthalene, m-dinitrobenzene, 1,3,5-trinitrobenzene, m-nitrobenzophenone, m-nitrobenzonitrile, methyl m-nitrobenzoate and m-nitro diphenylsulphone can be hydroxylated with cumene or tert-butyl hydroperoxide in dipolar aprotic solvents in the presence of strong bases. The hydroxyl group is introduced preferably in p-position to the nitro group. Attempts to hydroxylate benzophenone, anthraquinone, 2-ethyl anthraquinone, anthraquinone 2-sulphonate, benzonitrile and diphenyl sulphone under the same conditions failed. 1-Nitroanthraquinone delivered 1-hydroxy, 1,2-dihydroxy and 1,4-dihydroxy anthraquinone.