CAS: 98206-10-1; Flesinoxan

该化合物是一种化学化合物,被归类为选择性血清素受体激动剂,具体针对5-HT1A受体,主要研究其治疗焦虑和抑郁的潜在应用,因为它能够调节大脑中的血清素水平.Flesinoxan的特征是分子量相对较低,并且具有具体的结构特征,能够与血清素受体进行互动.该化合物通常在研究环境中进行,其药理学特征表明它可能会影响情绪和焦虑相关的行为.此外,对Flesinoxan进行了调查,以了解其对...

结构式图片

MSDS等安全信息

    上下游产品

    (+/-)-Flesinoxan 132741-86-7

    合成工艺路线路线简述

      📜(5-Nitro-2,3-Dihydro-1,4-Benzodioxin-2-yl)Methyl Acetate置于palladium On Activated Charcoal 氢气,Potassium Carbonate,三乙胺体系中,用 甲醇,乙醇,二氯甲烷,水,氯苯,丙酮 作为反应溶剂,化学反应生成 氟辛克生
      参考文献:The Synthesis Of (+)-And(−)-Flesinoxan: Application Of Enzymatic Resolution Methodology
      标题:The Synthesis Of (+)-And(−)-Flesinoxan: Application Of Enzymatic Resolution Methodology
      摘要:The Synthesis Of (+/-)-Flesinoxan Was Carried Out In Seven Steps Starting From Catechol. An Enzymatic Resolution Was Utilized To Prepare Each Enantiomer. Based Upon The Known Preferences Of The Enzyme System Used,We Have Assigned The (R)-Configuration To The (+)-Flesinoxan Isomer.
      DOI:10.1016/s0040-4039(00)60954-1

      海关参考信息

      专利信息


      专利号:US-2003083352-A1
      优先权日:2000-07-31
      标 题 :Synthesis of imidazole intermediates
      发明人:HELAL CHRISTOPHER J
      权利人:PFIZER
      摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.

      专利号:US-7576211-B2
      优先权日:2004-09-30
      标题 :Synthesis of thienopyridinone compounds and related intermediates
      发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
      权利人:EPIX DELAWARE INC
      摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

      专利号:US-8697888-B2
      优先权日:2012-01-06
      标题 :Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors
      发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; CHEUNG YIU-YIN
      权利人:UNIV VANDERBILT
      摘要:In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

      专利号:US-9056875-B2
      优先权日:2012-08-31
      标 题 :Substituted pyrazolo[3′,4′:4,5]thieno[2,3-C]pyridazin-3-amine analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
      发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; SALOVICH JAMES M
      权利人:UNIV VANDERBILT
      摘要:In one aspect, the invention relates to substituted pyrazolo[3′,4′:4,5]thieno[2,3-c]pyridazine-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

      专利号:US-9073935-B2
      优先权日:2011-11-11
      标 题:Substituted benzylspiroindolin-2-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M1
      发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; HOPKINS COREY R; MELANCON BRUCE J; POSLUSNEY MICHAEL S
      权利人:UNIV VANDERBILT
      摘要:In one aspect, the invention relates to substituted benzylspiroindolin-2-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

      专利号:US-7799829-B2
      优先权日:2006-07-28
      标 题 :Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use
      发明人:DAI XUEDONG; GANGAKHEDKAR ARCHANA; XIANG JIA-NING; GALLOP MARK A
      权利人:XENOPORT INC
      摘要:Acyloxyalkyl carbamate prodrugs of α-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of α-amino acids and methods of using acyloxyalkyl carbamate prodrugs of α-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of α-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.

      供应商参考报价(招募中)

      品牌试剂参考报价(招募中)

      📌 第三方产品分析报告

      ✅ COA系统入驻 | 共享模式

      主要参考文献


      1: Monti JM, Jantos H. Effects of the 5-HT1A receptor ligands flesinoxan and WAY 100635 given systemically or microinjected into the laterodorsal tegmental nucleus on REM sleep in the rat. Behav Brain Res. 2004 May 5;151(1-2):159-66. Epub 2007 May 22. Epub 2002 Oct 3.

      合成参考文献


      参考文献:10.1124/jpet.103.059030
      摘要:Zuideveld KP, Van der Graaf PH, Newgreen D, Thurlow R, Petty N, Jordan P, Peletier LA, Danhof M. Mechanism-Based Pharmacokinetic-Pharmacodynamic Modeling of 5-HT1A Receptor Agonists: Estimation of in Vivo Affinity and Intrinsic Efficacy on Body Temperature in Rats. The Journal of Pharmacology and Experimental Therapeutics. 2004 Mar;308(3):1012–20. doi: 10.1124/jpet.103.059030.
      参考文献:10.1021/jm960496o
      摘要:Kuipers W, Kruse CG, van Wijngaarden I, Standaar PJ, Tulp MTM, Veldman N, Spek AL, IJzerman AP. 5-HT1A- versus D2-Receptor Selectivity of Flesinoxan and AnalogousN 4-SubstitutedN 1-Arylpiperazines. J. Med. Chem. 1997 Jan 01;40(3):300–12. doi: 10.1021/jm960496o.
      参考文献:10.1038/sj.bjp.0706859
      摘要:Assié M, Lomenech H, Ravailhe V, Faucillon V, Newman‐Tancredi A. Rapid desensitization of somatodendritic 5‐HT1Areceptors by chronic administration of the high‐efficacy 5‐HT1Aagonist, F13714: a microdialysis study in the rat. British J Pharmacology. 2006 Sep;149(2):170–8. doi: 10.1038/sj.bjp.0706859.
      📝 需求与反馈
      尽可能描述清楚需求与问题信息
      ×

      通知