CAS: 95847-70-4; 2-(4-(4-(Pyrimidin-2-yl)Piperazin-1-yl)Butyl)Benzo[d]Isothiazol-3(2H)-One 1,1-Dioxide

结构式图片

上下游产品

N-[4-溴丁基]糖精 N-[4-Bromobutyl]Saccharin 103564-59-6
糖精 Saccharin 81-07-2

合成工艺路线路线简述

  • 103564-59-6 + 20980-22-7 = 95847-70-4
    反应条件:1.1 Reagents: Potassium Carbonate Catalysts: Tetrabutylammonium Bromide Solvents: Dimethylformamide,Acetonitrile; 3.5 Min,Rt1.2 Reagents: Hydrochloric Acid Solvents: Water
    标题:Radioligand And Computational Insight In Structure - Activity Relationship Of Saccharin Derivatives Being Ipsapirone And Revospirone Analogues
    作者:Kulaga,Damian; Jaskowska,Jolanta; Satala,Grzegorz
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2021 卷标:42]

    2173294-46-5 = 95847-70-4
    反应条件:1.1 Reagents: 2,6-Dimethyl-1,4-Benzoquinone Catalysts: Palladium Diacetate,4,5-Dihydro-2-[5-Methoxy-2-[(4-Methylphenyl)Sulfinyl]Phenyl]-4,4-Dimethyloxazole Solvents: Dibutyl Phosphate,1,4-Dioxane; 48 - 72 H,45 °C
    标题:Allylic C-H Amination Cross-Coupling Furnishes Tertiary Amines By Electrophilic Metal Catalysis
    作者:Ali,Siraj Z.; Budaitis,Brenna G.; Fontaine,Devon F. A.; Pace,Andria L.; Garwin,Jacob A.; Et Al
    参考文献:Science (Washington 日期:2022 卷标:376(6590) 页码:276-283]

    1841084-49-8 + 20980-22-7 = 95847-70-4
    反应条件:1.1 Reagents: Potassium Bicarbonate Solvents: Toluene; 22 H,95 - 100 °C
    标题:Preparation Of Alkylated Arylpiperazine And Alkylated Arylpiperidine Compounds
    参考文献:United States]

    = 95847-70-4 [标题:Reaction Conditions
    标题:Synthesis Of Metabolically Stable Arylpiperazine 5-Ht1A Receptor Agonists
    作者:Romero,Arthur G.; Darlington,William H.; Piercey,Montford F.; Lahti,Robert A.
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:1992 卷标:2(12) 页码:1703-6]

    2642160-33-4 + 31575-35-6 = 95847-70-4
    反应条件:1.1 Catalysts: Hydroxypropyl Methyl Cellulose Solvents: Water; 1 - 2 Min,Rt1.2 Reagents: Potassium Carbonate; 30 Min,Rt
    标题:Nucleophilic Aromatic Substitution Reactions Under Aqueous,Mild Conditions Using Polymeric Additive Hpmc
    作者:Borlinghaus,Niginia; Ansari,Tharique N.; Braje,Leon H.; Ogulu,Deborah; Handa,Sachin; Et Al
    参考文献:Green Chemistry 日期:2021 卷标:23(11) 页码:3955-3962]

    103564-59-6 + 78069-54-2 = 95847-70-4
    反应条件:1.1 Reagents: Potassium Carbonate Catalysts: Tetrabutylammonium Bromide; 30 Min1.2 Solvents: Water; 24 H,4 °C
    标题:Mechanochemical Synthesis Method For Drugs Used In The Treatment Of Cns Diseases Under Ptc Conditions
    作者:Jaskowska,Jolanta; Drabczyk,Anna Karolina; Michorczyk,Piotr; Kulaga,Damian; Zareba,Przemyslaw; Et Al
    参考文献:Catalysts 日期:2022 卷标:12(5)]

    94021-22-4 + 81-07-2 + 110-52-1 = 95847-70-4
    反应条件:1.1 Reagents: Potassium Carbonate Catalysts: Tetrabutylammonium Bromide Solvents: Dimethylformamide; 50 S1.2 120 S
    标题:Microwave-Assisted Solvent-Free Synthesis Of Ipsapirone
    作者:Kulaga,Damian; Jaskowska,Jolanta; Jasinski,Radomir
    参考文献:Journal Of Heterocyclic Chemistry 日期:2019 卷标:56(5) 页码:1498-1504]

    103564-59-6 + 20980-22-7 = 95847-70-4 [标题:Reaction Conditions
    标题:Use Of 2-Pyrimidinyl-1-Piperazine Derivatives For Prevention Of Aggressive Behavior Amongst Pigs
    参考文献:European Patent Organization]

    103564-59-6 + 20980-22-7 = 95847-70-4 [标题:Reaction Conditions
    标题:2-Pyrimidinyl-1-Piperazine Derivatives For Treating Alcoholism
    参考文献:European Patent Organization]

    = 95847-70-4 [标题:Reaction Conditions
    标题:Structure-Activity Relationship Studies Of Cns Agents. Part 14: Structural Requirements For The 5-Ht1A And 5-Ht2A Receptor Selectivity Of Simple 1-(2-Pyrimidinyl)Piperazine Derivatives
    作者:Mokrosz,J. L.; Strekowksi,L.; Duszynska,Beata; Harden,D. B.; Mokrosz,Maria J.; Et Al
    参考文献:Pharmazie 日期:1994 卷标:49(11) 页码:801-6]

    = 95847-70-4 [标题:Reaction Conditions
    标题:5-Hydroxytryptamine 1A Receptor Agonists For Improving Primary Memory And/or Learning
    参考文献:European Patent Organization]

    = 95847-70-4 [标题:Reaction Conditions
    标题:Suppression Of Nicotine Dependence With 2-Pyrimidinylpiperazine Derivatives
    参考文献:Federal Republic Of Germany]

    = 95847-70-4 [标题:Reaction Conditions
    标题:2-Pyrimidinyl-1-Piperazine Derivatives And Pharmaceuticals Containing Them
    参考文献:Federal Republic Of Germany
📜Potassium 4-(1,1-Dioxido-3-Oxobenzo[d]Isothiazol-2(3H)-yl)Butyl Sulfate置于硫酸,水,Potassium Hydrogencarbonate,三乙胺体系中,用 乙酸乙酯,甲苯,乙腈 作为反应溶剂,化学反应 42.0H,反应生成 伊沙匹隆
参考文献:Processes For Making Alkylated Arylpiperazine And Alkylated Arylpiperidine Compounds Including Novel Intermediates
标题:Processes For Making Alkylated Arylpiperazine And Alkylated Arylpiperidine Compounds Including Novel Intermediates
摘要:用于制备通式(I)和(Vii)中所示的烷基化芳基哌嗪和烷基化芳基哌啶化合物的新工艺和中间体,其中,R1和r2分别选择自氢,烷基,取代基或烷基;n=0,1或2;y=nr3R4,Or5或sr5,其中r3和r4分别选择自酰基或磺酰基,R5是芳基或杂芳基,或杂环烷基;ar是芳基,杂芳基或杂环烷基.

海关参考信息

专利信息


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-7309799-B2
优先权日:2004-06-01
标 题:Methods for the synthesis of milnacipran and congeners thereof
发明人:BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V
权利人:COLLEGIUM PHARMACEUTICAL INC
摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

专利号:US-2012282255-A1
优先权日:2011-04-07
标题 :Methods and compositions for the treatment of alcoholism and alcohol dependence
发明人:PLUCINSKI GREG
权利人:PLUCINSKI GREG
摘要:The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated. Accordingly, the methods and compositions of the invention are useful for preventing, treating, diagnosing, or monitoring the progression various alcohol and drug dependency diseases disclosed herein.

专利号:US-7585627-B2
优先权日:2004-05-21
标 题 :Polymorphism in tryptophan hydroxylase-2 controls brain serotonin synthesis
发明人:CARON MARC G; ZHANG XIAODONG; BEAULIEU MARTIN; GAINETDINOV RAUL R; SOTNIKOVA TATIANA D; KRISHNAN RANGA R; SCHWARTZ DAVID A; BURCH LAURANELL; WILLIAMS REDFORD B
权利人:UNIV DUKE
摘要:A method of screening a subject for a serotonergic neurotransmission dysregulation disorder comprises detecting the presence or absence of an Tph2 mutation in the subject; and then determining that the subject is at increased risk of a serotonergic neurotransmission dysregulation disorder due to the presence or absence of the Tph2 mutation.

专利号:RU-2726764-C1
优先权日:2019-12-18
标 题:Recombinant plasmid dna aav synh1-2_shrna freud-1, providing synthesis of shphk, suppressing expression of gene coding selective silenser 5-ht1a of receptor freud-1, in brains of mammals

专利号:US-10906888-B2
优先权日:2016-07-14
标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
权利人:PFIZER
摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

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✅ COA系统入驻 | 共享模式

主要参考文献


1: Johansen FF, Hasseldam H, Nybro Smith M, Rasmussen RS. Drug-induced hypothermia by 5HT1A agonists provide neuroprotection in experimental stroke: new perspectives for acute patient treatment. J Stroke Cerebrovasc Dis. 2014 Nov-Dec;23(10):2879-87. doi: 10.1016/j.jstrokecerebrovasdis.2014.07.019. Epub 2014 Oct 11. Review. doi: 10.1017/S0033291713002857. Epub 2013 Nov 21. Review. Epub 2007 Aug 22. Review. Review. Epub 2005 Nov 28. Review. Review. Review. Review. Review. Review. German. Review. Review. Review. German. Review. Review. Review. Review. Review. German. Review. Review. French.

合成参考文献


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参考文献:10.1021/jm950861w
摘要:Comoy C, Marot C, Podona T, Baudin M, Morin-Allory L, Guillaumet G, Pfeiffer B, Caignard D, Renard P, Rettori M, Adam G, Guardiola-Lemaître B. 3-Amino-3,4-dihydro-2H-1-benzopyran Derivatives as 5-HT1A Receptor Ligands and Potential Anxiolytic Agents. 2. Synthesis and Quantitative Structure−Activity Relationship Studies of Spiro[pyrrolidine- and piperidine-2,3‘(2‘H)-benzopyrans]. J. Med. Chem. 1996 Jan 01;39(21):4285–98. doi: 10.1021/jm950861w.
参考文献:10.1007/bf02247385
摘要:de Leeuw AS, Den Boer JA, Slaap BR, Westenberg HG. Pentagastrin has panic-inducing properties in obsessive compulsive disorder. Psychopharmacology (Berl). 1996 Aug;126(4):339–44. doi: 10.1007/bf02247385.
参考文献:10.1007/s002130050984
摘要:Griebel G, Rodgers RJ, Perrault G, Sanger DJ. Behavioural profiles in the mouse defence test battery suggest anxiolytic potential of 5-HT(1A) receptor antagonists. Psychopharmacology (Berl). 1999 May;144(2):121–30. doi: 10.1007/s002130050984.
参考文献:10.1016/j.devbrainres.2004.02.009|10.1016/s0165-3806(04)00075-6
摘要:Druse MJ, Tajuddin NF, Gillespie RA, Dickson E, Atieh M, Pietrzak CA, Le PT. The serotonin-1A agonist ipsapirone prevents ethanol-associated death of total rhombencephalic neurons and prevents the reduction of fetal serotonin neurons. Brain Res Dev Brain Res. 2004 Jun 21;150(2):79–88. doi: 10.1016/j.devbrainres.2004.02.009.
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