CAS: 82-92-8; Cyclizine

该化合物是一种属于管子子素类的抗口炎,主要用于预防和治疗与运动疾病有关的恶心,呕吐和眩晕,其特点是能够跨越血脑屏障,有助于有效减轻与外阴扰动有关的症状; 丙烯氨酸表现出抗胆碱性,导致口干,沉睡和视力模糊等副作用; 该物质通常通过口服施用,以各种配方形式提供,包括平板和可注射形式; 其行动机制包括阻塞抗头痛药H1受体,从而减少其体内的抗冲作用,因为体内有过敏反应和运动疾病; 丙烯酸一般都得到很好的缓解,但对于某些医疗条件的病人,如青罗科米或先质增生病人,则因其抗胆碱效应而给予告诫.

结构式图片

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ECHA物质ECHA物质化妆品禁用物质清单C&L通报REACH预注册

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CAS号109-01-3 N-甲基哌嗪 | CAS号90-99-3 二苯基氯甲烷 | CAS号105-59-9 N-甲基二乙醇胺 | CAS号91-00-9 二苯甲胺 | CAS号110-85-0 哌嗪 | CAS号776-74-9 二苯溴代甲烷 | CAS号74-88-4 碘甲烷 | CAS号102552-76-1 1-benzhydryl-4-... | CAS号841-77-0 二苯甲基哌嗪 | CAS号139329-22-9 ethyl 5-(4-benz...

合成工艺路线路线简述

  • 841-77-0 = 82-92-8
    反应条件:1.1 Catalysts: Triphenylphosphine,Di-μ-Chlorobis[(1,2,5,6-η)-1,5-Cyclooctadiene]Diiridium Solvents: 2,2,2-Trifluoroethanol; 20 Min,Rt1.2 Reagents: Hydrogen Solvents: 2,2,2-Trifluoroethanol; 24 H,20 Atm,Rt
    标题:Practical N-Alkylation Via Homogeneous Iridium-Catalyzed Direct Reductive Amination
    作者:Wang,Jing; Et Al
    参考文献:Science China: Chemistry 日期:2023 卷标:66(2) 页码:518-525]

    109-01-3 + 90-99-3 = 82-92-8
    反应条件:1.1 45 Min,100 °C
    标题:Continuous-Flow Multistep Synthesis Of Cinnarizine,Cyclizine,And A Buclizine Derivative From Bulk Alcohols
    作者:Borukhova,Svetlana; Et Al
    参考文献:Chemsuschem 日期:2016 卷标:9(1) 页码:67-74]

    109-01-3 + 90-99-3 = 82-92-8
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 10 Min,Rt1.2 Solvents: Dimethylformamide; Rt; 10 H,80 °C
    标题:Synthesis And Pharmacological Evaluation Of 1-Benzhydryl Piperazine Derivatives
    作者:Thakran,Atul Kumar; Et Al
    参考文献:International Journal Of Pharmaceutical Sciences And Research 日期:2012 卷标:3(1) 页码:213-217]

    91-00-9 = 82-92-8
    反应条件:1.1 Catalysts: Tributylphosphine,Ruthenium Trichloride Solvents: 1,4-Dioxane
    标题:Ruthenium Complex Catalyzed N-Heterocyclization. Syntheses Of N-Substituted Piperidines,Morpholines,And Piperazines From Amines And 1,5-Diols
    作者:Tsuji,Yasushi; Et Al
    参考文献:Journal Of Organic Chemistry 日期:1985 卷标:50(9) 页码:1365-70]

    100-52-7 = 82-92-8
    反应条件:1.1 Solvents: Tetrahydrofuran; Rt; 118 H,Reflux1.2 Reagents: Water,Ammonium Chloride2.1 Reagents: Thionyl Chloride Solvents: Dichloromethane; 210 H,Reflux2.2 Solvents: Acetonitrile; 280 H,Reflux
    标题:Synthesis And Antiinflammatory Effects Of New Piperazine And Ethanolamine Derivatives Of H1-Antihistaminic Drugs
    作者:Ahmadi,Abbas; Et Al
    参考文献:Mini-Reviews In Medicinal Chemistry 日期:2012 卷标:12(12) 页码:1282-1292]

    109-01-3 + 100-52-7 = 82-92-8
    反应条件:1.1 Reagents: Potassium Carbonate,Sodium Sulfate; 0 °C; 0 °C -> Rt; Overnight,Rt2.1 Reagents: Bis(2,3,4,5,6-Pentafluorophenyl)Zinc Solvents: Toluene; 1 H,Rt2.2 Reagents: Methanol
    标题:Atom-Efficient Transition-Metal-Free Arylation Of N,O-Acetals Using Diarylzinc Reagents Through Zn/zn Cooperativity
    作者:Borys,Andryj M.; Et Al
    参考文献:Chemical Communications (Cambridge 日期:2021 卷标:57(71) 页码:8905-8908]

    = 82-92-8
    反应条件:1.1 Reagents: Sodium Borohydride Solvents: Methanol; 0 °C -> Rt; Overnight,Rt1.2 Reagents: Sodium Hydroxide Solvents: Water; Rt2.1 Catalysts: Ruthenium(1+),[2-[[bis(1,1-Dimethylethyl)Phosphino-Kp]Methyl]Pyridine-Kn]Chloro...; Rt -> 130 °C; 72 H,130 °C
    标题:Synthesis Of 1,4-Diazacycles By Hydrogen Borrowing
    作者:Nalikezhathu,Anju; Et Al
    参考文献:Organic Letters 日期:2023 卷标:25(10) 页码:1754-1759]

    591-51-5 = 82-92-8
    反应条件:1.1 Reagents: Zinc Chloride Solvents: Diethyl Ether; -78 °C; -78 °C -> Rt; Overnight,Rt2.1 Reagents: Bis(2,3,4,5,6-Pentafluorophenyl)Zinc Solvents: Toluene; 1 H,Rt2.2 Reagents: Methanol
    标题:Atom-Efficient Transition-Metal-Free Arylation Of N,O-Acetals Using Diarylzinc Reagents Through Zn/zn Cooperativity
    作者:Borys,Andryj M.; Et Al
    参考文献:Chemical Communications (Cambridge 日期:2021 卷标:57(71) 页码:8905-8908]

    91-01-0 = 82-92-8
    反应条件:1.1 Reagents: Thionyl Chloride Solvents: Dichloromethane; 0 - 5 °C; 4 - 6 H,0 - 5 °C2.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 10 Min,Rt2.2 Solvents: Dimethylformamide; Rt; 10 H,80 °C
    标题:Synthesis And Pharmacological Evaluation Of 1-Benzhydryl Piperazine Derivatives
    作者:Thakran,Atul Kumar; Et Al
    参考文献:International Journal Of Pharmaceutical Sciences And Research 日期:2012 卷标:3(1) 页码:213-217]

    119-61-9 + 109-81-9 = 82-92-8
    反应条件:1.1 Catalysts: P-Toluenesulfonic Acid Solvents: Toluene; 48 H,Reflux1.2 Reagents: Sodium Hydroxide Solvents: Water; 10 Min,Basified2.1 Reagents: Sodium Borohydride Solvents: Methanol; 0 °C -> Rt; Overnight,Rt2.2 Reagents: Sodium Hydroxide Solvents: Water; Rt3.1 Catalysts: Ruthenium(1+),[2-[[bis(1,1-Dimethylethyl)Phosphino-Kp]Methyl]Pyridine-Kn]Chloro...; Rt -> 130 °C; 72 H,130 °C
    标题:Synthesis Of 1,4-Diazacycles By Hydrogen Borrowing
    作者:Nalikezhathu,Anju; Et Al
    参考文献:Organic Letters 日期:2023 卷标:25(10) 页码:1754-1759]

    841-77-0 = 82-92-8
    反应条件:1.1 Reagents: Trifluoroacetic Acid Catalysts: [2-[(Amino-Kn)Diphenylmethyl]Phenyl-Kc]Chloro[(1,2,3,4,5-η)-1,2,3,4,5-Pentamethy... Solvents: Methanol; 5 Min,24 °C; 2 H,110 °C
    标题:Scalable Synthesis Of Antihistamines And Sensipar Via Intensified Hydrogen Borrowing Methodology
    作者:Ng,Xiao Qian; Et Al
    参考文献:Acs Sustainable Chemistry & Engineering 日期:2023 卷标:11(33) 页码:12389-12396]

    109-01-3 + 90-99-3 = 82-92-8
    反应条件:1.1 Solvents: Acetonitrile; 280 H,Reflux1.2 Reagents: Sodium Hydroxide Solvents: Water; Neutralized
    标题:Synthesis And Anti-Inflammatory Performance Of Newly Cyclizine Derivatives On Adult Male Wistar Rats
    作者:Ahmadi,Abbas; Et Al
    参考文献:Iranian Journal Of Pharmaceutical Research 日期:2012 卷标:11(4) 页码:1027-1037]

    107-21-1 = 82-92-8
    反应条件:1.1 Catalysts: Ruthenium(1+),[2-[[bis(1,1-Dimethylethyl)Phosphino-Kp]Methyl]Pyridine-Kn]Chloro...; Rt -> 130 °C; 72 H,130 °C
    标题:Synthesis Of 1,4-Diazacycles By Hydrogen Borrowing
    作者:Nalikezhathu,Anju; Et Al
    参考文献:Organic Letters 日期:2023 卷标:25(10) 页码:1754-1759]

    109-01-3 + 101-81-5 = 82-92-8
    反应条件:1.1 Reagents: Azobisisobutyronitrile,N-Bromosuccinimide Solvents: Carbon Tetrachloride; 1 H,Reflux; Reflux -> Rt1.2 Reagents: Potassium Carbonate Solvents: Acetonitrile; 2 H,Reflux
    标题:A Pd-Catalyzed Organometallic-Free Homologation Of Arylboronic Acids Enabled By Chemoselective Transmetalation
    作者:Bastick,Kane A. C.; Et Al
    参考文献:Chemrxiv 日期:2023 卷标:1 页码:1-6]

    109-01-3 + 101-81-5 = 82-92-8
    反应条件:1.1 Reagents: Lithium Bis(Trimethylsilyl)Amide Catalysts: Nickelate(1-),[n2,N6-Bis[2,6-Bis(1-Methylethyl)Phenyl]-2,6-Pyridinedicarboxamid... Solvents: Dimethyl Sulfoxide; 3 H,100 °C
    标题:Highly Economical And Direct Amination Of Sp3 Carbon Using Low-Cost Nickel Pincer Catalyst
    作者:Brandt,Andrew; Et Al
    参考文献:Rsc Advances 日期:2021 卷标:11(3) 页码:1862-1874]

    109-01-3 + 119-61-9 = 82-92-8
    反应条件:1.1 Reagents: Carbon Dioxide,Carbon Monoxide Catalysts: Dirhodium Tetraacetate Solvents: Tetrahydrofuran; 48 H,45 Bar,130 °C
    标题:Catalytic Utilization Of Converter Gas - An Industrial Waste For The Synthesis Of Pharmaceuticals
    作者:Runikhina,Sofiya A.; Et Al
    参考文献:Chemical Science 日期:2023 卷标:14(16) 页码:4346-4350]

    1078-58-6 = 82-92-8
    反应条件:1.1 Reagents: Bis(2,3,4,5,6-Pentafluorophenyl)Zinc Solvents: Toluene; 1 H,Rt1.2 Reagents: Methanol
    标题:Atom-Efficient Transition-Metal-Free Arylation Of N,O-Acetals Using Diarylzinc Reagents Through Zn/zn Cooperativity
    作者:Borys,Andryj M.; Et Al
    参考文献:Chemical Communications (Cambridge 日期:2021 卷标:57(71) 页码:8905-8908]

    91-00-9 = 82-92-8
    反应条件:1.1 Catalysts: Iridium,Graphene (Oxide); 24 H,110 °C
    标题:Iridium/graphene Nanostructured Catalyst For The N-Alkylation Of Amines To Synthesize Nitrogen-Containing Derivatives And Heterocyclic Compounds In A Green Process
    作者:Chen,Tsun-Ren; Et Al
    参考文献:Rsc Advances 日期:2022 卷标:12(8) 页码:4760-4770]

    109-01-3 + 91-01-0 = 82-92-8
    反应条件:1.1 Reagents: Thionyl Chloride Solvents: Dichloromethane; 210 H,Reflux1.2 Solvents: Acetonitrile; 280 H,Reflux
    标题:Synthesis And Antiinflammatory Effects Of New Piperazine And Ethanolamine Derivatives Of H1-Antihistaminic Drugs
    作者:Ahmadi,Abbas; Et Al
    参考文献:Mini-Reviews In Medicinal Chemistry 日期:2012 卷标:12(12) 页码:1282-1292]

    100-52-7 = 82-92-8
    反应条件:1.1 Solvents: Tetrahydrofuran; Rt; 118 H,Reflux2.1 Reagents: Thionyl Chloride Solvents: Dichloromethane; 210 H,Reflux3.1 Solvents: Acetonitrile; 280 H,Reflux3.2 Reagents: Sodium Hydroxide Solvents: Water; Neutralized
    标题:Synthesis And Anti-Inflammatory Performance Of Newly Cyclizine Derivatives On Adult Male Wistar Rats
    作者:Ahmadi,Abbas; Et Al
    参考文献:Iranian Journal Of Pharmaceutical Research 日期:2012 卷标:11(4) 页码:1027-1037]

    91-01-0 = 82-92-8
    反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Water; 10 Min,100 °C2.1 45 Min,100 °C
    标题:Continuous-Flow Multistep Synthesis Of Cinnarizine,Cyclizine,And A Buclizine Derivative From Bulk Alcohols
    作者:Borukhova,Svetlana; Et Al
    参考文献:Chemsuschem 日期:2016 卷标:9(1) 页码:67-74]

    91-01-0 = 82-92-8
    反应条件:1.1 Reagents: Thionyl Chloride Solvents: Dichloromethane; 210 H,Reflux2.1 Solvents: Acetonitrile; 280 H,Reflux2.2 Reagents: Sodium Hydroxide Solvents: Water; Neutralized
    标题:Synthesis And Anti-Inflammatory Performance Of Newly Cyclizine Derivatives On Adult Male Wistar Rats
    作者:Ahmadi,Abbas; Et Al
    参考文献:Iranian Journal Of Pharmaceutical Research 日期:2012 卷标:11(4) 页码:1027-1037
4-(二苯基甲基)-1-哌嗪羧酸乙酯置于lithium Aluminium Tetrahydride,乙醚体系中,化学反应生成 苯甲嗪
参考文献:Be539693
标题:Be539693

海关参考信息

专利信息


专利号:WO-2025136243-A1
优先权日:2023-12-20
标题:Mechanochemical synthesis of histamine h1-receptor antagonists
发明人:AYDONAT SIMAY; OZEL MERTCAN; YIGITBASI JOANNA MARIANNA; BAYTEKIN BILGE; COLACINO EVELINA
权利人:IHSAN DOGRAMACI BILKENT UNIV; CENTRE NAT RECH SCIENT
摘要:The present invention relates to mechanochemical synthesis of histamine antagonists which are benzhydryl ethers and unsymmetrically disubstitutes piperazines and salts thereof. Said antihistamine active pharmaceutical ingredients can be diphenhydramine hydrochloride, cyclizine hydrochloride and diphenylpyraline hydrochloride. These antihistamines are used in the treatment of allergies, hives, hay fever (allergic rhinitis), conjunctivitis, reactions to insect bites and sings, nausea, motion sickness, insomnia.

专利号:US-7919505-B2
优先权日:2006-07-11
标题 :Xinafoate salt of a substituted 5-oxazol-2-yl-quinoline compound
发明人:TING PAULINE C; LEE JOE F; FENG KUNG-I; REEDER MICHAEL R; TRZASKA SCOTT T; ZHU MAN; MAO CHEN; FILIPOV DIMITAR L; ZARKADAS DIMITRIOS N
权利人:SCHERING CORP
摘要:The present invention relates to the compound of the formula n nTo methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to polymorphs and processes of synthesis of the polymorphic forms.

专利号:US-2024287041-A1
优先权日:2021-05-20
标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

专利号:US-2011003780-A1
优先权日:2007-07-10
标题:Hydrogen chloride salt of a substituted 5-oxazol-2-yl-quinoline compound and a process for the production thereof
发明人:ZHU MAN
权利人:SCHERING CORP
摘要:The present invention relates to the compound of the Formula I: n n n n n n n n n n and to methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to a particular crystalline form and processes of synthesis of the crystalline form. n IM=105109

专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

专利号:WO-0054773-A1
优先权日:1999-03-12
标题:Dopamine agonists in combination with nitric oxide donors, compositions and methods of use
发明人:GARVEY DAVID S
权利人:NITROMED INC; GARVEY DAVID S
摘要:The present invention is directed to novel compositions comprising at least one dopamine agonist in combination with at least one nitric oxide donor (i.e. compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are substrates for nitric oxide synthase). The novel compositions may optionally comprise at least one therapeutic agent, such as, a vasoactive agent, an antimetic agent, and mixtures thereof. The dopamine agonist is preferably apomorphine. The present invention is also directed to methods for treating and/or preventing sexual dysfunctions and/or enhancing sexual responses in patients. In other embodiments, the present invention is directed to methods treating or preventing neurodegenerative diseases, mitochondrial diseases, spinal cord injury, central or psychostimulant addiction, senile dementia, circulatory disorders, cardiovascular disorders, hyperprolactinaemia or myopia. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.
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摘要:P. B. Marshall. Brit. J. Pharmacol. 10, 270 (1955).
摘要:Sunshine, I. (ed.). CRC Handbook of Analytical Toxicology. Cleveland: The Chemical Rubber Co., 1969., p. 260
摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
参考文献:10.1016/s0379-0738(01)00460-1
摘要:Gergov M, Robson JN, Ojanperä I, Heinonen OP, Vuori E. Simultaneous screening and quantitation of 18 antihistamine drugs in blood by liquid chromatography ionspray tandem mass spectrometry. Forensic Sci Int. 2001 Sep 15;121(1-2):108–15. doi: 10.1016/s0379-0738(01)00460-1.
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