CAS: 91374-21-9; 4-(2-(Dipropylamino)Ethyl)Indolin-2-One

该化合物是主要用于治疗帕金森氏病和不动腿综合症(RLS)的非乙基多巴胺抗药剂,它对多巴胺D2类受体采取选择性行动,通过弥补脑中多巴胺缺乏症,帮助缓解运动症状.该化合物具有较高的生物利用率和快速吸收能力,血浆浓度在行政后1-2小时内达到峰值.罗皮尼罗的代谢性特征非常精细,其血清相互作用极少,降低了......

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CAS号76149-15-0 N-[2-(1H-indol-... | CAS号91374-25-3 2-[2-(二丙基氨基)乙基]... | CAS号720656-64-4 2-(2-N,N-二丙基氨基乙... | CAS号1975-50-4 2-甲基-3-硝基苯甲酸 | CAS号23876-13-3 2-甲基-3-硝基苯甲醇 | CAS号23876-15-5 2-甲基-3-硝基苯乙酸 | CAS号23876-14-4 2-甲基-3-硝基苯乙腈 | CAS号81654-62-8 4-[2-(dipropyla... | CAS号60468-54-4 2-甲基-3-硝基苄氯 | CAS号101566-00-1 (2-METHYL-3-NIT... | CAS号91374-20-8 盐酸罗匹尼罗

合成工艺路线路线简述

  • 106916-16-9 = 91374-21-9
    反应条件:1.1 Reagents: Sodium Borohydride Solvents: Toluene; 0 - 5 °C1.2 Catalysts: Nickel; 5 °C -> 30 °C1.3 30 °C -> 80 °C1.4 Reagents: Sodium Borohydride; 80 °C; 3 H,80 °C1.5 Reagents: Hydrochloric Acid Solvents: Water; Ph 7 - 8
    标题:Efficient Synthesis Of Tertiary Amine By Direct N-Alkylation Of Secondary Amine With Carboxylic Acid Using Ni (0) Encat Catalyst
    作者:Quadri,Syed Aziz Imam; Et Al
    参考文献:Synthetic Communications 日期:2018 卷标:48(3) 页码:267-277]

    139122-20-6 = 91374-21-9
    反应条件:1.1 Solvents: Water; 5 H,Reflux
    标题:Process For Preparation Of Ropinirole Hydrochloride From Benzeneethanol
    参考文献:China]

    720656-64-4 = 91374-21-9
    反应条件:1.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Ethanol
    标题:A Convenient Synthesis Of 4-(2-Hydroxyethyl)Indolin-2-One,A Useful Intermediate For The Preparation Of Both Dopamine Receptor Agonists And Protein Kinase Inhibitors
    作者:Matera,Carlo; Et Al
    参考文献:Monatshefte Fuer Chemie 日期:2014 卷标:145(7) 页码:1139-1144]

    91374-20-8 = 91374-21-9
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Water; 15 Min,Rt1.2 Solvents: Dichloromethane; 15 Min,Rt
    标题:Synthesis And Pharmacological Evaluation Of Dual Acting Ligands Targeting The Adenosine A2A And Dopamine D2 Receptors For The Potential Treatment Of Parkinson'S Disease
    作者:Jorg,Manuela; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2015 卷标:58(2) 页码:718-738]

    91374-20-8 = 91374-21-9
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Water; 15 Min,Rt
    标题:Investigation Of Novel Ropinirole Analogues: Synthesis,Pharmacological Evaluation And Computational Analysis Of Dopamine D2 Receptor Functionalized Congeners And Homobivalent Ligands
    作者:Jorg,Manuela; Et Al
    参考文献:Medchemcomm 日期:2014 卷标:5(7) 页码:891-898]

    76149-15-0 = 91374-21-9
    反应条件:1.1 Reagents: 3H-1,2-Benziodoxol-3-One,1-Fluoro- Solvents: 1,4-Dioxane,Water; 5 - 6 H,140 °C1.2 Reagents: Sodium Bicarbonate Solvents: Water
    标题:Synthesis Of 2-Oxindoles From Substituted Indoles By Hypervalent-Iodine Oxidation
    作者:Jiang,Xinpeng; Et Al
    参考文献:European Journal Of Organic Chemistry 日期:2018 卷标:2018(12) 页码:1437-1442]

    = 91374-21-9
    反应条件:1.1 Solvents: Dichloromethane; 5 Min,Rt1.2 Reagents: Acetic Acid; 10 Min,Rt1.3 Reagents: Sodium Cyanoborohydride; 1.5 H,Rt1.4 Reagents: Potassium Carbonate Solvents: Water; Rt
    标题:The Development Of A Short Route To The Api Ropinirole Hydrochloride
    作者:Yousuf,Zeshan; Et Al
    参考文献:Organic & Biomolecular Chemistry 日期:2015 卷标:13(42) 页码:10532-10539]

    720656-64-4 = 91374-21-9 [标题:Reaction Conditions
    标题:Product Class 13: Indole And Its Derivatives
    作者:Joule,J. A.
    参考文献:Science Of Synthesis 日期:2001 卷标:10 页码:361-652
在 Sodium Hydroxide,水体系中,用 1,4-二氧六环 作为反应溶剂,化学反应生成 累匹利洛
参考文献:Novel Process For Ropinirole Preparation
标题:Novel Process For Ropinirole Preparation
摘要:一种用于制备以下化合物的方法:其中r2选自氨基,低烷基氨基,二烷基氨基,烯丙氨基,二烯丙氨基,N-烷基-N-烯丙氨基,苄氨基,二苄氨基,苯乙基氨基,二苯乙基氨基,4-羟基苯乙基氨基或二-(4-羟基苯乙基氨基)等基团的方法;包括:A)将与wittig试剂反应以产生其中r1为烷氧基;f)在酸性条件下水解化合物ii以产生g)将化合物iii进行还原和胺化以产生三级胺,其中r2如上所定义;h)将化合物iv与4-氯苯氧乙腈反应,进行亲核取代以产生腈化合物,其中r2如上所定义;并i)在同一步骤中使用钯/c和氢氧化钠进行还原和水解以产生其中r2如上所定义.

海关参考信息

专利信息


专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-11766432-B2
优先权日:2018-07-27
标题 :Cleavable conjugates of catechol compounds and water-soluble polymers and methods of treatment using the same
发明人:BENTLEY MICHAEL; FANG ZHIHAO; WEIMER REBECCA; VIEGAS TACEY; MOREADITH RANDALL
权利人:SERINA THERAPEUTICS INC
摘要:Described are conjugates comprising a water-soluble polymer linked to a compound comprising a catechol moiety via a cleavable linkage, wherein the cleavable linkage is formed between the water-soluble polymer and a first phenolic hydroxyl group of the catechol moiety and a second phenolic hydroxyl group of the catechol moiety is linked to a blocking group wherein the rate of hydrolytic release of the compound comprising the catechol moiety is controlled, at least in part, through structure or design of the blocking group on the second phenolic hydroxyl group of the catechol moiety. Therefore, the rate of hydrolytic release of the compound comprising the catechol moiety can be tuned through structural design of the group on the second phenolic hydroxyl group of the catechol moiety. Compounds used in the synthesis of the described conjugates and methods of using the described conjugate and other compounds in the treatment of dopamine-responsive disorders are also described.

专利号:US-2008125354-A1
优先权日:2005-11-21
标题 :Selective inhibition of matrix metalloproteinases
发明人:FIELDS GREGG B; HAMMER ROBERT
权利人:UNIV FLORIDA ATLANTIC; UNIV LOUISIANA STATE
摘要:Synthetic triple-helical peptides (THPs) are used for the design and synthesis of triple-helical transition state analog inhibitors. These inhibitors feature a phosphonate ester or phosphinic moiety in place of the scissle bond. These groups inhibit MMPs, and methods been developed for their convenient incorporation within a peptide sequence by solid-phase methods.

专利号:WO-2025128098-A1
优先权日:2023-12-13
标 题 :Solid oral dosage forms, kits, and methods of using the same
发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO
权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

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-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
常州市金坛区水北医药化工厂
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主要参考文献


1: Mochizuki H, Hattori N, Hasegawa K, Nomoto M, Uchida E, Terahara T, Okawa K, Fukuta H. Long-term study of ropinirole patch in Parkinson's disease patients with/without basal l-dopa. Parkinsonism Relat Disord. 2021 Feb;83:105-109. doi: 10.1016/j.parkreldis.2020.12.023. Epub 2021 Jan 11.
167:605-619. doi: 10.1016/j.ijbiomac.2020.11.207. Epub 2020 Dec 2. 10(4):242. doi: 10.3390/jpm10040242.
4: Russell B, Barrus MM, Tremblay M, Ma L, Hrelja K, Wong C, Hynes TJ, Hobson S, Grottick AJ, Winstanley CA. GPR52 agonists attenuate ropinirole-induced preference for uncertain outcomes. Behav Neurosci. 2020 Oct 29. doi: 10.1037/bne0000391. Epub ahead of print.

合成参考文献


参考文献:10.1002/mds.22962
摘要:Karvonen MK, Kaasinen V, Korja M, Marttila RJ. Ropinirole diminishes myoclonus and improves writing and postural balance in an ULD patient. Mov Disord. 2010 Mar 15;25(4):520–1. doi: 10.1002/mds.22962.
参考文献:10.1007/s10928-005-0039-x
摘要:Chan PLS, Nutt JG, Holford NHG. Importance of Within Subject Variation in Levodopa Pharmacokinetics: A 4Year Cohort Study in Parkinson’s Disease. Journal of Pharmacokinetics and Pharmacodynamics. 2005 Aug;32(3-4):307–31. doi: 10.1007/s10928-005-0039-x.
参考文献:10.1016/j.neuropharm.2011.06.022
摘要:Sahlholm K, Barchad-Avitzur O, Marcellino D, Gómez-Soler M, Fuxe K, Ciruela F, Arhem P. Agonist-specific voltage sensitivity at the dopamine D2S receptor--molecular determinants and relevance to therapeutic ligands. Neuropharmacology. 2011 Oct;61(5-6):937–49. doi: 10.1016/j.neuropharm.2011.06.022.
参考文献:10.1007/s00702-011-0682-x
摘要:Gerlach M, Maetzler W, Broich K, Hampel H, Rems L, Reum T, Riederer P, Stöffler A, Streffer J, Berg D. Biomarker candidates of neurodegeneration in Parkinson’s disease for the evaluation of disease-modifying therapeutics. Journal of Neural Transmission. 2011 Jul 14;119(1):39–52. doi: 10.1007/s00702-011-0682-x.
参考文献:10.1007/s00415-011-6162-2
摘要:Antonini A, Pilleri M, Padoan A, Landi A, Ferla S, Biundo R, D'Avella D. Successful subthalamic stimulation in genetic Parkinson's disease caused by duplication of the α-synuclein gene. J Neurol. 2012 Jan;259(1):165–7. doi: 10.1007/s00415-011-6162-2.
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