CAS: 802539-81-7; N,1,4,4-Tetramethyl-8-((4-(4-Methylpiperazin-1-yl)Phenyl)Amino)-4,5-Dihydro-1H-Pyrazolo[4,3-H]Quinazoline-3-Carboxamide

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物理性质

MSDS等安全信息

上下游产品

methylamine 4-(4-Methyl-piperazino)-anilin8-[4-(4-methyl-piperazin-1-yl)-phenylamino]-1,4,4-trimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid methylamide glycolate

合成工艺路线路线简述

  • 16153-81-4 + 802540-46-1 = 802539-81-7
    反应条件:1.1 Catalysts: Palladium Diacetate,Binap Solvents: Dimethylformamide; 30 Min,Rt1.2 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 3 H,80 °C; 80 °C -> Rt
    标题:Identification Of N,1,4,4-Tetramethyl-8-{[4-(4-Methylpiperazin-1-Yl)Phenyl]Amino}-4,5-Dihydro-1H-Pyrazolo[4,3-H]Quinazoline-3-Carboxamide (Pha-848125),A Potent,Orally Available Cyclin Dependent Kinase Inhibitor
    作者:Brasca,Maria Gabriella; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2009 卷标:52(16) 页码:5152-5163]

    802534-92-5 = 802539-81-7
    反应条件:1.1 Reagents: Isoamyl Nitrite,Iodine,Cuprous Iodide,Cesium Iodide Solvents: 1,2-Dimethoxyethane; 18 H,65 °C; Cooled2.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane,Water; 30 H,Reflux; Cooled2.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified2.3 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: Dimethylformamide; Overnight,Rt3.1 Catalysts: Palladium Diacetate,Binap Solvents: Dimethylformamide; 30 Min,Rt3.2 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 3 H,80 °C; 80 °C -> Rt
    标题:Identification Of N,1,4,4-Tetramethyl-8-{[4-(4-Methylpiperazin-1-Yl)Phenyl]Amino}-4,5-Dihydro-1H-Pyrazolo[4,3-H]Quinazoline-3-Carboxamide (Pha-848125),A Potent,Orally Available Cyclin Dependent Kinase Inhibitor
    作者:Brasca,Maria Gabriella; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2009 卷标:52(16) 页码:5152-5163]

    50-01-1 + 802541-49-7 = 802539-81-7
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 6 H,110 °C; Cooled2.1 Reagents: Isoamyl Nitrite,Iodine,Cuprous Iodide,Cesium Iodide Solvents: 1,2-Dimethoxyethane; 18 H,65 °C; Cooled3.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane,Water; 30 H,Reflux; Cooled3.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified3.3 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: Dimethylformamide; Overnight,Rt4.1 Catalysts: Palladium Diacetate,Binap Solvents: Dimethylformamide; 30 Min,Rt4.2 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 3 H,80 °C; 80 °C -> Rt
    标题:Identification Of N,1,4,4-Tetramethyl-8-{[4-(4-Methylpiperazin-1-Yl)Phenyl]Amino}-4,5-Dihydro-1H-Pyrazolo[4,3-H]Quinazoline-3-Carboxamide (Pha-848125),A Potent,Orally Available Cyclin Dependent Kinase Inhibitor
    作者:Brasca,Maria Gabriella; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2009 卷标:52(16) 页码:5152-5163]

    17421-93-1 = 802539-81-7
    反应条件:1.1 Reagents: Potassium Hydroxide Solvents: Methanol; 20 H,Rt; Cooled2.1 Reagents: Sodium Hydride Solvents: Tetrahydrofuran; 15 Min,Rt2.2 Solvents: Tetrahydrofuran; 1 H,Reflux2.3 Reagents: Hydrochloric Acid Solvents: Water; Acidified2.4 Solvents: Acetic Acid; Rt; 12 H,Rt3.1 Solvents: Dimethylformamide; 2 H,60 °C4.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 6 H,110 °C; Cooled5.1 Reagents: Isoamyl Nitrite,Iodine,Cuprous Iodide,Cesium Iodide Solvents: 1,2-Dimethoxyethane; 18 H,65 °C; Cooled6.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane,Water; 30 H,Reflux; Cooled6.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified6.3 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: Dimethylformamide; Overnight,Rt7.1 Catalysts: Palladium Diacetate,Binap Solvents: Dimethylformamide; 30 Min,Rt7.2 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 3 H,80 °C; 80 °C -> Rt
    标题:Identification Of N,1,4,4-Tetramethyl-8-{[4-(4-Methylpiperazin-1-Yl)Phenyl]Amino}-4,5-Dihydro-1H-Pyrazolo[4,3-H]Quinazoline-3-Carboxamide (Pha-848125),A Potent,Orally Available Cyclin Dependent Kinase Inhibitor
    作者:Brasca,Maria Gabriella; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2009 卷标:52(16) 页码:5152-5163]

    802535-78-0 = 802539-81-7
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane,Water; 30 H,Reflux; Cooled1.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified1.3 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: Dimethylformamide; Overnight,Rt2.1 Catalysts: Palladium Diacetate,Binap Solvents: Dimethylformamide; 30 Min,Rt2.2 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 3 H,80 °C; 80 °C -> Rt
    标题:Identification Of N,1,4,4-Tetramethyl-8-{[4-(4-Methylpiperazin-1-Yl)Phenyl]Amino}-4,5-Dihydro-1H-Pyrazolo[4,3-H]Quinazoline-3-Carboxamide (Pha-848125),A Potent,Orally Available Cyclin Dependent Kinase Inhibitor
    作者:Brasca,Maria Gabriella; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2009 卷标:52(16) 页码:5152-5163]

    36805-97-7 + 802541-48-6 = 802539-81-7
    反应条件:1.1 Solvents: Dimethylformamide; 2 H,60 °C2.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 6 H,110 °C; Cooled3.1 Reagents: Isoamyl Nitrite,Iodine,Cuprous Iodide,Cesium Iodide Solvents: 1,2-Dimethoxyethane; 18 H,65 °C; Cooled4.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane,Water; 30 H,Reflux; Cooled4.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified4.3 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: Dimethylformamide; Overnight,Rt5.1 Catalysts: Palladium Diacetate,Binap Solvents: Dimethylformamide; 30 Min,Rt5.2 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 3 H,80 °C; 80 °C -> Rt
    标题:Identification Of N,1,4,4-Tetramethyl-8-{[4-(4-Methylpiperazin-1-Yl)Phenyl]Amino}-4,5-Dihydro-1H-Pyrazolo[4,3-H]Quinazoline-3-Carboxamide (Pha-848125),A Potent,Orally Available Cyclin Dependent Kinase Inhibitor
    作者:Brasca,Maria Gabriella; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2009 卷标:52(16) 页码:5152-5163]

    85312-29-4 = 802539-81-7
    反应条件:1.1 Reagents: Sodium Hydride Solvents: Tetrahydrofuran; 15 Min,Rt1.2 Solvents: Tetrahydrofuran; 1 H,Reflux1.3 Reagents: Hydrochloric Acid Solvents: Water; Acidified1.4 Solvents: Acetic Acid; Rt; 12 H,Rt2.1 Solvents: Dimethylformamide; 2 H,60 °C3.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 6 H,110 °C; Cooled4.1 Reagents: Isoamyl Nitrite,Iodine,Cuprous Iodide,Cesium Iodide Solvents: 1,2-Dimethoxyethane; 18 H,65 °C; Cooled5.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane,Water; 30 H,Reflux; Cooled5.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified5.3 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: Dimethylformamide; Overnight,Rt6.1 Catalysts: Palladium Diacetate,Binap Solvents: Dimethylformamide; 30 Min,Rt6.2 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 3 H,80 °C; 80 °C -> Rt
    标题:Identification Of N,1,4,4-Tetramethyl-8-{[4-(4-Methylpiperazin-1-Yl)Phenyl]Amino}-4,5-Dihydro-1H-Pyrazolo[4,3-H]Quinazoline-3-Carboxamide (Pha-848125),A Potent,Orally Available Cyclin Dependent Kinase Inhibitor
    作者:Brasca,Maria Gabriella; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2009 卷标:52(16) 页码:5152-5163]

    4683-45-8 = 802539-81-7
    反应条件:1.1 Reagents: Lithium Aluminum Hydride Solvents: Tetrahydrofuran; 0 - 5 °C; 5 °C -> 25 °C; 4 H,25 °C; Cooled1.2 Reagents: Ethyl Acetate1.3 Reagents: Sulfuric Acid Solvents: Water; Cooled1.4 Reagents: Sodium Hydroxide,Hydrogen Peroxide Solvents: Methanol,Water; Rt -> 0 °C; 0 °C; 20 H,4 °C2.1 Reagents: Potassium Hydroxide Solvents: Methanol; 20 H,Rt; Cooled3.1 Reagents: Sodium Hydride Solvents: Tetrahydrofuran; 15 Min,Rt3.2 Solvents: Tetrahydrofuran; 1 H,Reflux3.3 Reagents: Hydrochloric Acid Solvents: Water; Acidified3.4 Solvents: Acetic Acid; Rt; 12 H,Rt4.1 Solvents: Dimethylformamide; 2 H,60 °C5.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 6 H,110 °C; Cooled6.1 Reagents: Isoamyl Nitrite,Iodine,Cuprous Iodide,Cesium Iodide Solvents: 1,2-Dimethoxyethane; 18 H,65 °C; Cooled7.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane,Water; 30 H,Reflux; Cooled7.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified7.3 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: Dimethylformamide; Overnight,Rt8.1 Catalysts: Palladium Diacetate,Binap Solvents: Dimethylformamide; 30 Min,Rt8.2 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 3 H,80 °C; 80 °C -> Rt
    标题:Identification Of N,1,4,4-Tetramethyl-8-{[4-(4-Methylpiperazin-1-Yl)Phenyl]Amino}-4,5-Dihydro-1H-Pyrazolo[4,3-H]Quinazoline-3-Carboxamide (Pha-848125),A Potent,Orally Available Cyclin Dependent Kinase Inhibitor
    作者:Brasca,Maria Gabriella; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2009 卷标:52(16) 页码:5152-5163]

    126-81-8 = 802539-81-7
    反应条件:1.1 Reagents: Titanium Tetrachloride Solvents: Methanol,Dichloromethane; 1 H,Rt1.2 Reagents: Sodium Bicarbonate Solvents: Water; Cooled2.1 Reagents: Lithium Aluminum Hydride Solvents: Tetrahydrofuran; 0 - 5 °C; 5 °C -> 25 °C; 4 H,25 °C; Cooled2.2 Reagents: Ethyl Acetate2.3 Reagents: Sulfuric Acid Solvents: Water; Cooled2.4 Reagents: Sodium Hydroxide,Hydrogen Peroxide Solvents: Methanol,Water; Rt -> 0 °C; 0 °C; 20 H,4 °C3.1 Reagents: Potassium Hydroxide Solvents: Methanol; 20 H,Rt; Cooled4.1 Reagents: Sodium Hydride Solvents: Tetrahydrofuran; 15 Min,Rt4.2 Solvents: Tetrahydrofuran; 1 H,Reflux4.3 Reagents: Hydrochloric Acid Solvents: Water; Acidified4.4 Solvents: Acetic Acid; Rt; 12 H,Rt5.1 Solvents: Dimethylformamide; 2 H,60 °C6.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 6 H,110 °C; Cooled7.1 Reagents: Isoamyl Nitrite,Iodine,Cuprous Iodide,Cesium Iodide Solvents: 1,2-Dimethoxyethane; 18 H,65 °C; Cooled8.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane,Water; 30 H,Reflux; Cooled8.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified8.3 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: Dimethylformamide; Overnight,Rt9.1 Catalysts: Palladium Diacetate,Binap Solvents: Dimethylformamide; 30 Min,Rt9.2 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 3 H,80 °C; 80 °C -> Rt
    标题:Identification Of N,1,4,4-Tetramethyl-8-{[4-(4-Methylpiperazin-1-Yl)Phenyl]Amino}-4,5-Dihydro-1H-Pyrazolo[4,3-H]Quinazoline-3-Carboxamide (Pha-848125),A Potent,Orally Available Cyclin Dependent Kinase Inhibitor
    作者:Brasca,Maria Gabriella; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2009 卷标:52(16) 页码:5152-5163
📜4-(4-甲基哌嗪)苯胺置于palladium Diacetate,R-(+)-1,1'-联萘-2,2'-双二苯膦 氢氧化钾,Potassium Carbonate,1-羟基苯并三唑,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺体系中,用 四氢呋喃,Dmf (N,N-Dimethyl-Formamide),乙醇 作为反应溶剂,化学反应 25.0H,反应生成 4,5-二氢-N,1,4,4-四甲基-8-[[4-(4-甲基-1-哌嗪)苯基]氨基]-1H-吡唑并[4,3-H]喹唑啉-3-羧酰胺
参考文献: Pyrazolo-Quinazoline Derivatives,Process For Their Preparation And Their Use As Kinase Inhibitors[fr] Derives De Pyrazolo-Quinazoline,Procede De Preparation Associe Et Leur Utilisation En Tant Qu'Inhibiteurs De Kinase
标题: Pyrazolo-Quinazoline Derivatives,Process For Their Preparation And Their Use As Kinase Inhibitors[fr] Derives De Pyrazolo-Quinazoline,Procede De Preparation Associe Et Leur Utilisation En Tant Qu'Inhibiteurs De Kinase
摘要:公开了配方(Ia)或(Ib)中定义的吡唑喹唑啉衍生物及其药用盐,其制备方法以及包含它们的药物组合物;本发明的化合物可能在治疗中对与异常蛋白激酶活性相关的疾病,如癌症,具有用处.

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专利信息


专利号:US-2018371021-A1
优先权日:2017-05-11
标 题 :Peptidomimetic macrocycles and uses thereof
发明人：AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.

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主要参考文献


1: Degrassi A, Russo M, Nanni C, Patton V, Alzani R, Giusti AM, Fanti S, Ciomei M, Pesenti E, Texido G. Efficacy of PHA-848125, a cyclin-dependent kinase inhibitor, on the K-Ras(G12D)LA2 lung adenocarcinoma transgenic mouse model: evaluation by multimodality imaging. Mol Cancer Ther. 2010 Mar;9(3):673-81. Epub 2010 Mar 2. Epub 2009 Dec 21.

合成参考文献


参考文献:10.1021/jm9006559
摘要:Brasca MG, Amboldi N, Ballinari D, Cameron A, Casale E, Cervi G, Colombo M, Colotta F, Croci V, D’Alessio R, Fiorentini F, Isacchi A, Mercurio C, Moretti W, Panzeri A, Pastori W, Pevarello P, Quartieri F, Roletto F, Traquandi G, Vianello P, Vulpetti A, Ciomei M. Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor. J. Med. Chem. 2009 Jul 15;52(16):5152–63. doi: 10.1021/jm9006559.
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