CAS: 923036-25-3; N-((3R,4R)-1-Benzyl-4-Methylpiperidin-3-yl)-2-Chloro-N-Methyl-7H-Pyrrolo[2,3-D]Pyrimidin-4-Amine

结构式图片

相似化合物

2803420-43-9 1616760-97-4 477600-73-0

物理性质

MSDS等安全信息

上下游产品

2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine N-((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)-N-methylamine dihydr°Chloride cis-1-benzyl-4-methyl-3-methylaminopiperidine hydr°Chloride pyrimidin-2,4-dionepyrrolo2,3-dpyrimidin-2,4-dione

合成工艺路线路线简述

  • 90213-66-4 + 477600-70-7 + 32634-66-5 = 923036-25-3
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: Water; 10 H,Rt -> 105 °C; 105 °C -> 30 °C; 3 H,20 - 30 °C
    标题:Process For Preparation Of Piperidinylaminopyrrolopyrimidines From Activated Pyrrolopyrimidines And Piperidinylamines.
    参考文献:World Intellectual Property Organization]

    90213-66-4 + 477600-70-7 = 923036-25-3
    反应条件:1.1 Reagents: Sodium Bicarbonate Solvents: Water; 30 Min,Rt1.2 12 H,95 - 105 °C; 105 °C -> Rt; 1 H,Rt
    标题:Processes For The Preparation Of (3R,4R)-1-Benzyl-N,4-Dimethylpiperidin-3-Amine Or A Salt Thereof As Precursors For Preparing Tofacitinib
    参考文献:World Intellectual Property Organization]

    90213-66-4 + 1062580-52-2 = 923036-25-3
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: Water; Rt; 10 - 20 Min,Rt1.2 20 - 24 H,100 °C
    标题:Refining Method Of Tofacitinib Citrate
    参考文献:China]

    90213-66-4 + 477600-70-7 = 923036-25-3
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane,Water; 20 H,Rt -> 100 °C
    标题:Synthesis Method Of Tofacitinib Citrate As Janus Kinase Inhibitor For Treating Active Rheumatoid Arthritis
    参考文献:China]

    90213-66-4 + 1062580-52-2 = 923036-25-3
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: Water; Rt -> 102 °C; 10 H,98 - 102 °C; 102 °C -> 25 °C; 4 H,20 - 25 °C
    标题:Preparation Method Of Key Intermediate (3R,4R)-Methyl-(4-Methyl-Piperidin-3-Yl)-(7H-Pyrido[2,3-D]Pyrimidin-4-Yl)Amine Of Tofacitinib
    参考文献:China]

    90213-66-4 + 1062580-52-2 = 923036-25-3
    反应条件:1.1 Reagents: Sodium Carbonate Solvents: Ethanol; Rt -> 50 °C
    标题:Preparation Method Of Tofacitinib Citrate
    参考文献:China]

    90213-66-4 + 1062580-52-2 = 923036-25-3
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: Water; Rt -> Reflux; 10 H,Reflux
    标题:Preparation Method For Tofacitinib Citrate Avoiding Explosive Hydrogen Gas
    参考文献:China]

    90213-66-4 + 1820713-38-9 = 923036-25-3
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane,Water; 20 H,Rt -> 50 °C
    标题:Synthesis Method Of Tofacitinib Citrate
    参考文献:China]

    = 923036-25-3 [标题:Reaction Conditions
    标题:Pyrrolo[2,3-D]Pyrimidine Derivatives; Their Intermediates And Synthesis
    参考文献:United States
📜顺-1-苄基-4-甲基哌啶-3-氨基酸甲酯盐酸盐置于碳酸氢钠,Potassium Carbonate体系中,用 甲基叔丁基醚,水 作为反应溶剂,化学反应 23.75H,反应生成 托法替尼杂质7
参考文献: Processes For Preparing (3R,4R)-1-Benzyl-N,4-Dimethylpiperidin-3-Amine Or A Salt Thereof And Processes For Preparing Tofacitinib Using The Same[fr] Procédés De Préparation De (3R,4R)-1-Benzyl-N,4-Diméthylpipéridin-3-Amine Ou D'Un Sel De Celui-Ci Et Procédés De Préparation De Tofacitinib L'Utilisant
标题: Processes For Preparing (3R,4R)-1-Benzyl-N,4-Dimethylpiperidin-3-Amine Or A Salt Thereof And Processes For Preparing Tofacitinib Using The Same[fr] Procédés De Préparation De (3R,4R)-1-Benzyl-N,4-Diméthylpipéridin-3-Amine Ou D'Un Sel De Celui-Ci Et Procédés De Préparation De Tofacitinib L'Utilisant
摘要:本发明提供了一种新型制备(3R,4R)-1-苄基-N,4-二甲基哌啶-3-胺或其盐的方法,该中间体可用于制备托法替尼.本发明还提供了一种用于该方法的新型中间体,即甲醇异丙醇溶剂合成的甲基((3R,4R)-1-苄基-4-甲基哌啶-3-基)氨基甲酸酯二苯甲酰-L-酒石酸盐.本发明还提供了一种具有非常好稳定性的用于制备托法替尼的新型中间体,即(3R,4R)-1-苄基-N,4-二甲基哌啶-3-胺醋酸盐.此外,本发明还提供了一种使用该方法制备托法替尼或其药学上可接受的盐的方法.

海关参考信息

专利信息


专利号:US-8309716-B2
优先权日:2005-07-29
标题 :Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis
发明人：RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J
权利人:RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J; PFIZER
摘要:This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.

专利号:US-9828380-B2
优先权日:2015-04-10
标题 :Efficient method for the preparation of tofacitinib citrate
发明人：BONANOMI JACOPO; DEFIORE STELLA; NOVO BARBARA
权利人:OLON SPA
摘要:Disclosed is a novel process for the synthesis of tofacitinib citrate on an industrial scale with high yields and purity starting with cis-(1-benzyl-4-methyl-piperidin-3-yl)methylamine bis-hydrochloride racemate (intermediate VIII), which comprises:n 1. Condensation between intermediates VII and VIII to give intermediate VI 2. Hydrogenation of intermediate VI to give intermediate V 3. Resolution of intermediate V to give intermediate IV with enantiomeric purity >99% 4. Release of intermediate IV in a basic medium to give intermediate III 5. N-acylation reaction of intermediate III to give II (tofacitinib) 6. Salification of intermediate II to give tofacitinib monocitrate (I)

专利号:PT-1913000-E
优先权日:2005-07-29
标题 :DERIVATIVES OF PYRROLE [2,3-D] PYRIMIDINE, ITS INTERMEDIATE SUBSTANCES AND SYNTHESIS PROCESS

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合成参考文献


摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2014).
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