CAS: 944396-07-0; 5-(2,6-Dimorpholinopyrimidin-4-yl)-4-(Trifluoromethyl)Pyridin-2-Amine

该化合物是一种强效和选择性的口服全等级I磷酸丁醇3-kinase(PI3K)抑制剂,针对PI3K催化分管(p110α, β, γ 和)的所有四种异质体. PI3K路径的特性很高,它经常对癌症进行控制,使它成为肿瘤学研究的有希望的候选对象. Buparlisib 展示了有利的药用植物基因特性,包括临床前研究中良好的生物利用率和可控毒性特征. 它跨越血液-脑屏障的能力进一步扩大了其在中央...

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N-(5-(2,6-Dimorpholinopyrimidin-4-yl)-4-(Trifluoromethyl)Pyridin-2-yl)Acetamide 1607826-40-3

合成工艺路线路线简述

  • 944401-57-4 + 10244-24-3 = 944396-07-0
    反应条件:1.1 Reagents: Sodium Carbonate Catalysts: Dichloro[1,1′-Bis(Diphenylphosphino)Ferrocene]Palladium(Ii) Dichloromethane Addu... Solvents: 1,2-Dimethoxyethane,Water; 15 H,90 °C
    标题:Identification Of Nvp-Bkm120 As A Potent,Selective,Orally Bioavailable Class I Pi3 Kinase Inhibitor For Treating Cancer
    作者:Burger,Matthew T.; Pecchi,Sabina; Wagman,Allan; Ni,Zhi-Jie; Knapp,Mark; Et Al
    参考文献:Acs Medicinal Chemistry Letters 日期:2011 卷标:2(10) 页码:774-779]

    944401-57-4 + 10244-24-3 = 944396-07-0
    反应条件:1.1 Reagents: Sodium Carbonate Solvents: 1,2-Dimethoxyethane; 20 Min,Rt1.2 Catalysts: [1,1′-Bis(Diphenylphosphino)Ferrocene]Dichloropalladium; 15 H,90 °C
    标题:Preparation Of Dimorpholinopyrimidines For Inhibiting Hamartoma Tumor Cells
    参考文献:World Intellectual Property Organization]

    944401-57-4 + 10244-24-3 = 944396-07-0
    反应条件:1.1 Reagents: Sodium Carbonate Solvents: Water; 20 Min,Rt1.2 Catalysts: [1,1′-Bis(Diphenylphosphino)Ferrocene]Dichloropalladium; 15 H,90 °C
    标题:Pyrimidine Derivatives Used As Pi-3 Kinase Inhibitors And Their Preparation,Pharmaceutical Compositions And Use In The Treatment Of Cancer
    参考文献:World Intellectual Property Organization]

    10244-24-3 + 944401-56-3 = 944396-07-0
    反应条件:1.1 Reagents: Potassium Acetate,Bis(Pinacolato)Diborane Catalysts: Dichlorobis(Triphenylphosphine)Palladium Solvents: Dimethyl Sulfoxide; Rt -> 5 °C; 7 H,5 °C1.2 16 H,5 °C
    标题:New Process For The Preparation Of The Pi3K Inhibitor Buparlisib
    参考文献:United States
5-溴-4-(三氟甲基)吡啶-2-胺置于盐酸,Lithium Chloro-Isopropyl-Magnesium Chloride,Potassium Carbonate体系中,用 四氢呋喃,乙二醇二甲醚,正庚烷,水,乙酸乙酯 作为反应溶剂,80.0 °C,10.0 Kpa 条件下,反应 21.32H,反应生成 布帕尼西
参考文献: Improved Process For Manufacturing 5-(2,6-Di-4-Morpholinyl-4-Pyrimidinyl)-4-Trifluoromethylpyridin-2-Amine[fr] Procédé Amélioré Pour La Fabrication De 5-(2,6-Di-4-Morpholinyl-4-Pyrimidinyl)-4-Trifluorométhylpyridin-2-Amine
标题: Improved Process For Manufacturing 5-(2,6-Di-4-Morpholinyl-4-Pyrimidinyl)-4-Trifluoromethylpyridin-2-Amine[fr] Procédé Amélioré Pour La Fabrication De 5-(2,6-Di-4-Morpholinyl-4-Pyrimidinyl)-4-Trifluorométhylpyridin-2-Amine
摘要:该发明公开了改进的制备工艺,用于制造一种化合物,即5-(2,6-二-4-吗啉基-4-嘧啶基)-4-三氟甲基吡啶-2-胺,以及其单盐盐和中间体.

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专利信息


专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

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-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-2023192681-A1
优先权日:2019-11-14
标 题 :Improved synthesis of kras g12c inhibitor compound

专利号:US-2017107577-A1
优先权日:2014-03-11
标题:Determining Cancer Aggressiveness, Prognosis and Responsiveness to Treatment
发明人:AL-EJEH FARES
权利人:THE COUNCIL OF THE QUEENSLAND INST OF MEDICAL RES
摘要:The invention provides methods of determining the aggressiveness, prognosis and response to therapy for particular cancers, which include comparing the expression levels of one or a plurality of differentially expressed genes from one or more 5 functional metagenes, including a Carbohydrate/Lipid Metabolism metagene, a Cell Signalling metagene, a Cellular Development metagene, a Cellular Growth metagene, a Chromosome Segregation metagene, a DNA Replication/Recombination metagene, an Immune system metagene, a Metabolic Disease metagene, a Nucleic Acid Metabolism metagene, a Post-Translational Modification metagene, a Protein 10 Synthesis/Modification metagene and a Multiple Networks metagene. The method disclosed herein may be particularly suitable as a companion diagnostic for cancer therapies.
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主要参考文献


1: Shamaa KN, Ahmed BA, Helmy IM. Collaborative role of calcitriol with buparlisib in the tongue squamous cell carcinoma cell line by modulating the Casp3 and Akt1 gene expression. Dent Med Probl. 2025 Sep-Oct;62(5):891-898. doi: 10.17219/dmp/175583. 20(2):299-310. doi: 10.1007/s11523-024-01126-0. Epub 2025 Jan 14.
78:100291. doi: 10.1016/j.clinsp.2023.100291.
4: Kaewlert W, Sakonsinsiri C, Lert-Itthiporn W, Mahalapbutr P, Ali S, Rungrotmongkol T, Jusakul A, Armartmuntree N, Pairojkul C, Feng G, Ma N, Pinlaor S, Murata M, Thanan R. Buparlisib and ponatinib inhibit aggressiveness of cholangiocarcinoma cells via suppression of IRS1-related pathway by targeting oxidative stress resistance. Biomed Pharmacother. 2024 Nov;180:117569. doi: 10.1016/j.biopha.2024.117569. Epub 2024 Oct 17.

合成参考文献


参考文献:10.1158/2159-8290.cd-12-0262
摘要:Jia S, Gao X, Lee SH, Maira SM, Wu X, Stack EC, Signoretti S, Loda M, Zhao JJ, Roberts TM. Opposing effects of androgen deprivation and targeted therapy on prostate cancer prevention. Cancer Discov. 2013 Jan;3(1):44–51.
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