CAS: 895519-90-1; N-(6-Methyl-5-((4-(Pyridin-3-yl)Pyrimidin-2-yl)Amino)Pyridin-3-yl)-4-((4-Methylpiperazin-1-yl)Methyl)-3-(Trifluoromethyl)Benzamide

该化合物是一种小分子性强结结膜活性抑制剂,有选择性地针对BCR-ABL,小板原生长因子受体(PDGFR)和干细胞因子受体(c-KIT),主要为治疗慢性流线性白血病(CML)和胃肠炎肿瘤(GISTs)而进行调查;Flumatinib具有很高的威力和特殊性,与早期的TKI相比,与BCR-ABL的粘合性有所提高.其药用植物基因特征显示口服生物利用率和持续目标抑制作用,有助于提高治疗效果.临床和临床研究表明,克服抗药性突变和减少离目标效应有潜在优势.Flumatinib是抗性或耐性CML的病人的一个有前途的候选者.目前正在进行进一步的研究,以评价其长期安全和功效.

结构式图片

上下游产品

N-(2-Methyl-5-Aminopyridin-3-yl)-4-(Pyridin-3-yl)Pyrimidin-2-Amine 895519-81-0

合成工艺路线路线简述

  • 781613-02-3 + 895519-81-0 = 895519-90-1
    反应条件:1.1 Solvents: Pyridine; Rt; Overnight,Rt
    标题:Synthesis,Crystal Structure,And Spectral Characterization Of Flumatinib Mesylate
    作者:Xu,Gang; Shen,Hong; Tong,Taifeng; Lu,Aifeng; Gou,Shaohua
    参考文献:Synthetic Communications 日期:2010 卷标:40(17) 页码:2564-2570
📜4-甲基-3-三氟甲基苯甲腈置于n-溴代丁二酰亚胺(Nbs),Copper(L) Iodide,偶氮二异丁腈,Palladium Diacetate,Potassium Carbonate,乙二胺,特丁基对苯二酚体系中,用 四氢呋喃,水,N,N-二甲基甲酰胺,乙腈 作为反应溶剂,化学反应 14.0H,反应生成 4-[(4-甲基-1-哌嗪基)甲基]-N-[6-甲基-5-[[4-(3-吡啶基)-2-嘧啶基]氨基]-3-吡啶基]-3-(三氟甲基)苯甲酰胺
参考文献:氟马替尼的合成方法
标题:氟马替尼的合成方法
摘要:本发明公开一种甲磺酸氟马替尼的合成方法,具体是以4‑甲基‑3‑(三氟甲基)苯甲腈为起始原料经溴代,取代和偶联三步反应制备得到氟马替尼.该方法路线合理,操作简单,避免引入基因毒性杂质,并且收率和纯度较高,利于氟马替尼的工业化生产和提高药品质量.

海关参考信息

专利信息


专利号:US-12390420-B1
优先权日:2024-10-22
标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
发明人:EGUCHI MASAKATSU
权利人:BRYET US INC
摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

专利号:CN-107663151-B
优先权日:2016-07-28
标 题:Intermediate synthesis method of flumatinib mesylate

供应商参考报价(招募中)

品牌试剂参考报价(招募中)

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

主要参考文献


1: Zhang L, Meng L, Liu B, Zhang Y, Zhu H, Cui J, Sun A, Hu Y, Jin J, Jiang H, Zhang X, Li Y, Liu L, Zhang W, Liu X, Gu J, Qiao J, Ouyang G, Liu X, Luo J, Jiang M, Xie X, Li J, Zhao C, Zhang M, Yang T, Wang J. Flumatinib versus Imatinib for Newly Diagnosed Chronic Phase Chronic Myeloid Leukemia: A Phase III, Randomized, Open-label, Multi-center FESTnd Study. Clin Cancer Res. 2021 Jan 1;27(1):70-77. doi: 10.1158/1078-0432.CCR-20-1600. Epub 2020 Sep 14. 39(2):344-346. doi: 10.1007/s12288-022-01585-3. Epub 2022 Oct 17.
3: Chen J, Guo S, Yu X, Lei J, Xu T, Zhu S, Chen L, Xu P, Zhou X, Yu L. Metabolic interactions between flumatinib and the CYP3A4 inhibitors erythromycin, cyclosporine, and voriconazole. Pharmazie. 2020 Sep 1;75(9):424-429. doi: 10.1691/ph.2020.0068. 78(1):13-16. doi: 10.1691/ph.2023.2536. 105(1):117-25. doi: 10.1111/cas.12320. Epub 2014 Jan 4.
6: Huang SM, Tao T, Wan CL, Wu TM, Cao HY, Qiu Y, Shen XD, Wang BR, Ge SS, Li YY, Zhang TT, Wu B, Xue SL. Flumatinib plus venetoclax as an effective therapy for Philadelphia chromosome-positive acute myeloid leukemia: A case report. Clin Case Rep. 2023 Jan 3;11(1):e6688. doi: 10.1002/ccr3.6688.

合成参考文献


参考文献:10.1691/ph.2020.0068|10.31083/ph.2020.0068
摘要:Chen J, Guo S, Yu X, Lei J, Xu T, Zhu S, Chen L, Xu P, Zhou X, Yu L. Metabolic interactions between flumatinib and the CYP3A4 inhibitors erythromycin, cyclosporine, and voriconazole. Pharmazie. 2020 Sep 01;75(9):424–9. doi: 10.1691/ph.2020.0068.
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