CAS: 1898283-02-7; 2-(4-((4-((1-Cyclopropyl-3-(Tetrahydro-2H-Pyran-4-yl)-1H-Pyrazol-4-yl)Oxy)Pyridin-2-yl)Amino)Pyridin-2-yl)Propan-2-Ol

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合成工艺路线路线简述

    📜4-溴吡啶-2-甲酸乙酯置于ammonium Hydroxide,Palladium Diacetate,铜,Caesium Carbonate,4,5-双二苯基膦-9,9-二甲基氧杂蒽体系中,用 四氢呋喃,2-甲基四氢呋喃,1,4-二氧六环,水 用作溶剂,化学反应 0.5H,反应生成4-[[4-[[1-环丙基-3-(四氢-2H-吡喃-4-基)-1H-吡唑-4-基]氧基]-2-吡啶基]氨基]-Alpha,Alpha-二甲基-2-吡啶甲醇
    参考文献:Aminopyridyloxypyrazole Compounds
    标题:Aminopyridyloxypyrazole Compounds
    摘要:本发明涉及新型氨基吡啶氧吡唑化合物,其抑制转化生长因子β受体1(tgfβr1)的活性,包括所述化合物的药物组合物,以及使用所述化合物治疗癌症的方法,优选结肠癌,黑色素瘤,肝细胞癌,肾癌,胶质母细胞瘤,胰腺癌,骨髓增生异常综合征,肺癌和胃癌,和/或纤维化,优选肝纤维化和慢性肾病.

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    主要参考文献

    [1]. Huaxing Pei, et al. Abstract
    955: LY3200882, a novel, highly selective TGFβRI small molecule inhibitor. AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 955. https://aacrjournals.org/cancerres/article/77/13_Supplement/955/622127/Abstract-955-LY3200882-a-novel-highly-selective [2]. Xu G, Zhang Y, Wang H, Guo Z, Wang X, Li X, Chang S, Sun T, Yu Z, Xu T, Zhao L, Wang Y, Yu W. Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-β type 1 receptor inhibitors. Eur J Med Chem. 2020 Jul 15;198:112354. doi: 10.1016/j.ejmech.2020.112354. Epub 2020 Apr 29.

    合成参考文献


    参考文献:10.1016/j.bmcl.2022.128552
    摘要:Wang Z, Zhang Y, Wang H, Wang X, Yu Z, Zhao L. Synthesis and biological evaluation of 4-(pyridine-4-oxy)-3-(tetrahydro-2H-pyran-4-yl)-pyrazole derivatives as novel, potent of ALK5 receptor inhibitors. Bioorganic & Medicinal Chemistry Letters. 2022 Apr;61():128552. doi: 10.1016/j.bmcl.2022.128552.
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