CAS: 1254473-64-7; (R,E)-2-(4-(2-(5-(1-(3,5-Dichloropyridin-4-yl)Ethoxy)-1H-Indazol-3-yl)Vinyl)-1H-Pyrazol-1-yl)Ethan-1-Ol

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CAS号15579-15-4 1H-吲唑-5-醇 | CAS号879487-88-4 4-碘-1-(2-(四氢-2H... | CAS号2457-47-8 3,5-二氯吡啶 | CAS号1370347-50-4 (S)-1-(3,5-二氯吡啶...

合成工艺路线路线简述

    📜5-((R)-1-(3,5-Dichloropyridin-4-yl)Ethoxy)-1-(Tetrahydro-2H-Pyran-2-yl)-3-((E)-2-(1-(2-(Tetrahydro-2H-Pyran-2-Yloxy)Ethyl)-1H-Pyrazol-4-yl)Vinyl)-1H-Indazole置于甲醇,乙酰氯,Sodium Carbonate体系中,用 水 用作溶剂,化学反应 4.5H,以41%的收率获得4-[(1E)-2-[5-[(1R)-1-(3,5-二氯-4-吡啶基)乙氧基]-1H-吲唑-3-基]乙烯基]-1H-吡唑-1-乙醇
    参考文献:Crystalline (R)-(E)-2-(4-(2-(5-(1-(3,5-Dichloropyridin-4-yl)Ethoxy)-1H-Indazol-3-yl)Vinyl)-1H-Pyrazol-1-yl)Ethanol
    标题:Crystalline (R)-(E)-2-(4-(2-(5-(1-(3,5-Dichloropyridin-4-yl)Ethoxy)-1H-Indazol-3-yl)Vinyl)-1H-Pyrazol-1-yl)Ethanol
    摘要:这项发明提供了结晶的(R)-(E)-2-(4-(2-(5-(1-(3,5-二氯吡啶-4-基)乙氧基)-1H-吲哚-3-基)乙烯基)-1H-吡唑-1-基)乙醇,用于治疗癌症.

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    主要参考文献

    1. Zhao G, Li WY, Chen D, Henry JR, Li HY, Chen Z, Zia-Ebrahimi M, Bloem L, Zhai Y, Huss K, Peng SB, McCann DJ. A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models. Mol Cancer Ther. 2011 Nov;10(11):2200-10. Epub 2011 Sep 7.

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    参考文献:10.1021/acs.jmedchem.2c00096
    摘要:Shao M, Chen X, Yang F, Song X, Zhou Y, Lin Q, Fu Y, Ortega R, Lin X, Tu Z, Patterson AV, Smaill JB, Chen Y, Lu X. Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4. J Med Chem. 2022 Mar 24;65(6):5113–33. doi: 10.1021/acs.jmedchem.2c00096.
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