CAS: 784-57-6; 2-Morpholino-5-(Trifluoromethyl)Aniline

该化合物是一种有机化合物,其独特的分子结构特征包括一个模光环和三氟甲基替代苯基组,该化合物通常具有极地有机溶剂中中溶性等特性,由于存在三氟硫基氢恐惧物组,水中的溶解性可能有限;该化合物经常用于制药研究和开发,特别是生物活性分子的合成;氨基化合物组在结构上可以参与氢的结合,影响其再活性和与生物目标的相互作用;此外,三氟甲基化合物组可以提高亲脂性和代谢性稳定性,使其在药物设计中具有宝贵的敏感性;在处理和储存准则方面,应参考安全数据表,因为与三氟甲基化合物的化合物可展示独特的毒性特征;

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上下游产品

4-(2-nitro-4-trifluoromethylphenyl)morpholine 2-chloro-3-nitro-5-trifluoromethylbenzene 1-fluoro-2-nitro-4-trifluoromethyl-benzene N-[2-(morpholinyl)-5-(trifluoromethyl)phenyl]-2-pyridinecarboxamide 3-hydroxy-4-methyl-N-(2-morpholin-4-yl-5-trifluoromethyl-phenyl)-benzamide 2-morpholino-5-trifluoromethylphenyl isothi°Cyanate N-(2-morpholin-4-yl-5-trifluoromethyl-phenyl)-acetamideN-(2-morpholin-4-yl-5-trifluoromethyl-phenyl)-acetamide 1,4-dichloro-phthalazine-6-carboxylic acid (2-morpholin-4-yl-5-trifluoromethyl-phenyl)-amide

合成工艺路线路线简述

    📜N-(3-(Trifluoromethyl)Phenyl)Picolinamide置于氧气,Copper(L) Chloride,Sodium Hydroxide体系中,用 乙醇,甲苯 作为反应溶剂,化学反应 15.0H,反应生成 3-氨基-4-(4-吗啉基)三氟甲苯
    参考文献:Copper-Catalyzed Ortho-C(Sp2)-h Amination Of Benzamides And Picolinamides With Alkylamines Using Oxygen As A Green Oxidant
    标题:Copper-Catalyzed Ortho-C(Sp2)-h Amination Of Benzamides And Picolinamides With Alkylamines Using Oxygen As A Green Oxidant
    摘要:一种多功能的铜催化直接对位c(Sp2)-H胺化反应已成功实现,该反应使用苯甲酰胺和吡啶甲酰胺与烷基胺进行.
    DOI:10.1039/d0Ob00784F

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    主要参考文献

    参考标题:Novel Quinolinylaminoisoquinoline Bioisosteres Of Sorafenib As Selective Raf1 Kinase Inhibitors: Design, Synthesis, And Antiproliferative Activity Against Melanoma Cell Line
    作者:Hye Jung Cho,Mohammed Ibrahim El-Gamal,Chang-Hyun Oh,So Ha Lee,Taebo Sim,Garam Kim,Hong Seok Choi,Jung Hoon Choi,Kyung Ho Yoo
    摘要:Design And Synthesis Of A New Series Of Quinolinylaminoisoquinoline Derivatives As Conformationally Restricted Bioisosteres Of Sorafenib Are Described. Their In Vitro Antiproliferative Activity Against A375P Melanoma Cell Line Was Tested. Compounds 1B, 1D, 1G, And 1J Showed The Highest Potency Against A375P Cell Line With Ic50 Values In Sub-Micromolar Scale. In Addition, Compound 1D Exerted High Selectivity Towards Raf1 Serine/threonine Kinase With 96.47% Inhibition At 10 µm, And Ic50 Of 0.96 µm. This Compound Can Possess Antiproliferative Activity Against Melanoma Cells Through Inhibition Of Raf1 Kinase.

    合成参考文献


    参考文献:10.1016/j.bbrc.2023.08.050
    摘要:Ikeda Y, Davis MI, Sumita K, Zheng Y, Kofuji S, Sasaki M, Hirota Y, Pragani R, Shen M, Boxer MB, Takeuchi K, Senda T, Simeonov A, Sasaki AT. Multimodal action of KRP203 on phosphoinositide kinases in vitro and in cells. Biochemical and Biophysical Research Communications. 2023 Oct;679():116–21. doi: 10.1016/j.bbrc.2023.08.050.
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