邻氨基三氟甲苯置于盐酸,Sodium Nitrite,Sodium Hydrogensulfite体系中,用 水 用作溶剂,化学反应 3.5H,反应生成2-(三氟甲基)苯肼盐酸盐
参考文献:Design,Synthesis And Pharmacological Evaluation Of 6,7-Disubstituted-4-Phenoxyquinoline Derivatives As Potential Antitumor Agents
标题:Design,Synthesis And Pharmacological Evaluation Of 6,7-Disubstituted-4-Phenoxyquinoline Derivatives As Potential Antitumor Agents
摘要:Two Series Of 6,7-Disubstituted-4-Phenoxyquinoline Derivatives Bearing 2,4-Imidazolinedione/pyrazolone Scaffold Were Designed,Synthesized And Evaluated For Their C-Met Kinase Inhibition And Cytotoxicity Against Ht-29,H460,A549,Mkn-45,And U87Mg Cancer Cell Lines In Vitro. The Pharmacological Data Indicated That Most Of The Tested Compounds Showed Moderate To Significant Cytotoxicity And High Selectivity Against Ht-29,H460 And A549 Cancer Cell Lines As Compared With Foretinib. The Sar Analyses Indicated That Compounds With Halogen Groups,Especially Trifluoromethyl Groups At 2-Position On The Phenyl Ring (Moiety B) Were More Effective. In This Study,A Promising Compound 17 (C-Met Ic50 = 2.20 Nm,A Multi-Target Tyrosine Kinase Inhibitor) Showed The Most Potent Antitumor Activities With Ic50 Values Of 0.14 Mu M,0.18 Mu M,0.09 Mu M,0.03 Mu M,And 1.06 Mu M Against Ht-29,H460,A549,Mkn-45,And U87Mg Cell Lines,Respectively. (C) 2014 Elsevier Inc. All Rights Reserved.
Doi:10.1016/j.Bioorg.2014.07.011