CAS: 1247859-37-5; 1-((3-Fluorophenyl)Carbamoyl)Cyclopropane-1-Carboxylic Acid

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meta-fluoroaniline 1-(chlor°Carbonyl)cyclopropane-1-carboxylic acid cyclopropane-1,1-dicarboxylic acid dimethyl 1,1-cyclopropanedicarboxylate N-(3-fluoro-4-((2-((3-((methylsulfonyl)methyl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)-N'-(3-fluorophenyl)cyclopropane-1,1-dicarboxamide

📜1,1-环丙基二羧酸置于三乙胺体系中,用 四氢呋喃 用作溶剂,化学反应 2.5H,反应生成卡博替尼杂质46
参考文献:Discovery Of Anilinopyrimidines As Dual Inhibitors Of C-Met And Vegfr-2: Synthesis,Sar,And Cellular Activity
标题:Discovery Of Anilinopyrimidines As Dual Inhibitors Of C-Met And Vegfr-2: Synthesis,Sar,And Cellular Activity
摘要:Both C-Met And Vegfr-2 Are Important Targets For Cancer Therapies. Here We Report A Series Of Potent Dual C-Met And Vegfr-2 Inhibitors Bearing An Anilinopyrimidine Scaffold. Two Novel Synthetic Protocols Were Employed For Rapid Analoguing Of The Designed Molecules For Structure Activity Relationship (Sar) Exploration. Some Analogues Displayed Nanomolar Potency Against C-Met And Vegfr-2 At Enzymatic Level. Privileged Compounds 3A,3B,3G,3H,And 18A Exhibited Potent Antiproliferative Effect Against C-Met Addictive Cell Lines With Ic50 Values Ranged From 0.33 To 1.7 Mu M. In Addition,A Cocrystal Structure Of C-Met In Complex With 3H Has Been Determined,Which Reveals The Binding Mode Of C-Met To Its Inhibitor And Helps To Interpret The Sar Of The Analogues.
Doi:10.1021/ml500066M