CAS: 101712-20-3; 2,6-Difluorophenylacetone

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CAS号437-81-0 2,6-二氟苯甲醛 | CAS号108-22-5 醋酸异丙烯酯 | CAS号5509-65-9 2,6-二氟苯胺

📜2,6-二氟苯甲醛置于乙酸铵,盐酸,三氯化铁,铁粉体系中,用 水 用作溶剂,化学反应生成2,6-双氟苯基丙酮
参考文献:Antimalarial Drugs. 60. Synthesis,Antimalarial Activity,And Quantitative Structure-Activity Relationships Of Tebuquine And A Series Of Related 5-[(7-Chloro-4-Quinolinyl)Amino]-3-[(Alkylamino)Methyl][1,1'-Biphenyl]-2-Ols And N.Omega.-Oxides
标题:Antimalarial Drugs. 60. Synthesis,Antimalarial Activity,And Quantitative Structure-Activity Relationships Of Tebuquine And A Series Of Related 5-[(7-Chloro-4-Quinolinyl)Amino]-3-[(Alkylamino)Methyl][1,1'-Biphenyl]-2-Ols And N.Omega.-Oxides
摘要:A Series Of 5-[(7-Chloro-4-Quinolinyl)Amino]-3-[(Alkylamino)Methyl] [1,1'-Biphenyl]-2-Ols And N Omega-Oxides Was Prepared From The Substituted 1-Phenyl-2-Propanones Proceeding Through The 5-Nitro[1,1'-Biphenyl]-2-Ols,The Corresponding Amino,And Acetamido Derivatives To The N-[5-[(Alkylamino)Methyl]-6-Hydroxy[1,1'-Biphenyl]-3-Yl]Acetamides And Final Condensation With 4,7-Dichloroquinoline Or The N-Oxide. In A Quantitative Structure-Activity Relationship Study First Run On 28 And Later Expanded To 40 Substituted Phenyl Analogues And Their N Omega-Oxides,Increasing Antimalarial Potency Vs. Plasmodium Berghei In Mice Was Found To Be Correlated With Decreasing Size (Sigma Mr) And Electron Donation (Sigma Sigma) Of The Phenyl Ring Substituents. A Significant Correlation With N Omega-Oxidation Could Not Be Demonstrated. Initial High Activity Against P. Berghei Infections In Mice Led To Expanded Studies That Demonstrated In Addition Excellent Activity Against Resistant Strains Of Parasite,Activity In Primate Models,And Pharmacokinetic Properties Apparently Allowing Protection Against Infection For Extended Periods Of Time Even After Oral Administration. Such Properties Encourage The Clinical Trial Of A Member Of This Class In Man.
Doi:10.1021/jm00156A009