Synthesis Of5-trifluoromethyl-3-(4-methyl-1H-imidazol-1-yl)-aniline

Objective5-trifluoromethyl-3-(4-methyl-1H-imidazol-1-yl)aniline is one of theimportant imtermediates for the synthesis of Nilotinib,which is a new type oftargeting anticancer drugs. Research a new simple route with higheryield,through studying the various experimental factors.This way can provide abasic research for industrial production of the target compound.It also willprovide a basic research for industrial production of Nilotinib.MethodsAccording to the reports of the Synthesis of5-trifluoromethyl-3-(4-methyl-1H-imidazol-1-yl)-aniline, I will explore the synthesis cfafts. Thefluorination started with3,5-dinitrobenzotrifluoride, then the mono fluorosubstituted intermediate and4-methyl-1H-imidazole was heated with microwaveradiation. After the substitution, the materials converted into5-trifluoro-methyl-3-(4-methyl-1H-imidazol-1-yl)nitro-benzen. Then the hydrogenationconverted the nitro group into amino group with palladium on activated carbon.The target compound was5-trifluoromethyl-3-(4-methyl-1H-imidazol-1-yl)-aniline.And optimize the reaction conditions of each step to improve the yield oftarget compounds and simplify the experimental operation,so we can get the best way. The last their molecular structures were confirmed by1H NMR andMS,and the target compound’s purity were demonstrated by HPLC.ResultsAnalys and investigate the influencing factors of the reactions,adjustingthe reaction conditions can simplify the operations of the reactions,and the yieldwas higher than before.It is easy to get the raw materials and the operations aresimple.The structures of the compounds were right by analysis.ConclusionsAs raw material3-fluoro-5-nitro-1-trifluoromethylbenzene was substitutedby fluoro and imidazolyl,then was reduced to5-trifluoromethyl-3-(4-methyl-1H-imidazol-1-yl)aniline.This method was right,and optimize the reactionconditions,the structures were ri confirmed by NMR and mass spectrometry.