Study On Synthesis Of 4-trifluoromethylnicotinic Acid And Its Derivatives

4-trifluoromethylnicotinic acid is useful as an active ingredient for agricultural chemicals and as a precursor for production of agricultural chemicals or pharmaceuticals. In addition, nicotinamide compounds derived from 4-trifluoromethylnicotinic acid are useful as active ingredients for pesticides. They are more effective against pests and thus able to protect fish, shellfish and domestic animals from the harmfulness of pesticide, which overcome the hard problem of the resistance of pests to other pesticide. Therefore, research on synthesis of 4-trifluoromethylnicotinic acid and its derivatives is of great practical value.According to the reference and mechanism analysis, several possible synthesis methods were designed in this dissertation. After a full evaluation, a best synthetic route was determined. Starting from ethyl vinyl ether and trifluoroacetic anhydride, pulling the trifluoromethyl in the chain, then through amination, condensation reaction, ring closure and hydrolysis,4-trifluoromethylnicotinic acid was obtained. On this basis, its two derivatives 4-(trifluoromethyl)nicotinamide and N-benzyl-4-trifluoromethyl-3-pyridine carboxamide were also synthesized.Each step was optimized during Synthesis processes and single factor experiments were carried out to determine the most effective conditions such as solvent, time, material ratio and so on. Finally, the prospect of the application and further research of 4-trifluoromethyl nicotinic acid was given.Each intermediate was characterized by the melting point determination, IR, MS, NMR. The results showed that they were in line with the target products, which verified the route of synthesis of 4-trifluoromethylnicotinic acid to be efficient.