4-三氟甲基烟酸的合成

Synthesis of 4-(Trifluoromethyl)nicotinic Acid

4-三氟甲基烟酸是高效杀虫剂氟啶虫酰胺的重要中间体。以三氟乙酰乙酸乙酯和氰基乙酰胺为原料,经环合、氯代、氢化还原、水解反应得到目标产物。经优化反应条件,以三氟乙酰乙酸乙酯计4-三氟甲基烟酸的总收率达到38.6%。该路线原料易得、收率高,适合工业化生产。

4-（Trifluoromethyl）nicotinic acid was an important intermediate for the preparation of flonicamid. With ethyl 4,4,4-trifluoroacetoacetate and cyanoacetamide as starting materials, the desired product was prepared via optimized cyclization, chlorination, hydrogenolysis, hydrolysis. The total yield was 38.6%based on ethyl 4,4,4-trifluoroacetoacetate. The method benefited from readily available materials, satisfactory yield, and was suitable for industrial production.