Rapid Synthesis of 5-(trifluoromethyl)pyridin-2-amine and 2-((5-(trifluoromethyl)pyridin-2-yl)oxy)ethan-1-ol by Microwave Heating
5-Trifluoromethylpyridine-2-amine and 2-((5-trifluoromethylpyridine-2-yl)oxy)ethanol were synthesized by C-N and C-O coupling reactions under microwave heating,respectively.The influence of reaction substrate,reaction time,reaction temperature and alkali on the reaction yield were discussed.The compounds were characterized by 1 H-NMR spectroscopy.The results showed that the optimum reaction conditions for the synthesis of 5-trifluoromethylpyridine 2-amine were as follows:coupling reaction of 2-bromo-5-trifluoromethylpyridine with ammonia in ethylene glycol in the presence of cuprous iodide as a catalyst occurred at 110℃for 30 min.The optimum reaction conditions for the synthesis of 2-((5-trifluoromethylpyridine-2-yl)oxy)ethanol were as follows:coupling reaction of 2-bromo-5-trifluoromethylpyridine with ethylene glycol in the presence of cuprous iodide as a catalyst and potassium phosphate as a base occurred at 130℃for 20 min.Under the optimal reaction conditions,5-trifluoromethylpyridine-2-amine and 2-((5-trifluoromethylpyridine-2-yl)oxy)ethanol were obtained in 83%and 87%yield,respectively.
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