Novel method for preparing N-phenyl-3-morpholine propanamide
A technology of phenylpropionamide and methylthiopropionamide, applied in the field of preparation of N-phenyl-3-morpholine propionamide, which can solve the problems of low yield, low synthetic application value, long reaction time, etc.
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specific Embodiment 1
[0015] In a 100mL round bottom flask, N-phenyl-3-methylthiopropionamide (10mmol, 1.95g), morpholine (20mmol, 1.74g), 1-chloromethyl-4-fluoro-1,4 -Diazabicyclo[2.2.2]octane bis(tetrafluoroborate) salt (10mmol, 1.78g), sodium carbonate (10mmol, 1.06g) and 20mL of 1,4-dioxane, the reaction temperature was controlled at 100 degrees Celsius, and vigorously stirred for 12 hours. After the reaction, it was cooled to room temperature, and the reaction solution was concentrated and separated by column chromatography in sequence to obtain N-phenyl-3-morpholine propionamide (1.87 g, 80%).
[0016] The equations involved in the reaction are as follows:
[0017]
specific Embodiment 2
[0018] In a 100mL round bottom flask, N-phenyl-3-methylthiopropionamide (10mmol, 1.95g), morpholine (20mmol, 1.74g), 1-chloromethyl-4-fluoro-1,4 -Diazabicyclo[2.2.2]octane bis(tetrafluoroborate) salt (10mmol, 1.78g), sodium carbonate (10mmol, 1.06g) and 20mL of 1,4-dioxane, the reaction temperature was controlled at 80 degrees Celsius, and vigorously stirred for 12 hours. After the reaction, it was cooled to room temperature, and the reaction solution was concentrated and separated by column chromatography in sequence to obtain N-phenyl-3-morpholine propionamide (1.52 g, 65%).
[0019] The equations involved in the reaction are as follows:
[0020]
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