反应详情

To N-methyl-N-phenyl-6-(5-trichloromethyl-[1,2,4]oxadiazol-3-yl)-[1,3,5]triazine-2,4-diamine (prepared in an analogous manner to Intermediate 60, 63 mg, 0.16 mmol) was added 3-(4-fluoro-phenyl)-azetidine hydrochloride (Intermediate 122, 39 mg, 0.19 mmol). Disiopropylethylamine (42 μL) and dioxane (1 mL) were added and the mixture heated at 70 C for 4 h. The mixture was diluted with 1 M citric acid to give a precipitate which was filtered. The pad was washed with a 1 M aq. solution of sodium bicarbonate (2 mL), water (2 mL) and then the solid was slurried in MeOH (2 mL) to give the title compound (48 mg, 65%).

1. temperaturethe mixture heated at 70 C for 4 h
2. customto give a precipitate which
3. filtrationwas filtered
4. washThe pad was washed with a 1 M aq. solution of sodium bicarbonate (2 mL), water (2 mL)