反应详情

温度

20 °C

To a suspension of tert-butyl 4-(2-(5-amino-6-cyano-4-(methylamino)-5′-(trifluoromethyl)-2,3′-bipyridin-6′-yloxy)ethyl)piperidine-1-carboxylate (5.20 g) in water (40 ml) and 1,4-dioxane (40 ml) was added 2N hydrichloric acid (6.89 ml) at 0° C. To above suspension was then added dropwise sodium nitrite (0.92 g) in water (10 ml). The mixture was then stirred at 0° C. for 10 min and at 20° C. for 16 h. The solid product was collected by filtration and washed with water, dried in vacuum oven to give 4.61 g tert-butyl 4-(2-(5-(4-cyano-1-methyl-1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl)-3-(trifluoro-methyl)pyridin-2-yloxy)ethyl)piperidine-1-carboxylate (94%).

1. filtrationThe solid product was collected by filtration
2. washwashed with water
3. customdried in vacuum oven