反应详情

温度

150 °C

A solution of N-(3,3-difluoropiperidin-4-yl)-8-(2,3,4-trifluorophenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine (75 mg, 196 μmol), 4-chloro-6-methylpyrimidine (27.7 mg, 215 μmol) and N,N-diisopropylethylamine (37.9 mg, 49.9 μL, 293 μmol) in dioxane (4 mL) was heated to 150° C. in the microwave for 1 hour. Further 4-chloro-6-methylpyrimidine (27.7 mg, 215 μmol) and N,N-diisopropylethylamine (37.9 mg, 49.9 μL, 293 μmol) were added and heated to 150° C. in the microwave for another hour. Further 4-chloro-6-methylpyrimidine (27.7 mg, 215 μmol) and N,N-diisopropylethylamine (37.9 mg, 49.9 μL, 293 μmol) were added and heated to 110° C. for 12 hours. The crude material was directly purified by flash chromatography (silica gel, 70 g, 0% to 15% MeOH/NH4OH (9:1) in dichloromethane). The title compound was obtained as light yellow foam (25 mg, 22%). MS ISP (m/e): 476.1 (100) [(M+H)+].

1. temperatureheated to 110° C. for 12 hours
2. customThe crude material was directly purified by flash chromatography (silica gel, 70 g, 0% to 15% MeOH/NH4OH (9:1) in dichloromethane)