反应详情

To a solution of 1-(6-methylpyrimidin-4-yl)piperidin-4-one (see example 93b, 100 mg, 0.523 mmol) and 8-(3,4-difluorophenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine (129 mg, 0.523 mmol) in AcOH was added dropwise trimethylsilyl cyanide (196 μL, 1.57 mmol) and the resulting mixture stirred at room temperature for 88 hours. The mixture was then poured onto NaOH (6 M, 6 mL) and stirred for 10 minutes. The precipitate was then filtered off and dried. Purification by chromatography (silica gel, 20 g, 30 to 100% ethyl acetate in heptane) afforded the title compound (20 mg, 9%) as a yellow solid. MS ISP (m/e): 447.4 [(M+H)+].

1. additionThe mixture was then poured onto NaOH (6 M, 6 mL)
2. stirringstirred for 10 minutes
3. filtrationThe precipitate was then filtered off
4. customdried
5. customPurification by chromatography (silica gel, 20 g, 30 to 100% ethyl acetate in heptane)