反应详情

温度

80 °C

A mixture of: 4-(6-amino-4-chloro-pyrazolo[3,4-d]pyrimidin-1-yl)-piperidine-1-carboxylic acid tert-butyl ester (Intermediate 33; 224 mg, 0.64 mmol), 2-hydroxybenzonitrile (available from Alfa Aesar, Ward Hill, Mass., USA; 95.2 mg, 0.8 mmol), and potassium carbonate (220 mg, 1.6 mmol) in N,N-dimethylformamide (5 mL) was heated at 80° C. for 3 h, and then cooled. Volatiles were evaporated and the residue was chromatographed (50-65% ethyl acetate/hexanes) to give 4-[6-Amino-4-(2-cyano-phenoxy)-pyrazolo[3,4-d]pyrimidin-1-yl]-piperidine-1-carboxylic acid tert-butyl ester (261 mg, 94%) as a white solid.

1. temperaturecooled
2. customVolatiles were evaporated
3. customthe residue was chromatographed (50-65% ethyl acetate/hexanes)