反应详情

温度

180 °C

A mixture of 2-fluoro-4-methanesulfonyl-phenol (Intermediate 1; 93 mg, 0.49 mmol), 4-chloro-1-[4-(3-isopropyl-[1,2,4]oxadiazol-5-yl)-trans-cyclohexyl]-1H-pyrazolo[3,4-d]pyrimidine (Intermediate 26; 170 mg, 0.49 mmol) and potassium carbonate (81 mg, 0.59 mmol) in anhydrous DMF (5 mL) was heated in a microwave at 180° C. for 10 min. The mixture was filtered. The filtrate was concentrated and purified using a Supelco 23 g column, eluting with 0-3% methanol/dichloromethane to give 4-(2-fluoro-4-methanesulfonyl-phenoxy)-1-[4-(3-isopropyl-[1,2,4]oxadiazol-5-yl)-trans-cyclohexyl]-1H-pyrazolo[3,4-d]pyrimidine (153 mg, 62%).

1. filtrationThe mixture was filtered
2. concentrationThe filtrate was concentrated
3. custompurified
4. washeluting with 0-3% methanol/dichloromethane