反应详情

温度

120 °C

To a solution of (1R,2S)-2-(3-iodo-1H-indazol-spiro[cyclopropane-1,3′-indolin]-2′-one (50 mg, 0.12 mmol) in DMF (0.4 mL) and water (0.1 mL) was added (E)-3-(2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)vinyl)pyridine (50 mg, 0.2 mmol) potassium fluoride (14 mg, 0.24 mmol) and Pd(PPh3)4 (7 mg, 0.006 mmol). The mixture was heated to 120° C. for 2 h under microwave irradiation. Ethyl acetate (50 mL) was added and the solution was washed with water (2×5 mL), brine (5 mL) and dried over MgSO4. Purification by reverse phase preparatory HPLC gave the title compound as a yellow solid (20 mg, 44%).

1. washthe solution was washed with water (2×5 mL), brine (5 mL)
2. dry with materialdried over MgSO4
3. customPurification by reverse phase preparatory HPLC