反应详情

温度

165 °C

To a microwave vial was added (S)-1-(5-fluoropyrimidin-2-yl)ethanamine hydrochloride (Method 7, 155 mg, 0.77 mmol), 5-bromo-2-chloro-N-(5-methoxy-1H-pyrazol-3-yl)pyrimidin-4-amine (Method 39, 180 mg, 0.59 mmol), and DIEA (181 mg, 1.48 mmol). Anhydrous n-BuOH (2.5 mL) was added, and the vial was heated in microwave oven at 165° C. for 5 hours. The reaction mixture was concentrated. The resulting residue was separated by silica gel column to afford desired product (80 mg, 33%). LC-MS, 409 (M+1). 1H NMR δ 12.03 (s, 1H), 9.38 (s, 1H), 8.82 (s, 2H), 7.97-8.12 (m, 2H), 5.60 (s, 1H), 5.13 (s, 1H), 3.75 (m, 3H), 1.49 (m, 3H).

1. concentrationThe reaction mixture was concentrated
2. customThe resulting residue was separated by silica gel column