反应详情

温度

120 °C

1-Ethyl-3-(4-(4-morpholino-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidin-2-yl)phenyl)urea (d, 0.15 mmol), chloropyrimidine (0.21 mmol) and i-PrN2Et (0.6 mmol) were mixed in DMF (0.6 mL) in a microwave reaction tube. The mixture was heated to 120° C. and stirred for 15 min. After cooling to room temperature, the mixture was diluted with DMF. The resulting mixture was purified by reverse-phase HPLC to give 1-ethyl-3-(4-(4-morpholino-6-(pyrimidin-2-yl)-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidin-2-yl)phenyl)urea (e): 1H NMR (500 MHz, DMSO) δ 8.71 (s, 1H), 8.47 (d, J=4.8, 2H), 8.21 (d, J=8.8, 2H), 7.51 (d, J=8.8, 2H), 6.77 (t, J=2.5, 1H), 6.18 (m, 1H), 4.99 (s, 2H), 4.68 (s, 2H), 3.78 (m, 8H), 3.20-3.15 (m, 2H), 1.26 (t, J=6.9, 3H); LC-MS: m/z=+447 (M+H)+.

1. temperatureAfter cooling to room temperature
2. customThe resulting mixture was purified by reverse-phase HPLC