Реакция #144
ord-56a1dc90e93f4e37a4c4dceba5d45c4e
Уравнение реакции
COc1ccc(Br)cc1[N+](=
CC(=O)N1CCNCC1
→
COc1ccc(N2CCN(C(C)=O
Выход 1.2%
Растворители
Условия реакции
Температура
120°CELSIUS
Методика
4-bromo-1-methoxy-2-nitrobenzene (1.5 g, 6.46 mmol), 1-(piperazin-1-yl)ethanone (0.829 g, 6.46 mmol), CESIUM CARBONATE (4.21 g, 12.93 mmol), XANTPHOS (0.449 g, 0.78 mmol) and PdOAc2 (0.116 g, 0.52 mmol) were suspended in dioxane (20 ml) and sealed into a microwave tube. The reaction was heated to 120 °C for 90 minutes in the microwave reactor and cooled to RT. The reaction mixture was filtered through celite with ethyl acetate (50 mL). The filtrate was evaporated to dryness. The crude product was purified by flash silica chromatography in EtOAc. Pure fractions were evaporated to dryness to afford 1-(4-(4-methoxy-3-nitrophenyl)piperazin-1-yl)ethanone (0.022 g, 1.218 %) as a brown solid.
Источник
750 AstraZeneca ELN dataset