反応 #287

ord-f3dd88e6019442749a56a95e7a33ac6e

反応方程式

COc1ccc(Br)cc1[N+](=O)[O-]
COc1ccc(Br)cc1[N+](=
CC(=O)N1CCNCC1
CC(=O)N1CCNCC1
COc1ccc(N2CCN(C(C)=O)CC2)cc1[N+](=O)[O-]
COc1ccc(N2CCN(C(C)=O
収率 77.5%

溶媒

反応条件

温度
120°CELSIUS

実験手順

diacetoxypalladium (0.116 g, 0.52 mmol) was added to a stirred mixture of 4-bromo-1-methoxy-2-nitrobenzene (1.5 g, 6.46 mmol), 1-(piperazin-1-yl)ethanone (0.829 g, 6.46 mmol) and (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (0.449 g, 0.78 mmol) and cesium carbonate (4.21 g, 12.93 mmol) dissolved in dioxane (10 mL) , degased and under argon. The resulting suspension was stirred at 120 °C for 2 hours.At 25°C, the mixture was filtered and evaporated under reduce pressure.The mixture was adsorbed on silica gel.The crude product was purified by flash chromatography on silica gel eluting with 1 to 5% methanol in ethyle acetate. The solvent was evaporated to dryness to afford 1-(4-(4-methoxy-3-nitrophenyl)piperazin-1-yl)ethanone (1.400 g, 78 %) as a orange solid.

出典

750 AstraZeneca ELN dataset