反应详情

温度

80 °C

To a solution of 4-amino-2-fluoro-5-nitrobenzonitrile (132 mg, 0.730 mmol) and tert-butyl piperazine-1-carboxylate (136 mg, 0.730 mmol) in DMF (3 ml) was added triethylamine (0.102 ml, 0.730 mmol). The mixture was heated to 80° C. in a Microwave reactor for 50 min., cooled to r.t., purified by prep-HPLC to afford tert-butyl 4-(5-amino-2-cyano-4-nitrophenyl)piperazine-1-carboxylate (120 mg, 0.328 mmol, 44.9% yield). 1H-NMR (CD3OD, 500 MHz): δ 8.42 (1H, s), 6.45 (1H, s), 3.65-3.61 (4H, m), 3.28-3.25 (4H, m), 1.51 (9H, s). m/e (M+H): 348.3.

1. temperaturecooled to r.t.
2. custompurified by prep-HPLC