反应详情

(4-Amino-3-chlorophenyl)(4-(4-(2-(tert-butyldimethylsilyloxy)-1,1,1,3,3,3-hexafluoropropan-2-yl)benzyl)piperazin-1-yl)methanone (0.410 mmol, 250 mg) and 4-nitrophenyl carbonochloridate (0.410 mmol, 83 mg) in dichloromethane (1 ml) were combined and heated at reflux for 1 hour. The reaction was allowed to cool to room temperature before the addition of 1-amino-2-methylpropan-2-ol (0.820 mmol, 73.1 mg) and triethylamine (0.410 mmol, 0.057 mL, 41.5 mg). The reaction was stirred at room temperature overnight. The reaction mixture was concentrated under vacuum and the resulting residue was purified by column chromatography (2-5% methanol in dichloromethane) to afford the title compound (190 mg).

1. temperatureheated
2. temperatureat reflux for 1 hour
3. concentrationThe reaction mixture was concentrated under vacuum
4. customthe resulting residue was purified by column chromatography (2-5% methanol in dichloromethane)