反应详情

To a stirred solution of bis(trichloromethyl) carbonate (0.353 mmol, 105 mg) in dichloromethane (10 mL) was added a solution of 3-((4-(4-amino-3,5-difluorobenzoyl)piperazin-1-yl)methyl)-N-tert-butylbenzamide (0.929 mmol. 400 mg) and N-ethyl-N-iosopropylpropan-2-amine (0.3 mL) in dichloromethane (10 mL) (dropwise). After 2 hours stirring, a solution of cyclopropylmethylamine (1.022 mmol, 0.089 mL, 72.7 mg) and N-ethyl-N-isopropylpropan-2-amine (0.222 mL) in dichloromethane (10 mL) was added. The reaction mixture was stirred for 24 hours. Chromatography on silica (eluting with dichloromethane then dichloromethane/methanol (1% to 5%)) gave the title compound (220 mg). MS (ESI) m/z 528.3 [M+H]+

1. stirringThe reaction mixture was stirred for 24 hours
2. washChromatography on silica (eluting with dichloromethane