反应详情

温度

80 °C

A mixture of 3-(5-morpholin-4-ylmethyl-1H-benzimidazol-2-yl)-1H-pyrazol-4-ylamine (50 mg, 0.16 mmol), 2,4 difluorophenyl isocyanate (26 mg, 0.16 mmol) and Et3N (0.024 ml) suspended in a mixture of toluene (2 ml) and IPA (1 ml) was stirred at 80° C. for 1 h and then diluted with EtOAc. The reaction mixture was washed with water then brine, organics dried (MgSO4) and reduced in vacuo The residue was purified by flash column chromatography [SiO2, CH2Cl2-MeOH (90:10)] to give 1-(2,6-Difluorophenyl)-N-[3-(5-morpholin-4-ylmethyl-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]-urea (AT7787) as a colourless solid (30 mg, 39%). (LC/MS (acidic method): Rt 1.80, [M+H]+ 454).

1. washThe reaction mixture was washed with water
2. dry with materialbrine, organics dried (MgSO4)
3. customwas purified by flash column chromatography [SiO2, CH2Cl2-MeOH (90:10)]