反应详情

温度

0 °C

A mixture of 3-(5-morpholin-4-ylmethyl-1H-benzimidazol-2-yl)-1H-pyrazol-4-ylamine (70 mg, 0.23 mmol), morpholine-4-carbonyl chloride (80 μl, 0.7 mmol) and diisopropylethylamine (170 μl, 0.92 mmol) in THF (2 ml) was stirred at 0° C. and then allowed to warm to room temperature over 16 h. The reaction was quenched by the addition of conc. aq. NH3 and then concentrated in vacuo. The residue was purified through preparative LC/MS to give 4-morpholinyl-N-[3-(5-morpholin-4-ylmethyl-1H-benzimidazol-2-yl)-1-H-pyrazol-4-yl]-urea as a white solid (35 mg). (LC/MS (basic method): Rt 2.28 min, [M−H+]− 415).

1. temperatureto warm to room temperature over 16 h
2. customThe reaction was quenched by the addition of conc. aq. NH3
3. concentrationconcentrated in vacuo
4. customThe residue was purified through preparative LC/MS