反应详情

Triethylamine (0.073 mL) was added to a mixture of 5-(1H-pyrazolo[3,4-b]pyridin-3-yl)-1H-pyrrole-3-carboxylic acid (100 mg, 0.44 mmol) (from Example 12) and 4-(2-aminoethyl)morpholine (62.8 mg, 1.1 eq.) (Aldrich, Milwaukee, Wis.) in acetonitrile (1 mL) and DMF (1 mL). The mixture was cooled in an ice bath and to it was added diethyl cyanophosphonate (86 mg, 1.2 eq.). The mixture was allowed to warm up slowly to room temperature and stirred for overnight. The reaction was diluted with DCM, washed with NaHCO3 and water, dried and concentrated. The residue was purified on a silica gel column to give the titled compound.

1. temperatureThe mixture was cooled in an ice bath and to it
2. washwashed with NaHCO3 and water
3. customdried
4. concentrationconcentrated
5. customThe residue was purified on a silica gel column