反应详情

To a solution of 2-[3-Methylcarbamoyl-1-(tetrahydro-pyran-2-yl)-1H-indazol-6-ylamino]-benzoic acid (150 mg, 0.381 mmol) in DMF (3.6 mL) was added propargylamine (0.052 mL, 0.761 mmol), triethylamine(TEA) (0.264 mL, 1.90 mmol), and HATU (217 mg, 0.571 mmol). The reaction was stirred for 4 hours, and then diluted with EtOAc (30 mL) and water (30 mL). The layers were separated, and the aqueous was extracted with EtOAc (2×20 mL). The combined organics were washed with saturated NaCl (15 mL) and then dried over Na2SO4. The solids were removed by filtration, and the liquid was concentrated by rotary evaporation to a yellow oil (164 mg, 100%).

1. customThe layers were separated
2. extractionthe aqueous was extracted with EtOAc (2×20 mL)
3. washThe combined organics were washed with saturated NaCl (15 mL)
4. dry with materialdried over Na2SO4
5. customThe solids were removed by filtration
6. concentrationthe liquid was concentrated by rotary evaporation to a yellow oil (164 mg, 100%)