反应详情

To a solution of 5-(2,4-dichloro-5-(pyridin-2-yl)benzamido)-1-phenyl-1H-pyrazole-3-carboxylic acid (Example 111, 150 mg, 0.33 mmol) and 1-amino-2-methylpropan-2-ol (50 mg, 0.66 mmol) in DMF (2 mL) was added DIPEA (0.11 mL, 0.66 mmol, 2 eq) and HATU (188 mg, 0.50 mmol). The reaction was stirred at room temperature for 18 hours. The reaction was partitioned between saturated aqueous sodium carbonate solution (50 mL) and EtOAc (50 mL). The organic layer was collected, washed with brine, dried over magnesium sulphate and concentrated in vacuo. The residue was triturated with acetonitrile to afford the title compound (63 mg, 36%).

1. customThe reaction was partitioned between saturated aqueous sodium carbonate solution (50 mL) and EtOAc (50 mL)
2. customThe organic layer was collected
3. washwashed with brine
4. dry with materialdried over magnesium sulphate
5. concentrationconcentrated in vacuo
6. customThe residue was triturated with acetonitrile