反应详情

To a DMF 3 mL solution of 2-{[(tert-butoxycarbonyl)amino]methyl}-3H-imidazo[4,5-b]pyridine-6-carboxylic acid (293 mg, 1.0 mmol) were added HOBt (162 mg, 1.2 mmol), 2,2,2-trifluoroethanamine (130 mg, 1.5 mmol), DIPEA (388 mg, 3.0 mmol) and EDC (288 mg, 1.5 mmol). The reaction mixture was stirred at room temperature overnight and was partitioned between EtOAc and water. The organic layer was washed with brine twice, dried over anhydrous Na2SO4, and concentrated under reduced pressure. The residue was purified by prep TLC (MeOH/CH2Cl2=1/10, v/v) to give the title compound (0.26 g, 70%).

1. customwas partitioned between EtOAc and water
2. washThe organic layer was washed with brine twice
3. dry with materialdried over anhydrous Na2SO4
4. concentrationconcentrated under reduced pressure
5. customThe residue was purified by prep TLC (MeOH/CH2Cl2=1/10