反应详情

8-amino-2-(3-(trifluoromethyl)phenyl)-4H-chromen-4-one (178) (70 mg, 0.23 mmol) was taken up in 2 mL of DMF along with thiazole-4-carboxylic acid 3 (30 mg, 0.23 mmol), HATU (175 mg, 0.46 mmol) and DIEA (80 μL, 0.46 mmol). The reaction mixture was stirred at room temperature for 18 h. It was then diluted with 5 mL of H2O. The resulting solids were collected by filtration, washed successively with a solution of dilute NaHCO3/MeOH (1:1), aqueous MeOH, dilute 1 N HCl/MeOH (1:1), aqueous MeOH, and then pure MeOH. After drying under high vacuum, 28 mg of Compound 204 was obtained as an off-white solid. MS (ESI) calcd for C20H11F3N2O3S: 416.04. found: 417 [M+H].

1. filtrationThe resulting solids were collected by filtration
2. washwashed successively with a solution of dilute NaHCO3/MeOH (1:1), aqueous MeOH
3. additiondilute 1 N HCl/MeOH (1:1), aqueous MeOH
4. customAfter drying under high vacuum