反应详情

Crude 6-(3-methoxy-phenyl)-7-pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-3-ol (120 mg, 0.369 mmol) was dissolved in dry dimethoxyethane (2 mL) under nitrogen. Trifluoroacetic anhydride (0.200 mL, 1.416 mmol, 3.8 eq) and triethylamine (0.100 mL, 0.718 mmol, 2 eq) were added and the mixture was stirred at room temperature for 20 hours. The solution was then diluted with ethyl acetate and washed with saturated aqueous NaHCO3 and brine, dried and evaporated to dryness. The crude product was purified by chromatography on silica gel (eluant: DCM/MeOH 97:3) to give 69 mg (61%) of 6-(3-methoxy-phenyl)-7-pyridin-4-yl-pyrazolo[5,1-b]thiazole as white solid.

1. washwashed with saturated aqueous NaHCO3 and brine
2. customdried
3. customevaporated to dryness
4. customThe crude product was purified by chromatography on silica gel (eluant: DCM/MeOH 97:3)