反应详情

A mixture of 6-bromo-4-hydroxy-3-(pyrimidin-5-ylmethyl)quinolin-2(1H)-one (0.5 g, 1.51 mmol, Intermediate 49: step a) methyl 2-chloro-2,2-difluoroacetate (0.24 mL, 2.26 mmol) and K2CO3 (0.52 mg, 3.76 mmol) in DMF (0.6 mL) was stirred at 80° C. for 2 hours, cooled to room temperature, diluted with H2O and extracted with EtOAc (2×). The combined organic extracts were washed with brine, dried, filtered, evaporated in-vacuo and purified by chromatography (0-10% MeOH in DCM, gradient) to provide the title compound.

1. extractionextracted with EtOAc (2×)
2. washThe combined organic extracts were washed with brine
3. customdried
4. filtrationfiltered
5. customevaporated in-vacuo
6. custompurified by chromatography (0-10% MeOH in DCM, gradient)