反应详情

温度

85 °C

To a solution of 3-(7-bromo-1-methyl-2,4-dioxo-6-(3-(trifluoromethoxy)phenyl)-1H-pyrrolo[3,2-d]pyrimidin-3(2H,4H,5H)-yl)propyl acetate (See Compound 36, Step 1, 25 mg, 0.050 mmol) in DMF (1 mL) was added CH3I (14.1 mg, 0.10 mmol) followed by K2CO3 (20.6 mg, 0.15 mmol). The reaction was heated at 85° C. for 1.5 h, cooled to RT then diluted with EA (10 mL) and brine (5 mL). The organic layer was washed with aq. 1N LiCl (3×20 mL), dried over Na2SO4 and concentrated to give 3-(7-bromo-1,5-dimethyl-2,4-dioxo-6-(3-(trifluoromethoxy)phenyl)-1H-pyrrolo[3,2-d]pyrimidin-3(2H,4H,5H)-yl)propyl acetate (25 mg, 97.3% yield) as an oil. LCMS: MH+ 518 and TR=1.877 min. Used without further purification.

1. temperaturecooled to RT
2. washThe organic layer was washed with aq. 1N LiCl (3×20 mL)
3. dry with materialdried over Na2SO4
4. concentrationconcentrated