反应详情

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 (150 mg, 0.297 mmol) in dioxane (2 mL) was added 2,4,6-trimethyl-1,3,5,2,4,6-trioxatriborinane (112.0 mg, 0.892 mmol), Cs2CO3 (290.8 mg, 0.892 mmol) and Pd(dppf)Cl2 (20 mg, 0.0274 mmol). The reaction was heated at 150° C. (MW) for 30 min, cooled to RT then diluted with EA (5 mL) and water (5 mL). The organic layer was dried over Na2SO4 and concentrated to give 3-(1,7-dimethyl-2,4-dioxo-6-(3-(trifluoromethoxy) phenyl)-1H-pyrrolo[3,2-d]pyrimidin-3(2H,4H,5H)-yl)propyl acetate (120 mg, 91.8% yield) as a solid. LCMS: MH+ 440 and TR=1.571 min.

1. temperatureThe reaction was heated at 150° C. (MW) for 30 min
2. dry with materialThe organic layer was dried over Na2SO4
3. concentrationconcentrated