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With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; caesium carbonate; In 1,4-dioxane; water; at 100℃;Inert atmosphere;
[00150] A mixture of 4-bromo-1-methylpyridin-2(1H)-one (80 mg, 0.43 mmol), 33(100 mg, 0.43 mmol) and Cs2CO3 (419 mg, 1.29 mmol) in dioxane / H20 (3/1, 8 mL) was added Pd(dppf)C12 (62 mg, 0.085 mmol) at rt under N2. After addition, the mixture was stirred at 100 °C overnight. The mixture was concentrated under reduced pressure. The residue was added ethyl acetate (5 mL) and filtered. The filtrate was dried over anhydrous Na2SO4, filtered, concentrated and purified by preparative TLC with dichloromethane/ methanol 10/1 to afford 34 (90 mg, 98percent) as a grey solid. LC-MS tR = 0.589 mm in 5-95 AB_1.5 mm chromatography (Welch Xtimate MK RP-18e 25-2mm), MS (ESI) m/z 215.9 [M+H].
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