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With potassium phosphate; tetrakis(triphenylphosphine) palladium(0); In 1,4-dioxane; water; at 80℃;Inert atmosphere;
To a solution of 2-( 1-methyl-i ,2,3 ,6-tetrahydropyridin-4-yl)-4,4,5 ,5 -tetramethyl- 1,3,2- dioxaborolane (1.542 g; 6.912 mmol) in water (4.00 mL) and 1,4 dioxane (20 mL) was added K3P04 (4.40 g; 20.74 mmol), tetrakis(triphenylphosphine)palladium(0) (Pd(PPh3)4) (798.70 mg, 0.69 mmol), 5-bromo-2-methyl-3-nitropyridine (1.50 g; 6.91mmol) under N2. The mixture was stirred at 80°C overnight under N2. The mixture was then poured into water (20 mL) and extracted three times with EtOAc (30 mL). The organic layer was washed with water (15 mL) and then brine (15 mL), dried over Na2SO4, filtered and the solvent was evaporated under vacuum. The residue was purified by flash column chromatography over silica gel (Mobile phase: petroleumether/EtOAc Gradient from: 100:0 to 31:69 then EtOAc/MeOH Gradient from 100:0 to90:10). The desired fractions were collected and the solvent was concentrated to dryness under vacuum to give 900 mg (56percent yield) of intermediate 503 as a yellow oil
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