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4-chloro-6-(1-methyl-1H-pyrazol-4-yl)-1H-indole[ No CAS ]
Yield
Reaction Conditions
Operation in experiment
76%
With bis-triphenylphosphine-palladium(II) chloride; sodium carbonate; In 1,2-dimethoxyethane; water; at 120℃; for 12h;Inert atmosphere;
To a solution of <strong>[885519-01-7]6-bromo-4-chloro-1H-indole</strong> (500 mg, 2.17 mmol), 1-methyl-4-(4,4,5,5-tetramcthyl-I ,3,2-dioxaborolan-2-yl)-1H-pyrazole (0.54 g, 2.60 mmol) and Na2CO3 (0.69 g,6.51 minol) in DME/T-120 (10 mL, 4: 1) was added bis(triphenylphosphine)palladium(II) dichloride (140 mg, 0.22 mmol). The mixture was heated to 120 C for 12 h under a nitrogen the mixture was extracted with EtOAc (10 mL x3). The combined organic layers werewashed with sat. aq. NaHCO3 (10 mL x 3), dried over anhydrous Na2SO4 and concentrated in vacuo. The crude residue was purified by silica gel chromatography (petroleum ether EtOAc= 3: 1) to give the title compound (0.38 g, 76%) as a light yellow solid.