Potassium Carbonate → (1-(5-(5-Ethoxy-2-fluorophenyl)pyrimidin-2-yl)-3-(methylsulfinyl)-1H-indol-6-yl)(morpholino)methanone

関与物質

反応条件

反応手順

Potassium carbonate (0.185 g, 1.34 mmol) and (Ataphos)2PdCl2 (0.032 g, 0.044 mmol) were added under an argon atmosphere to a solution of (1-(5-bromopyrimidin-2-yl)-3-(methylsulfinyl)-1H-indol-6-yl)(morpholino)methanone (0.2 g, 0.445 mmol) and 2-fluoro-5-ethoxyphenylboronic acid (0.165 g, 0.89 mmol) in tert-amylalcohol (8.0 mL) and water (0.8 mL). The reaction mixture was stirred at 90° C. for 4 h, then cooled to ambient temperatures and filtered over celite. The filtrate was concentrated and the residue purified by flash column chromatography [silica; dichloromethane with 2% methanol]. White solid. Yield: 0.14 g (62% of theory)

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