Cesium fluoride → [2-(2,5-Difluoro-phenyl)-6-methoxy-naphthalen-1-yl]-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-methanone

참여 물질

반응 조건

반응 단계

Add trifluoromethanesulfonic acid 6-methoxy-1-[4-(2-piperidin-1-yl-ethoxy)-benzoyl]-naphthalen-2-yl ester (552 mg, 1.0 mmol), 2,6-difluorophenyl boronic acid (320 mg, 2.0 mmol), trans dichlorobis(triphenylphosphine)palladium II (70 mg, 0.1 mmol) and cesium fluoride (1.3 g, 8.6 mmol) to a 20 mL vial along with 8.0 mL degassed acetonitrile. Seal the vial with a septum and purge with nitrogen gas. Heat the mixture with stirring at 80° C. for three hours. Cool, filter and purify on an SCX column, eluting with 2N ammonia/methanol. The compound is further purified on a silica gel column, eluting with a 0-5% 2N ammonia in methanol/methylene chloride gradient. The yield is 260 mg (50%).

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