Cesium carbonate → 1-[(6-Chloro-3-pyridyl)methyl]-3-(4-cyanophenyl)-4-oxo-pyrido[1,2-a]pyrimidin-1-ium-2-olate

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Reaction Conditions

Reaction Steps

To a mixture of 53 mg (0.36 mmol) (4-cyanophenyl)boronic acid, 100 mg (0.24 mmol) 1-[(6-chloro-3-pyridyl)methyl]-3-iodo-4-oxo-pyrido[1,2-a]pyrimidin-1-ium-2-olate (Synthesis described in WO 2009/099929), 35 mg (0.05 mmol) bis(triphenylphosphino)-palladium dichloride and 17 mg (0.05 mmol) caesium carbonate was added 160 ml of dioxane. The mixture was heated to 100° C. for 18 hours. Silica was added and the product was obtained by column chromatographie (dichloromethane/methanol) (24 mg).

Provenance & Evidence