Cesium carbonate → N-(4-(3-(2-methylpyridin-4-yl)pyrazin-2-yloxy)phenyl)pyridin-2-amine

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Reaction Steps

To a 50 mL round-bottomed flask was added N-(4-(3-chloropyrazin-2-yloxy)phenyl)pyridin-2-amine (0.2890 g, 0.967 mmol), 2-methylpyridin-4-ylboronic acid (0.1684 g, 1.20 mmol), and trans-dichlorobis(triphenylphosphine)palladium (II) (0.0355 g, 0.0484 mmol) in DME. An aqueous solution of cesium carbonate (0.213 ml, 2.61 mmol) was added and the temperature was brought to 80° C. to stir overnight. The crude product was adsorbed onto a plug of silica gel and chromatographed to provide N-(4-(3-(2-methylpyridin-4-yl)pyrazin-2-yloxy)phenyl)pyridin-2-amine. MS (ESI, pos. ion) m/z: 356.1. IC50 (uM)=0.033.

Provenance & Evidence