Cesium carbonate → 4-(((3,3-Difluorocyclobutyl)methoxy)methyl)-6-(1-ethoxyvinyl)-N-(3-methoxy-4-(6-methylpyridazin-4-yl)phenyl)pyrimidin-2-amine

Participants

Reaction Conditions

Reaction Steps

A mixture of 2-chloro-4-(((3,3-difluorocyclobutyl)methoxy)methyl)-6-(1-ethoxyvinyl)pyrimidine (0.068 g, 0.21 mmol), 3-methoxy-4-(6-methylpyridazin-4-yl)aniline (0.046 g, 0.21 mmol), cesium carbonate (0.139 g, 0.43 mmol), palladium (II) acetate (7 mg, 0.03 mmol) and (2-biphenylyl)dicyclohexylphosphine (0.011 g, 0.03 mmol) in dioxane (2 mL) was heated under argon at 120° C. for 90 min in microwave reactor. The mixture was filtered through a short silica plug and was eluted with 10% MeOH in EtOAc. The solvents were evaporated to give the title compound (0.109 g, quant).

Provenance & Evidence