Cesium carbonate → 4-(((3,3-Difluorocyclobutyl)methoxy)methyl)-6-(1-ethoxyvinyl)-N-(3-methoxy-4-(4-methyl-1H-imidazol-1-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 (0.048 g, 0.15 mmol), 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline (0.031 g, 0.15 mmol), cesium carbonate (0.098 g, 0.30 mmol), palladium (II) acetate (5 mg, 0.02 mmol) and (2-biphenylyl)dicyclohexylphosphine (8 mg, 0.02 mmol) in dioxane (2 mL) was heated under argon at 120° C. for 90 minutes in micro wave reactor. The mixture was filtered through a short silica and was eluted with EtOAc. The residue was purified by preparative HPLC to give the title compound (0.019 g, 26.0%).

Provenance & Evidence