Reacción #87458

Ecuación de reacción

2-(2-chloro-6-(1-ethoxy-2,2-difluorocyclopropyl)pyrimidin-4-yl)propan-2-ol

3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline

cesium carbonate

2-(dicyclohexylphosphino)biphenyl

→

title compound

2-(6-(1-Ethoxy-2,2-difluorocyclopropyl)-2-(3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenylamino)pyrimidin-4-yl)propan-2-ol

Disolventes

dioxane

Condiciones de reacción

Tratamiento posterior

1. 1
   FiltraciónThe crude mixture was filtered through a short silica plug which
2. 2
   Lavadowas washed with 10% MeOH in EtOAc (35 mL)
3. 3
   OtroThe residue was purified by preparative HPLC

Procedimiento

A mixture of 2-(2-chloro-6-(1-ethoxy-2,2-difluorocyclopropyl)pyrimidin-4-yl)propan-2-ol (8 mg, 0.03 mmol), 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline (6 mg, 0.03 mmol), cesium carbonate (17.81 mg, 0.05 mmol), palladium acetate (1 mg, 4 μmol) and 2-(dicyclohexylphosphino)biphenyl (1.5 mg, 4 μmol) in dioxane (1.5 mL) was heated under argon atmosphere at 120° C. for 90 minutes in microwave reactor. The crude mixture was filtered through a short silica plug which was washed with 10% MeOH in EtOAc (35 mL). The residue was purified by preparative HPLC to give the title compound as a dry film, 6 mg (48%).

Fuente