Reaktion #87439

Reaktionsgleichung

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

2-chloro-N-(cyclopropylmethyl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidin-4-amine

cesium carbonate

2-(dicyclohexylphosphino)biphenyl

→

title compound

N4-(Cyclopropylmethyl)-N2-(3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidine-2,4-diamine

Lösungsmittel

dioxane

Reaktionsbedingungen

Aufarbeitung

1. 1
   FiltrationThe mixture was filtered through diatomeous earth
2. 2
   Waschenthe pad was eluted with methanol
3. 3
   EinengenThe eluate was concentrated
4. 4
   Sonstigethe residue was purified by preparative chromatography

Vorschrift

A mixture of 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline (99 mg, 0.49 mmol), 2-chloro-N-(cyclopropylmethyl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidin-4-amine (72 mg, 0.24 mmol), cesium carbonate (159 mg, 0.49 mmol), palladium(II) acetate (8.20 mg, 0.04 mmol) and 2-(dicyclohexylphosphino)biphenyl (12.80 mg, 0.04 mmol) in dioxane (1.5 mL) was heated at 120° C. by microwave irradiation under nitrogen atmosphere for 90 minutes. The mixture was filtered through diatomeous earth, the pad was eluted with methanol. The eluate was concentrated and the residue was purified by preparative chromatography to give the title compound as a dry film, 65 mg (58%).

Quelle