Reaktion #87440

Reaktionsgleichung

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

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

cesium carbonate

2-(dicyclohexyl-phosphino)biphenyl

→

title compound

N4-Cyclopropyl-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 filter pad was eluted with methanol
3. 3
   EinengenThe eluate was concentrated in vacuum
4. 4
   Sonstigethe residue purified by preparative chromatography

Vorschrift

A mixture of 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline (91 mg, 0.45 mmol), 2-chloro-N-cyclopropyl-6-((2,2,2-trifluoroethoxy)methyl)pyrimidin-4-amine (63 mg, 0.22 mmol), cesium carbonate (146 mg, 0.45 mmol), palladium(II) acetate (8 mg, 0.03 mmol) and 2-(dicyclohexyl-phosphino)biphenyl (12 mg, 0.03 mmol) in dioxane (1.5 mL) was heated at 120° C. in a microwave reactor for 90 minutes. The mixture was filtered through diatomeous earth, the filter pad was eluted with methanol. The eluate was concentrated in vacuum and the residue purified by preparative chromatography to give the title compound as a solid, 45 mg (45%).

Quelle