Cesium carbonate → HCID 53371804, Verbindung

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

To a solution of 307 mg (0.94 mmol) 4-chloro-2-(2-fluoro-5-trifluoromethyl-phenyl)-[1,8]naphthyridine in 10 ml dioxane under nitrogen, 89 mg (0.94 mmol) 4-aminopyrimidine, 612 mg (1.88 mmol) cesium carbonate, 54 mg (0.093 mmol) 9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene and 34 mg (0.038 mmol) tris(dibenzylideneaceton)-dipalladium(0) were added and heated in a microwave apparatus to 140° C. for 30 minutes. The reaction mixture was partitioned between dichloromethane and water. The organic phase was dried and the product chromatographed on a silica gel column with dichloro-methane/methanol. This yielded [2-(2-fluoro-5-trifluoromethyl-phenyl)-[1,8]naphthyridin-4-yl]-pyrimidin-4-yl-amine as beige crystals; HPLC-MS: 1.72 min, [M+H] 386.

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