6-Methoxy-5-(4-methyl-1H-imidazol-1-YL)pyridin-2-amine → N-(6-Methoxy-5-(4-methyl-1H-imidazol-1-yl)pyridin-2-yl)-4-methyl-2-(4-methylthiazol-2-yl)-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepin-8-amine

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

To 8-chloro-4-methyl-2-(4-methylthiazol-2-yl)-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepine (50 mg, 0.17 mmol) in DME (3 mL) were 6-methoxy-5-(4-methyl-1H-imidazol-1-yl)pyridin-2-amine (34.5 mg, 0.17 mmol), cesium carbonate (83 mg, 0.25 mmol), 2-(Dicyclohexylphosphino)biphenyl (5.92 mg, 0.02 mmol) and Palladium acetate (3.80 mg, 0.02 mmol) added. The reaction was heated to 110°C for 90 min under N2 atmosphere. The solids were filtered off and washed with DCM, the solvents were evaporated and the crude product was purified by silica flash chromatography, MeOH, 0-10%, in DCM yielding N-(6-methoxy-5-(4-methyl-1H-imidazol-1-yl)pyridin-2-yl)-4-methyl-2-(4-methylthiazol-2-yl)-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepin-8-amine (16.00 mg, 20.42 %)

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