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

関与物質

反応条件

反応手順

To 8-chloro-4-methyl-2-(4-methylthiazol-2-yl)-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepine (120 mg, 0.41 mmol) in DME (3 mL) were 6-methoxy-5-(4-methyl-1H-imidazol-1-yl)pyridin-2-amine (83 mg, 0.41 mmol), cesium carbonate (198 mg, 0.61 mmol), 2-(Dicyclohexylphosphino)biphenyl (14.22 mg, 0.04 mmol) and Palladium acetate (9.11 mg, 0.04 mmol) added. The reaction was heated to 110°C for 180 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 (20.00 mg, 10.63 %)

情報源と証拠