反应详情

To a solution of 6,8-dichloro-2-[1-(3-chloro-2-pyridinyl)-3-[(methylsulfonyl)oxy]-1H-pyrazol-5-yl]-4H-3,1-benzoxazin-4-one (i.e. the product of step D) (0.05 g, 0.10 mmol) in acetonitrile (3 mL) was added methylamine (2.0 M solution in THF, 0.5 mL, 1 mmol). The resulting solution was stirred at room temperature overnight. Thin layer chromatography showed the reaction to be incomplete. Methylamine (2.0 M solution in THF, 0.5 mL, 1 mmol) was added dropwise and the reaction stirred 1 hour at room temperature. Thin layer chromatography showed the reaction was complete. The reaction mixture was concentrated to dryness to yield 0.057 g of the title compound, a compound of present invention, as a white solid.

1. customthe reaction
2. stirringthe reaction stirred 1 hour at room temperature
3. concentrationThe reaction mixture was concentrated to dryness