反应详情

To a mixture of 2-[1-methyl-1-(5-(pyridin-2-yl)-1H-pyrrol-2-yl)-2-(tetrahydro-2H-pyran-4-yl)ethyl]-5-(methylsulfanyl)pyridine (84.0 mg), tetrahydrofuran (1 mL), water (1 mL) and methanol (1 mL) was added Oxone (registered trademark) (157 mg), and the mixture was stirred at room temperature for 1.5 hr. The reaction mixture was diluted with ethyl acetate, and washed with saturated aqueous sodium hydrogen carbonate solution. The ethyl acetate layer was dried (MgSO4) and concentrated. The residue was subjected to silica gel column chromatography, and the title compound (55.5 mg, yield 61%) was obtained as white crystals from a fraction eluted with ethyl acetate-hexane (2:1, volume ratio). melting point 135-136° C. MS: 426 (MH+).

1. washwashed with saturated aqueous sodium hydrogen carbonate solution
2. dry with materialThe ethyl acetate layer was dried (MgSO4)
3. concentrationconcentrated