反应详情

A solution of oxone (179 mg, 0.29 mmol) in water (10 mL) was added dropwise to a stirred solution of 2-(5-bromo-2-(methylthio)pyrimidin-4-yl)thiazolo[5,4-c]pyridine (66 mg, 0.19 mmol) in dichloromethane (12 mL) at 0° C. The bright yellow suspension was allowed to warm to r.t. overnight. After 14 h the organic layer was separated, dried over sodium sulfate, filtered and the solvent evaporated in vacuo. The residue was purified by flash chromatography (ethyl acetate/hexane 25:75 to 50:50) to yield 2-(5-bromo-2-(methylsulfonyl)pyrimidin-4-yl)thiazolo[5,4-c]pyridine (59 mg, 82%) as a white amorphous solid. 1H NMR: δ (CDCl3, 400 MHz) 3.47 (s, 3 H), 8.13 (d, J=5.5 Hz, 1 H), 8.79 (d, J=5.5 Hz, 1 H), 9.29 (s, 1 H), 9.39 (s, 1 H).

1. customAfter 14 h the organic layer was separated
2. dry with materialdried over sodium sulfate
3. filtrationfiltered
4. customthe solvent evaporated in vacuo
5. customThe residue was purified by flash chromatography (ethyl acetate/hexane 25:75 to 50:50)