反应详情

A solution of Oxone® (3.17 g, 5.15 mmol) in water (9 mL) was added to a solution of 2-(4-fluoro-phenyl)-8-isopropoxy-3-(2-methylsulfanylpyrimidin-4-yl)-imidazo[1,2-a]pyrazine (1.02 g, 2.57 mmol) in 41 mL of DCM/MeOH (1:1). The resulting reaction mixture was stirred overnight at ambient temperature, neutralized with a saturated aqueous solution of Na2CO3, and extracted with DCM. The organic phase was dried over MgSO4, filtered, and concentrated. The crude material was sequentially triturated with MeOH and ACN to give 0.387 g (35%) of the title compound: LC/MS (Table 1, Method g) Rt=2.69 min; MS m/z: 428.2 (M+H)+.

1. customThe resulting reaction mixture
2. extractionextracted with DCM
3. dry with materialThe organic phase was dried over MgSO4
4. filtrationfiltered
5. concentrationconcentrated
6. customThe crude material was sequentially triturated with MeOH and ACN