反应详情

To a solution of 4-(3-iodo-1-isopropyl-1H-pyrazol-4-yl)-2-(methylthio)pyrimidine B-1-1 (15.5 g, 43 mmol) in THF (350 mL) and water (350 mL) was added oxone (39.6 g, 64.6 mmol) at 0-5° C. After the addition, the mixture was stirred at rt overnight. TLC (hexane:EtOAc=5:1) showed the reaction was complete, EtOAc (500 mL) was added. The organic layer was separated, washed with saturated aqueous NaCl, dried over Na2SO4 and concentrated to give 4-(3-iodo-1-isopropyl-1H-pyrazol-4-yl)-2-(methylsulfonyl)pyrimidine B-1-2 (16 g, 94.9%).

1. additionAfter the addition
2. customThe organic layer was separated
3. washwashed with saturated aqueous NaCl
4. dry with materialdried over Na2SO4
5. concentrationconcentrated