反应详情

To a solution of N-(3-isobutyryl-1-methyl-1H-indol-5-yl)formamide (450 mg, 1.84 mmol) in anhydrous THF (3 mL) and anhydrous DMF (3 mL) was added 60% NaH (228 mg, 5.52 mmol) at 0° C. After being stirred for 30 min at room temperature, it was cooled to 0° C. To this, was added 4-chloro-2-(methylsulfonyl)pyrimidine (466 mg, 2.43 mmol) and then stirred for 2 hours. Quenching the reaction by addition of ice and 2N solution of sodium hydroxide (2 mL) resulted precipitation of brown solids. Additional 20 mL of water was added to complete of solid formation. The resulted solids were collected by filtration, rinsed with water and the dried in vacuo to provide the desired intermediate 5 as a brown solid (542 mg, 89%); MS (ESI) m/z 329 [M+H]+.

1. temperatureit was cooled to 0° C
2. stirringstirred for 2 hours
3. customQuenching
4. customthe reaction
5. customresulted
6. customprecipitation of brown solids
7. additionAdditional 20 mL of water was added to complete of solid formation
8. filtrationThe resulted solids were collected by filtration
9. washrinsed with water
10. customthe dried in vacuo