反应详情

To a solution of N-(5-cyano-2-methylsulfanyl-pyrimidin-4-yl)-N-methyl-acetamide (400 mg, 1.80 mmol) in THF (18 mL) was added a solution of lithium bis(trimethyl-silyl)amide (1.0 M in hexane, 7.2 mL, 7.20 mmol) at RT. The reaction mixture was stirred at RT for 1 h, then quenched with water (100 mL). The resulting mixture was extracted with EtOAc (100 mL); the organic layer dried over MgSO4, filtered and concentrated under reduced pressure. The crude residue was purified by flash chromatography (from 10 to >100% EtOAc/hexane in 10 min.) to give 163 mg (41% yield) of 5-amino-8-methyl-2-methylsulfanyl-8H-pyrido[2,3-d]-pyrimidin-7-one as a yellow solid.

1. customquenched with water (100 mL)
2. extractionThe resulting mixture was extracted with EtOAc (100 mL)
3. dry with materialthe organic layer dried over MgSO4
4. filtrationfiltered
5. concentrationconcentrated under reduced pressure
6. customThe crude residue was purified by flash chromatography (from 10 to >100% EtOAc/hexane in 10 min.)