反应详情

To a solution of 0.050 g (0.21 mmol) of (+/−)9-amino-2-pyridin -4-yl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one dissolved in 2.2 mL of tetrahydrofuran was added 30 μl (0.25 mmol) of triethylamine and 0.0484 g (0.25 mmol) of 1-methyl-1H-1,2,3-benzotriazole-5-carbonyl chloride. The resulting mixture was stirred at room temperature for 16 h. Water was added and the mixture extracted with ethyl acetate. The extracts were washed with a saturated aqueous solution of ammonium chloride, dried and evaporated. The residue was purified by silica gel chromatography, eluting with dichloromethane/methanol/ammonia in the proportions 95/5/0.5 to give 0.041 g of pure product obtained in the form of free base.

1. extractionthe mixture extracted with ethyl acetate
2. washThe extracts were washed with a saturated aqueous solution of ammonium chloride
3. customdried
4. customevaporated
5. customThe residue was purified by silica gel chromatography
6. washeluting with dichloromethane/methanol/ammonia in the proportions 95/5/0.5