反应 #1005972

反应方程式

2-bromo-2′-ethylsulfonylacetophenone

2-amino-4-trifluoromethylpyridine

→

2-(2-ethylsulfonylphenyl)-7-trifluoromethyl-imidazo[1,2-a]pyridine

收率 26.0%

溶剂

ethanol

反应条件

后处理

1. 1
   温度was refluxed for 1 hour
2. 2
   浓缩concentrated under reduced pressure
3. 3
   workup.ADDITIONA mixture of the residue, 250 mg of sodium bicarbonate and 1.5 ml of DMF
4. 4
   workup.ADDITIONWater was poured to the cooled reaction mixture
5. 5
   萃取the mixture was extracted with ethyl acetate
6. 6
   洗涤The organic layer was washed with water
7. 7
   干燥dried over anhydrous magnesium sulfate
8. 8
   浓缩concentrated under reduced pressure

实验过程

A mixture of 1.0 g of 2-bromo-2′-ethylsulfonylacetophenone, 334 mg of 2-amino-4-trifluoromethylpyridine and 4 ml of ethanol was refluxed for 1 hour and concentrated under reduced pressure. A mixture of the residue, 250 mg of sodium bicarbonate and 1.5 ml of DMF was stirred at 130° C. for 1 hour. Water was poured to the cooled reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous magnesium sulfate, and then concentrated under reduced pressure. The resulting residue was applied to a silica gel column chromatography to obtain 190 mg of 2-(2-ethylsulfonylphenyl)-7-trifluoromethyl-imidazo[1,2-a]pyridine (hereinafter, referred to as Compound of Present Invention 8).

来源