反応 #1005972

反応方程式

2-bromo-2′-ethylsulfonylacetophenone

2-amino-4-trifluoromethylpyridine

→

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

収率 26.0%

溶媒

ethanol

反応条件

後処理

1. 1
   温度was refluxed for 1 hour
2. 2
   濃縮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
   抽出the mixture was extracted with ethyl acetate
6. 6
   洗浄The organic layer was washed with water
7. 7
   乾燥dried over anhydrous magnesium sulfate
8. 8
   濃縮concentrated under reduced pressure

実験手順

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).

出典