反応 #1005968

反応方程式

2-bromo-6-trifluoromethyl-imidazo[1,2-a]pyridine

2-ethylsulfanyl-4-trifluoromethylphenylboronic acid pinacol ester

tricyclohexylphosphine

tripotassium phosphate

→

2-(2-ethylsulfanyl-4-trifluoromethylphenyl)-6-trifluoromethyl-imidazo[1,2-a]pyridine

収率 80.1%

溶媒

Water

water

1,4-dioxane

反応条件

後処理

1. 1
   抽出the mixture was extracted with ethyl acetate
2. 2
   洗浄The organic layer was washed with water
3. 3
   乾燥dried over anhydrous magnesium sulfate
4. 4
   濃縮concentrated under reduced pressure

実験手順

A mixture of 200 mg of 2-bromo-6-trifluoromethyl-imidazo[1,2-a]pyridine, 332 mg of 2-ethylsulfanyl-4-trifluoromethylphenylboronic acid pinacol ester, 21 mg of tris(dibenzylideneacetone) dipalladium(0), 85 mg of tricyclohexylphosphine (18% toluene solution), 480 mg of tripotassium phosphate, 1.5 ml of 1,4-dioxane and 0.5 ml of water was stirred at 100° C. for 4 hours. 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 236 mg of 2-(2-ethylsulfanyl-4-trifluoromethylphenyl)-6-trifluoromethyl-imidazo[1,2-a]pyridine (hereinafter, referred to as Compound of Present Invention 6).

出典