反应 #1005968

反应方程式

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

收率 80.1%

溶剂

Water

water

1,4-dioxane

反应条件

后处理

1. 1
   萃取the mixture was extracted with ethyl acetate
2. 2
   洗涤The organic layer was washed with water
3. 3
   干燥dried over anhydrous magnesium sulfate
4. 4
   浓缩concentrated under reduced pressure

实验过程

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).

来源