反应详情

450 mg of (2-bromobenzyloxy)-tert-butyldimethylsilane, 500 mg of 2-chloro-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)imidazo[1,2-a]pyridine and 1.46 g of caesium carbonate are dissolved in 8 ml of tetrahydrofuran and 1 ml of water. The mixture is degassed with argon for 10 min, 110 mg of [1,1′-bis(diphenylphosphino)-ferrocene]dichloropalladium are added and the mixture is heated at the reflux of the solvent for 16 hours. After cooling, the reaction mixture is hydrolysed with water, and the organic phase, which has been extracted with dichloromethane, is separated, dried and concentrated under reduced pressure. The oil obtained is purified by silica gel chromatography, elution being carried out with a heptane/ethyl acetate mixture. 260 mg of compound are obtained.

1. customThe mixture is degassed with argon for 10 min
2. addition110 mg of [1,1′-bis(diphenylphosphino)-ferrocene]dichloropalladium are added
3. temperaturethe mixture is heated at the
4. temperaturereflux of the solvent for 16 hours
5. temperatureAfter cooling
6. extractionthe organic phase, which has been extracted with dichloromethane
7. customis separated
8. customdried
9. concentrationconcentrated under reduced pressure
10. customThe oil obtained
11. customis purified by silica gel chromatography, elution