反应详情

At −20° C., 5.30 g of boron tribromide were added dropwise with stirring to a solution of 6.72 g of 7-chloro-2-(4-methoxy-3,5-dimethylphenyl)-5-methylsulfanyloxazolo[5,4-d]pyrimidine in 140 ml of dichloromethane. The reaction mixture was allowed to warm to room temperature and stirred for 2 hours. With ice cooling, another 1.33 g of boron tribromide were then added dropwise. After a further 2 hours, the reaction was once more cooled to −20° C., and sat. aqueous sodium bicarbonate solution was carefully added dropwise. The phases were separated at room temperature. The organic phase was washed with water, dried over sodium sulfate, filtered and concentrated under reduced pressure. The residue was triturated with diisopropyl ether, filtered off with suction and air-dried. This gave 6.20 g (96%) of the title compound, which was reacted further without any further purification.

1. waitAfter a further 2 hours
2. temperaturethe reaction was once more cooled to −20° C.
3. customThe phases were separated at room temperature
4. washThe organic phase was washed with water
5. dry with materialdried over sodium sulfate
6. filtrationfiltered
7. concentrationconcentrated under reduced pressure
8. customThe residue was triturated with diisopropyl ether
9. filtrationfiltered off with suction
10. customair-dried
11. customThis gave 6.20 g (96%) of the title compound, which was reacted further without any further purification