反应详情

温度

110 °C

5-(Benzylthio)-7-chloro[1,3]thiazolo[4,5-d]pyrimidin-2-amine (1.5 g, 4.86 mmol), DIPEA (691 mg, 5.35 mmol) and (R)—N-methylleucinol (956 mg, 7.29 mmol) were mixed in NMP (7.5 mL). The resulting solution was stirred at 110° C. under a nitrogen atmosphere for 2 days. After cooling to room temperature the reaction mixture was poured onto ice. The resulting yellow precipitate was collected by filtration, washed with water and dried in vacuo. The crude product was purified by flash column chromatography on silica (DCM:EtOAc 50:50 to 0:100) to give 1.42 g (72% yield) of the title compound as a yellow solid.

1. temperatureAfter cooling to room temperature the reaction mixture
2. additionwas poured onto ice
3. filtrationThe resulting yellow precipitate was collected by filtration
4. washwashed with water
5. customdried in vacuo
6. customThe crude product was purified by flash column chromatography on silica (DCM:EtOAc 50:50 to 0:100)