反应详情

温度

60 °C

A solution of 6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole in tetrahydrofuran (THF) (7.5 mL) was heated to 60° C. under nitrogen. 2M hydrochloric acid in diethyl ether (0.567 mL, 1.135 mmol) and tetrahydrofuran (THF) (0.5 mL) were mixed and added via a dropping funnel. The solution was stirred at 60° C. for 30 mins before being slowly cooled to RT. After stirring at RT for a further 30mins the solid was filtered off, then recombined with the liquors and evaporated to dryness. THF (10 mL) was added and the slurry was cycled from RT to reflux 3 times (30 mins hold at higher/low temp). The slurry was stirred at RT for one hour then filtered under vacuum and the resultant solid dried in a vacuum oven at 50° C. overnight to give the title compound as a an off-white solid (322 mg).

1. additionadded via a dropping funnel
2. temperaturebefore being slowly cooled to RT
3. stirringAfter stirring at RT for a further 30mins the solid
4. filtrationwas filtered off
5. customevaporated to dryness
6. additionTHF (10 mL) was added
7. customwas cycled from RT
8. temperatureto reflux 3 times (30 mins hold at higher/low temp)
9. stirringThe slurry was stirred at RT for one hour
10. filtrationthen filtered under vacuum
11. customthe resultant solid dried in a vacuum oven at 50° C. overnight