反应详情

温度

130 °C

Compound 517 (30 mg, 0.08 mmol) was dissolved in acetonitrile (2 mL) in a reaction vial. 4-(2-Chloro-ethyl)-morpholine hydrochloride (44 mg, 0.24 mmol) and K2CO3 (33 mg, 0.24 mmol) were added. The reaction vial was flushed with argon, closed and then stirred at 130° C. for a total of 105 min. in a microwave oven. The reaction mixture was poured into a mixture of EtOAc:H2O (1:1, 10 mL). The layers were separated and the aqueous phase was extracted with EtOAc (2×10 mL). The combined organic layers were dried (MgSO4), filtered, concentrated in vacuo and purified by continuously gradient flash chromatography using EtOAc/petroleum ether (40-60)(v:v=1:9 to 3:2) as the eluent, affording the title compound as a light yellow oil.

1. customThe reaction
2. customvial was flushed with argon
3. customclosed
4. additionThe reaction mixture was poured into a mixture of EtOAc:H2O (1:1, 10 mL)
5. customThe layers were separated
6. extractionthe aqueous phase was extracted with EtOAc (2×10 mL)
7. dry with materialThe combined organic layers were dried (MgSO4)
8. filtrationfiltered
9. concentrationconcentrated in vacuo
10. custompurified by continuously gradient flash chromatography