反应详情

温度

100 °C

A mixture of ethyl 3-{[(benzyloxy)carbonyl]amino}-7-bromoquinoline-2-carboxylate (300 mg, 0.7 mmol), 1-methylpiperazine (200 mg, 2 mmol), Pd(OAc)2 (20 mg), dicyclohexyl(2′,6′-diisopropoxybiphenyl-2-yl)phosphine (49 mg, 0.10 mmol), and K3PO4 (580 mg, 2.8 mmol) in tert-butyl alcohol (10 mL) was purged with N2 prior and then heated at 100° C. in a sealed vial for 2 h. The mixture was allowed to cool, diluted with EtOAc, and then filtered through a diatomaceous earth plug. The filtrate was concentrated under reduced pressure. To the resulting residue, 10 mL of dioxane and 4 mL of 2.5 M NaOH were added.

1. customwas purged with N2
2. temperatureto cool
3. additiondiluted with EtOAc
4. filtrationfiltered through a diatomaceous earth plug
5. concentrationThe filtrate was concentrated under reduced pressure
6. additionTo the resulting residue, 10 mL of dioxane and 4 mL of 2.5 M NaOH were added