反应详情

温度

80 °C

tert-Butyl 4-((6-(4-methoxybenzyl)-5-oxo-5,6-dihydropyrido[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-9-yl)methyl)piperazine-1-carboxylate. 9-Bromo-6-(4-methoxybenzyl)pyrido[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one (Example 1, 562.00 mg; 1.46 mmol), potassium ((4-(tert-butoxycarbonyl)piperazin-1-yl)methyl)trifluoroborate (568.00 mg; 1.86 mmol), dicyclohexyl(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphine (60.00 mg; 0.13 mmol;), Pd(OAc)2 (30.00 mg; 0.13 mmol), Cs2CO3 (1.76 g; 5.40 mmol), and degassed dioxane-water (9:1; 10 mL) were combined in that order and heated at 80° C. for 4 days. The mixture concentrated under reduced pressure. Purification (FCC, SiO2, 20-100% EtOAc/hexanes) afforded the title compound (216 mg, 29%).

1. concentrationThe mixture concentrated under reduced pressure
2. customPurification (FCC, SiO2, 20-100% EtOAc/hexanes)