反应详情

[4-(6-Bromo-imidazo[1,2-a]pyridin-8-ylamino)-phenyl]-morpholin-4-yl-methanone (270 mg, 0.68 mmol), 2-(6-tert-butyl-8-fluoro-1-oxophthalazin-2(1H)-yl)-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl acetate (670 mg, 1.35 mmol) and K2CO3 (188 mg, 1.36 mmol) were dissolved in a 10:1 mixture of dioxane in H2O (11 ml). Under N2 atmosphere, Pd2(dba)3 (62 mg, 0.068 mmol) and X-phos (129 mg, 0.27 mmol) were added and the mixture was stirred at reflux temperature overnight. After the completion of the reaction, the mixture was cooled to room temperature, poured into water (100 mL) and extracted by DCM (100 ml). The organic extracts were washed with saturated aqueous solution of sodium chloride (100 ml), dried over sodium sulfate and concentrated. The residue was purified by silica gel column (petroleum ether:ethyl acetate 2:1) to afford the desired product as a yellow solid (60 mg, yield 25%). LC-MS: 689[M+1]+, tR=1.506 min.

1. temperatureat reflux temperature overnight
2. customAfter the completion of the reaction
3. extractionextracted by DCM (100 ml)
4. washThe organic extracts were washed with saturated aqueous solution of sodium chloride (100 ml)
5. dry with materialdried over sodium sulfate
6. concentrationconcentrated
7. customThe residue was purified by silica gel column (petroleum ether:ethyl acetate 2:1)