反应详情

温度

80 °C

(S)-4-(5-bromopyrimidin-2-yl)-2-((6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl)morpholine 500 mg (1.09 mmol) was dissolved in dimethoxymethane 8 ml, and then tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolane-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate 406 mg (1.31 mol) was added. Potassium carbonate 453 mg (3.28 mmol) was dissolved in distilled water 2 ml, which was then added to the reaction solution. PdCl2(dppf)2 45 mg (0.0547 mmol) was added, and the mixture was purged with N2 (g), followed by stirring at 80° C. for 2 hours. After the completion of the reaction, the reaction mixture was extracted with ethyl acetate and brine, and the organic layer was dried over Na2SO4. 3% MeOH/MC chromatography gave a product 478 mg (78%).

1. additionwhich was then added to the reaction solution
2. customthe mixture was purged with N2 (g)
3. customAfter the completion of the reaction
4. extractionthe reaction mixture was extracted with ethyl acetate and brine
5. dry with materialthe organic layer was dried over Na2SO4