反应详情

In a pressure tube reactor, (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 (40 mg, 0.08 mmol) was added, and then K2CO3 (36 mg, 0.26 mmol) was added. Pd(dppf)2Cl2 (4 mg, 0.004 mmol) was further added, and 1,4-dioxane (2 mL) and water (0.5 mL) were added. 4-(2-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolane-2-yl)benzyl)morpholine (42 mg, 0.13 mmol) was added, and then stirred at room temperature under nitrogen gas for 10 minutes, followed by stirring at 85° C. for 2 hours. When the reaction was completed, the organic layer was extracted with ethyl acetate and water, and the extra water was removed by sodium sulfate, followed by concentration under reduced pressure. Column chromatography using 50% ethyl acetate/hexane gave (S)-4-(5-(3-fluoro-4-(morpholinomethyl)phenyl)pyrimidin-2-yl)-2-((6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl)morpholine (51 mg, 0.089 mmol) with a yield of 46%.

1. stirringby stirring at 85° C. for 2 hours
2. extractionthe organic layer was extracted with ethyl acetate and water
3. customthe extra water was removed by sodium sulfate
4. concentrationfollowed by concentration under reduced pressure