反应详情

温度

95 °C

(S)-tert-butyl 4-(2-(2-((6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl)morpholino)pyrimidin-5-yl)-5,6-dihydropyridine-1(2H)-carboxylate (36 mg, 0.06 mmol) was dissolved in 35% HCHO (0.1 ml) and acetic acid (0.5 ml), followed by stirring at 95° C. overnight. After the completion of the reaction, the reaction mixture was adjusted to pH 11-12 with NaOH (aq.), and extracted with H2O and EA, followed by drying (Na2SO4), filtration and concentration under reduced pressure, and the residue was purified by column chromatography (MeOH:MC=1:10), to give (S)-4-(5-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)pyrimidin-2-yl)-2-((6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl)morpholine (16.9 mg, 56%).

1. customAfter the completion of the reaction
2. extractionextracted with H2O and EA
3. customby drying
4. filtration(Na2SO4), filtration and concentration under reduced pressure
5. customthe residue was purified by column chromatography (MeOH:MC=1:10)