反应详情

Method as intermediate 5 using (S)-tert-butyl 2-chloro-4-(3-methylmorpholino)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (intermediate 1) and 2-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline as starting materials. The crude reaction mixture was then partitioned between water and EtOAc, the phases separated and the organic layer washed with brine, dried over magnesium sulfate, filtered and the solvent removed in vacuo. The residue was purified by flash chromatography (0-80% EtOAc/Petroleum Ether 40-60) to yield a white solid (660 mg, 1.54 mmol, 22%).

1. customThe crude reaction mixture
2. customwas then partitioned between water and EtOAc
3. customthe phases separated
4. washthe organic layer washed with brine
5. dry with materialdried over magnesium sulfate
6. filtrationfiltered
7. customthe solvent removed in vacuo
8. customThe residue was purified by flash chromatography (0-80% EtOAc/Petroleum Ether 40-60)