反应详情

Method as described for intermediate 5 using (S)-ethyl 2-chloro-4-(3-methylmorpholino)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (intermediate 11), 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazin-2-amine as starting materials, and [1,1′-bis(diphenylphosphino)ferrocene]dichloropalladium(II) as catalyst. The reaction mixture was filtered through a celite 545 pre-packed cartridge (2.5 g), washed with MeOH and solvent removed in vacuo. The residue was purified by flash chromatography using a gradient of 0-40% DCM/MeOH yielding the title compound (69 mg, 0.18 mmol, 58%).

1. filtrationThe reaction mixture was filtered through a celite 545 pre-packed cartridge (2.5 g)
2. washwashed with MeOH and solvent
3. customremoved in vacuo
4. customThe residue was purified by flash chromatography