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) and 1-(pyridin-3-yl)-3-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)urea 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 reduced in vacuo. The residue was purified first by flash chromatography using a gradient of 0-40% DCM/MeOH, then triturating with a mixture of petrol ether/ethyl acetate (9:1) affording the title compound after filtration and drying of the solid obtained (23 mg, 0.05 mmol, 30%).

1. filtrationThe reaction mixture was filtered through a celite 545 pre-packed cartridge (2.5 g)
2. washwashed with MeOH
3. customThe residue was purified first by flash chromatography
4. customtriturating with a mixture of petrol ether/ethyl acetate (9:1)