反应详情

Method as described for intermediate 5 using (S)-4-(2-chloro-7-methyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-3-methylmorpholine (intermediate 13) and as 3-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline as starting materials. The reaction mixture was filtered through a celite 545 pre-packed cartridge (2.5 g), washed with methanol and solvent removed in vacuo. The residue was purified by trituration with a (9:1) mixture of petrol ether (40-60)/ethyl acetate, yielding the title compound after filtration and drying of the solid obtained (85 mg, 0.24 mmol, 67%).

1. filtrationThe reaction mixture was filtered through a celite 545 pre-packed cartridge (2.5 g)
2. washwashed with methanol and solvent
3. customremoved in vacuo
4. customThe residue was purified by trituration with a (9:1) mixture of petrol ether (40-60)/ethyl acetate