反应详情

A solution of 2-chloro-4-morpholin-4-ylfuro[3,2-d]pyrimidine-6-carbaldehyde (78 mg, 0.29 mmol) and 2-piperidin-4-ylpropan-2-ol (50 mg, 0.35 mmol) in DCE (3 mL) was stirred at ambient temperature for 45 min. Sodium triacetoxyborohydride (93 mg, 0.44 mmol) was added and the mixture stirred for 2 h, then loaded onto an Isolute® SCX-2 cartridge (10 g). The cartridge was then washed with methanol and the desired product was subsequently eluted using 2 M NH3 in MeOH. The product was collected and concentrated in vacuo. The resultant residue was purified by flash chromatography (Si—PPC, DCM:MeOH; 100:0 to 98:2 to 95:5) to afford the title compound as a tan solid (110 mg, 96%). LCMS (Method H): RT=2.33 min, M+H+=395.

1. washThe cartridge was then washed with methanol
2. washthe desired product was subsequently eluted
3. customThe product was collected
4. concentrationconcentrated in vacuo
5. customThe resultant residue was purified by flash chromatography (Si—PPC, DCM:MeOH; 100:0 to 98:2 to 95:5)