反应详情

温度

80 °C

Ethyl 1-[5-[7-bromo-2-(ethylcarbamoylamino)-1,3-benzothiazol-5-yl]pyrimidin-2-yl]-4-methyl-piperidine-4-carboxylate (3.11 g, 5.68 mmol) was suspended in EtOH (120 mL). To the stirred suspension was added, NMM (3.1 mL, 28.4 mmol), aqueous formaldehyde (4.61 mL, 56.8 mmol) and methylamine solution (14.2 mL, 28.4 mmol). The reaction mixture was then stirred at 80° C. for 16 h. The reaction mixture was cooled to rt and filtered. The precipitate was washed with EtOH, Et2O and dried to afford the desired compound (2.58 g, 75%) as an off-white solid. m/z=602.09 and 604.02 [M+H]+.

1. additionTo the stirred suspension was added
2. temperatureThe reaction mixture was cooled to rt
3. filtrationfiltered
4. washThe precipitate was washed with EtOH, Et2O
5. customdried