反应详情

温度

0 °C

Piperidine-3-carboxylic acid [6-(2-methoxy-phenyl)-pyrimidin-4-yl]amide (compound #16A) (110 mg, 0.352 mmol) was dissolved in 5 ml of anhydrous dichloromethane, cooled to 0° C. and 4-N,N-dimethylaminopyridine (90 mg, 0.70 mmol) and acetic anhydride (54 mg, 0.53 mmol) were added simultaneously. The reaction mixture was stirred for 3 hours at room temperature, treated with crushed ice and partitioned between water and dichloromethane. The organic layer was separated, dried over sodium sulfate and concentrated to provide 1-acetyl-piperidine-3-carboxylic acid [6-(2-methoxy-phenyl)-pyrimidin-4-yl]-amide (compound #20A) (105 mg, 84.13%).

1. additiontreated with crushed ice
2. custompartitioned between water and dichloromethane
3. customThe organic layer was separated
4. dry with materialdried over sodium sulfate
5. concentrationconcentrated