反应详情

A mixture of the product of Step 1 (4.8 g, 25 mmol), sodium methoxide (1.35 g, 25 mmol) and 4-acetyl-piperidine-1-carboxylic acid benzyl ester (6.4 g, 25 mmol) (WO97/05877) in methanol (100 ml) was heated at reflux for 8 hours. After cooling to room temperature the solution was concentrated in vacuo and the residue diluted with ethyl acetate and water. The organic phase was washed with water and brine, dried and concentrated in vacuo and the residue purified by silica gel chromatography to give the title compound (6.92 g, 64%); MS(ES+) m/e 433 [M+H]+.

1. temperaturewas heated
2. temperatureat reflux for 8 hours
3. concentrationwas concentrated in vacuo
4. additionthe residue diluted with ethyl acetate and water
5. washThe organic phase was washed with water and brine
6. customdried
7. concentrationconcentrated in vacuo
8. customthe residue purified by silica gel chromatography