反应详情

To a solution of 1-(4-Fluoro-benzoyl)-piperidine-3-carboxylicacid (1.13 g, 4.50 mmol) in DCM (6.5 ml) was successively added Hydrazinecarboxylic acid tert-butyl ester (0.59 g, 4.50 mmol), HOBT (0.69 g, 4.50 g) anf EDCI.HCl (1.29 g, 6.758 mmol). The mixture was stirred at R.T for 72 h. The solvent was removed under reduced pressure and the residue was diluted with DCM was added. The organic layer was washed twice with water, twice with HCl 1N and twice with water. The organic layer was dried over Na2SO4, filtered and evaporated to afford 1.19 g (73%) of N′-[1-(4-Fluoro-benzoyl)-piperidine-3-carbonyl]-hydrazinecarboxylic acid tert-butyl ester as a colorless semi-solid.

1. customThe solvent was removed under reduced pressure
2. additionthe residue was diluted with DCM
3. additionwas added
4. washThe organic layer was washed twice with water, twice with HCl 1N and twice with water
5. dry with materialThe organic layer was dried over Na2SO4
6. filtrationfiltered
7. customevaporated