反应详情

To a solution of 1-benzyl-4-(2-methoxy-ethyl)-3-oxo-piperidine-4-carboxylic acid ethyl ester (774 mg, 2.42 mmol) in MeOH (5 mL) at 0° C. was carefully added sodium borohydride (110 mg, 2.91 mmol) and the reaction mixture was stirred at room temperature for 4 h. The reaction mixture was quenched with 1N NaOH and diluted with further 1N NaOH and ethyl acetate. The organic layer was separated washed with brine, dried (Na2SO4), filtered and concentrated in vacuo to give a crude residue which was purified by flash column chromatography to give 1-benzyl-3-hydroxy-4-(2-methoxy-ethyl)-piperidine-4-carboxylic acid ethyl ester (610 mg, 78%) as a white solid. MS (ESI): 322.3 (MH+).

1. customat 0° C.
2. customThe reaction mixture was quenched with 1N NaOH
3. additiondiluted with further 1N NaOH and ethyl acetate
4. customThe organic layer was separated
5. washwashed with brine
6. dry with materialdried (Na2SO4)
7. filtrationfiltered
8. concentrationconcentrated in vacuo
9. customto give a crude residue which
10. customwas purified by flash column chromatography