Synthesis
General procedure for the synthesis of ethyl piperidin-4-one-3-carboxylate hydrochloride from ethyl 1-benzyl-4-oxo-3-piperidinecarboxylate hydrochloride: in a 50 mL reactor, ethyl N-benzyl-4-oxo-piperidine-3-carboxylate hydrochloride (12 g, 40.29 mmol) and Pd(OH)2/C catalyst (120 mg, 1 wt%) were added. The reaction was stirred for 48 h under 5 bar hydrogen pressure using a dry solvent mixture of dichloromethane and methanol (4:1, v/v) as the reaction medium. Upon completion of the reaction, the catalyst was removed by filtration through a diatomaceous earth pad followed by evaporation of the solvent under reduced pressure to afford 8.3 g of the target product, ethyl piperidin-4-one-3-carboxylate hydrochloride, as a light brown solid in 99% yield.
References
[1] Tetrahedron, 1991, vol. 50, # 2, p. 515 - 528
[2] Tetrahedron Letters, 2012, vol. 53, # 26, p. 3296 - 3300
[3] Bioorganic and Medicinal Chemistry, 2018, vol. 26, # 8, p. 1784 - 1796
[4] Archiv der Pharmazie, 2018, vol. 351, # 9,
[5] Patent: CN108586454, 2018, A. Location in patent: Paragraph 0134; 0136; 0137
