Synthesis
General procedure for the synthesis of tert-butyl 4-(2-amino-1-hydroxyethyl)piperidine-1-carboxylate from tert-butyl 4-(1-hydroxy-2-nitro-ethyl)-piperidine-1-carboxylate: Compound 1013B (1.24 g, 4.5 mmol) was dissolved in methanol, Pd/C catalyst was added, and the reaction was carried out in a Parr shaker in a hydrogen atmosphere (50 psi) The reaction was carried out in a Parr shaker under hydrogen atmosphere (50 psi) overnight. Upon completion of the reaction, the catalyst was removed by filtration and the filtrate was concentrated to remove the solvent to afford compound 1013C (1.1 g, 99% yield), which can be used in the next reaction without further purification.
References
[1] Patent: WO2006/19768, 2006, A1. Location in patent: Page/Page column 140
[2] Patent: WO2013/50448, 2013, A1. Location in patent: Page/Page column 64; 65
[3] Patent: US2014/249146, 2014, A1. Location in patent: Page/Page column
[4] Bioorganic and Medicinal Chemistry Letters, 2004, vol. 14, # 13, p. 3419 - 3424
[5] Patent: US2012/252815, 2012, A1. Location in patent: Page/Page column 60
