Yield: 100%

Reaction Conditions:

with palladium 10% on activated carbon;ammonia;hydrogen in methanol under 2585.81 Torr; for 60 h;

Steps:

[0550] Preparation of tert-butyl 4-amino-2-methylpiperidine-l-carboxylate (26.37)
[0550] Preparation of tert-butyl 4-amino-2-methylpiperidine-l-carboxylate (26.37): To a solution of tert-butyl 2-methyl-4-oxopiperidine-l-carboxylate 26.36 (2.0 g, 9.38 mmol) in methanolic ammonia (~4N, 200 mL) was added Pd/C (10 mol%, 0.2 g). The resulting reaction mixture was stirred at 50 PSI for 60 h under hydrogen atmosphere. After completion of the reaction (TLC monitoring), the reaction mass was filtered through celite bed. The filtrate was dried under reduced pressure to get desired product 26.37 (2.0 g, quantitative yield) as semi solid. MS : 215.17 (M+H)⁺.

References:

ALGOMEDIX, INC.;HERZ, Jeffrey M.;KESICKI, Edward A. WO2015/103060, 2015, A1 Location in patent:Paragraph 0550