2-(3-Methoxy-piperidin-1-yl)-ethylaMine synthesis

Yield:911300-67-9 97%

Reaction Conditions:

with ammonia;hydrogen;nickel in ethanol;water; under 3102.97 Torr; for 22 h;

Steps:

184

2-(3-Methoxy-1-piperidinyl)ethylamine (283). A mixture of nitrile 282 (3.5 g, 22.7 mmol) and Raney Nickel (50% w/w suspension in water, 8 g) in EtOH (100 mL) and cNH₃ (10 mL) was stirred under H₂ (60 psi) for 22 h. The mixture was filtered through Celite, the solid washed with EtOH (60 mL) and the solvent evaporated to give diamine 283 as a crude colourless oil (3.48 g, 97%) which was used without further purification: HRMS (FAB⁺) calcd for C₈H₁₉N₂O (MH⁺) m/z 159.14974, found 159.14976.

References:

WO2006/104406,2006,A1 Location in patent:Page/Page column 166