Tert-butyl 3-cyano-3-(1-methylpiperidin-2-yl)azetidine-1-carboxylate → Tert-butyl 3-(aminomethyl)-3-(1-methylpiperidin-2-yl)azetidine-1-carboxylate

Participants

Reaction Steps

tert-Butyl 3-cyano-3-(1-methylpiperidin-2-yl)azetidine-1-carboxylate (8.1 g, 29 mmol) was dissolved in 2M ammonia in methanol (100 ml) and Raney nickel (50% slurry in water, 5.0 g (2.5 g Raney nickel)) was added and the mixture hydrogenated on a parr at 45 psi for 1 day until tlc showed completion. The reaction was filtered under nitrogen and the filtrate was evaporated to dryness to give tert-Butyl 3-(aminomethyl)-3-(1-methylpiperidin-2-yl)azetidine-1-carboxylate as an oil. m/z (M++H) 284.

Provenance & Evidence