Ammonia → 4-(4-Piperidinyl)-2-pyridinamine

Participants

Reaction Steps

To a stirred solution of tert-butyl 4-(2-chloropyridin-4-yl)piperidine-1-carboxylate (24 g, 0.08 mol, 1 equiv) in ammonia (250 mL) was added copper(I) oxide (5 g, 0.03 mols, 0.4 equiv.) and stirred 10 h at 200° C. under 2.2 MPa of ammonia. The reaction was monitored by LC-MS to completion. The mixture was cooled, extracted with dichloromethane (5×250 mL), dried over Na2SO4, then concentrated to obtain compound 4-(piperidin-4-yl)pyridin-2-amine (8.5 g, 36%).

Provenance & Evidence