Hydrochloric Acid → Diethyl [(5-aminopyridin-2-yl)methyl]phosphonate hydrochloride

Participants

Reaction Steps

To a solution of diethyl ({5-[bis(tert-butoxycarbonyl)amino]pyridin-2-yl}methyl)phosphonate (Compound 260B, 2.5 g, 5.6 mmol) in dry EtOAc (150 mL) was added HCl in EtOAc solution dropwise. The reaction mixture was stirred at room temperature for 1 h. The solids were collected by filtration, dried to give 2.1 g of the desired product as a white solid. 1H NMR (DMSO-d6, 400 MHz): δ=1.16 (t, J=7.2 Hz, 6 H), 3.64 (d, J=22.0 Hz 2 H), 3.97-4.04 (m, 4H), 7.50 (dd, J=2.0, 8.8 Hz, 1 H), 7.64 (dd, J=2.0, 8.8 Hz, 1 H), 7.95 (d, J=2.4 Hz, 1 H).

Provenance & Evidence