Hydrochloric Acid → N-[(R)-1-[3-(4-piperidyl)-(E)-acryloyl]-3-piperidylcarbonyl]-beta-alanine ethyl ester

Participants

Reaction Steps

To a solution of N-[(R)-1-[3-(1-tert-butoxycarbonyl-4-piperidyl)-(E)-acryloyl]-3-piperidylcarbonyl]-β-alanine ethyl ester (0.8 g) in ethyl acetate (8 ml) was added 4N HCl in ethyl acetate (4.3 ml) at 0° C., and the reaction mixture was stirred for 2 hours at room temperature. The reaction mixture was concentrated in vacuo, and resolved in water, neutralized with saturated aqueous NaHCO3, desalted by using the resin of HP-20 eluting with isopropanol-H2O (1:1), then freeze-dried to give N-[(R)-1-[3-(4-piperidyl)-(E)-acryloyl]-3-piperidylcarbonyl]-β-alanine ethyl ester (458 mg).

Provenance & Evidence