Hydrochloric Acid → HCID 86758038, compound

Participants

Reaction Steps

To a stirred solution of N-[(R)-1-[3-(4-piperidyl)-(E)-acryloyl]-3-piperidylcarbonyl]-2(S)-trifluoroacetylamino-β-alanine ethyl ester (334 mg, 0.58 mmol) in ethyl acetate (1.5 ml) was added a solution of 4N-hydrogen chloride in ethyl acetate (1.0 ml, 4 mmol). After the solution was stirred for 2 hours at ambient temperature, the solvent was evaporated in vacuo. The residue was dissolved in 0.1M phosphate buffer (pH=7.3, 200 ml). To the solution was added Porcine liver esterase (0.5 ml), and the solution was stirred for 7 days at ambient temperature. Solvent was evaporated, and the residue was purified by HPLC to give N-[(R)-1-[3-(4-piperidyl)-(E)-acryloyl]-3-piperidylcarbonyl]-2(S)-trifluoroacetylamino-β-alanine trifluoroacetate as a colorless oil (220 mg, 67.5%).

Provenance & Evidence