Hydrochloric Acid → 4'-((R)-1-Amino-ethyl)-3-chloro-3'-fluoro-biphenyl-2-carboxylic acid methyl ester hydrochloride

Participants

Reaction Steps

4′-((R)-1-tert-Butoxycarbonylamino-ethyl)-3-chloro-3′-fluoro-biphenyl-2-carboxylic acid methyl ester (350 mg, 858 μmol, step A) was added to a solution of HCl in dioxane (4N, 4.29 ml, 17.2 mmol) and the reaction mixture was stirred at room temperature for 2 h. The reaction mixture was evaporated to dryness and the remaining solid was triturated with heptane/EtOAc 2:1 for 4 h. Filtration delivered the title compound as white solid (217 mg, 74%). MS: 308.2 [M+H]+.

Provenance & Evidence