Hydrochloric Acid → 4-Fluoro-beta-(4-fluorophenyl)-N-(5-fluoro-4-{2-[(2R,5S)-5-({[(2,2,2-trifluoroethyl)carbamoyl]oxy}methyl)morpholin-2-yl]ethyl}pyridin-3-yl)-L-phenylalaninamide trihydrochloride

Participants

Reaction Steps

4M HCl (3.54 mL, 14.17 mmol) in dioxane was added to a solution of tert-Butyl (2R,5S)-2-[2-(3-{[N-(tert-butoxycarbonyl)-4-fluoro-β-(4-fluorophenyl)-L-phenylalanyl]amino}-5-fluoropyridin-4-yl)ethyl]-5-({[(2,2,2-trifluoroethyl)carbamoyl]oxy}methyl)morpholine-4-carboxylate (1.19 g, 1.42 mmol) in Dioxane (14 mL) at ambient temperature and the reaction stirred for 4 hours. The solvent was removed in vacuo and ether was added to the residue. The title compound was filtered off as a white solid (1.00 g, 1.34 mmol, 94% yield), MS (ESI): m/z=640.40 (MH+); 100% pure by LCMS.

Provenance & Evidence