Hydrochloric Acid → HCID 86726340, compound

Participants

Reaction Steps

4M HCl (44.5 mL, 178 mmol) in dioxane was added to a solution of tert-Butyl (2R,5S)-2-[2-(2-{[N-(tert-butoxycarbonyl)-4-fluoro-β-(4-fluorophenyl)-L-phenylalanyl]amino}-6-fluorophenyl)ethyl]-5-({[(2,2,2-trifluoroethyl)carbamoyl]oxy}methyl)morpholine-4-carboxylate (7.46 g, 8.89 mmol) in Dioxane (89 mL) at 0° C. and then the reaction was stirred at rt for 4 hours. The solvent was removed in vacuo and ether was added to the residue to afford a white ppt. The ppt was triturated with ether (×3) and the residing white solid dried under high vacuum to afford the title compound (5.84 g, 8.21 mmol, 92% yield) as a white powder, MS (ESI): m/z=639.5 (MH+); 100% pure by LCMS.

Provenance & Evidence