反应详情

4M HCl (922 μl, 3.69 mmol) in dioxane was added to a solution of tert-butyl (2S,5S)-2-[(2-{[N-(tert-butoxycarbonyl)-4-fluoro-β-(4-fluorophenyl)-L-phenylalanyl]amino}-6-fluorophenoxy)methyl]-5-[({[(2,2,2-trifluoroethyl)amino]carbonyl}oxy)methyl]morpholine-4-carboxylate (310 mg, 0.369 mmol) in Dioxane (3.69 ml) at room temperature and the reaction stirred until complete by LC/MS (8 hrs). The solvent was removed in vacuo and ether was added to the residue. The desired product was filtered off to afford the title compound (253 mg, 0.355 mmol, 96% yield) as a white solid, MS (ESI): m/z=641.4 (M+H); 100% pure by LC/MS.

1. customThe solvent was removed in vacuo and ether
2. additionwas added to the residue
3. filtrationThe desired product was filtered off