J. Branalt et al., A CONVENIENT SYNTHESIS OF )-(T-BUTYLOXYCARBONYLAMINO)-2'-PHENYLETHYL]OXIRANE - A USEFUL BUILDING-BLOCK IN THE SYNTHESIS OF HIV PROTEASE INHIBITORS, Tetrahedron letters, 38(19), 1997, pp. 3483-3486
A new short route to epoxide 6b, a pivotal intermediate for the prepar
ation of hydroxyethylamine dipeptide isosteres has been developed. Ope
ning of the epoxide by anthranilic acid, followed by extensions in the
PZ/P3-region gave the target compounds which were evaluated as HIV-1
protease inhibitors. (C) 1997 Elsevier Science Ltd.