A convenient synthesis of 1-(S)-[1'-(S)-(t-butyloxycarbonylamino)-2'- phenylethyl]oxirane. A useful building block in the synthesis of HIV protease inhibitors

Article abstract of DOI:10.1016/S0040-4039(97)00662-X

A new short route to epoxide 6b, a pivotal intermediate for the preparation of hydroxyethylamine dipeptide isosteres has been developed. Opening of the epoxide by anthranilic acid, followed by extensions in the P2/P3-region gave the target compounds which were evaluated as HIV-1 protease inhibitors.