✦ LIBER ✦

A convenient synthesis of 1-(S)-[1′-(S)-(t-butyloxycarbonylamino)-2′-phenylethyl]oxirane. A useful building block in the synthesis of HIV protease inhibitors

✍ Scribed by Jonas Brånalt; Ingemar Kvarnström; Björn Classon; Bertil Samuelsson; Ulrika Nillroth; U.Helena Danielson; Anders Karlén; Anders Hallberg

Book ID: 104257026
Publisher: Elsevier Science
Year: 1997
Tongue: French
Weight: 206 KB
Volume: 38
Category: Article
ISSN: 0040-4039
DOI: 10.1016/s0040-4039(97)00662-x

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✦ Synopsis

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-I protease inhibitors.

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