Abstract

A serie sof analogues of LY289612 were prepared as HIV-1 protease inhibitors and evaluated in vitro for their enzyme inhibitory and antiviral activities. Compound 1, a potent HIV-1 protease inhibitor, and its analogues were synthesized from key intermediate 9, which was prepared by alkylation of mercaptan 4 with α-bromo ketone 7 followed by stereroselective reduction of the ketone intermediate 8.

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