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Issue 14, 2004
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New approaches to the industrial synthesis of HIV protease inhibitors

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Abstract

Efficient and industrially applicable synthetic processes for precursors of HIV protease inhibitors (Amprenavir, Fosamprenavir) are described. These involve a novel and economical method for the preparation of a key intermediate, (3S)-hydroxytetrahydrofuran, from L-malic acid. Three new approaches to the assembly of Amprenavir are also discussed. Of these, a synthetic route in which an (S)-tetrahydrofuranyloxy carbonyl is attached to L-phenylalanine appears to be the most promising manufacturing process, in that it offers satisfactory stereoselectivity in fewer steps.

Graphical abstract: New approaches to the industrial synthesis of HIV protease inhibitors

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Publication details

The article was received on 18 Mar 2004, accepted on 26 May 2004 and first published on 23 Jun 2004


Article type: Paper
DOI: 10.1039/B404071F
Citation: Org. Biomol. Chem., 2004,2, 2061-2070

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    New approaches to the industrial synthesis of HIV protease inhibitors

    Y. Honda, S. Katayama, M. Kojima, T. Suzuki, N. Kishibata and K. Izawa, Org. Biomol. Chem., 2004, 2, 2061
    DOI: 10.1039/B404071F

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