- Functionalised pyrrolidinones derived from (S)-pyroglutamic acid
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The generation of the lactam enolate derived from bicyclic lactams 2a-c, prepared from (S)-pyroglutamic acid 1a, and subsequent reaction with a range of electrophiles, is reported. Exo-diastereoselectivity is generally favoured. The deprotection of some of these adducts to give functionalised hydroxymethylpyrrolidinones is readily achieved by simple hemiaminal ether cleavage under acidic conditions.
- Beard, Mark J.,Bailey, Jonathan H.,Cherry, David T.,Moloney, Mark G.,Shim, Sung Bo,Statham, Kathryn A.,Bamford, Mark J.,Lamont, R. Brian
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p. 3719 - 3740
(2007/10/03)
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- HIV protease inhibitors useful for the treatment of AIDS
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Compounds of formula STR1 where R1 and R2 are independently hydrogen or optionally-substituted C1-4 alkyl or aryl, or R1 and R2 are joined together to form a monocyclic or bicyclic ring system, are HIV protease inhibitors. These compounds are useful in the treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of treating infection by HIV are also described.
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- A CONSISE APPROACH TO FUNCTIONALISED, HOMOCHIRAL PYRROLIDINONES
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Acylation of O,N-acetal 1 gives excellent yields of the C-7 substituted products 2a,b.Alkylation of 2a under mild conditions gives high yields of the exo- 3 and endo- 4 substituted products in varying ratios, depending on the alkylating agent.The unsatura
- Bamford, Mark J.,Beard, Mark,Cherry, David T.,Moloney, Mark G.
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p. 337 - 340
(2007/10/02)
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