A protocol has been kvelopedjiu rht generation qf hylroxyehyhnine peptide bond isosmes in a poipcr- sqprted synthesis. This has been used to produce the potent HlV-I Protease inhibitor JG345 rqidiy and in good yield. Protease inhibitors have outstanding potential as therapeutic agentst. Recently it
Solid-phase synthesis of potential aspartic acid protease inhibitors containing a hydroxyethylamine isostere
โ Scribed by Jinglan Zhou; Andreas Termin; Melissa Wayland; Christine M. Tarby
- Publisher
- Elsevier Science
- Year
- 1999
- Tongue
- French
- Weight
- 189 KB
- Volume
- 40
- Category
- Article
- ISSN
- 0040-4039
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โฆ Synopsis
A series of 1,3-diamino-2-propanol derivatives have been synthesized on solid phase as potential aspar'tic acid protease irdaibitors. The developed methodology allows the incorporation of either an alkyl group or H at the R 2 site of hydroxyethylamine isostere.
๐ SIMILAR VOLUMES
A short synthesis of a novel Fmoc-derivative 2b of the phosphonic acid isostere I of aspartic acid is presented. Incorporation of 2b into peptides was readily achieved using standard Fmoc-solid phase synthesis. Efficient removal of the allyl protecting groups after sequence assembly under mild condi
## Abstract The Fmocโbased SPPS of HโXaaโAsp(OBzl)โYaaโGlyโNH~2~ sequences results in side reactions yielding not only aspartimide peptides and piperidide derivatives, but also 1,4โdiazepineโ2,5โdioneโpeptides. Evidence is presented to show that the 1,4โdiazepineโ2,5โdione derivative is formed from