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Large-scale production of peptides using the solid-phase continuous flow method. Preparative synthesis of the novel tachykinin antagonist MEN 10627

✍ Scribed by Valerio Caciagli; Franco Cardinali; Andre Hänsicke; Gisbert Tuchalski; Paolo Lombardi

Publisher: John Wiley and Sons
Year: 1997
Tongue: English
Weight: 109 KB
Volume: 3
Category: Article
ISSN: 1075-2617
DOI: 10.1002/(sici)1099-1387(199705)3:3<224::aid-psc104>3.0.co;2-z

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✦ Synopsis

The large-scale solid-phase continuous flow synthesis of the bicyclic peptide MEN 10627, a new potent Neurokinin A receptor antagonist, is described using the Fmoc-polyamide method on both Macrosorb 125 and Macrosorb 250 resin. A new synthesizer designed in-house was realized by assembling Whitey valves and a Waters pump in order to allow small-scale (0.0001 mol; 1 610cm Omnifit columns) synthetic studies which were strongly predictive of the conditions required for large-scale (0.01-0.10 mol; 3.6 or 4.9 646cm Bu ¨chi columns) production, performed on the same apparatus.

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✍ Valerio Caciagli; Franco Cardinali; Fabio Bonelli; Paolo Lombardi 📂 Article 📅 1998 🏛 John Wiley and Sons 🌐 English ⚖ 115 KB 👁 1 views

A preparative method for the preparation of large peptides is described. An advantageous theoretical weight of peptide/weight of starting resin ratio (tP w /R w ) of about 0.3 was successfully experimented. The esterification of the first amino acid was realized with a racemization of less than 1%.