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

V Caciagli; F Cardinali; A Hänsicke; G Tuchalski; P Lombardi

doi:10.1002/(sici)1099-1387(199705)3:3%3c224::aid-psc104%3e3.0.co;2-z

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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.

V Caciagli·F Cardinali·A Hänsicke·G Tuchalski·P Lombardi

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Abstract

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 Waters pump in order to allow small-scale (0.0001 mol; 1 x 10 cm Omnifit columns) synthetic studies which were strongly predictive of the conditions required for large-scale (0.01-0.10 mol; 3.6 or 5.9 x 46 cm Büchi columns) production, performed on the same apparatus.

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Models, Chemical Peptides, Cyclic Protein Engineering Tachykinins Journal Article

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V Caciagli, F Cardinali, A Hänsicke, G Tuchalski, P Lombardi. Large-scale production of peptides using the solid-phase continuous flow method. Preparative synthesis of the novel tachykinin antagonist MEN 10627.. https://doi.org/10.1002/(sici)1099-1387(199705)3%3A3%253c224%3A%3Aaid-psc104%253e3.0.co%3B2-z

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