Synthesis of a novel conformationally restricted Val-Phe dipeptidomimetic. |
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| Authors: | Pauline Gilleron Régis Millet Juozas Domarkas Amaury Farce Raymond Houssin Jean-Pierre Hénichart |
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| Institution: | Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, Université de Lille 2, BP 83, 59006 Lille, France. |
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| Abstract: | A method for the synthesis of (3(R,S),6S,11b(R,S))-1,3,4,6,7,11b-hexahydro-4-oxo-3-phthalimidopyrido2,1-a]isoquinoline-6-carboxylic acid 2 as a new conformationally restricted dipeptidomimetic of Val-Phe is reported. It involved cyclisation via an intramolecular electrophilic addition at the reactive bridgehead carbon. This new scaffold can be used as a building block in the preparation of libraries of peptidomimetics. |
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| Keywords: | Val‐Phe peptidomimetic pyridoisoquinoline building block |
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