An expeditious total synthesis of (±)-jamtine using condensation between imine and acid anhydride total synthesis of (±)-jamtine using condensation between imines and acid anhydride - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Tetrahedron Letters Année : 2010

An expeditious total synthesis of (±)-jamtine using condensation between imine and acid anhydride total synthesis of (±)-jamtine using condensation between imines and acid anhydride

Résumé

In silico optimisation, synthesis and binding evaluation of avb3 integrin's affinity for precursors of a new RGD peptidomimetics family are presented. The 2-pyrrolidinone building block was obtained by condensation of L-lysine with dimethoxydihydrofuran followed by reduction. The ring was functionalized with a carboxylic acid and a guanidinium appendage. On the pyrrolidinone heterocycle, the effects on affinity of position, length and relative geometry of the two acid or basic functionalized side chains introduced on the pyrrolidinone ring have been previously evaluated by docking studies. Peptidomimetics have finally been evaluated by competition binding assays for avb3 integrin's affinity using radioligands
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hal-01904955 , version 1 (25-10-2018)

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Joelle Pérard-Viret, Florence Souquet, Marie-Line Manisse, Jacques Royer. An expeditious total synthesis of (±)-jamtine using condensation between imine and acid anhydride total synthesis of (±)-jamtine using condensation between imines and acid anhydride. Tetrahedron Letters, 2010, 51 (1), pp.96-98. ⟨10.1016/j.tetlet.2009.10.091⟩. ⟨hal-01904955⟩

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