| abstract |
The invention relates to a method for producing chiral peptides using a solvent and a proton donor element, the pKa in water of which is higher than 7, in the presence of a base pertaining to an acid-base pair, the pKa in water of which is higher than 4, said chiral peptides comprising at least one α-or β-amino acid, or at least one derivative of an α- or β-amino acid, with an enantiomer excess of at least 90% or a diastereoisomer excess of at least 85%, by reacting a starting product consisting of an α-aminoacrylate or an α-aminoacrylamide with an organometallic derivative or an organoboron derivative, particularly with a boron derivative, by means of a chiral phosphorus ligand depleted of electrons, in the presence of a catalyst containing a transition metal, at a temperature varying between 10°C and 80°C, the chiral compounds consisting of an α- or β-amino acid -the amino group of which is non-substituted or of a derivative of an α- or β-amino acid, said derivative being an α- or β-amino acid of which one of the two carboxylic acid and amino acid groups of the main chain is protected by a protecting group, the other being non-substituted or also protected by a protecting group - being excluded. |