Solvay Sa

Baxter International Inc.

Baxter Healthcare Sa

Solvay

Cyrille Pousset

Roland Callens

Georges Blondeel

Zouaoui Bourezg

Ronan Gire

Marc Larcheveque

Process for producing enantiopure &#x3b2;-amino acid derivatives corresponding to general formula (I) R1-NZ-CHR2-CH&#x2014;COOR3 (I) in which R1 and R2 independently denote organic residues optionally forming a cyclic substituent, R3 denotes H or an organic residue, and Z represents H or an amino function-protecting group, comprising a step in which a mixture of enantiomers of a compound corresponding to general formula (II) R1-NZ-CHR2&#x2014;CH&#x2014;COOR4 (II) in which R1, R2 and Z are as defined for formula (I), and R4 is an organic residue, is subjected to hydrolysis in the presence of a lipase.

Process for producing enantiopure &#x3b2;-amino acid derivatives, and enantiopure &#x3b2;-amino acid derivatives

Process for the manufacture of an enantiopure compound comprising at least one functional group capable of reacting with an activated carboxyl group, starting from a mixture of enantiomers of the said compound, in which process: (a) a reaction medium comprising the mixture of enantiomers and a reagent based on an enantiopure amino acid, in which reagent at least one amino group of the amino acid is protected by a protective group and in which reagent at least one carboxyl group of the amino acid is activated, is subjected to conditions appropriate for bringing about the reaction of the functional group capable of reacting with the activated carboxyl group with the activated carboxyl group, so as to form a carbonyl bond; (b) the mixture of diastereomers obtained is subjected to a separation operation, so as to obtain at least one fraction composed essentially of a diastereomer, (c) at least a portion of the said fraction is subjected to a stage of cleavage of the carbonyl bond under conditions under which the protective group is essentially stable; and (d) the enantiopure compound and an enantiopure derivative of the amino acid in which at least one amino group is protected by the protective group are recovered.

Process for the manufacture of an enantiopure compound

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Brussels, Belgium

Cyrille Pousset