Process for the preparation of a dipeptide and intermediate...

Details Process for the preparation of a dipeptide and intermediate... Process for the preparation of a dipeptide and intermediate...

C - Chemistry, Metallurgy

07

K

C07K 5/06 (2006.01)

Patent

CA 2389024

Process for the preparation of an N-formyl-L-leucyl-L-tert.-leucine-N- methylamide in which N-formyl L-leucine is coupled to L-tert.-leucine-N- methylamide in the presence of an activating agent. Preferably, use is made of L-tert.-leucine-N-methylamide with an enantiomeric excess greater than 98 % and N-formyl-L-leucine with an enantiomeric excess greater than 98 %. If desired, the dipeptide obtained is subsequently deformylated and the resulting N-formyl-L-tert.-leucine-N-methylamide or the L-leucyl-L-tert.-leucine-N- methylamide is further subjected to one or more crystallizations. The invention also relates to the N-formyl-L-leucyl-L-tert.-leucine-N-methylamide and the use of N-formyl-L-leucyl-L-tert.-leucine-N-methylamide in the preparation of pharmaceuticals.

L'invention concerne un procédé de préparation d'un N-formyl-L-leucyl-L-tert.-leucine-N-méthylamide dans lequel N-formyl L-leucine est couplé à L-tert.-leucine-N-méthylamide en présence d'un agent activant. De préférence, on utilise L-tert.-leucine-N-méthylamide avec un excès d'énantiomère supérieur à 98 % N-formyl-L-leucine avec un excès d'énantiomère supérieur à 98 %. Si on le désire, le dipeptide obtenu est par la suite déformylé et le N-formyl-L-leucyl-L-tert.-leucine-N-méthylamide ou le L-leucyl-L-tert.-leucine-N-méthylamide est par la suite soumis à une ou plusieurs cristallisations. L'invention concerne également le N-formyl-L-leucyl-L-tert.-leucine-N-méthylamide et l'utilisation du L-leucyl-L-tert.-leucine-N-méthylamide dans la préparation de produits pharmaceutiques.

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