[EN] PROCESS FOR THE PREPARATION OF A DIPEPTIDE AND INTERMEDIATE PRODUCT IN SUCH A PROCESS<br/>[FR] PROCEDE DE PREPARATION D'UN DIPEPTIDE ET D'UN PRODUIT INTERMEDIAIRE DANS UN TEL PROCEDE
申请人:DSM NV
公开号:WO2001030807A1
公开(公告)日:2001-05-03
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.