Preparation process of .alpha.-aspartyl-l-phenylalanine...

C - Chemistry – Metallurgy – 07 – K

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C07K 5/075 (2006.01)

Patent

CA 2066464

.alpha.-L-Aspartyl-L-phenylalanine methyl ester (.alpha.-APM) is prepared by catalytic hydrogenation of N-benzyloxy- carbonyl-.alpha.-L-aspartyl-L-phenylalanine methyl ester (Z- .alpha.-APM). The catalytic hydrogenation is conducted in an aqueous suspension containing the Z-.alpha.-APM in the form of particles whose average particle size is not greater than 800 µm. The starting Z-.alpha.-APM may contain up to 30 wt.% of its .beta.-isomer provided that the process additionally includes recrystallization of the .alpha.-APM, collection of the .alpha.-APM by filtration and recycling of the filtrate for use in the aqueous suspension of Z-.alpha.-APM.

Ester méthylique d'alpha-L-Aspartyl-L-phénylalanine (alpha-APM), préparé par hydrogénation catalytique de l'ester méthylique de N-benzyloxy-carbonyl-alpha-L-aspartyl-L-phénylalanine (Z-alpha-APM). L'hydrogénation catalytique est faite dans une suspension aqueuse renfermant le Z-alpha-APM sous forme de particules dont la taille moyenne ne dépasse pas 800 microns. Le Z-alpha-APM de départ peut contenir jusqu'à 30 % en poids de son isomère bêta, à la condition que le procédé comprenne également la recristallisation de l'alpha-APM, la collecte du alpha-APM par filtration et le recyclage du filtrat pour utilisation dans la suspension aqueuse du Z-alpha-APM.

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