Process for the preparation of aspartylphenylalanine methyl...

C - Chemistry – Metallurgy – 07 – K

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530/5.06

C07K 5/06 (2006.01) C07K 5/075 (2006.01)

Patent

CA 1322626

AE 5682 A B S T R A C T The invention relates to a process for the preparation of aspartylphenylalanine methyl ester from N-formylaspartylalanine methyl ester by treatment with an acid, characterized in that N-formyl-aspartylalanine methyl ester is treated at 30-60°C with at least 0.5 molar equivalent oxalic acid per mole of N-formyl-aspartylphenyl- alanine methyl ester in a solvent mixture in which N-formylaspartylphenylalanine methyl ester dissolves well and in which the oxalic acid salt of aspartylphenylalanine methyl ester is poorly soluble, after which the oxalic acid salt of aspartylphenylalanine methyl ester is removed by filtration, dissolved in water and subsequently neutralized with the aid of an inorganic base with formation of free aspartylphenylalanine methyl ester.

565465

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