Patent ID: 6822111
Filing Date: 2004-11-23
Classification: A23L,C07K

Abstract:
A process for producing an aspartyl dipeptide ester derivative represented by formula (2): wherein said compound is in any form of the free form and the salt form, said process comprising: reductively alkylating aspartame with an aldehyde represented by formula (1), and hydrogen in the presence of a catalyst and a base: wherein said base is at least one member selected from the group consisting of metal hydrides, metal alkoxides, metal hydrozides, diethylamine, triethylamine, sodium carbonate, sodium hydrogen carbonate, and mixtures thereof, and wherein R1, R2, R3, R4, and R5 satisfy one of the following definitions (a), (b), (c), or (d): (a) in said formulae (1) and (2), R1 is a hydrogen atom, a methyl group or a methoxy group, R2 is a hydrogen atom, a methyl group or a methoxy group, R3 is a hydroxyl group, and R4 and R5 are a hydrogen atom; (b) in said formulae (1) and (2), R1, R4 and R5 are a hydrogen atom, R2 is a hydroxyl group, and R3 is a methoxy group; (c) in said formula (2), R1 is a hydrogen atom, a methyl group or a methoxy group, R2 is a hydrogen atom, a methyl group or a methoxy group, R3 is a hydroxyl group, and R4 and R5 are a hydrogen atom, and in said formula (1), R1 is a hydrogen atom, a methyl group or a methoxy group, R2 is a hydrogen atom, a methyl group or a methoxy group, R3 is a benzyloxy group, and R4 and R5 are a hydrogen atom; or (d) in said formula (2), R1, R4 and R5 are a hydrogen atom, R2 is a hydroxyl group, and R3 is a methoxy group, and in said formula (1), R1, R4 and R5 are a hydrogen atom, R2 is a benzyloxy group, and R3 is a methoxy group.