Preparation of n-benzyloxycarbonyl aspartic acid

Details Preparation of n-benzyloxycarbonyl aspartic acid Preparation of n-benzyloxycarbonyl aspartic acid

C - Chemistry, Metallurgy

07

C

260/468.1

C07C 125/065 (1980.01)

Patent

CA 1154457

ABSTRACT OF THE DISCLOSURE N-Benzyloxycarbonyl aspartic acid substantially free of N-benzyl- oxycarbonyl aspartyl aspartic acid is prepared by introducing benzyl chlo- roformate gradually into an aqueous solution of the disodium salt of aspar- tic acid at temperatures of between 10°C. and about 45°C. while maintaining the pH of the aqueous solution at between 10.75 and 11.75. In a further embodiment, the mole ratio of unreacted benzyl chloroformate to the aspar- tic acid salt in the reaction medium is maintained preferably at no greater than 0.2. The resulting reaction mixture is acidified, e.g., with hydro- chloric acid, to convert the reaction product to the free acid, which is separated from the reaction mixture, washed with water and dried to yield an essentially pure white granular product.

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