Method of preparing...

Details Method of preparing... Method of preparing...

C - Chemistry, Metallurgy

07

K

C07K 5/072 (2006.01) A23L 1/236 (2006.01) C07K 1/06 (2006.01)

Patent

CA 2157639

L-aspartyl-D-.alpha.-aminoalkanecarboxylic acid- (S)-N-.alpha.-alkylbenzylamide is prepared by a method comprising the steps of (a) reacting N-protected-L- aspartic anhydride and D-.alpha.-aminoalkanecarboxylic acid- (S)-N-.alpha.-alkylbenzylamide in the presence of acetic acid and an organic solvent which is immiscible with water; (b) without isolating N-protected-L-aspartyl-D-.alpha.- aminoalkanecarboxylic acid-(S)-N-.alpha.-alkylbenzylamide thus produced, adding an aqueous solvent directly to the reaction mixture to form a diphasic system comprising an organic phase and an aqueous phase; (c) deprotecting the N-protected-L-aspartyl-D-.alpha.- aminoalkanecarboxylic acid-(S)-N-.alpha.-alkylbenzylamide in the diphasic system; (d) separating the organic phase; and (e) crystallizing L-aspartyl-D-.alpha.-aminoalkane- carboxylic acid-(S)-N-.alpha.-alkylbenzylamide in the aqueous phase. The method according to the invention is less expensive and more efficient than previous methods using N-protected-L-aspartic anhydride.

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